| 摘要 |
The present invention provides a compound of Formula I;;or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon. |
| 主权项 |
1. A compound of Formula Ia′ or a pharmaceutically acceptable salt thereof, wherein
R1 is (C1-C6)alkyl which is optionally substituted with one to three fluoro, hydroxy or methoxy; (C3-C7)cycloalkyl which is optionally substituted with one to two fluoro or one to two (C1-C3)alkyl which are each optionally substituted with one to three fluoro and wherein one carbon of the (C3-C7)cycloalkyl can be replaced with an O; or (C3-C7)cycloalkyl-(C1-C6)alkyl wherein the (C3-C7)cycloalkyl group of said (C3-C7)cycloalkyl-(C1-C6)alkyl is optionally substituted with one to two (C1-C3)alkyl which are each optionally substituted with one to three fluoro;R2 is hydrogen or (C1-C3)alkyl;R3′ is —(CH2)2CO2R, —CH2CHFCO2R, or —CH2CH(OH)CO2R;R is (C1-C4)alkyl, benzyl, para-methoxybenzyl, or diphenylmethylene;A1 and A2 are each independently CR4 or N, with the proviso that at least one of A1 and A2 is CR4;R4 at each occurrence is independently hydrogen, halo, cyano, (C1-C3)alkyl optionally substituted with one to three fluoro, (C1-C3)alkoxy optionally substituted with one to three fluoro, or (C3-C5)cycloalkyl; B1, B2, B3 and B4 are each independently CR5 or N, with the proviso that no more than two of B1, B2, B3 and B4 are N; and
R5 at each occurrence is independently hydrogen, halo, cyano, (C1-C3)alkyl optionally substituted with one to three fluoro, or (C1-C3)alkoxy optionally substituted with one to three fluoro, or (C3-C5)cycloalkyl. |
