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US 8,134,004 B2Granted
Substituted N-bicyclicalkyl bicycliccarboxyamide compounds
AssigneePfizer Inc.
InventorsTadashi Kawashima, Satoshi Nagayama, Kazunari Nakao, Hirotaka Tanaka
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Abstract
This invention provides a compound of the formula (I): And their use for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.
Claims12
A compound of the formula (I):
- wherein ring A is
- wherein
- one of X1 and X3 is N, another of X1 and X3 is NH or S, and X2 is N or CR5,
- one of X1 and X3 is CH2, another of X1 and X3 is NH or N, and X2 is C═O or N,
- one of X1 and X3 is CR6, another of X1 and X3 is NH, and X2 is N or CR5,
- X1 and X3 are NH and X2 is C═O, or
- Y1 is N or CR7, Y2 is N or CR8, Y3 is N or CR9 and Y4 is N or CR10;
- the substitution site of ring B is the alpha- or beta-position;
- E is CH or N;
- G, J and K are each CH;
- F is CH or C—CH3;
- L is N and T is CH;
- R1 and R2 are each independently hydrogen, (C1-C6)alkyl, or hydroxy(C1-C6)alkyl;
- R3 is hydrogen;
- R4 is (C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkyl(C3-C6)cycloalkyl, (C1-C4)alkoxy(C1-C6)alkyl optionally substituted with halo or halo(C2-C6)alkyl optionally substituted with hydroxy, R5 and R6 are each independently hydrogen, (C1-C6)alkyl, hydroxy(C1-C6)alkyl or hydroxy(C1-C6)alkoxy-(C1-C6)alkyl;
- R7, R8, R9 and R10 are each independently hydrogen, halo, (C1-C6)alkyl, hydroxy(C1-C6)alkyl or hydroxy(C1-C6)alkoxy-(C1-C6)alkyl;
- and each dotted bond is a single or a double bond;
- or a pharmaceutically acceptable salt thereof.
15 more elements
A compound according to 8 wherein said compound being of formula (Ia)
- wherein R1 is methyl and R2 is H, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.