申请人:Bayer Corporation
公开号:US06218431B1
公开(公告)日:2001-04-17
Substituted biphenyls having glucagon receptor antagonistic activity. Claimed compounds have the formula
wherein
R1a and R1b independently represent (C1-C6) alkyl; R2 represents (C1-C10) alkyl or substituted (C1-C10) alkyl wherein the substituents are independently from 1 to 3 of —SR7; R7 represents phenyl, or substituted phenyl wherein the substituents are independently 1-5 of halogen, trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, nitro, cyano, or hydroxyl; R3 represents substituted (C1-C6) alkyl wherein the substituents are 1-2 hydroxyl groups; G represents a substituent selected from the group consisting of halogen, (C1-C6) alkyl, and OR4 wherein R4 is H or (C1-C6) alkyl; and y is 0 or an integer of 1-3. Pharmaceutical compositions containing such compounds and methods of treatment of glucagon-mediated conditions by administering such compounds are also claimed.
具有胰高血糖素受体拮抗活性的取代联苯。所述化合物的结构式如下:其中R1a和R1b分别代表(C1-C6)烷基;R2代表(C1-C10)烷基或取代的(C1-C10)烷基,其中取代基独立地为1至3个-SR7;R7代表苯基,或取代的苯基,其中取代基独立地为1-5个卤素、三氟甲基、(C1-C6)烷基、(C1-C6)烷氧基、硝基、氰基或羟基;R3代表取代的(C1-C6)烷基,其中取代基为1-2个羟基;G代表从卤素、(C1-C6)烷基和OR4(其中R4为H或(C1-C6)烷基)组成的取代基;y为0或1-3的整数。还声明了含有这类化合物的药物组合物以及通过给予这类化合物治疗胰高血糖素介导疾病的方法。