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US 2010/0160384 A1Published application
Dihydropyridone amides as p2x7 modulators
AssigneeRoche Palo Alto LLC
InventorsJacob Berger, Christine E. Brotherton-Pleiss, Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker, Shu-Hai Zhao
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Abstract
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, R1, R2, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Claims25
A compound of formula I:
- or pharmaceutically acceptable salts thereof,
- wherein:
- m is 0 or 1;
- n is 0 or 1;
- p is from 0 to 4;
- q is 0 or 1;
- R1 is:
- hydrogen;
- C1-6alkyl;
- hydroxy-C1-6alkyl;
- C1-6alkoxy-C1-6alkyl;
- hydroxy C1-6alkoxy-C1-6alkyl;
- or
- aminocarbonyl-C1-6alkyl;
- R2 is:
- optionally substituted aryl;
- optionally substituted heteroaryl;
- C3-6cycloalkyl;
- or
- C1-6alkyl;
- and
- R3 is:
- hydrogen;
- C1-6alkyl;
- alkylcarbonylalkyl;
- or
- alkoxycarbonylalkyl;
- R4 and R5 each independently is:
- hydrogen;
- or
- C1-6alkyl;
- each R6 is independently:
- halo;
- C1-6alkyl;
- C1-6alkoxy;
- halo-C1-6alkyl;
- halo-C1-6alkoxy;
- C1-6alkylsulfonyl;
- C1-6alkylsulfanyl;
- C1-6alkylsulfinyl;
- phenylsulfonyl wherein the phenyl portion is optionally substituted with C1-6alkyl;
- nitrile;
- hydroxy;
- C1-6alkylcarbonyl;
- aminocarbonyl;
- C1-6alkoxycarbonyl;
- C1-6alkoxycarbonyl-C1-6alkoxy;
- hydroxycarbonyl;
- hydroxycarbonyl-C1-6alkoxy;
- C1-6alkylaminocarbonyl-C1-6alkoxy;
- C1-6alkoxy-C1-6alkoxy;
- hydroxy-C1-6alkoxy;
- C1-6alkylamino-C1-6alkoxy;
- C1-6alkylsulfonyl-C1-6alkoxy;
- hydroxy-C1-6alkyl;
- C3-6cycloalkyl-C1-6alkoxy;
- amino;
- amino-C1-6alkyl;
- C1-6alkenyl;
- C1-6alkynyl;
- morpholinyl;
- morpholinyl-C1-6alkyl;
- piperazinyl;
- piperidinyloxy;
- aminocarbonyl-C1-6alkoxy;
- C1-6alkoxyamino-C1-6alkyl;
- hydroxy-C1-6alkylamino-C1-6alkyl;
- C1-6alkoxycarbonylamino-C1-6alkyl;
- C1-6alkylcarbonylamino-C1-6alkyl;
- C1-6alkylaminocarbonyl;
- C1-6alkoxycarbonylC1-6alkyl;
- C1-6alkylaminocarbonyl-C1-6alkyl;
- C1-6alkylamino-C1-6alkyl;
- hydroxycarbonyl-C1-6alkyl;
- hydroxy C1-6alkoxy-C1-6alkyl;
- or nitro;
- or two adjacent substituents may form a C1-2alkylenedioxy or halo-C1-2alkylenedioxy;
- and
- A is a five or six membered heteroaryl ring that is optionally substituted.
76 more elements
Dependencies are inferred from the claim text.