Substituted octahydrocyclopenta[c]pyrroles as calcium channel modulators

摘要

The present application relates to calcium channel inhibitors containing compounds of formula (I);
wherein α, R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

主权项

1. A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein α is a single bond; R1 is —N(Rx)C(O)G3; Ra and Rb, at each occurrence, are each independently hydrogen, alkyl, arylalkyl, halogen, haloalkyl, hydroxy, hydroxyalkyl, or OR1a; wherein the aryl of arylalkyl is unsubstituted or substituted with 1, 2 3, 4, or 5 substituents independently selected from the group consisting of alkyl, haloalkyl, and halogen; R1a is alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, or haloalkyl; wherein said aryl, the aryl of arylalkyl, cycloalkyl and the cycloalkyl of cycloalkylalkyl are independently unsubstituted or substituted with 1, 2 3, 4, or 5 substituents independently selected from the group consisting of alkyl, haloalkyl, and halogen; Rx is hydrogen or alkyl; R2a is hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, or haloalkyl; wherein said aryl, the aryl of arylalkyl, cycloalkyl, and the cycloalkyl of cycloalkylalkyl are independently unsubstituted or substituted with 1, 2 3, 4, or 5 substituents independently selected from the group consisting of alkyl, haloalkyl, and halogen; R2b is alkyl or haloalkyl; G3, at each occurrence, is independently aryl or heteroaryl; wherein G3 at each occurrence is independently unsubstituted or substituted with 1, 2, 3, 4, or 5 substituents selected from the group consisting of alkyl, alkenyl, alkynyl, cyano, haloalkyl, halogen, nitro, N(R2a)2, N(R2a)C(O)R2a, OR2a, C(O)R2a, C(O)OR2a, C(O)N(R2a)2, SO2R2b, and SO2N(R2a)2; m, at each occurrence, is independently 1, 2, 3, 4, 5, or 6; R2 is alkyl, haloalkyl, G3 or —(CRaRb)m-G3; R3 is hydrogen, alkyl, haloalkyl, G3 or —(CRaRb)m-G3; R4 is hydrogen, G5, or —(CRaRb)m-G3; and G5 is aryl or heteroaryl; wherein G5 is independently unsubstituted or substituted with 1, 2, 3, 4, or 5 substituents selected from the group consisting of alkyl, alkenyl, alkynyl, cyano, haloalkyl, halogen, nitro, N(R2a)2, N(R2a)C(O)R2a, OR2a, C(O)R2a, C(O)OR2a, C(O)N(R2a)2, SO2R2b, and SO2N(R2a)2; and wherein the G5 is other than quinolizinone or quinolone.