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US 8,895,589 B2Granted
Pyridinyl amides as P2X3 and P2X2/3 inhibitors
AssigneeRoche Palo Alto LLC
InventorsChris Allen Broka, Ronald Charles Hawley
Life of this patent
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Abstract
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 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.
Claims16
A compound of formula I
- wherein:
- R1 is:
- pyridinyl substituted with methyl or halo at the 5-position;
- R2 is:
- hydrogen;
- or
- C1-6alkyl;
- R3 is:
- C1-6alkyl;
- hydroxy-C1-6alkyl;
- C1-6alkoxy-C1-6alkyl;
- halo-C16alkyl;
- C3-7cycloalkyl;
- heteroaryl which may be substituted once or twice with methyl;
- heterocyclyl;
- heterocyclyl-C1-6alkyl;
- or
- C3-7cycloalkyl-C1-6alkyl;
- or R2 and R3 together form a C3-7cycloalkyl;
- R4 is:
- hydrogen;
- C1-6alkyl;
- C3-7cycloalkyl;
- C3-7cycloalkyl-C1-6alkyl;
- or
- pyrimidinyl;
- R5 is:
- C1-6alkyl;
- C1-6alkoxy;
- C3-7cycloalkyl;
- C1-6alkoxy-C1-6alkyl;
- amino-C1-6alkyl;
- oxetanyl which may be substituted once or twice with C1-6alkyl;
- phenyl which may be substituted once or twice with a group or groups independently selected from C1-6alkyl, halo, halo-C1-6alkyl and C1-6alkoxy;
- thienyl which may be substituted once or twice with a group or groups independently selected from C1-6alkyl and C1-6alkoxy;
- furanyl which may be substituted once or twice with C1-6alkyl;
- thiazolyl which may be substituted once or twice with C1-6alkyl;
- oxazolyl which may be substituted once or twice with C1-6alkyl;
- isoxazolyl which may be substituted once or twice with a group or groups independently selected from C1-6alkyl and phenyl;
- pyrazolyl which may be substituted once or twice with C1-6alkyl;
- thiadiazolyl which may be substituted once with C1-6alkyl;
- tetrahydropyranyl;
- morpholinyl;
- piperidinyl which may be substituted with C1-6alkyl or acetyl;
- pyrimidinyl;
- or
- pyridinyl which may be substituted once or twice with C1-6alkyl;
- and
- R6, R7 and R8 each independently is:
- hydrogen;
- or
- halo.
49 more elements
Dependencies are inferred from the claim text.