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1. 发明申请

WO1994014806A1 SEROTONINERGIC ERGOLINE DERIVATIVES 审中-公开
标题翻译：丝氨酸蛋白衍生物
公开(公告)号：WO1994014806A1
公开(公告)日：1994-07-07
申请号：PCT/EP1993003337
申请日：1993-11-26
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , MANTEGANI, Sergio , BRAMBILLA, Enzo , CACCIA, Carla , CARFAGNA, Nicola
IPC分类号： C07D457/04
CPC分类号： C07D457/04 , C07D457/02 , C07D457/08 , C07D457/12
摘要： The present invention provides compounds of formula (I) wherein A represents OH, NH2, COOR3', OCONHR4, CONHR4, NHCOR4, NHCO2R4, NHC(X)NHR4, NHC(X)NHCOR4, (a) or (b), R1 is hydrogen or C1-4 linear or branched alkyl; R2 is hydrogen, chlorine, bromine or an S-C1-4 alkyl group; R3 and R3' are, independently, C1-5 alkyl or hydrogen, n is 0,1 or 2, m is 1 or 2; R4 is hydrogen, C1-7 alkyl, C3-7 cycloalkyl, adamantidyl (tricyclo 3.3.1.1. ) decan-1-yl, C1-5 alkylphenyl, C2 alkenylphenyl; C2 alkynylphenyl, phenyl optionally substituted by one or more groups selected from C1-4 alkyl, C1-3 alkoxy, methylendioxy, cyano, trifluoromethyl, hydroxy, nitro and acetyl; an optionally substituted naphthyl ring or phenyl condensed with a heterocyclic ring system having 5- or 6- ring members including 1 to 4 heteroatoms selected from nitrogen, oxygen and sulphur; a heterocyclic ring having 5 or 6 ring members including 1 or 2 heteroatoms selected from nitrogen, oxygen and sulphur which is optionally substituted by a group selected from C1-4 alkyl, phenyl optionally substituted as defined above, C1-3 alkoxy and halogen; R5 is hydrogen, C1-4 alkyl or a phenyl group and X is NH, O, S; or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.
摘要翻译：本发明提供式（I）化合物，其中A代表OH，NH2，COOR3'，OCONHR4，CONHR4，NHCOR4，NHCO2R4，NHC（X）NHR4，NHC（X）NHCOR4，（a）或（b）氢或C 1-4直链或支链烷基; R2是氢，氯，溴或S-C1-4烷基; R3和R3'独立地为C1-5烷基或氢，n为0,1或2，m为1或2; R4是氢，C1-7烷基，C3-7环烷基，金刚烷基（三环3.3.1.1。<3,7>）癸烷-1-基，C1-5烷基苯基，C2链烯基苯基; C 2炔基苯基，任选被一个或多个选自C 1-4烷基，C 1-3烷氧基，甲氧基，氰基，三氟甲基，羟基，硝基和乙酰基的基团取代的苯基; 任选取代的萘基环或与具有5-或6-个环成员的杂环系统缩合的苯基，包括1至4个选自氮，氧和硫的杂原子; 具有5或6个环成员的杂环，包括1或2个选自氮，氧和硫的杂原子，其任选被选自C 1-4烷基，任选如上所定义的苯基，C 1-3烷氧基和卤素的基团取代; R5是氢，C1-4烷基或苯基，X是NH，O，S; 或其药学上可接受的盐。还提供了其制备方法和包含它们的药物组合物。

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