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US 8,476,457 B2Granted
Indole, indazole and benzimidazole arylamides as P2X3 and P2X2/3 antagonists
AssigneeRoche Palo Alto LLC
InventorsMichael Patrick Dillon, Nancy Elisabeth Krauss
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Abstract
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
Claims14
A compound of formula III:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is:
- C1-6alkyl;
- or
- halo;
- R2 is:
- C3-6cycloalkyl;
- C1-6alkoxy-C1-6alkyl;
- hydroxy-C1-6alkyl;
- or
- heteroaryl-C1-6alkyl selected from:
- pyrazinyl-methyl;
- pyridazinyl-methyl;
- pyrimidinyl-methyl;
- 1-pyrazinyl-ethyl;
- 1-pyridazinyl-ethyl;
- and 1-pyrimidinyl-ethyl;
- wherein the pyrazinyl, pyridazinyl and pyrimidinyl portions thereof may be optionally substituted once with methyl;
- R3 is:
- C1-6alkyl;
- hydroxy-C1-6alkyl;
- C1-6alkoxy-C1-6alkyl;
- halo-C1-6alkyl;
- C3-6cycloalkyl;
- C3-6cycloalkyl-C1-6alkyl;
- phenyl optionally substituted with:
- halo, C1-6alkyl, C1-6alkoxy or halo-C1-6alkyl;
- or
- phenyl-C1-6alkyl wherein the phenyl portion thereof is optionally substituted with:
- halo, C1-6alkyl, C1-6alkoxy or halo-C1-6alkyl;
- and
- X is:
- N or CRa wherein Ra is hydrogen, C1-6alkyl or halo.
31 more elements
Dependencies are inferred from the claim text.