申请人:Dainippon Sumitomo Pharma Co., Ltd.
公开号:US07601728B2
公开(公告)日:2009-10-13
Compounds represented by the general formula (I), prodrugs thereof, or pharmaceutically acceptable salts of both are provided as compounds which have high DPP-IV inhibiting activity and are improved in safety, toxicity and so on: (I)
wherein the solid line and dotted line between A1 and A2 represents a double bond (A1═A2) or the like; A1 is C(R4) or the like; A2 is nitrogen atom or the like; R1 is hydrogen atom, optionally substituted alkly group, or the like; R2 is hydrogen atom, optionally substituted alkyl group, or the like; R3 is hydrogen atom, halogen atom, or the like; R4 is hydrogen atom, hydroxyl, halogen atom, or the like; and Y is a group represented by the general formula (A) or the like; (A)
[wherein m1 is 0, 1, 2 or 3; and the group (A) may be freed from R6 or substituted with one or two R6's which are each independently halogen atom or the like.]
提供了由一般式(I)表示的化合物、其前药或两者的药学上可接受的盐,这些化合物具有高DPP-IV抑制活性,并在安全性、毒性等方面得到改善:(I)其中A1和A2之间的实线和虚线表示双键(A1═A2)或类似物;A1是C(R4)或类似物;A2是氮原子或类似物;R1是氢原子、可选择的取代烷基或类似物;R2是氢原子、可选择的取代烷基或类似物;R3是氢原子、卤原子或类似物;R4是氢原子、羟基、卤原子或类似物;Y是由一般式(A)或类似物表示的基团;(A)[其中m1为0、1、2或3;基团(A)可以从R6中解放出来,或用一个或两个R6取代,这些R6各自独立地是卤原子或类似物。]