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1. 发明授权

US4277470A Heterocyclic spiro-linked amidines, compositions and use thereof 失效
标题翻译：杂环螺连脒，其组合物和用途
公开(公告)号：US4277470A
公开(公告)日：1981-07-07
申请号：US123200
申请日：1980-02-21
申请人： Manfred Forsch , Wolfgang Schaub , Hermann Gerhards
发明人： Manfred Forsch , Wolfgang Schaub , Hermann Gerhards
IPC分类号： A61K31/40 , A61K31/403 , A61P25/24 , A61P25/26 , C07C205/05 , C07D209/96 , C07D401/04 , C07D401/14 , C07D413/04 , C07D471/10 , A61K31/54 , C07D207/22 , C07D295/00
CPC分类号： C07D471/10 , C07C205/05 , C07D209/96
摘要： Heterocyclic, spiro-linked amidines of the formula I ##STR1## and their physiologically acceptable salts, in which (a) n is 1 or 2; (b) R.sup.1 and R.sup.2 are hydrogen or alkyl radicals which, together with the nitrogen atom, can form a 5-, 6- or 7-membered ring which can be substituted by C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.2 -alkoxy, hydroxyl or C.sub.1 -C.sub.4 -alkoxy-carbonyl groups and in which one of the carbon atoms can also be replaced by an oxygen, sulfur or nitrogen atom, it being possible for the nitrogen atom to be substituted by hydrogen, by the formyl group or by a phenyl radical, which can in turn be monosubstituted or polysubstituted by a C.sub.1 to C.sub.4 -alkyl group or an alkoxy, methylenedioxy, hydroxyl, halogen, nitro or amino group, or it being possible for the nitrogen atom to be substituted by a C.sub.1 -C.sub.4 -alkyl group, or in which R.sup.1 represents hydrogen and R.sup.2 represents a C.sub.5 -C.sub.8 -cycloalkyl radical which can be substituted by C.sub.1 -C.sub.4 -dialkylamino groups; (c) R.sup.3 is hydrogen or methyl and (d) R.sup. 4 denotes a phenyl radical which is optionally monosubstituted or polysubstituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, methylenedioxy, hydroxyl, halogen, cyano, nitro, trifluoromethyl, amino, C.sub.2 -C.sub.5 -acylamino or mono- or di-C.sub.1 -C.sub.4 -alkylamino groups, or a thiophene radical, their stereoisomers and optical isomers, processes for their preparation and antidepressive medicaments containing these compounds.
摘要翻译：式（I）的杂环，螺相连的脒和它们的生理上可接受的盐，其中（a）n为1或2; （b）R 1和R 2是氢或烷基，其与氮原子一起可以形成可被C 1 -C 3烷基，C 1 -C 2烷氧基，羟基取代的5-，6-或7-元环或C 1 -C 4 - 烷氧基 - 羰基，并且其中一个碳原子也可以被氧，硫或氮原子替代，氮原子可被氢取代，甲酰基或甲酰基取代苯基，其又可以被C1至C4-烷基或烷氧基，亚甲二氧基，羟基，卤素，硝基或氨基单取代或多取代，或者氮原子可被C1-C4 - 烷基，或其中R1表示氢，R2表示可被C1-C4二烷基氨基取代的C5-C8-环烷基; （c）R 3是氢或甲基，（d）R 4表示苯基，其任选被C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，亚甲二氧基，羟基，卤素，氰基，硝基，三氟甲基，氨基，C 2 -C 5酰基氨基或单或二C 1 -C 4烷基氨基或噻吩基团，它们的立体异构体和光学异构体，其制备方法和含有这些化合物的抗抑郁药物。

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