Back to results
US 2018/0022701 A1Published application
4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
AssigneeMerck Sharp & Dohme Corp.
InventorsKenneth J. Barr, Corey E. Bienstock, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Dongshan Zhang, Neville J. Anthony, Blair T. Lapointe, Yuan Tian
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
Claims33
A compound according to Formula I
- or a pharmaceutically acceptable salt or solvate thereof, wherein:
- Y is CH, CRa, or N;
- n=0, 1, 2, 3 or 4;
- A4 is CR4,
- A5 is CR5,
- A6 is CR6,
- A7 is CR7,
- Ra is (C1-4)alkyl or (C3-7)cycloalkyl;
- R1 is
- (i) (C3-12)carbocyclyl(C0-4)alkyl, or
- (ii) a 4- to 12-membered heterocyclyl(C0-4)alkyl,
- each being substituted with (i) one occurrence of R8 that is (C3-7) cycloalkyl and (ii) optionally one, two, three, or four other occurrences of R8;
- R2 is hydroxycarbonyl, hydroxycarbonyl(C1-10)alkyl, (C1-10)alkylsulfoxyaminocarbonyl, or carbamoyl;
- R3 is hydrogen, halogen, cyano, nitro, hydroxy, (C1-4alkylcarbonyloxy, (C1-4) alkylsulfonylamino, (C1-4) alkylcarbonylamino, (C0-4) alkylamino, (C1-4)alkyl, hydroxyl(C1-4)alkyl or (C1-4)alkoxy, wherein (C1-4)alkyl and (C1-4)alkoxy are optionally substituted with one or more halogen;
- R4-R7 independently are hydrogen, halogen, amino, cyano, hydroxy, (C1-3)alkoxy, (C1-4)-alkyl, (C0-10)alkylaminocarbonyl, (C0-6)alkyoxycarbonylamino, (di)(C1-6)alkylaminocarbonyl, (C1-6)alkylcarbonylamino, (C1-4alkylamino, amino(C1-4)alkyl or —C(O)H, wherein (C1-3)alkoxy, (C1-4)alkyl, (C0-10)alkyl)aminocarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkylamino and amino(C1-4)alkyl are optionally substituted with one or more halogen, hydroxyl or (C1-3)alkoxy;
- or a group having the formula
- optionally substituted with one or more of the following:
- (C1-10)alkyl, halogen, amino, cyano, hydroxy, (C1-3)alkoxy, and wherein m is 1, 2, 3, or 4;
- or R6 is additionally selected from:
- (i) (C3-7)cycloalkyl or (C3-5)heterocycloalkyl, both optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (ii) (C2-9)heteroaryl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (iii) (C6-14)aryl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (iv) (C3-5)heterocycloalkylcarbonyl or (C3-5)heterocycloalkylcarbonyl(C1-4)alkyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (v) (C3-5)heterocycloalkylamino, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (vi) (C3-5)cycloalkylaminocarbonyl or di(C3-5)cycloalkylaminocarbonyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (vii) (C3-5)cycloalkylcarbonylamino, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (viii) (C3-5)cycloalkyl(C1-4alkyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (ix) (C3-5)cycloalkylamino, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (x) (C3-5)cycloalkylcarbonyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (xi) (C2-9)heteroaryl(C1-4alkyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (xii) (C2-9)heteroarylcarbonyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (xiii)
- (xiv) (C2-4)alkynyl, optionally substituted with one or more (C1-4)alkyl, which (C1-4)alkyl may be substituted with hydroxyl or amino;
- or
- (xv) (C1-6)alkoxycarbonylamino,
- (C1-6)alkylcarbonylamino,
- (C1-6)alkylsulfonylamino(C0-4)alkyl,
- (C1-6)alkylaminocarbonylamino,
- (C1-6)alkoxycarbonylamino(C0-4)alkyl,
- Hydroxycarbonyl(C1-4)alkylamino,
- Hydroxycarbonyl,
- (C1-6)alkylamino,
- (C1-6)alkoxyamino,
- (C0-6)alkylaminocarbonyl(C1-6)alkyl, or
- di(C1-6)alkylaminocarbonyl(C1-6)alkyl,
- each optionally substituted with one or more (C1-4)alkyl, hydroxyl or amino;
- and
- R8 is halogen, cyano, amino, nitro, hydroxy, oxo(=O), H2NC(O)—, di(C1-3)alkylamino, (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl, (C3-7)cycloalkyl, (C3-5)heterocycloalkyl, (C1-4alkenyl, (C3-6)cycloalkoxy or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one, two or three halogens.
45 more elements
(canceled)
A compound selected from:
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-4-formyl-1H-indazol-3-yl)benzoic acid;
- 3-fluoro-4-(1-(2-phenylpropanoyl)-1H-indazol-3-yl)benzoic acid;
- 3-fluoro-4-[1-(methoxyacetyl)-1H-indazol-3-yl]benzoic acid;
- 3-fluoro-4-[1-(pyridin-3-ylcarbonyl)-1H-indazol-3-yl]benzoic acid;
- 3-fluoro-4-{1-[(2-oxopyrrolidin-1-yl)acetyl]-1H-indazol-3-yl}benzoic acid;
- 3-fluoro-4-[1-(naphthalen-1-ylcarbonyl)-1H-indazol-3-yl]benzoic acid;
- 3-fluoro-4-{1-[(1-methyl-1H-indol-2-yl)carbonyl]-1H-indazol-3-yl}benzoic acid;
- 4-{1-[(2-bromo-3-methylphenyl)carbonyl]-1H-indazol-3-yl}-3-fluorobenzoic acid;
- 4-[1-(2,3-dihydro-1H-inden-4-ylcarbonyl)-1H-indazol-3-yl]-3-fluorobenzoic acid;
- 4-(1-{[3-(tertbutoxycarbonyl)-3-azabicyclo[3.1.0]hex-6-yl]carbonyl}-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-[1-(2,3-dihydro-1-benzofuran-7-ylcarbonyl)-1H-indazol-3-yl]-3-fluorobenzoic acid;
- 4-[1-(1-benzofuran-7-ylcarbonyl)-1H-indazol-3-yl]-3-fluorobenzoic acid;
- 4-{1-[(2-bromo-3-chlorophenyl)carbonyl]-1H-indazol-3-yl}-3-fluorobenzoic acid;
- 3-fluoro-4-(1-(tetrahydrofuran-2-carbonyl)-1H-indazol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(morpholine-4-carbonyl)-1H-indazol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-((2S,6R)-2,6-dimethylmorpholine-4-carbonyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(4-oxopiperidine-1-carbonyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 2-acetamido-4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol -3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl) benzoyl)-6-(3-hydroxyazetidin-1-yl)-1H-indazol-3-yl)benzoic acid;
- 4-(6-(azetidin-1-yl)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(cyclopropylamino)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(oxetan-3-ylamino)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-hydroxypyrrolidin-1-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-morpholino-1H-indazol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(methoxycarbonylamino)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(N-methylacetamido)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(cyclopropanecarboxamido)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(methylsulfonamido)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-methylureido)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(6-acetamido-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(N-methylmethylsulfonamido)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(1,3-dimethylureido)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(2-oxo-imidazolidin-1-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(2-oxoazetidin-1-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(6-(2-carboxyethylamino)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-methyl-2-oxoimidazolidin-1-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(2-oxopyrrolidin-1-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(morpholine-4-carbonyl)-1H-indazol-3-yl)benzoic acid;
- 3-(4-carboxyphenyl)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazole-6-carboxylic acid;
- sodium 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(5-methyloxazol-2-yl)-1H-indazol-3-yl)benzoate;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(5-methyloxazol-2-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-hydroxyprop-1-ynyl)-1H-indazol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-hydroxybut-1-ynyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(6-(3-aminoprop-1-ynyl)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-ethynyl-1H-indazol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-methyl-1,2,4-oxadiazol-5-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(5-(hydroxymethyl)oxazol-2-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(1-methyl-1H-imidazol-4-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(oxazol-2-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(6-(5-bromooxazol-2-yl)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- (E)-4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(N′-cyano-N,N-dimethylcarbamimidoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(4H-1,2,4-triazol-3-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(1-methyl-1H-imidazol-2-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(1-methyl-1H-imidazol-5-yl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(5-methylthiophen-3-yl)-1H-indazol-3-yl]benzoic acid;
- 4-(1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-pyrimidin-2-yl-1H-indazol-3-yl)benzoic acid;
- 4-(1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-pyrimidin-4-yl-1H-indazol-3-yl)benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(1-methyl-1H-imidazol-4-yl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(1,3-thiazol-4-yl)-1H-indazol-3-yl]benzoic acid;
- 4-(6-[4-(aminomethyl)pyridin-2-yl]-1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-1H-indazol-3-yl)benzoic acid;
- 4-(1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-pyridin-2-yl-1H-indazol-3-yl)benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(1,3-thiazol-5-yl)-1H-indazol-3-yl]benzoic acid;
- 4-(1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-pyridin-4-yl-1H-indazol-3-yl)benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(4-cyanophenyl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(3-cyanophenyl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(2-cyanophenyl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(2-fluorophenyl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(3-fluorophenyl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(4-fluorophenyl)-1H-indazol-3-yl]benzoic acid;
- 4-[1-{[2-chloro-6-(trifluoromethyl)phenyl]carbonyl}-6-(1-methyl-1H-pyrazol-5-yl)-1H-indazol-3-yl]benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(methylsulfonamidomethyl)-1H-indazol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(2,5-dioxoimidazolidin-4-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(4-chloro-1-(2-chloro-6-cyclopropylbenzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-cyclopropylbenzoyl)-4-fluoro-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-cyclopropylbenzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-2-methyl-1H-indol-3-yl)-3-fluorobenzoic acid;
- 4-(2-methyl-1-(2-(trifluoromethyl)benzoyl)-1H-indol-3-yl)benzoic acid;
- 4-(1-(2-chloro-6-cyclopropylbenzoyl)-1H-indazol-3-yl)-3,5-difluorobenzoic acid;
- 4-(1-(2-chloro-6-cyclopropylbenzoyl)-4-fluoro-1H-indazol-3-yl)-3,5-difluorobenzoic acid;
- 4-(6-(azetidine-1-carbonyl)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indol-3-yl)-3-fluorobenzoic acid;
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(3-methoxy-azetidine-1-carbonyl)-1H-indol-3-yl)-3-fluorobenzoic acid;
- and
- 4-(1-(2-chloro-6-(trifluoromethyl)benzoyl)-6-(oxetan-3-yl)-1H-indazol-3-yl)-3-fluorobenzoic acid.
82 more elements
(canceled)
(canceled)
(canceled)
A compound according to the Formula:
- or a pharmaceutically acceptable salt or solvate thereof, wherein:
- Y is CH, CRa, or N;
- n=0, 1, 2, 3 or 4;
- A4 is CR4,
- A5 is CR5,
- A6 is CR6,
- A7 is CR7,
- Ra is (C1-4)alkyl or (C3-7)cycloalkyl;
- R1 is
- (i) (C3-12)carbocyclyl(C0-4)alkyl, or
- (ii) a 4- to 12-membered heterocyclyl(C0-4)alkyl,
- each optionally substituted with one, two, three, four or five R8;
- R2 is hydroxycarbonyl, hydroxycarbonyl(C1-10)alkyl, (C1-10)alkylsulfoxyaminocarbonyl, or carbamoyl;
- R3 is hydrogen, halogen, cyano, nitro, hydroxy, (C1-4)alkylcarbonyloxy, (C1-4) alkylsulfonylamino, (C1-4) alkylcarbonylamino, (C0-4) alkylamino, (C1-4)alkyl, hydroxyl(C1-4)alkyl or (C1-4)alkoxy, wherein (C1-4)alkyl and (C1-4)alkoxy are optionally substituted with one or more halogen;
- R4, R5, and R7 independently are hydrogen, halogen, amino, cyano, hydroxy, (C1-3)alkoxy, (C1-4)alkyl, (C0-10)alkylaminocarbonyl, (C0-6)alkyoxycarbonylamino, (di)(C1-6)alkylaminocarbonyl, (C1-6)alkylcarbonylamino, (C1-4)alkylamino, amino(C1-4)alkyl or —C(O)H, wherein (C1-3)alkoxy, (C1-4)alkyl, (C0-10)alkyl)aminocarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkylamino and amino(C1-4)alkyl are optionally substituted with one or more halogen, hydroxyl or (C1-3)alkoxy;
- or a group having the formula
- optionally substituted with one or more of the following:
- (C1-10)alkyl, halogen, amino, cyano, hydroxy, (C1-3)alkoxy, and wherein m is 1, 2, 3, or 4;
- R6 is:
- (i) (C3-7)cycloalkyl or (C3-5)heterocycloalkyl, both optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (ii) (C2-9)heteroaryl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (iii) (C6-14)aryl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (iv) (C3-5)heterocycloalkylamino, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (v) (C3-5)cycloalkyl(C1-4)alkyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (vi) (C3-5)cycloalkylamino, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (vii) (C3-5)cycloalkylcarbonyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, oxo (═O), H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (viii) (C2-9)heteroaryl(C1-4)alkyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4)alkyl, cyano, nitro, hydroxyl, H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (ix) (C2-9)heteroarylcarbonyl, optionally substituted with one or more groups selected from halogen, amino, amino(C1-4alkyl, cyano, nitro, hydroxyl, H2NC(O), (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogen, amino or hydroxyl;
- (x)
- (xi) (C2-4)alkynyl, optionally substituted with one or more (C1-4alkyl, which (C1-4)alkyl may be substituted with hydroxyl or amino;
- or
- (xii) Hydroxycarbonyl(C1-4alkylamino,
- Hydroxycarbonyl,
- (C1-6)alkylamino, or
- (C1-6)alkoxyamino,
- each optionally substituted with one or more (C1-4)alkyl, hydroxyl or amino;
- and
- R8 is halogen, cyano, amino, nitro, hydroxy, oxo(═O), H2NC(O)—, di(C1-3)alkylamino, (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl, (C3-7)cycloalkyl, (C3-5)heterocycloalkyl, (C1-4)alkenyl, (C3-6)cycloalkoxy or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one, two or three halogens.
35 more elements
Dependencies are inferred from the claim text.