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US 8,524,763 B2Granted
Inhibitors of store operated calcium release
AssigneeCalcimedica, Inc.
InventorJeffrey P. Whitten
Life of this patent
Estimating the term…
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.
Claims13
A pharmaceutical composition comprising a pharmaceutically acceptable diluent, excipient or binder, and a compound of Formula (I):
- wherein:
- L is a bond;
- R is hydrogen, CO2R1, an optionally substituted heteroaryl, or an optionally substituted heterocycloalkyl;
- R1 is hydrogen, C1-C6alkyl, C1-C6cycloalkyl, C1-C6haloalkyl, phenyl or benzyl;
- R2 is cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, or heteroarylalkenyl, wherein cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, or heteroarylalkenyl is optionally substituted with at least one R5;
- R3 and R6 are each independently hydrogen, C1-C6alkyl, —C(O)—C1-C6alkyl, or —C(O)NR1—C1-C6alkyl, wherein C1-C6alkyl is optionally substituted with at least one R5;
- R4 is aryl or heteroaryl;
- wherein aryl or heteroaryl is optionally substituted with at least one R5;
- each R5 is independently selected from F, Cl, Br, I, —CN, alkyne, C1-C6 alkylalkyne, —NO2, —OH, —CF3, —OCF3, —OR8, C1-C6alkyl, C3-C8 cycloalkyl, C1-C6heteroalkyl, C1-C6haloalkyl, tetrazolyl, C2-C8heterocycloalkyl, optionally substituted 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;
- each R8 is independently selected from C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl;
- and
- each R9 is independently selected from H, C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl;
- or pharmaceutically acceptable salt thereof.
10 more elements
A pharmaceutical composition comprising a pharmaceutically acceptable diluent, excipient or binder, and a compound selected from:
- or pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof.
A compound of Formula (I):
- wherein:
- L is a bond;
- R is hydrogen, CO2R1, an optionally substituted heteroaryl, or an optionally substituted heterocycloalkyl;
- R1 is hydrogen, C1-C6alkyl, C1-C6cycloalkyl, C1-C6haloalkyl, phenyl or benzyl;
- R2 is cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, or heteroarylalkenyl, wherein cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, or heteroarylalkenyl is optionally substituted with at least one R5;
- R3 and R6 are each independently hydrogen, C1-C6alkyl, —C(O)—C1-C6alkyl, or —C(O)NR1—C1-C6alkyl, wherein C1-C6alkyl is optionally substituted with at least one R5;
- R4 is aryl or heteroaryl;
- wherein aryl or heteroaryl is optionally substituted with at least one R5;
- each R5 is independently selected from F, Cl, Br, I, —CN, alkyne, C1-C6 alkylalkyne, —NO2, —OH, —CF3, —OCF3, —OR8, C1-C6alkyl, C3-C8cycloalkyl, C1-C6heteroalkyl, C1-C6haloalkyl, tetrazolyl, C2-C8heterocycloalkyl, optionally substituted 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;
- each R8 is independently selected from C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl;
- and
- each R9 is independently selected from H, C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl;
- or
- a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.