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US 2008/0188502 A1Published application
New Compounds I
AssigneeAstraZeneca AB
InventorsJeremy Burrows, Fernando Huerta, Fredrik Lake, Torben Pedersen, Didier Rotticci, Tobias Rein, Karin Staaf, Ulrika Yngve
Life of this patent
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Abstract
The present invention relates to a compound of formula (I): as a free base or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical formulations containing said compound and to the use of said compound in therapy. The present invention further relates to a process for the preparation of compound of formula (I) and to new intermediates used therein.
Claims53
1-77. (canceled)
A compound of formula (I):
- wherein:
- R1 is selected from sulphamoyl, carbamoyl, a group —R5-R6 and a nitrogen linked 4-7 membered saturated ring which optionally contains an additional nitrogen, oxygen or sulphur atom;
- wherein said ring is optionally substituted on carbon by one or more R7;
- and wherein if said ring contains an additional nitrogen atom that nitrogen is optionally substituted by R8;
- at least one of X1, X2, X3 and X4 is selected from N, the other three X1, X2, X3 or X4 are independently selected from N or C(R9), provided that not more than two of X1, X2, X3 or X4 are selected from N;
- R2 is halo or cyano;
- R3 is methyl, 3-tetrahydropyranyl or 4-tetrahydropyranyl, wherein the tetrahydropyranyl group is optionally substituted on carbon by one or more R10;
- R4 is selected from hydrogen, halo, cyano and C1-3alkyl, wherein C1-3alkyl is optionally substituted with one or more halo;
- R5 is selected from —O—, —C(O)—, —C(O)O—, —C(O)N(R11)—, —S(O)r, and —SO2N(R12)—;
- wherein R11 and R12 are independently selected from hydrogen or C1-6alkyl and said alkyl is optionally substituted by one or more R13;
- and r is 0, 1 or 2;
- R6 is selected from C1-6alkyl, carbocyclyl and heterocyclyl;
- wherein R6 is optionally substituted on carbon by one or more R14;
- and wherein if said heterocyclyl contains an —NH— moiety that nitrogen is optionally substituted by a group selected from R15;
- R7 is selected from halo, cyano, hydroxy, trifluoromethoxy, C1-3alkoxy and C1-3alkyl, wherein said C1-3alkyl is optionally substituted by one or more halo;
- R9 is selected from hydrogen, halo, cyano, hydroxy, amino, C1-3alkyl and C1-3alkoxy;
- R10, R13 and R14 are independently selected from halo, cyano, hydroxy, amino, sulphamoyl, C1-16alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkoxy, N—(C1-6alkyl)amino, N,N—(C1-6alkyl)2amino, C1-6alkanoylamino, N—(C1-6alkyl)carbamoyl, N,N—(C1-6alkyl)2carbamoyl, C1-6alkylS(O)a wherein a is 0 to 2, N—(C1-6alkyl)sulphamoyl, N,N—(C1-6alkyl)2sulphamoyl, C1-6alkylsulphonylamino, carbocyclyl, heterocyclyl, carbocyclylC1-3alkyl-R16—, heterocyclylC1-3alkyl-R17—, carbocyclyl-R18— and heterocyclyl-R19—;
- wherein R10, R13 and R14 are independently of each other substituted on carbon by one or more R20;
- and wherein if said heterocyclyl contains an —NH— moiety that nitrogen is optionally substituted by a group selected from R21;
- R16, R17, R18 and R19 are independently selected from —O—, —N(R22)—, —C(O)—, —N(R23)C(O)—, —C(O)N(R24)—, —S(O)s—, —SO2N(R25)— and —N(R26)SO2—;
- wherein R22, R23, R24, R25 and R26 are independently selected from hydrogen and C1-6alkyl;
- and s is 0, 1 or 2;
- R8, R15 and R21 are independently selected from C1-4alkyl, carbocyclyl, heterocyclyl, —C1-4alkylcarbocyclyl, —C1-4alkylheterocyclyl, C1-4alkanoyl, C1-4alkylsulphonyl and C1-4alkoxycarbonyl;
- wherein R8, R15 and R21 independently of each other may be optionally substituted on carbon by one or more R27;
- and
- R20 and R27 are independently selected from halo, cyano, hydroxy, trifluoromethoxy, trifluoromethyl, amino, methyl, ethyl, phenyl, cyclopropyl, cyclobutyl, methoxy, ethoxy, methylamino, ethylamino, dimethylamino, diethylamino, mesyl, ethylsulphonyl and phenyl;
- as a free base or a pharmaceutically acceptable salt thereof.
24 more elements
Dependencies are inferred from the claim text.