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公开(公告)号：EP1062212A1
公开(公告)日：2000-12-27
申请号：EP99915564.1
申请日：1999-03-04
发明人： MANTEGANI, Sergio , TRAQUANDI, Gabriella , BANDIERA, Tiziano , LANSEN, Jacqueline , VARASI, Mario
IPC分类号： C07D277/42 , C07D233/88 , A61K31/425 , A61K31/415
CPC分类号： C07D417/04 , C07D233/88 , C07D277/40 , C07D277/42
摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy; R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
摘要翻译： 其中R 1为氢，羟基，式OR 5基团其中R 5为C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 8环烷基，卤素，可未被取代或被C 1单或二取代的氨基的式（1） -C6烷基，C2-C6链烯基，芳烷基，酰基或三氟乙酰基; R 2是氢，羟基，基团NR 6 R 7，其中R 6和R 7独立地表示氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或与氮原子一起表示任选取代的C 3 -C 8 杂环; R3是氢，羟基; R4是2-取代的噻唑基或咪唑基系统及其药学上可接受的盐，可用于治疗淀粉样变性。 还描述了用于制备和药物组合物的方法。
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公开(公告)号：EP0907651A1
公开(公告)日：1999-04-14
申请号：EP97927149.0
申请日：1997-05-29
CPC分类号： C07D457/10 , A61K31/48 , C07D457/02
摘要： The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) wherein R1 represents a hydrogen atom or a linear or branched C1-C5 alkyl or C2-C5 alkenyl group optionally substituted with a C3-C7 cycloalkyl, a hydroxy group or a R3-substituted phenyl group wherein R3 is a hydroxy or a hydroxymethyl group; R2 represents a hydrogen atom or a linear or branched C1-C5 alkyl or a C2-C5 alkenyl group optionally substituted with a hydroxy group, or a R3-substituted phenyl group wherein R3 is as above defined, or with a C1-C5 alkoxy group; the symbols -- at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH2)nOH, wherein n is 0 or an integer from 1 to 3, or a group C(R4)2OH wherein R4 is a C1-C5 alkyl or a phenyl group, or a pharmaceutically acceptable salt thereof. Some compounds of formula (I) are novel. Processes for their preparation and pharmaceutical compositions containing them are also described.
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公开(公告)号：EP0628042B1
公开(公告)日：2001-08-16
申请号：EP94901903.8
申请日：1993-11-26
IPC分类号： C07D457/04 , A61K31/48 , C07D457/02 , C07D457/06
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 3.3.1.1.3,7) decan-1-yl, C¿1-5? 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.
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公开(公告)号：EP0885222B1
公开(公告)日：2001-05-30
申请号：EP97903245.5
申请日：1997-02-07
IPC分类号： C07D457/04 , A61K31/48 , C07D457/02
CPC分类号： C07D457/02 , C07D457/00
摘要： Ergoline derivative having formula (I) wherein R1 is hydrogen atom or C1-4 alkyl group; R2 is hydrogen, chlorine, or bromine atom, methyl or C1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in α or β configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.
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公开(公告)号：EP0853619B1
公开(公告)日：2000-11-02
申请号：EP96932552.1
申请日：1996-09-16
IPC分类号： C07D413/06 , A61K31/42
CPC分类号： C07D413/06
摘要： Disubstituted piperidine derivatives of formula (I), wherein R1 is hydrogen; bromo; chloro; a linear or branched C1-C5 alkyl group; a linear or branched C1-C5 alkoxy group; or an optionally substituted phenyl group; R2 is hydrogen, a linear or branched C1-C5 alkyl group or an optionally substituted phenyl group; X is CH2, C=O, CHOH or C=NOH; R3 is hydrogen or a linear or branched C1-C5 alkyl group; Y is a (CH2)n group in which n is an integer from 0 to 4, CHOH, C=O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; if the case, either as single isomers or as racemic mixtures, and their pharmaceutically acceptable salts, which possess selective neuroprotective activity, are useful in the treatment of an acute or a degenerative CNS disease. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
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公开(公告)号：EP0885222A1
公开(公告)日：1998-12-23
申请号：EP97903245.0
申请日：1997-02-07
IPC分类号： C07D457
CPC分类号： C07D457/02 , C07D457/00
摘要： Ergoline derivative having formula (I) wherein R1 is hydrogen atom or C1-4 alkyl group; R2 is hydrogen, chlorine, or bromine atom, methyl or C1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in α or β configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.
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公开(公告)号：EP1037890A1
公开(公告)日：2000-09-27
申请号：EP98959879.2
申请日：1998-11-23
IPC分类号： C07D417/12 , A61K31/425
CPC分类号： C07D417/06
摘要： The present invention relates to novel amino-benzothiazole derivatives, to their pharmaceutically acceptable salts, to a process for their preparation, to their use as neuroprotective agents and to pharmaceutically compositions comprising them.
摘要翻译： 本发明涉及新的氨基苯并噻唑衍生物，其药学上可接受的盐，它们的制备方法，它们作为神经保护剂的用途以及包含它们的药物组合物。
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公开(公告)号：EP0853619A1
公开(公告)日：1998-07-22
申请号：EP96932552.0
申请日：1996-09-16
CPC分类号： C07D413/06
摘要： Disubstituted piperidine derivatives of formula (I), wherein R1 is hydrogen; bromo; chloro; a linear or branched C1-C5 alkyl group; a linear or branched C1-C5 alkoxy group; or an optionally substituted phenyl group; R2 is hydrogen, a linear or branched C1-C5 alkyl group or an optionally substituted phenyl group; X is CH2, C=O, CHOH or C=NOH; R3 is hydrogen or a linear or branched C1-C5 alkyl group; Y is a (CH2)n group in which n is an integer from 0 to 4, CHOH, C=O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; if the case, either as single isomers or as racemic mixtures, and their pharmaceutically acceptable salts, which possess selective neuroprotective activity, are useful in the treatment of an acute or a degenerative CNS disease. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
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