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    • 36. 发明授权
    • Thiazolidinediones and drugs containing them
    • 噻唑烷二酮类和含有它们的药物
    • US5599826A
    • 1997-02-04
    • US578561
    • 1995-11-21
    • Alfred MertensHans-Peter WolffPeter Freund
    • Alfred MertensHans-Peter WolffPeter Freund
    • C07D277/20A61K31/42A61K31/425A61K31/426A61K31/427A61P3/06A61P3/10C07D277/34C07D417/06C07D417/10C07D417/12C07D417/14
    • C07D417/12
    • Compounds of formula I ##STR1## in which A denotes a carbocyclic ring with 5 or 6 carbon atoms or a heterocyclic ring with a maximum of 4 heteroatoms in which the heteroatoms can be the same or different and denote oxygen, nitrogen or sulphur and the heterocycles can if desired carry an oxygen atom on one or several nitrogen atoms,B denotes --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N--, O or S,W denotes CH.sub.2, O, CH(OH), CO or --CH.dbd.CH--,X denotes S, O or NR.sup.2 in which the residue R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl,Y is CH or N,R denotes naphthyl, pyridyl, furyl, thienyl or phenyl which if desired is mono- or disubstituted with C.sub.1 -C.sub.3 alkyl, CF.sub.3, C.sub.1 -C.sub.3 alkoxy, F, Cl or bromine,R.sup.1 denotes hydrogen or C.sub.1 -C.sub.6 alkyl andn equals 1-3as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts,processes for their production as well as pharmaceutical agents that contain these compounds for the treatment of diabetes.
    • PCT No.PCT / EP94 / 01619 Sec。 371日期:1995年11月21日 102(e)日期1995年11月21日PCT 1994年5月19日PCT PCT。 第WO94 / 27995号公报 日期1994年12月8日,式I的化合物(I)其中A表示碳原子数5或6的碳环或最多有4个杂原子的杂环,其中杂原子可以相同或不同,表示 氧,氮或硫,如果需要,可以在一个或多个氮原子上带有氧原子,B表示-CH = CH-,-N = CH-,-CH = N-,O或S,W表示CH 2, O,CH(OH),CO或-CH = CH-,X表示残基R2为氢或C1-C6烷基,Y为CH或N的S,O或NR2,R为萘基,吡啶基,呋喃基,噻吩基 或苯基,如果需要,可以被C 1 -C 3烷基,CF 3,C 1 -C 3烷氧基,F,Cl或溴单取代或被二取代,R 1表示氢或C 1 -C 6烷基,n等于1-3,以及它们的互变异构体,对映异构体 ,非对映异构体和生理上耐受的盐,其生产方法以及含有这些化合物用于治疗糖尿病的药剂。
    • 39. 发明授权
    • Isoquinolinedione derivatives, pharmaceutical compositions and methods
of use
    • 异喹啉二酮衍生物,药物组合物和使用方法
    • US4824835A
    • 1989-04-25
    • US42300
    • 1987-04-24
    • Alfred MertensBernd Muller-Beckmann
    • Alfred MertensBernd Muller-Beckmann
    • C07D401/12A61K31/47A61K31/472A61P7/00A61P9/00A61P9/04A61P9/12C07D217/24C07D221/20C07D401/04
    • C07D221/20C07D217/24C07D401/04
    • The present invention provides isoquinolinedione derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical which is optionally interrupted by a heteroatom or by a heteroatom substituted with an alkyl radical, R.sub.2 is a hydrogen atom or an alkyl or alkenyl radical, or together with R.sub.1, represents a cycloalkylene, alkylidene or cycloalkylidene radical which is optionally interrupted by a heteroatom or by a heteroatom substituted by an alkyl radical and R.sub.3 is a radical of the general formula: ##STR2## which can be in the 5- 6-, 7- or 8-position of the isoquinoline-1,3-dione and in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or alkyl, trihaloalkyl, cycloalkyl, cycloalkenyl, dealkylaminoalkyl, alkoxycarbonylalkyl, alkylcarbonyl, aryl or heterayl radicals and X is an oxygen or sulphur atom or a radical of the general formula .dbd.N--R.sub.6, in which R.sub.6 is a hydrogen atom, a cyano group of an alkyl radical; and the physiologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. These new compounds have a blood pressure lowering effect and/or influence thrombocyte aggregation, improve the microcirculation, and exert a positive intropic effect, thus having therapeutic and prophylactic effects.
    • 本发明提供以下通式的异喹啉二酮衍生物:其中R 1是氢原子或任选地被杂原子或被烷基取代的杂原子间隔的烷基,烯基或环烷基,R2是 氢原子或烷基或链烯基,或与R 1一起表示亚环烷基,亚烷基或环亚烷基,其任选地被杂原子或被烷基取代的杂原子中断,并且R 3是以下通式的基团: 其可以在异喹啉-1,3-二酮的5-6,7-或8-位,其中可以相同或不同的R 4和R 5是氢原子或烷基,三卤代烷基, 环烷基,环烯基,脱烷基氨基烷基,烷氧基羰基烷基,烷基羰基,芳基或杂原子,X是氧或硫原子或通式= N-R6的基团,其中R6是氢原子,烷基的氰基; 及其生理上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。 这些新化合物具有降血压作用和/或影响血栓细胞聚集,改善微循环,并发挥阳性的临床效果,具有治疗和预防作用。