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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：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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3.发明公开AMINO ANTHRACYCLINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF AMYLOIDOSIS 有权AMINOANTHRACYCLINONDERIVATE及其用于治疗淀粉样变性
公开(公告)号：EP1062206A2
公开(公告)日：2000-12-27
申请号：EP99910304.7
申请日：1999-02-25
发明人： BANDIERA, Tiziano , FANCELLI, Daniele , VARASI, Mario , CARUSO, Michele , LANSEN, Jacqueline , SUARATO, Antonino
IPC分类号： C07D211/70 , C07D405/06 , A61K31/65
CPC分类号： C07D405/06 , C07D211/70
摘要： A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represents hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
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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：EP0843675A1
公开(公告)日：1998-05-27
申请号：EP96927580.0
申请日：1996-07-23
CPC分类号： C07D401/06 , C07D209/56 , C07H15/24
摘要： Compounds of formula (1) wherein X1 and X2 are C=O, C=NH or CH2, X3 is CH2, CO, CHOH, formula (III), formula (IV) wherein n=2 or 3, and C=N(R9) wherein R9 is hydroxy or amino-aryl, and each of R1, R2, R3, R4, R5, R6, R7 and R8 are hydrogen, halogen or an organic residue, are useful in the treatment of amyloidosis. A process for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译： 其中X 1和X 2为C = O，C = NH或CH 2，X 3为CH 2，CO，CHOH，式（III），式（IV），其中n = 2或3，和C = N R9），其中R9是羟基或氨基 - 芳基，并且R1，R2，R3，R4，R5，R6，R7和R8中的每一个是氢，卤素或有机残基，可用于治疗淀粉样变性。 还描述了它们的制备方法和含有它们的药物组合物。
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7.发明公开IMINO-AZA-ANTHRACYCLINONE DERIVATIVES FOR THE TREATMENT OF AMYLOIDOSIS 失效亚胺基AZA-ANTHRACYCLONDERIVATE用于治疗淀粉样变性
公开(公告)号：EP0970080A1
公开(公告)日：2000-01-12
申请号：EP98901964.1
申请日：1998-01-09
发明人： CARUSO, Michele , FAIARDI, Daniela , BANDIERA, Tiziano , LANSEN, Jacqueline , SUARATO, Antonino
IPC分类号： C07D471/08 , A61K31/435
CPC分类号： C07D471/08 , A61K31/435
摘要： A compound of formula (1), wherein R1 and R2 are independently selected from hydrogen and an organic residue, and R3 is a group of the formula OR6 or NR7R8, or a pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis.
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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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9.发明公开COMPOUNDS AND METHODS FOR DIAGNOSING AND TREATING AMYLOID-RELATED CONDITIONS 审中-公开化合物和方法进行诊断和治疗淀粉样蛋白相关疾病
公开(公告)号：EP1318982A1
公开(公告)日：2003-06-18
申请号：EP01968919.9
申请日：2001-09-17
发明人： RAUB, Thomas, J. , TANIS, Steven, P. , BUHL, Allen, Edwin , CARTER, Donald, Bainbridge , BANDIERA, Tiziano , LANSEN, Jacqueline , PELLERANO, Cesare , SAVINI, Luisa
IPC分类号： C07D215/38 , A61K31/47
CPC分类号： C07D215/38 , A61K31/47 , A61K45/06 , A61K51/0455 , A61K2300/00 , A61K31/00
摘要： The invention provides methods for diagnosing and treating amyloid-related conditions and compounds useful for the same. The invention provides for detecting, imaging, monitoring, diagnosing, and treating conditions characterized by the binding or aggregation of amyloid fibrils. More particularly, the invention relates to using quinolinehydrazone compounds for diagnosing and treating amyloidotic conditions and also as an antioxidant.
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公开(公告)号：EP0910415A1
公开(公告)日：1999-04-28
申请号：EP97928258.0
申请日：1997-06-18
发明人： BANDIERA, Tiziano , FANCELLI, Daniele , CARUSO, Michele , LANSEN, Jacqueline , SUARATO, Antonino
CPC分类号： C07D295/185 , A61K49/06 , C07C225/24 , C07C2603/44 , C07D295/112 , C07D295/26 , C07H15/252
摘要： Compounds of formula (A), wherein R1, R2, R3, Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their preparation, and pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP97 / 03234。 371日期1998年12月14日第 102（e）日期1998年12月14日PCT提交1997年6月18日PCT公布。 公开号WO97 / 49433 日期：1997年12月31日其中R1，R2，R3，Y和Z为有机取代基的式（A）化合物可用于诊断淀粉样变性; 一些式（A）的化合物是新的。 还描述了它们的制备方法和含有它们的药物组合物。
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