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3-substituted pyrido4,3:4,5thieno2,3-dpyrimidine derivatives, their preparation and their use

机译:3-取代的吡啶并4,3:4,5thieno2,3-dpyrimidine衍生物,其制备方法和用途

摘要

A 3-substituted 3,4,5,6,7,8-hexahydropyrido4,3:4,5thieno2,3-dpyrimidine compound of formula I ;wherein;R1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,;R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,;A is NH or oxygen,;B is hydrogen or methyl,;C is hydrogen, methyl or hydroxyl,;X is nitrogen,;Y is CH2, CH2C2, CH2C2CH2 or CH2CH,;Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, and;n is 2, 3 or 4,;or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.
机译:化学式I的3-取代的3,4,5,6,7,8-六氢吡啶基4,3:4,5thieno2,3-dpyrimidine化合物<化学ID =“ CHEM-US-00001”> <图像文件=“ US06222034- 20010424-C00001.GIF“ imgContent =” undefined“ imgFormat =” GIF“ /> ;其中; R 1 是氢,C 1 -C 4 -烷基,乙酰基或苯甲酰基,可选取代的苯基-C 1 -C 4 -烷基,萘基-C 1 -C 3 -烷基,苯基-C 2 -C 3 -烷酮或苯基氨基甲酰基-C 2 -烷基,; R 2 是任选取代的苯基,吡啶基,嘧啶基或吡嗪基,或任选取代的双环,其中两个稠合环之一是苯基,吡啶基,嘧啶基或吡嗪基环;; A是NH或氧, ; B为氢或甲基;; C为氢,甲基或羟基;; X为氮;; Y为CH 2 ,CH 2 C 2 ,CH 2 C 2 CH 2 或CH 2 CH,; Z为N,C或CH以及Y和Z之间的键是单键或双键,并且n是2、3或4;或其生理上可耐受的盐,以及包含它们的组合物及其作为5HT拮抗剂的用途 1B 和5HT 1A ,用于治疗抑郁症和相关疾病。

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