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US 2013/0096122 A1Published application
Fused heterocyclic compounds as ion channel modulators
AssigneeGilead Sciences, Inc.
InventorsMatthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
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Abstract
The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
Claims24
A compound of Formula (I):
- wherein:
- R1 is hydrogen or alkyl of 1-6 carbon atoms optionally substituted by 1, 2 or 3 groups chosen from hydroxyl, alkoxy, halo, —C(O)R, aryl, cycloalkyl, heterocyclyl, and heteroaryl, wherein said aryl, cycloalkyl, heterocyclyl, or heteroaryl groups are optionally substituted by one, two, or three groups independently chosen from halo, hydroxyl, alkyl, —C(O)R, haloalkyl, alkoxy, aryl, or cycloalkyl;
- in which R is hydroxy, alkoxy, or —NH2,
- R2 and R3 are each independently hydrogen, halo, alkoxy of 1-6 carbon atoms, optionally substituted alkyl of 1-6 carbon atoms, —CF3, —O—CF3, or —CN, or
- R2 and R3, taken together with the carbon to which they are both attached form an optionally substituted cycloalkyl;
- R4 is phenyl optionally substituted by 1, 2, or 3 substituents independently selected from the group consisting of alkyl of 1-6 carbon atoms, cycloalkyl, aryl, heteroaryl, heterocyclyl, halo, —NO2, —CF3, —O—CF3, —CN, —O—R8, —S—R8, —N(R8)(R9), —S(═O)—R8, —S(═O)2R8, —S(═O)2—N(R8)(R9), —S(═O)2—O—R8, —N(R8)—C(O)—R9, —N(R8)—C(O)—O—R9, —N(R8)—C(O)—N(R8)(R9), —C(O)—R8, —C(O)—O—R8, —C(O)—N(R8)(R9), and —N(R8)—S(═O)2—R9, wherein each said alkyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl is further optionally substituted with halo, —NO2, —CF3, —O—CF3, —N(R8)(R9), —C(O)—R8, —C(O)—O—R8, —C(O)—N(R8)(R9), —CN, or —O—R8,
- in which R8 and R9 are independently chosen from the group consisting of hydrogen, alkyl of 1-6 carbon atoms, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, heterocyclyl, aryl, and heteroaryl are optionally substituted with one, two, or three substituents independently selected from halo, alkyl, mono- or dialkylamino, alkyl or aryl;
- R5 and R6 are each independently hydrogen, halo, alkoxy, optionally substituted alkyl of 1-6 carbon atoms, —CF3, —O—CF3, or —CN, or
- R5 and R6, taken together with the carbon to which they are both attached form an optionally substituted cycloalkyl;
- R7 is hydrogen, halo, cyano, or alkyl of 1-6 carbon atoms optionally substituted by hydroxyl, alkoxy, halo, or —C(O)R,
- X1 and X2 are independently —N═ or —C(R10)═, wherein R10 is selected from hydrogen, halo, hydroxyl, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, —CF3, —O—CF3, —CN, or —N(R8)(R9);
- or a pharmaceutically acceptable salt, ester, prodrug, or solvate thereof.
9 more elements
Dependencies are inferred from the claim text.