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    • 4. 发明申请
    • Novel condensed imidazole derivative
    • 新型稠合咪唑衍生物
    • US20070105890A1
    • 2007-05-10
    • US10580321
    • 2004-11-24
    • Hiroyuki NakahiraHidenori KimuraTomonori KobayashiHitoshi Hochigai
    • Hiroyuki NakahiraHidenori KimuraTomonori KobayashiHitoshi Hochigai
    • A61K31/4745C07D471/02
    • C07D471/14C07D471/04C07D491/14C07D495/14
    • Disclosed is a compound represented by the formula (1) below which has a high DPP-IV inhibitory activity and is improved in safety, toxicity and the like. Also disclosed is a prodrug of such a compound and pharmaceutically acceptable salts of them. (In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like; R2 and R3 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; R4 and R5 independently represent a hydrogen atom, an optionally substituted alkyl group or the like: R6 represents a hydrogen atom, an optionally substituted aryl group or the like; and —Y—NH2, represents a group represented by the following formula (A): (wherein m is 0, 1 or 2; and R7 may not exist or one or two R7 may exist and independently represent an optionally substituted alkyl group or the like) or the like.]
    • 公开了由下式(1)表示的化合物,其具有高的DPP-IV抑制活性,并且其安全性和毒性等得到改善。 还公开了这种化合物的前药和它们的药学上可接受的盐。 (式中,R 1表示氢原子,任选取代的烷基等; R 2和R 3独立地表示氢原子, 氢原子,任选取代的烷基等; R 4和R 5独立地表示氢原子,任选取代的烷基等: 6表示氢原子,任选取代的芳基等; -Y-NH 2表示由下式(A)表示的基团:(其中m为0 ,1或2; R 7可以不存在或一个或两个R 7可以存在并且独立地表示任选取代的烷基等)。
    • 5. 发明申请
    • Bicycle pyrazole derivative
    • 自行车吡唑衍生物
    • US20070082908A1
    • 2007-04-12
    • US10595125
    • 2004-08-25
    • Hiroyuki NakahiraHitoshi HochigaiTatsuya TakedaTomonori KobayashiWilliam Hume
    • Hiroyuki NakahiraHitoshi HochigaiTatsuya TakedaTomonori KobayashiWilliam Hume
    • A61K31/53A61K31/498C07D487/04
    • C07D487/04
    • A compound represented by the following formula (I), a prodrug thereof, or a pharmaceutically acceptable salt of either. These are compounds having high DPP-IV inhibitory activity and improved in safety, nontoxicity, etc. (I) [In the formula, R1 represents hydrogen, optionally substituted alkyl, etc.; the solid line and dotted line between A1 and A2 indicate a double bond (A1=A2), etc.; A1 represents a group represented by the formula C(R2), etc.; A2 represents a group represented by the formula C(R4), etc.; R2 represents hydrogen, optionally substituted alkyl, etc.; R4 represents hydrogen, optionally substituted alkyl, etc.; R6 represents hydrogen, optionally substituted aryl, etc.; and —Y represents, e.g.; a group represented by the formula (A): (A) (wherein m1 is 0, 1, 2, or 3; and R7 is absent, or one or two R7's are present and each independently represents optionally substituted alkyl, etc.).]
    • 由下式(I)表示的化合物,其前药或其药学上可接受的盐。 这些是具有高DPP-IV抑制活性和安全性,无毒性等改善的化合物。(I)[式中,R 1表示氢,任选取代的烷基等; A 1和A 2之间的实线和虚线表示双键(A 1 SUP 1 = A 2) )等 A 1表示由式C(R 2 O 2)表示的基团等; A <2>表示由式C(R 4)表示的基团等。 R 2表示氢,任选取代的烷基等; R 4表示氢,任选取代的烷基等; R 6表示氢,任选取代的芳基等; -Y表示例如 由式(A)表示的基团:(A)(其中m1为0,1,2或3; R 7为不存在,或一个或两个R 7为氢, SUP'是存在的,各自独立地表示任选取代的烷基等)。