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81. 发明公开

EP1392699A1 6H-OXAZOLO 4,5-E]INDOLE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND/OR SEROTONERGIC LIGANDS 有权
标题翻译： 6H-唑并[4,5-E]吲哚衍生物作为烟碱乙酰胆碱受体配体和/或血清素配体
公开(公告)号：EP1392699A1
公开(公告)日：2004-03-03
申请号：EP02727527.0
申请日：2002-04-05
申请人： MERCK PATENT GmbH
发明人： SCHIEMANN, Kai , BÖTTCHER, Henning , LEIBROCK, Joachim
IPC分类号： C07D498/04 , C07D519/00 , A61K31/42 , A61K31/435
CPC分类号： C07D498/04 , 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, compulsvie 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.

82. 发明公开

EP1368346A1 SUBSTITUTED BENZOFURAN-2-CARBOXAMIDES DERIVATIVES 审中-公开
标题翻译：取代的苯并呋喃-2-甲酰胺
公开(公告)号：EP1368346A1
公开(公告)日：2003-12-10
申请号：EP02729940.3
申请日：2002-02-27
申请人： MERCK PATENT GmbH
发明人： DORSCH, Dieter , BÖTTCHER, Henning , VAN AMSTERDAM, Christoph , RAUTENBERG, Wilfried , BARTOSZYK, Gerd
IPC分类号： C07D405/12 , C07D405/14 , A61K31/495
CPC分类号： C07D405/12
摘要： Compounds of the formula (I), in which D, R1, R2 and n are defined in Claim 1, are potent 5-HT¿1A? agonists and 5-HT reuptake inhibitors and are suitable for the treatment of depression, anxiety states, panic attacks, obsessive-compulsive disorders, psychiatric illnesses, cerebral infarction, cerebral ischaemia, tension states, side-effects in the treatment of high blood pressure, for the prophylaxis and therapy of cerebral illnesses, acromegaly, hypogonadism, secondary amenorrhoea, premenstrual syndrome, undesired puerperal lactation, pain, sleep disorders, narcolepsy, bipolar illnesses, mania, dementia, addiction illnesses, sexual dysfunction, eating disorders, obesity or fibromyalgia.

83. 发明授权

EP1228041B1 INDOLDERIVATE UND DEREN VERWENDUNG ALS 5HT2A LIGANDEN 有权
标题翻译：吲哚衍生物及其作为5HT2A配体的用途
公开(公告)号：EP1228041B1
公开(公告)日：2003-10-15
申请号：EP00954447.9
申请日：2000-07-07
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , MÄRZ, Joachim , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D209/12 , A61K31/404 , A61P43/00 , C07D403/06 , C07D409/06
CPC分类号： C07D209/12

84. 发明授权

EP0993458B1 3-BENZYLPIPERIDINE 失效
标题翻译： 3苄基哌啶
公开(公告)号：EP0993458B1
公开(公告)日：2003-04-09
申请号：EP98932135.1
申请日：1998-06-08
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , PRÜCHER, Helmut , GREINER, Hartmut , SEYFRIED, Christoph , BARBER, Andrew , MARTINEZ, Joseph-Maria
IPC分类号： C07D401/06 , A61K31/445 , C07D491/04
CPC分类号： C07D401/06

85. 发明公开

EP1292592A1 HETEROCYCLISCHE AMINOALKYLPYRIDINDERIVATE ALS PSYCHOPHARMAKA 有权
标题翻译：杂环烯丙基氨基甲酰基吡啶二胺
公开(公告)号：EP1292592A1
公开(公告)日：2003-03-19
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.
摘要翻译：本发明涉及式（1）杂环氨基烷基吡啶衍生物，其中R 1代表包含1至3个饱和，不饱和或芳族环结构的杂环基团，并且任选与其它环结构稠合形成稠合环体系，并且其包含总共1至4个N-，O-和/或S-原子，所述杂环任选被至少一个以下基团取代一次，两次或三次：-A，-OR 4，-N（ R4）2，-NO2，-CN，Hal，-COOR4，-CON（R4）2，-COR4，= O; R2表示任选被至少一个下列基团取代一次，两次，三次，四次或五次的苯基：Hal，A，-O-A，-NO 2，或CN，或任选被至少一个下列基团取代一次或两次的噻吩基：Hal，A，-O-A，-NO 2，-CN或噻吩基; -X-表示-O - ， - S-，亚磺酰基，磺酰基或-C（R 4）2 - -Y-代表 - [C（R4）2] n-; -Z-代表-C（R4）2-; 并且n代表1,2,3或4.本发明还涉及杂环氨基烷基吡啶衍生物的相容性盐和溶剂化物及其作为药物的用途。

86. 发明公开

EP1228041A2 INDOLDERIVATE UND DEREN VERWENDUNG ALS 5HT2A LIGANDEN 有权
标题翻译：吲哚衍生物及其作为5HT2A配体的用途
公开(公告)号：EP1228041A2
公开(公告)日：2002-08-07
申请号：EP00954447.9
申请日：2000-07-07
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , MÄRZ, Joachim , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D209/12 , A61K31/404 , A61P43/00 , C07D403/06 , C07D409/06
CPC分类号： C07D209/12
摘要： The invention relates to compounds of formula (I), wherein R?1 and R3¿ 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).

87. 发明公开

EP1202966A1 PIPERIDINALKOHOLE 有权
公开(公告)号：EP1202966A1
公开(公告)日：2002-05-08
申请号：EP00964004.6
申请日：2000-08-08
申请人： MERCK PATENT GmbH
发明人： PRÜCHER, Helmut , BÖTTCHER, Henning , ACKERMANN, Karl-August , GOTTSCHLICH, Rudolf , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D211/18 , C07D409/06 , C07D405/06 , C07D417/06 , C07D401/06 , A61K31/445 , A61K31/4523 , A61P25/00 , A61P25/16 , A61P25/18
CPC分类号： C07D401/06 , C07D211/22 , C07D405/06 , C07D409/06 , C07D417/06
摘要： The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT¿2A? antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).
摘要翻译：本发明涉及式（I）的化合物，其中R1，R2和A具有权利要求1中给出的含义，是有效的5-HT2A 拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经疾病，记忆障碍，帕金森病，肌萎缩侧索硬化症，阿尔茨海默氏病，亨廷顿舞蹈病，食欲紊乱如神经性贪食症和神经性厌食症，月经前期综合征和/ 强迫症（OCD）。

88. 发明公开

EP1194426A2 BENZOFURANDERIVATE 有权
标题翻译：苯并呋喃
公开(公告)号：EP1194426A2
公开(公告)日：2002-04-10
申请号：EP00949229.9
申请日：2000-06-29
申请人： MERCK PATENT GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , BÖTTCHER, Henning
IPC分类号： C07D405/06 , C07D307/85 , C07D307/80 , C07D413/06 , A61K31/343 , A61K31/4025 , A61K31/497 , A61K31/502 , A61K31/536 , A61P25/00
CPC分类号： C07D307/79 , C07D307/85 , C07D405/06 , Y02P20/55
摘要： Benzofurane derivatives of formula (I), wherein R and R' have the meanings given in claim no. (1), and salts thereof are suitable for use as intermediate products in the synthesis of medicaments.

89. 发明公开

EP1185272A2 NOVEL USE OF 1-[4-(5-CYANOINDOL-3YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE AND ITS PHYSIOLOGICAL ACCEPTABLE SALTS 有权
标题翻译： 1- USE [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪和其生理学可接受的盐用于治疗双相疾病和MANIE的
公开(公告)号：EP1185272A2
公开(公告)日：2002-03-13
申请号：EP00935031.5
申请日：2000-05-16
申请人： MERCK PATENT GmbH
发明人： BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph , BÖTTCHER, Henning , SEDMAN, Ewen
IPC分类号： A61K31/495
CPC分类号： A61K31/496 , A61K31/00 , A61K31/495 , A61K31/497
摘要： 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of sub-type anxiety disorders chosen from the sub-types panic disorder with or without agoraphobia, agoraphobia, obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized-anxiety disorder, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.

90. 发明公开

EP0993458A1 3-BENZYLPIPERIDINE 失效
标题翻译： 3苄基哌啶
公开(公告)号：EP0993458A1
公开(公告)日：2000-04-19
申请号：EP98932135.1
申请日：1998-06-08
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , PRÜCHER, Helmut , GREINER, Hartmut , SEYFRIED, Christoph , BARBER, Andrew , MARTINEZ, Joseph-Maria
IPC分类号： C07D401/06 , A61K31/445 , C07D491/04
CPC分类号： C07D401/06
摘要： The invention relates to piperidine derivatives of formula (I), wherein R1, R2, m and k have the meaning cited in Claim 1, and to their salts, to novel intermediate products and to a method for producing the inventive compounds. The compounds of formula (I) are potent σ-receptor ligands and have a 5-HT-reuptake inhibiting effect. They can be used to produce medicaments, e.g. in the treatment of disorders of the nervous system, cerebrovascular accidents, craniocerebral or spinal chord injuries or ischemic conditions.
摘要翻译：本发明涉及式（I）的哌啶衍生物，其中R 1，R 2，m和k具有权利要求1中引用的含义及其盐，涉及新的中间产物和制备本发明化合物的方法。式（I）化合物是有效的σ-受体配体并具有5-HT-再摄取抑制作用。它们可以用于生产药物，例如用于治疗神经系统疾病，脑血管意外，颅脑或脊髓损伤或缺血性疾病。

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