Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
OwnerChristopher Franklin Bigge, Agustin Casimiro-Garcia +5inventors
InventorsChristopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
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Abstract
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
Claims83
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment;
- Q is NH or is absent;
- and wherein R1′ is OH, —O—(C1-C6), or NR3′R4′, wherein R3′ and R4′ are independently H, (C1-C6)alkyl, or are joined together to form a optionally substituted saturated or unsaturated 5 to 7 membered ring;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—CR9—CH2—, or —CH2—CH2—CR9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkaxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment, or B is optionally substituted phenyl or pyridyl;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—C═R9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C1-C6)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is phenyl which is substituted at the ortho position with formyl, H2NSO2, MeSO2, MeSO, MeS, (C1-C6)alkoxycarbonyl, cyano, H2N—CH2—, HN—(C1-C6)alkyl—CH2—, (C1-C6)alkyl2N—CH2—, or hydroxyl;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—C═R9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment and which is an optionally substituted 4, 5, 6 or 7-membered ring;
- Rx and Ry are H, halo, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)carboxyalkyl, or taken together are O═;
- XIII is CH2, CH—OH, CH—CO2(C1-C6)alkyl, O, S, NH, or N(C1-C6)alkyl;
- provided that when Rx and Ry taken together are O, XIII is CH2;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—C═R9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3 R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- or a tautomer thereof, wherein YII is CH2, CH(C1-C6)alkyl, or N and R18 is H, (C1-C6)alkyl, hydromethyl, CH2O—(C1-C6)alkyl, CONR2R2′, or CH2NR2R2′;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—C═R9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, any of which may be optionally substituted with halo, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, CH2O—(C1-C6)alkyl, N2R2′, (C1-C6)alkylNR2R2′ or (or halo(C1-C6)alkyl;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—CR9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment;
- J1, J2, J3, and J4 are each C, or one of J1, J2, J3, and J4 is N;
- and
- R19, R20, R21, and R22 are each independently H, halo, hydroxy, NH2, N23R24, , NO2, SH, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkoxy, wherein R23 and R24 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring, or R19 and R20, R20 and R21, or R21 and R22, together with the carbons to which they are attached, form a 5, 6, or seven membered saturated or unsaturated cycloalkyl or heterocycloalkyl ring, or an aryl or heteroaryl ring;
- provided that when any of J1, J2, J3, or J4 is N, R19, R20, R21 or R22, respectively, is absent at that position;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —H2—CR7R8—CH2—, —CH2—C═R9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring and;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl;
- and
- R7 and R8 are each independently halo;
- and
- R9 is ═O or ═NOR2.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment,
- Q is NH or is absent;
- and wherein R1′ is OH, —O—(C1-C6), or NR3′R4′, wherein R3′ and R4′ are independently H, (C1-C6)alkyl, or are joined together to form a optionally substituted saturated or unsaturated 5 to 7 membered ring;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein;
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment, or B is optionally substituted phenyl or pyridyl;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is phenyl which is substituted at the ortho position with formyl, H2NSO2, MeSO2, MeSO, MeS, (C1-C6)alkoxycarbonyl, cyano, aminomethyl, (C1-C6)alkoxy , or hydroxy;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment and which is an optionally substituted 4, 5, 6 or 7-membered ring;
- wherein Rx and Ry are H, halo, (C1-C6)alkyl, (C1-C6)alkoxy, or (C1-C6)carboxyalkyl, or taken together are O═;
- XIII is CH2, CH—OH, CH—CO2(C1-C6)alkyl, O, S, NH, or N(C1-C6)alkyl,
- provided that when Rx and Ry taken together are O═, XIII is CH2;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- or a tautomer thereof, wherein YII is CH2, CH(C1-C6)alkyl, or N and R18 is H, (C1-C6)alkyl, hydroxymethyl, CH2O—(C1-C6)alkyl, CONR2R2′, or CH2NR2R2′;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, any of which may be optionally substituted with halo, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, CH2O—(C1-C6)alkyl, or halo(C1-C6)alkyl;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula II:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment;
- J1, J2, J3, and J4 are each C, or one of J1, J2, J3, and J4 is N;
- and
- R19, R20, R21, and R22 are each independently H, halo, hydroxy, NH2, NR23R24, NO2, SH, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkoxy, wherein R23 and R24 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring, or R19 and R20, R20 and R21, or R21 and R22, together with the carbons to which they are attached, form a 5, 6, or seven membered saturated or unsaturated cycloalkyl or heterocycloalkyl ring, or an aryl or heteroaryl ring;
- provided that when any of ii, J2, J3, or J4 is N, R19, R20, R21 or R22, respectively, is absent at that position;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- or —CH2—CONH(C1-C6)alkyl;
- R2 is H or (C1-C6)alkyl;
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment,
- Q is NH or is absent;
- and
- wherein R1′ is OH, —O—(C1-6), or NR3′R4′, wherein R3′ and R4′ are independently H, (C1-C6)alkyl, or are joined together to form a optionally substituted saturated or unsaturated 5 to 7 membered ring;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from aryl, heteroaryl, halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment, or B is optionally substituted phenyl or pyridyl;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is phenyl which is substituted at the ortho position with formyl, H2NSO2, MeSO2, MeSO, MeS, (C1-C6)alkoxycarbonyl, cyano, aminomethyl, or hydroxy;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- wherein “” indicates the point of attachment and which is an optionally substituted 4, 5, 6 or 7-membered ring;
- wherein Rx and Ry are H, halo, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)carboxyalkyl, or taken together are O═;
- XIII is CH2, CH—OH, CH—CO2(C1-C6)alkyl, O, S, NH, or N(C1-C6)alkyl,
- provided that when Rx and Ry taken together are O, XIII is CH2;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or —CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- or a tautomer thereof, wherein YII is CH2, CH(C1-C6)alkyl, or N and R18 is H, (C1-C6)alkyl, hydroxymethyl, CH2O—(C1-C6)alkyl, CONR2R2′, or CH2NR2R2′;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- and
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, any of which may be optionally substituted with halo, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, CH2O—(C1-C6)alkyl, or halo(C1-C6)alkyl;
- and
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula III:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- A is aryl and substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- wherein B is
- wherein “” indicates the point of attachment;
- J1, J2, J3, and J4 are each C, or one of J1, J2, J3, and J4 is N;
- and
- R19, R20, R21, and R22 are each independently H, halo, hydroxy, NH2, N2R23R24, NO2, SH, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkoxy, wherein R23 and R24 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring, or R19 and R20, R20 and R21, or R21 and R22, together with the carbons to which they are attached, form a 5, 6, or seven membered saturated or unsaturated cycloalkyl or heterocycloalkyl ring, or an aryl or heteroaryl ring;
- provided that when any of J1, J2, J3, or J4 is N, R19, R20, R21 or R22, respectively, is absent at that position and;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R8 and R9 are as defined for R3 and R4;
- and
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, or (C1-C6)alkoxy.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is
- wherein “” indicates the point of attachment,
- Q is NH or is absent;
- and wherein R1′ is OH, —O—(C1-C6), or NR3′R4′, wherein R3′ and R4′ are independently H, (C1-C6)alkyl, or are joined together to form a optionally substituted saturated or unsaturated 5 to 7 membered ring;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is
- wherein “” indicates the point of attachment, or B is optionally substituted phenyl or pyridyl;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, hale, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CR2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is phenyl which is substituted at the ortho position with formyl, H2NSO2, MeSO2, MeSO, MeS, (C1-C6)alkoxycarbonyl, cyano, aminomethyl, methoxy, or hydroxy
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CR2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is
- wherein “” indicates the point of attachment and which is an optionally substituted 4, 5, 6 or 7-membered ring;
- wherein Rx and Ry are H, halo, (C1-C6)alkyl, (C1-C6)alkoxy, or (C1-C6)carboxyalkyl, or taken together are O═;
- XIII is CH2, CH—OH, CH—CO2(C1-C6)alkyl, O, S, NH, or N(C1-C6)alkyl,
- provided that when Rx and Ry taken together are O═, XIII is CH2;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CR2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is
- or a tautomer thereof, wherein YII is CH2, CH(C1-C6)alkyl, or N and R18 is H, (C1-C6)alkyl, hydroxymethyl, CH2O—(C1-C6)alkyl, CONR2R2′, or CH2NR2R2′;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, any of which may be optionally substituted with halo, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, CH2O—(C1-C6)alkyl, or halo(C1-C6)alkyl;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula IV:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- B is
- wherein “” indicates the point of attachment;
- J1, J2, J3, and J4 are each C, or any of J1, J2, J3, or J4 is N;
- and R19, R20, R21, and R22 are each independently H, halo, hydroxy, NH2, N2R23R24, NO2, SH, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkoxy, wherein R23 and R24 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring, or R19 and R20, R20 and R21, or R21 and R22, together with the carbons to which they are attached, form a 5, 6, or seven membered saturated or unsaturated cycloalkyl or heterocycloalkyl ring, or an aryl or heteroaryl ring;
- provided that when any of J1, J2, J3, or J4 is N, R19, R20, R21 or R22, respectively, is absent at that position;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each C, or one of X and Y is C and the other is N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
The invention also provides a compound of formula V:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- R2 is H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or N8R9, wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each independently C or N, provided that when one of X or Y is N, R14 or R15 is absent at that position;
- X′ and Y′ are each independently CH or N;
- is absent or is a fused heterocyclic or fused heteroaryl ring, provided that when
- is present, Y′ is C;
- and
- R16 and R17 are each independently H, halo, cyano, (C1-C6)alkoxy carbonyl, aminomethyl, t-butyl, H2NSO2—, Me2NSC)2—, (C1-C6)alkoxy, MeSO—, MeSO—, MeS—, NR8R9, or hydroxy.
A compound of formula VI:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- Q is NH or is absent;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- R1 is OH, —O—(C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C1-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4, wherein R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 5 to 7 membered ring;
- R2 is H or (C1-C6)alkyl;
- and
- R3 and R4 are independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a 5 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4,
- X and Y are each independently C or N, provided that when one of X or Y is N, R14 or R15 is absent at that position.
A compound of formula VII:
- or a pharmaceutically acceptable salt thereof wherein
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4,
- X and Y are each independently C or N, provided that when one of X or Y is N, R14 or
- R15 is absent at that position;
- and
- is an optionally substituted 4, 5, 6 or 7-membered ring;
- wherein Rx and Ry are H, halo, hydroxymethyl, (C1-C6)alkyl, (C1-C6)alkoxy, or taken together are O═;
- XIII is CH2, O, S, NH, or N(C1-C6)alkyl, provided that when Rx and Ry taken together are O═, XIII is CH2.
The invention also provides a compound of formula VIII:
- or a pharmaceutically acceptable salt or tautomer thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring;
- R12 and R13 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each independently C or N, provided that when one of X or Y is N, R14 or R15 is absent at that position;
- and
- YII is CH2, CH(C1-C6alkyl), NH, or N(C1-C6 alkyl);
- and
- R18 is H, (C1-C6)alkyl, hydroxymethyl, CH2O—(C1-C6)alkyl, or NR3R4.
A compound of formula IX:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- XII is CH2;
- R10 is H or F;
- R11 is H or F, hydroxy, methoxy, ethoxy, cyano, amino,
- trifluoromethyl, MeSO2N,
- wherein “” indicates the point of attachment;
- or R10 and R11 are taken together to form C═O or C═NOH;
- R12 and R13 are each independently H, fluoro, chloro, bromo, methyl, or methoxy;
- R14 and R15 are each independently H, fluoro, chloro, methyl, or trifluoromethyl;
- X and Y are each independently C, or N, provided that X or Y is N, R14 or R15 is absent at that position;
- and
A compound of formula X:
- or a pharmaceutically acceptable salt thereof wherein
- “- - -” is absent;
- Z is C—H, C-halo, C—(C1-C6)alkyl, C-halo(C1-C6)alkyl, C—(C1-C6)alkoxy, or N;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—CONH2, or —CH2—CONH(C1-C6)alkyl;
- XII is CH2;
- R10 and R11 are each independently H, —OH, halo, alkyl, haloalkyl, —NR8R9, —OR2, —CN, —CH2OH, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CH═O, —CH2OR2, —COR2, —CO2R2, or —CONR3R4 or are taken together to form ═O, ═NOR2, ═C(C1-C6alkyl)2, or ═CR2H;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring;
- R12 and R3 are each independently H, halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, or (C1-C6)alkoxy;
- R14 and R15 are each independently H, halo, alkyl, or haloalkyl, or NR8R9 wherein R8 and R9 are as defined for R3 and R4;
- X and Y are each independently C or N, provided that when one of X or Y is N, R14 or R15 is absent at that position;
- J1, J2, J3, and J4 are C or one of J1, J2, J3, and J4 is N;
- R19, R20, R21, and R22 are each independently H, halo, hydroxy, NH2, NR23R24, NO2, SH, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkoxy, wherein R23 and R24 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring, or R19 and R20, R20 and R21, or R21 and R22, together with the carbons to which they are attached, form a 5, 6, or 7 membered saturated or unsaturated cycloalkyl or heterocycloalkyl ring, or an aryl or heteroaryl ring;
- provided that when any of J1, J2, J3, or J4 is N, R19, R20, R21, or R22 is absent at that position.
A compound which is:
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(2,4-difluoro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-p-tolylamide;
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-[(4-methoxy-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-bromo-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-[(4-isopropyl-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-phenylamide;
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-[(4-trifluoromethyl-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-[(3-methoxy-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-ethyl-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(3,4-difluoro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(3-fluoro-4-methyl-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2′-sulfamoyl-phenyl)-pyridin-2-yl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-chloro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(5-chloro-pyridin-2-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-chloro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(4-chloro-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[5-(2′-sulfamoyl-phenyl)-pyridin-2-yl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(1H-tetrazol-5-yl)-phenyl]-amide};
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Oxo-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methylene-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4,4-Difluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Amino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxymethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 1-(4-Chloro-phenylcarbamoyl)-5-(3-fluoro-2′-methanesulfonyl-biphenyl-4-ylcarbamoyl)-pyrrolidine-3-carboxylic acid;
- 1-(4-Chloro-phenylcarbamoyl)-5-(3-fluoro-2′-methanesulfonyl-biphenyl-4-ylcarbamoyl)-pyrrolidine-3-carboxylic acid methyl ester;
- Pyrrolidine-1,2,4-tricarboxylic acid 4-amide 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Aminomethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methoxymethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methylamino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Acetylamino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methanesulfonylamino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 5-Oxo-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2′-methanesulfonyl-phenyl)-pyrimidin-2-yl]-amide};
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2-methanesulfonyl-phenyl)-pyrimidin-2-yl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2′-methanesulfonyl-phenyl)-3-methyl-pyridin-2-yl]-amide};
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2-methanesulfonyl-phenyl)-3-methyl-pyridin-2-yl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-trifluoromethyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-trifluoromethyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2′-methanesulfonyl-phenyl)-6-methyl-pyridin-2-yl]-amide};
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2-methanesulfonyl-phenyl)-6-methyl-pyridin-2-yl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-ethyl-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-ethyl-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5-difluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5-dichloro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5-dichloro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3,5-dimethyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3,5-dimethyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-chloro-2′-methanesulfonyl-5-methyl-biphenyl-4-yl)-amide] 1-[(4-chloro-phenyl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(3-chloro-2′-methanesulfonyl-5-methyl-biphenyl-4-yl)-amide] 1-[(4-chloro-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(2-chloro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(4-chloro-phenyl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(2-chloro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(4-chloro-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-2-methyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-2-methyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-{[1-(4-Chloro-phenylcarbamoyl)-pyrrolidine-2-carbonyl]-amino}-2′-methanesulfonyl-biphenyl-3-carboxylic acid methyl ester;
- 4-{[1-(4-Chloro-phenylcarbamoyl)-4-hydroxy-pyrrolidine-2-carbonyl]-amino}-2-methanesulfonyl-biphenyl-3-carboxylic acid methyl ester;
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-[(4-trifluoromethyl-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-m-tolylamide;
- Pyrrolidine-1,2-dicarboxylic acid 1-[(3-acetyl-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-2-methyl-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(2-fluoro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(3-chloro-4-fluoro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(3-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-cyano-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-2-methyl-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(3,4-dichloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] 1-[(3-trifluoromethyl-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-dimethylamino-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- (2S)-Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-cyano-phenyl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(4-fluoro-phenyl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-p-tolylamide;
- 4-Oxo-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- and
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- or
- a pharmaceutically acceptable salt thereof.
A compound which is:
- (R)-Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- (S)-Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4S)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(4-fluoro-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-p-tolylamide;
- (2R)-4-Oxo-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- and
- (2R,4S)-4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- or
- a pharmaceutically acceptable salt thereof.
A compound which is:
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Propoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Propoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide];
- 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-azetidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-azetidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-azepan-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-azepan-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-hydroxymethyl-5-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,3-dimethyl-5-oxo-2,5-dihydro-pyrazol-1-yl)-phenyl]-amide};
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-hydroxymethyl-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-pyrrolidin-1-yl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-[1,2,4]triazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-[1,2,3]triazol-2-yl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-[1,2,3]triazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(4-acetylamino-phenyl)-amide] 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(cyclopentanecarbonyl-amino)-phenyl]-amide};
- and
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-pyrimidin-5-yl-phenyl)-amide];
- or
- a pharmaceutically acceptable salt thereof.
A compound which is:
- 1-(4-Chloro-phenylcarbamoyl)-5-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-pyrrolidine-3-carboxylic acid;
- 1-(4-Chloro-phenylcarbamoyl)-5-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-pyrrolidine-3-carboxylic acid methyl ester;
- 1-(4-Chloro-phenylcarbamoyl)-5-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-pyrrolidine-3-carboxylic acid ethyl ester;
- Pyrrolidine-1,2,4-tricarboxylic acid 4-amide 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Cyano-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-(1H-Tetrazol-5-yl)-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Aminomethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Methylaminomethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Dimethylaminomethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Acetyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- Pyrrolidine-1,2,4-tricarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide} 4-methylamide;
- Pyrrolidine-1,2,4-tricarboxylic acid 1-[(4-chloro-phenyl)-amide] 4-dimethylamide 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Trifluoromethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Methyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Isopropoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4,4-Difluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-flouro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-phenyl)-pyrrolidine-2-carboxylic acid;
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-hydroxy-pyrrolidine-2-carbonyl]-amino}-phenyl)-pyrrolidine-2-carboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[5-(2-oxo-piperidin-1-yl)-pyrimidin-2-yl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-(2-oxo-piperidin-1-yl)-pyrimidin-5-yl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2-oxo-piperidin-1-yl)-pyrimidin-2-yl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-(2-oxo-piperidin-1-yl)-pyrimidin-5-yl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide} 1-[(5-fluoro-pyridin-2-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-fluoro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-fluoro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-yl)-amide];
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(5-fluoro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-yl)-amide];
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-yl)-amide];
- 4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(5-fluoro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-hydroxymethyl-5-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-5-oxo-pyrrolidine-2-carboxylic acid;
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-5-oxo-pyrrolidine-2-carboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(4,4-dimethyl-2,5-dioxo-imidazolidin-1-yl)-2-fluoro-phenyl]-amide};
- [1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2,5-dioxo-imidazolidin-4-yl]-acetic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(5,5-dimethyl-2,4-dioxo-oxazolidin-3-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-oxazolidin-3-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-oxazolidin-3-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-imidazolidin-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-2,5-dioxo-imidazolidin-1-yl)-phenyl]-amide};
- 3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-imidazolidine-4-carboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2,4,5-trioxo-imidazolidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(2-aminomethyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(2-aminomethyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(2-carbamoyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(2-carbamoyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(2,2-bis-hydroxymethyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-imidazolidine-4-carboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,3-dimethyl-2,5-dioxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3,3,4-trimethyl-2,5-dioxo-pyrrolidin-1-yl)-phenyl]-amide};
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-5-oxo-pyrrolidine-2,2-dicarboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-methyl-5-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-methyl-6-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-hydroxy-2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-2,6-dioxo-tetrahydro-pyrimidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-tetrahydro-pyrimidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-piperazin-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-hydroxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-methyl-2-oxo-4-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,6-dioxo-piperidin-1-yl)-2-fluoro-phenyl]-amide};
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-piperidine-3-carboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(5,5-dihydroxy-2,4,6-trioxo-tetrahydro-pyrimidin-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2,4,6-trioxo-tetrahydro-pyrimidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(4,4-dimethyl-2,6-dioxo-piperidin-1-yl)-2-fluoro-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-hydroxy-4-oxo-azetidin-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(acetyl-methyl-amino)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 4-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-1H-pyrrole-3-carboxylic acid;
- 2-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2H-pyrazole-3-carboxylic acid;
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-1H-imidazole-2-carboxylic acid;
- 1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-1H-pyrrole-2-carboxylic acid;
- 3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-1H-pyrrole-2-carboxylic acid;
- 3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-furan-2-carboxylic acid;
- 3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-thiophene-2-carboxylic acid;
- 4-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-furan-3-carboxylic acid;
- 4-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-thiophene-3-carboxylic acid;
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3,5′-difluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(5′-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3,5′-difluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5′-difluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(5′-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5′-difluoro-2′-methanesulfonyl-biphenyl)-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3,5′-difluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5′-difluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5′-difluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide], or
- a pharmaceutically acceptable salt thereof.
A compound which is:
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(5-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,5-dimethyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,5-dimethyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,5-dimethyl-pyrazol-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4S)-4-Amino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Amino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- (2R)-4-Hydroxyimino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methylsulfamoyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-dimethylsulfamoyl-3-fluoro-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- (2R,4S)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Fluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R)-4,4-Difluoro-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide] 1-[(4-fluoro-phenyl)-amide];
- (2R,4R)-4-Acetylamino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methanesulfonylamino-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4S)-4-(1H-Tetrazol-5-yl)-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl).phenyl]-amide};
- (2R,4S)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Cyano-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-(1H-Tetrazol-5-yl)-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Trifluoromethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-cyano-3-fluoro-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-[(2′-aminomethyl-3-fluoro-biphenyl-4-yl)-amide] 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4′-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3′-fluoro-biphenyl-2-carboxylic acid methyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-2-fluoro-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-methyl-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(ethyl-methyl-carbamoyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2R-methyl-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2S-methyl-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(pyrrolidine-1-carbonyl)-2-pyrrolidin-1-yl-phenyl]-amide};
- (2R,4R)-4-{[1-(4-Chloro-phenylcarbamoyl)-4-hydroxy-pyrrolidine-2-carbonyl]-amino}-3-pyrrolidin-1-yl-benzoic acid methyl ester;
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(azetidine-1-carbonyl)-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-aide] 2-{[4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(4-dimethylcarbamoyl-phenyl)-amide];
- (2R,4R)-4-{[1-(4-Chloro-phenylcarbamoyl)-4-hydroxy-pyrrolidine-2-carbonyl]-amino}-3-dimethylamino-benzoic acid methyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-phenyl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-2-fluoro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-methyl-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-methyl-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-4-quinolin-8-yl-phenyl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,5-difluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- Pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-2-methyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfinyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-methyl-2′-methylsulfanyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-2′-methanesulfonyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-trifluoromethyl-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methoxy-biphenyl-4-yl)-amide];
- (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-hydroxy-biphenyl-4-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-4-iodo-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-hydroxy-2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-tetrahydro-pyrimidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-oxazolidin-3-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-piperidine-3-carboxylic acid ethyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-morpholin-4-yl-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-methyl-5-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2-methyl-5-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 2-[(4-tert-butyl-phenyl)-amide] 1-[(4-chloro-phenyl)-amide];
- 4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2[(3,5′difluoro-2′-sulfamoyl-biphenyl-4-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2,3-dimethyl-5-oxo-2,5-dihydro-pyrazol-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,3-dimethyl-5-oxo-2,5-dihydro-pyrazol-1-yl)-phenyl]-amide};
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide]-TFA Salt;
- 4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- 4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- or
- 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-oxo-6H-pyridazin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-methyl-5-oxo-5H-[1,2,4]triazin-4-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-chloro-5-methyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-methyl-5-oxo-4,5-dihydro-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-chloro-3-methyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,5-dimethoxy-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-3-pyrrol-1-yl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-3-phenyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,5-dimethyl-2-oxo-imidazolidin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3,5,5-trimethyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-isopropyl-5,5-dimethyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(5,5-dimethyl-2-oxo-imidazolidin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,4-dimethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3,5-dimethyl-2-oxo-imidazolidin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3,5,5-trimethyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-isopropyl-5,5-dimethyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(5-methyl-2-oxo-imidazolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(5,5-dimethyl-2-oxo-imidazolidin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3,4-dimethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- or a pharmaceutically acceptable salt thereof.
A compound which is:
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-quinolin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-oxo-3H-isoquinolin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(1-oxo-1H-isoquinolin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-oxo-5H-[1,2,4]triazin-4-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-oxo-6H-pyrimidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyrazin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyrimidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-[1,3,5]triazin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(6-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(1-methyl-1H-imidazol-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(1-methyl-1H-pyrrolidine-2-yl)-phenyl]-amide};
- (2R,4R)-5-Aza-spiro[2.4]heptane-5,6-dicarboxylic acid 5-[(4-chloro-phenyl)-amide] 6-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-3H-imidazol-4-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-methyl-2H-pyrazol-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(2,5-dihydro-pyrrolidine-1-carbonyl)-pyridin-2-yl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-5-oxo-2,5-dihydro-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methoxymethyl-3-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methoxymethyl-5-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-ethyl-3-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-isobutyl-3-methyl-pyrazol-1-yl)-phenyl)-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-isopropyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-ethyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-isobutyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-2-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolodine-2-carbonyl]-amino}-3-fluoro-phenyl)-2H-pyrazole-3-carboxylic acid methyl ester;
- (2R,4R)-2-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolodine-2-carbonyl]-amino}-3-fluoro-phenyl)-2H-pyrazole-3-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methoxymethyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-5-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-oxazole-4-carboxylic acid ethyl ester;
- (2R,4R)-5-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-hydroxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-oxazole-4-carboxylic acid ethyl ester;
- (2R,4R)-5-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-oxazole-4-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methoxymethyl-oxazol-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(4-ethyl-oxazol-5-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-isopropyl-oxazol-5-yl)-phenyl]-amide};
- (2R,4R)-5-(6-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-pyridin-3-yl)-oxazole-4-carboxylic acid ethyl ester;
- (2R,4R)-5-(6-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-pyridin-3-yl)-oxazole-4-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(4-methoxymethyl-oxazol-5-yl)-pyridin-2-yl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(4-ethyl-oxazol-5-yl)-pyridin-2-yl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(4-vinyl-oxazol-5-yl)-pyridin-2-yl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[5-(4-isobutyl-oxazol-5-yl)-pyridin-2-yl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methyl-isoxazol-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(4-methyl-isoxazol-3-yl)-phenyl]-amide};
- (2R,4R)-3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-isoxazole-4-carboxylic acid methyl ester;
- (2R,4R)-3-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-isoxazole-4-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(4-methoxymethyl-isoxazol-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-isopropyl-isoxazol-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-cyclopropyl-isoxazol-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(4-cyclopropyl-isoxazol-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-methyl-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-methyl-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-methyl-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-[(4-chloro-phenyl)-amide] 1-{[2,6-difluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-[(5-chloro-pyridin-2-yl)-amide] 1-{[2,6-difluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 2-[(4-chloro-phenyl)-amide] 1-{[2,6-difluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 2-[(5-chloro-pyridin-2-yl)-amide] 1-{[2,6-difluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(5′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(5′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(5′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(5′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(2′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6t-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-[(2′-methyl-2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(ethyl-isopropyl-carbamoyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(ethyl-isopropyl-carbamoyl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-ethyl-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-ethyl-pyrrolidine-1-carbonyl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3R-amino-pyrrolidine-1-carbonyl)-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3R-amino-pyrrolidine-1-carbonyl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3S-amino-pyrrolidine-1-carbonyl)-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3S-amino-pyrrolidine-1-carbonyl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3R-methylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3R-methylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3S-methylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3S-methylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3R-ethylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3R-ethylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3S-ethylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3,5-ethylamino-pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-fluoro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-3-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-hydroxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid;
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-2-carboxylic acid methyl ester;
- (2R,4R)-[1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-phenyl)-2,5-dioxo-imidazolidin-4-yl]-acetic acid;
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid methyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-3-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-hydroxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-2-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(6-cyclopropyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-3-carboxylic acid ethyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,3-dimethyl-2-oxo-azetidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(7-oxo-7H-thieno[2,3-c]pyridin-6-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-1-aza-spiro[4.5]dec-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-benzoyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-acetylsulfamoyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-thiazolidin-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-3-sulfamoyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-amino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-3-phenoxy-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,2-dimethyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(4-Chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid tert-butyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dioxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-benzothiazol-2-yl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-amino-4,6-dimethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-diethylaminomethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-aminomethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-5-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-Acetic acid 1-(4-{[1-(4-chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridin-3-yl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-({4-[3-(cyclopentanecarbonyl-amino)-2-oxo-2H-pyridin-1-yl]-2-fluoro-phenyl}-amide);
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-amino-3-methyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-({2-fluoro-4-[2-oxo-3-(pyridin-4-ylcarbamoyl)-2H-pyridin-1-yl]-phenyl}-amide);
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3,5-dichloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-amino-5-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-cyano-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-cyano-2-oxo-5-phenyl-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-ethyl-6-methyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-cyano-4-dimethylamino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-nitro-2-oxo-3-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-amino-6-oxo-6H-[3,4′]bipyridinyl-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-chloro-3-nitro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-carbamoyl-2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-5-Bromo-1-(4-{[1-(4-chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid isobutyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-chloro-2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-bromo-5-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-bromo-3-nitro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-nitro-2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-5-Chloro-1-(4-{[1-(4-chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid methyl ester;
- (2R,4R)-5-Chloro-1-(4-{[1-(4-chloro-phenylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-benzyloxy-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-amino-5-fluoro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-methyl-3-oxo-3H-isoquinolin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methyl-5-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-acetylamino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-amino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-oxo-6H-[3,4′]bipyridinyl-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-oxo-4H-furo[3,2-c]pyridin-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(1-oxo-1H-[2,6]naphthyridin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-oxo-4H-thieno[3,2-c]pyridin-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-oxo-1,4-dihydro-imidazo[4,5-c]pyridin-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(5-fluoro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-3-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(6-hydroxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid;
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-2-carboxylic acid methyl ester;
- (2R,4R)-[1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-phenyl)-2,5-dioxo-imidazolidin-4-yl]-acetic acid;
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid methyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-3-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-hydroxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-2-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(6-cyclopropyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]amino}-3-fluoro-phenyl)-6-oxo-1,6-dihydro-pyridine-3-carboxylic acid ethyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-hydroxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3,3-dimethyl-2-oxo-azetidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(7-oxo-7H-thieno[2,3-c]pyridin-6-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-1-aza-spiro[4,5]dec-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-benzoyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-methyl-5-oxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-methyl-6-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-acetylsulfamoyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-thiazolidin-3-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-3-sulfamoyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-amino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-3-phenoxy-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2,2-dimethyl-5-oxo-pyrrolidin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-1-(4-{[1-(5-Chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid tert-butyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2,5-dioxo-pyrrolidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-benzothiazol-2-yl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-amino-4,6-dimethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-diethylaminomethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-aminomethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-methyl-5-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-Acetic acid 1-(4-{[1-(5-chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridin-3-yl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-({4-[3-(cyclopentanecarbonyl-amino)-2-oxo-2H-pyridin-1-yl]-2-fluoro-phenyl}-amide);
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-amino-3-methyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-({2-fluoro-4-[2-oxo-3-(pyridin-4-ylcarbamoyl)-2H-pyridin-1-yl]-phenyl}-amide);
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3,5-dichloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-amino-5-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-cyano-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-cyano-2-oxo-5-phenyl-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-ethyl-6-methyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-cyano-4-dimethylamino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(5-nitro-2-oxo-3-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-amino-6-oxo-6H-[3,4′]bipyridinyl-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-chloro-3-nitro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-carbamoyl-2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-5-Bromo-1-(4-{[1-(5-chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid isobutyl ester;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-chloro-2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-bromo-5-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{f4-(5-bromo-3-nitro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-nitro-2-oxo-5-trifluoromethyl-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(5-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-5-Chloro-1-(4-{[1-(5-chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid methyl ester;
- (2R,4R)-5-Chloro-1-(4-{[1-(5-chloro-pyridin-2-ylcarbamoyl)-4-methoxy-pyrrolidine-2-carbonyl]-amino}-3-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-benzyloxy-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-amino-5-fluoro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(5-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(6-methyl-3-oxo-3H-isoquinolin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-methyl-5-nitro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-acetylamino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(1-oxo-1H-isoquinolin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-amino-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(6-oxo-6H-[3,4′]bipyridinyl-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-oxo-3H-isoquinolin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(4-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-oxo-4H-furo[3,2-c]pyridin-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(1-oxo-1H-[2,6]naphthyridin-2-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(5-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-oxo-4H-thieno[3,2-c]pyridin-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-oxo-1,4-dihydro-imidazo[4,5-c]pyridin-5-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-2-methyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3,4,5,6-tetrahydro-2H-[1,4′]bipyridinyl-4-ylmethyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-dimethylaminomethyl-imidazol-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[2-chloro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[2-chloro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-methylamino-imidazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-isopropyl-imidazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2-ethyl-imidazol-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(2-ethyl-imidazol-1-yl)-2-fluoro-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-isopropyl-imidazol-1-yl)-phenyl]-amide};
- (2R,4R)-2-Ethyl-4-methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 4-Methoxy-2-methoxymethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- 2-Hydroxymethyl-4-methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- {1-(4-Chloro-phenylcarbamoyl)-2-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-4-methoxy-pyrrolidin-2-yl}-acetic acid methyl ester;
- {1-(4-Chloro-phenylcarbamoyl)-2-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-4-methoxy-pyrrolidin-2-yl}-acetic acid;
- 4-Hydroxymethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- {1-(4-Chloro-phenylcarbamoyl)-5-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-pyrrolidin-3-yl}-acetic acid;
- {1-(4-Chloro-phenylcarbamoyl)-5-[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenylcarbamoyl]-pyrrolidin-3-yl}-acetic acid methyl ester;
- (2R,4R)-2-Ethyl-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-fluoro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-fluoro-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-chloro-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[4-(3-bromo-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide} 1-[(5-chloro-pyridin-2-yl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-iodo-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-iodo-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[4-(3-ethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide};
- and
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-ethyl-2-oxo-2H-pyridin-1-yl)-2-fluoro-phenyl]-amide;
- or
- a pharmaceutically acceptable salt thereof.
A compound which is:
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R) 4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methoxy-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-methyl-imidazol-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-2-fluoro-phenyl)-amide];
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-fluoro-4-pyrazol-1-yl-phenyl)-amide];
- (2R,4R) 4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(3-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-methyl-imidazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide];
- (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(4-dimethylcarbamoyl-2-fluoro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 2-{[2-chloro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} 1-[(4-chloro-phenyl)-amide];
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-methyl-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(6-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(3-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(5-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(5-methyl-2-oxo-2E-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(5-chloro-pyridin-2-yl)-amide] 2-{[2-fluoro-4-(4-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide;
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-2-fluoro-phenyl-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-phenyl-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(4-methyl-2-oxo-2H-pyridin-1-yl)-phenyl]-amide};
- (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[4-(2,5-dihydro-pyrrole-1-carbonyl)-2-fluoro-phenyl]-amide};
- or
- a pharmaceutically acceptable salt thereof.
The compound (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] or a pharmaceutically acceptable salt thereof.
The compound (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide].
The compound (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} or a pharmaceutically acceptable salt thereof.
The compound (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide}.
The compound (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide] or a pharmaceutically acceptable salt thereof.
The compound (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide].
The compound (2R,4R)-4-Propoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide} or a pharmaceutically acceptable salt thereof.
The compound (2R,4R)-4-Propoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide}.
The compound 4-(2,4-Difluoro-phenyl)-4-hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-1,3′]bipyridinyl-6′-yl)-amide] or a pharmaceutically acceptable salt thereof.
The compound 4-(2,4-Difluoro-phenyl)-4-hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-(1,3′]bipyridinyl-6′-yl)-amide].
A pharmaceutical composition comprising (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] or a pharmaceutically acceptable salt thereof and a carrier diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Ethoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(3-fluoro-2′-sulfamoyl-biphenyl-4-yl)-amide] and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} or a pharmaceutically acceptable salt thereof and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Methoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide] or a pharmaceutically acceptable salt thereof and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2′-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide] and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Propoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide} or a pharmaceutically acceptable salt thereof and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (2R,4R)-4-Propoxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-{[2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl]-amide} and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (4-(2,4-Difluoro-phenyl)-4-hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide] or a pharmaceutically acceptable salt thereof and a carrier, diluent, or excipient.
A pharmaceutical composition comprising (4-(2,4-Difluoro-phenyl)-4-hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 2-[(2-oxo-2H-[1,3′]bipyridinyl-6′-yl)-amide] and a carrier, diluent, or excipient.
A process for preparing a compound of Formula I:
- or a pharmaceutically acceptable salt thereof wherein:
- A is aryl or substituted aryl or monocyclic heteroaryl or substituted monocyclic heteroaryl;
- B is
- —NH(C1-C6)alkanoyl,
- (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, or heteroaryl, any of which may be optionally substituted by halo, (C1-C6)alkyl, or halo(C1-C6)alkyl, (C1-C6)alkoxy, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- C is phenyl or heteroaryl, wherein phenyl or heteroaryl is optionally substituted with one or more substituents selected from halogen, hydroxy, —CO2R2, —COR2, —CONR2R2′, alkoxy, alkyl, —CN, haloalkyl, amino, alkylamino, amidino, amido, or sulfonamido;
- G is H, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl,
- —CH2O—(C1-C6)alkyl, —CH2—CO2(C1-C6)alkyl, —CH2—NR2R2′, or —CH2—CONH(C1-C6)alkyl;
- W1 is —CH2—CH2—CH2—, —CH2—CH2—CR5R6—, —CH2—CR5R6—CH2—, —CH2—CH2—CR7—R8—, —CH2—CR7R8—CH2—, —CH2—C═R9—CH2—, or —CH2—CH2—C═R9—, wherein W1 connects the nitrogen atom at position 1 to the carbon atom at position 2 to form a five membered ring;
- R1 is (C1-C6)alkoxy, (C3-C7)cycloalkyl, (C3-C7)heterocycloalkyl, (C4-C7)cycloalkenyl, (C4-C7)heterocycloalkenyl, aryl, monocyclic heteroaryl, or —NR3R4;
- R2 and R2′ are each independently H or (C1-C6)alkyl;
- and
- R3 and R4 are each independently H, (C1-C6)alkyl, aralkyl, aryl, monocyclic heteroaryl, alkoxycarbonyl, aralkoxycarbonyl, —SO2alkyl, or joined together to form a saturated or unsaturated 3 to 7 membered ring;
- R5 is —OH, alkyl, halo(C1-C6)alkyl, —NR3R4, —OR2, halo, —CN, —CH2OR2, —CH2—NR3R4, aryl, monocyclic heteroaryl, alkylaryl, —CONR3R4, —COR2, halo(C1-C6)alkyl, or —CO2R2 and;
- R6 is H, alkyl, aralkyl, aryl, or monocyclic heteroaryl and;
- R7 and R8 are each independently halo and;
- R9 is ═O or ═NOR2;
- comprising:
- (a) reacting an amino acid of formula IA
- with a reagent capable of placing a protecting group P1 on the amino group of an amino acid to form a protected amino acid given by formula IB:
- wherein P1 is a protecting group arid W1 is the same as defined above;
- (b) converting the acid moiety in the compound of formula IB to a acid halide;
- (c) reacting the acid halide with a haloaniline or a haloamino-heterocycle to form a compound having formula IC:
- wherein Z1 is a halogen and A is as defined above;
- (d) coupling the compound of formula IC with a compound H—B to give a compound having formula ID:
- (e) removing the protecting group from Compound ID and reacting the resulting acid moiety with a C-isocyanate to form a compound of the invention.
Dependencies are inferred from the claim text.