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US 7,402,596 B2Granted
Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
AssigneeRenovis, Inc.
InventorsMichael G. Kelly, John Kincaid
Life of this patent
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Abstract
Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Claims41
A bicycloheteroaryl compound having a formula:
- wherein
- A is selected from CO;
- B and Y are independently selected from CR2a and CR2aR2b;
- W, W′ and Z are independently selected from CR4;
- L1 is a bond or a C1-C5 alkylene group which can be optionally substituted by a substituent selected from alkyl, hydroxy, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, halogen, carbamoyl, and C1-C6 alkoxy;
- n is 0, 1, 2 or 3;
- R1 is selected from 3-13 membered cycloalkyl, which can be optionally substituted with one or more substituents independently selected from halo, hydroxyl, amino, cyano, sulfo, sulfanyl, sulfinyl, amido, carboxy, ester, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, and sulfonamido;
- each of R2a, R2b, R2′ and R2″ is independently selected from hydrogen, substituted or unsubstituted C1-C6 alkyl;
- or any of R2′ and R2″ can join together to form a cycloalkyl or cycloheteroalkyl ring of 3-7 atoms;
- R3 is selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted bicycloaryl, and substituted or unsubstituted bicycloheteroaryl;
- provided that, when L1 is a bond, R3 may be selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl;
- R4 is selected from H, alkyl, substituted alkyl, acyl, substituted acyl, substituted or unsubstituted acylamino, substituted or unsubstituted alkylamino, substituted or unsubstituted alkythio, substituted or unsubstituted alkoxy, alkoxycarbonyl, substituted alkoxycarbonyl, substituted or unsubstituted alkylarylamino, arylalkyloxy, substituted arylalkyloxy, amino, aryl, substituted aryl, arylalkyl, substituted or unsubstituted sulfo, substituted or unsubstituted sulfonyl, substututed or unsubstituted sulfanyl, substituted or unsubstituted aminosulfonyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted dihydroxyphosphoryl, substituted or unsubstituted aminodihydroxyphosphoryl, azido, carboxy, substituted or unsubstituted carbamoyl, cyano, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloheteroalkyl, substituted or unsubstituted dialkylamino, halo, heteroaryloxy, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroalkyl, hydroxy, nitro, and thiol;
- and the dotted bond is a single or a double bond;
- or a pharmaceutically acceptable salt;
- and stereoisomers and tautomers thereof.
12 more elements
Dependencies are inferred from the claim text.