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51. 发明公开

EP1397357A2 POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 有权
标题翻译： 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基）哌嗪盐酸盐的多晶型形式
公开(公告)号：EP1397357A2
公开(公告)日：2004-03-17
申请号：EP02754627.4
申请日：2002-06-05
申请人： MERCK PATENT GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
IPC分类号： C07D405/12
CPC分类号： A61K31/496 , C07D405/12 , C07D405/14
摘要： The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.

52. 发明公开

EP1383774A2 DIHYDROIMIDAZO[4,5-E]INDOLE AND 7H-PYRROLO[3,2-F]QUINOXALINE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND/OR SEROTONERGIC LIGANDS 有权
标题翻译： DIHYDROIMIDAZO¬4,5E-吲哚和7H-PYRROLO¬3,2-F喹喔啉ALS烟碱乙酰胆碱受体配体和/或血清素配体
公开(公告)号：EP1383774A2
公开(公告)日：2004-01-28
申请号：EP02735200.4
申请日：2002-03-30
申请人： MERCK PATENT GmbH
发明人： SCHIEMANN, Kai , BÖTTCHER, Henning , LEIBROCK, Joachim
IPC分类号： C07D519/00 , A61K31/4985 , A61K31/4188 , A61P25/00
CPC分类号： C07D519/00
摘要： Compounds of the formula (I) in which R?1, R2, R3 and R4¿ are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence. Strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.

53. 发明授权

EP0964863B1 OXAZOLIDINONE ALS 5-HT2A-ANTAGONISTEN 失效
标题翻译：恶唑烷酮的5-HT 2A拮抗剂
公开(公告)号：EP0964863B1
公开(公告)日：2003-05-21
申请号：EP98909397.6
申请日：1998-02-06
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , PRÜCHER, Helmut , GREINER, Helmut , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D413/14 , A61K31/445 , C07D491/056
CPC分类号： C07D413/14
摘要： The invention relates to novel oxazolidine derivatives of formula (I), wherein R?1, R2 and R3¿ have the meaning cited in Claim 1. The invention further relates to the salts thereof and to a method for the production of the inventive compounds. The compounds of formula (I) act as 5-HT¿2A? antagonists having a reuptake-inhibiting, antidepressant or anxiolytic effect and can be used in the production of medicaments.

54. 发明授权

EP1198453B1 N-(INDOLCARBONYL-)PIPERAZINDERIVATE ALS 5-HT2A-REZEPTOR LIGANDEN 有权
标题翻译： N-（吲哚羰基）哌嗪衍生物作为5-HT2A受体的配体
公开(公告)号：EP1198453B1
公开(公告)日：2003-04-09
申请号：EP00949288.5
申请日：2000-07-07
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D209/08 , A61K31/404 , A61P43/00 , C07D409/12 , C07D209/12 , C07D209/42 , C07D209/88 , C07D209/38
CPC分类号： C07D409/12 , C07D209/08

55. 发明公开

EP1233963A2 SULFONYLOXAZOLAMINE UND DEREN VERWENDUNG ALS 5-HT6 REZEPTORLIGANDEN 审中-公开
标题翻译： Sulfonyloxazolamines及其作为5-HT 6受体配体
公开(公告)号：EP1233963A2
公开(公告)日：2002-08-28
申请号：EP00990614.0
申请日：2000-11-24
申请人： MERCK PATENT GmbH
发明人： GERICKE, Rolf , BÖTTCHER, Henning , GASSEN, Michael , GREINER, Hartmut
IPC分类号： C07D413/04 , C07D263/48 , C07D213/81 , C07D213/82 , C07D333/38 , C07D307/68 , A61K31/422 , A61P25/00
CPC分类号： C07D213/81 , C07D213/82 , C07D307/68 , C07D333/38 , C07D413/04
摘要： The invention relates to compounds of the general formula (I), wherein R1 and R2 independently of one another represent H, -R6, C3-C8-cycloalkyl, -(CH2)n-R7, -(CH2)n-O-R6, -(CH2)n-NH2, -(CH2)n-NHR6, -(CH2)-N(R6)2, C2-C6-alkenyl or optionally together form a mononuclear saturated heterocycle with one or two nitrogen, oxygen and/or sulphur atoms; R3 and R4 independently of one another represent H, -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, or -N(R6)2; R5 represents a 5- or 6-member, saturated or unsaturated heterocycle with one or two nitrogen, oxygen and/or sulphur atoms, which is optionally monosubstituted or disubstituted by -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, or -N(R6)2; and R6 represents C1-C6-alkyl; R7 together with R3 and/or R4 represents substituted phenyl, n represents 0 to 2. The invention also relates to the physiologically safe salts or solvates of said compounds and to the use of the compounds of the general formula (I) as medicaments.

56. 发明公开

EP1198453A2 N-(INDOLCARBONYL-)PIPERAZINDERIVATE ALS 5-HT2A-REZEPTOR LIGANDEN 有权
标题翻译： N-（吲哚羰基）哌嗪衍生物作为5-HT2A受体的配体
公开(公告)号：EP1198453A2
公开(公告)日：2002-04-24
申请号：EP00949288.5
申请日：2000-07-07
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D209/08 , A61K31/404 , A61P43/00 , C07D409/12 , C07D209/12 , C07D209/42 , C07D209/88 , C07D209/38
CPC分类号： C07D409/12 , C07D209/08
摘要： The invention relates to compounds of formula (I) wherein R?1, R2, R4 and R5¿ have the meaning given in Claim 1. Said compounds are potent 5-HT¿2A?-antagonists and are suitable for the treatment of psychosis, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, e.g. nervous bulimia and anorexia, and premenstrual syndrome and/or for positively influencing compulsive behaviours (obsessive-compulsive disorder, OCD).

57. 发明公开

EP1098892A1 BIPHENYL DERIVATIVES 审中-公开
标题翻译： BIPHENYL DERIVATE
公开(公告)号：EP1098892A1
公开(公告)日：2001-05-16
申请号：EP99934632.3
申请日：1999-07-08
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , VAN AMSTERDAM, Christoph , HARTING, Jürgen , WIKSTRÖM, Hakan, Vilhelm , LIAO, Yi
IPC分类号： C07D295/135 , A61K31/496 , C07D295/18 , C07D271/10 , C07D271/06 , A61K31/4245
CPC分类号： C07D271/06 , C07D271/10 , C07D295/135 , C07D295/192
摘要： Biphenyl derivatives of formula (I) wherein R, X, Y, A?1, A2, A3¿, Q and n are as defined in Claim 1, and their salts, are active on the central nervous system showing serotonin antagonistic properties.

58. 发明公开

EP0998474A1 PIPERAZIN-DERIVATE 失效
标题翻译：哌嗪衍生物
公开(公告)号：EP0998474A1
公开(公告)日：2000-05-10
申请号：EP98938671.9
申请日：1998-06-29
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , BARTOSZYK, Gerd , GREINER, Hartmut , SEYFRIED, Christoph
IPC分类号： C07D405/12 , A61K31/495
CPC分类号： C07D405/12
摘要： The invention relates to piperazine derivatives of formula (I), wherein R1, m, k and R2 have the meaning given in Claim 1. Said piperazine derivatives are potent 5-HT¿1A? agonists, have 5-HT-re-uptake inhibiting effects and are suitable for treating and preventing anxiety states, depression, schizophrenia, obsessive thoughts, tardive dyskensia, learning impairments and memory disturbances caused by age, for positively influencing compulsive behaviour, and for treating and combating the effects of cerebral infarctions, such as strokes and cerebral ischaemia.

59. 发明授权

EP1292592B1 HETEROCYCLISCHE AMINOALKYLPYRIDINDERIVATE ALS PSYCHOPHARMAKA 有权
标题翻译：杂环AMINOALKYLPYRIDINDERIVATE AS药物
公开(公告)号：EP1292592B1
公开(公告)日：2011-04-20
申请号：EP01956484.8
申请日：2001-06-19
申请人： Merck Patent GmbH
发明人： DORSCH, Dieter , BÖTTCHER, Henning , ARLT, Michael , GOTTSCHLICH, Rudolf , SEYFRIED, Christoph , BARTOSZYK, Gerd , HARTING, Jürgen
IPC分类号： C07D401/12 , C07D417/12 , A61K31/4427 , C07D405/12 , C07D213/64
CPC分类号： C07D213/64 , C07D213/38 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to formula (1) heterocyclic aminoalkyl pyridine derivatives, whereby R1 represents the radical of a heterocycle comprising 1 to 3 ring structures which are saturated, unsaturated or aromatic and optionally annellated with other ring structures to form a condensed ring system, and which comprise a total of 1 to 4 N-, O- and/or S-atoms, said heterocycle being optionally substituted once, twice or three times by at least one of the following groups: -A, -OR?4, -N(R4)¿2, -NO2, -CN, Hal, -COOR4, -CON(R4)2, -COR4, = O; R2 represents a phenyl group which is optionally substituted once, twice, three, four or five times by at least one of the following groups: Hal, A, -O-A, -NO¿2? or CN, or a thienyl group which is optionally substituted once or twice by at least one of the following groups: Hal, A, -O-A, -NO2, -CN or thienyl; -X- represents -O-, -S-, sulfinyl, sulfonyl, or -C(R?4)¿2-; -Y- represents -[C(R4)2]n-; -Z- represents -C(R4)2-; and n represents 1, 2, 3 or 4. The invention also relates to the compatible salts and solvates of the heterocyclic aminoalkyl pyridine derivatives and the use thereof as pharmaceuticals.

60. 发明授权

EP1397357B1 POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 有权
标题翻译： 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基苯并呋喃-5-基）哌嗪盐酸盐的多晶型
公开(公告)号：EP1397357B1
公开(公告)日：2009-07-29
申请号：EP02754627.4
申请日：2002-06-05
申请人： Merck Patent GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
IPC分类号： C07D405/12
CPC分类号： A61K31/496 , C07D405/12 , C07D405/14
摘要： The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
摘要翻译：本发明涉及1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪的盐酸盐的新晶体改性，二盐酸盐 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪和无定形1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪盐酸盐，其特别适用于制备用于治疗或预防抑郁症，焦虑症，双相性精神障碍，躁狂症，痴呆症，物质相关的固体药物功能障碍，性功能障碍，进食障碍，肥胖症，纤维肌痛，睡眠障碍，精神障碍，脑梗塞，紧张症，用于治疗性腺功能减退症，继发性闭经，经前期综合症和不希望的产褥期泌乳的副作用。

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