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US 2011/0257177 A1Published application
Benzylthiotetrazole inhibitors of store operated calcium release
AssigneeCalcimedica, Inc.
InventorsJeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
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Abstract
Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
Claims19
-66. (canceled)
A compound of Formula (I):
- wherein:
- X is H, C(O)NR3R4, C(O)OR4, C(O)R4, NR3C(O)NR3R4, C(O)NR3—C(O)NR3R4, CH2NHSO2-aryl, C1-C6alkyl, C1-C6alkenyl, C1-C6heteroalkyl or aryl;
- wherein C1-C6alkyl, C1-C6alkenyl, C1-C6heteroalkyl and aryl is optionally substituted with at least one R5;
- or
- when X is C(O)NR3R4, then R3 and R4 together with the nitrogen atom to which they are attached form a C2-C6heterocycloalkyl;
- Y is H, C1-C6alkyl, C1-C6alkenyl, C1-C6heteroalkyl;
- wherein C1-C6alkyl, C1-C6alkenyl, C1-C6heteroalkyl is optionally substituted with at least one Rs;
- R1 and R2 are each independently H, F, Cl, Br, I, —CN, —NO2, —OH, —CF3, —OR9, C1-C6alkyl, C3-C8cycloalkyl, C1-C6heteroalkyl, C1-C6haloalkyl, C2-C8heterocycloalkyl, optionally substituted aryl, optionally substituted O-aryl, optionally substituted heteroaryl, —NHS(═O)2R8, —S(═O)2N(R9)2, —N(R9)S(═O)2N(R9)2, —C(═O)CF3, —C(═O)NHS(═O)2R8, —S(═O)2NHC(═O)R8, —N(R9)2, —N(R9)C(═O)R8, —N(R9)C(═O)N(R9)2, —N(R9)C(═O)OR8, —CO2R9, —C(═O)R8, —OC(═O)R8, —OC(═O)N(R9)2, —CON(R9)2, —SR8, —S(═O)R8, and —S(═O)2R8;
- or
- two R2 and the carbon atoms to which they are attached form
- R3 is selected from H, C1-C6alkyl, C1-C6alkenyl, C1-C6heteroalkyl, C3-C8cycloalkyl;
- R4 is selected from H, aryl or heteroaryl;
- wherein aryl or heteroaryl is optionally substituted with at least one R5;
- R5 is selected from F, Cl, Br, I, —CN, —NO2, —OH, —CF3, —OR9, C1-C6alkyl, C3-C8cycloalkyl, C1-C6heteroalkyl, C1-C6haloalkyl, C2-C8heterocycloalkyl, optionally substituted aryl, optionally substituted O-aryl, optionally substituted heteroaryl, —NHS(═O)2R8, —S(═O)2N(R9)2, —N(R9)S(═O)2, N(R9)2, —C(═O)CF3, —C(═O)NHS(═O)2R8, —S(═O)2NHC(═O)R8, —N(R9)2, —N(R9)C(═O)R8, —N(R9)C(═O)N(R9)2, —N(R9)C(═O)OR8, —CO2R9, —C(═O)R8, —OC(═O)R8, —OC(═O)N(R9)2, —CON(R9)2, —SR8, —S(═O)R8, and —S(═O)2R8;
- n is an integer from 0-5;
- m is an integer from 0-5;
- each R8 is independently selected from C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl;
- each R9 is independently selected from H, C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl;
- or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof.
16 more elements
Dependencies are inferred from the claim text.