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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。

2. 发明申请

WO98054183A3 ERGOLINE DERIVATIVES 审中-公开
标题翻译： ERGOLINE衍生物
公开(公告)号：WO98054183A3
公开(公告)日：1999-03-04
申请号：PCT/EP1998/003125
申请日：1998-05-27
IPC分类号： A61K31/48 , A61K31/496 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D457/08 , C07D519/00 , C07D457/00
CPC分类号： C07D457/08
摘要： The invention provides compounds of formula (I), wherein R1 to R6 are as defined in the description, and a process for preparing them. The compounds of formula (I) are useful as pharmaceuticals.

3. 发明申请

WO2006128658A1 ERGOLINE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR LIGANDS 审中-公开
标题翻译： ERGOLINE衍生物及其作为化合物受体配体使用
公开(公告)号：WO2006128658A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005106
申请日：2006-05-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BAENTELI, Rolf , GLICKMAN, Fraser , KOVARIK, Jiri , LEWIS, Ian , STREIFF, Markus , THOMA, Gebhard , ZERWES, Hans-Günter
发明人： BAENTELI, Rolf , GLICKMAN, Fraser , KOVARIK, Jiri , LEWIS, Ian , STREIFF, Markus , THOMA, Gebhard , ZERWES, Hans-Günter
IPC分类号： C07D457/06 , C07D457/08 , A61K31/48
CPC分类号： C07D457/06 , C07D457/08
摘要： Disclosed are ergoline derivatives, Formula (I), wherein either each of R 1 and R 2 , independently, is H; optionally R 10 and/or R 11 -substituted-phenyl or - phenyl-C 1-4 alkyl; optionally R 10 and/or R 11 -substituted-heteroaryl or -heteroaryl-C 1-4 alkyl; optionally R 10 and/or R 11 -substituted heteroaryl N-oxide; optionally R 10 -substituted C 1 -C 8 alkyl; optionally R 10 -substituted C 2 -C 8 alkenyl, optionally R 10 -substituted C 2 -C 8 alkynyl; optionally R 10 -substituted C 3 -C 8 cycloalkyl, or optionally R 10 -substituted C 4 -C 8 cycloalkenyl; or R 1 and R 2 form together with the nitrogen atom to which they are attached an optionally R 10 -substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R 3 is H; OR 1 ; CH 2 R 1 R 2 ; (CH 2 ) 1-2 NR 1 R 2 ; CH 2 -CH 2 -OR 1 ; CH 2 -CO-NR 1 R 2 ; or CO-CH 2 R 1 R 2 ; R 4 is F; CI; Br; I; OR 1 ; NR 1 R 2 or has one of the significances given for R 1 ; and R 5 has one of the significances given for R 1 , in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.
摘要翻译：公开了麦角灵衍生物，式（I），其中R 1和R 2中的每一个独立地是H; 任选的R 10和/或R 11取代的苯基或 - 苯基-C 1-4烷基; 任选的R 10和/或R 11 - 取代的 - 杂芳基或 - 杂芳基-C 1-4 - 烷基; 任选的R 10和/或R 11 - 取代的杂芳基N-氧化物; 任选的R 10取代的C 1 -C 8烷基; 任选的R 10取代的C 2 -C 8链烯基，任选地R 10取代的C 2 C 8 -C 15炔基; 任选的R 10取代的C 3 -C 8环烷基，或任选地R 10取代的C 1 -C 10 - 4 -C 8环烯基; 或R 1和R 2 2与它们所连接的氮原子一起形成任选的R 10取代的3-8元环，其含有除了氮原子多达2个独立于N，O和S选择的杂原子; R 3是H; OR _{1 ; CH _{2 - [R _{1 - [R _{2 ; （CH _{2 ）_{1-2 NR _{1 - [R _{2 ; CH _{2 -CH _{2 -OR _{1 ; CH _{2 -CO-NR _{1 - [R _{2 ; 或CO-CH 2 R 1 R 2 R 2; R 4是F; CI; BR; 一世; OR _{1 ; NR 1 R 2 R 2或具有对R 1 1给出的含义之一; 和R 5具有游离形式或盐形式的R 1 1给出的意义之一，用于预防或治疗由趋化因子受体及其配体之间的相互作用介导的疾病或疾病。}}}}}}}}}}}}}}}

4. 发明申请

WO9854183A2 ERGOLINE DERIVATIVES 审中-公开
标题翻译： ERGOLINE衍生物
公开(公告)号：WO9854183A2
公开(公告)日：1998-12-03
申请号：PCT/EP9803125
申请日：1998-05-27
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , PFAEFFLI PAUL , NEUMANN PETER , SWOBODA ROBERT , STUETZ PETER
发明人： PFAEFFLI PAUL , NEUMANN PETER , SWOBODA ROBERT , STUETZ PETER
IPC分类号： A61K31/48 , A61K31/496 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D457/08 , C07D519/00 , C07D457/00
CPC分类号： C07D457/08
摘要： The invention provides compounds of formula (I), wherein R1 to R6 are as defined in the description, and a process for preparing them. The compounds of formula (I) are useful as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中R 1至R 6如说明书中所定义，及其制备方法。式（I）的化合物可用作药物。

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