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91. 发明公开

EP1633741A1 INDOL-DERIVATE ALS SEROTONIN-WIEDERAUFNAHME-INHIBITOREN 审中-公开
标题翻译：吲哚衍生物血清素回收抑制剂
公开(公告)号：EP1633741A1
公开(公告)日：2006-03-15
申请号：EP04734515.2
申请日：2004-05-24
申请人： Merck Patent GmbH
发明人： HEINRICH, Timo , BÖTTCHER, Henning , SCHIEMANN, Kai , HÖLZEMANN, Günter , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , LEIBROCK, Joachim , SEYFRIED, Christoph
IPC分类号： C07D405/12 , A61K31/4045 , A61P25/00
CPC分类号： C07D405/12
摘要： Disclosed are compounds of formula (I), the use thereof for producing a medicament utilized for treating diseases related to the serotonin receptor and/or serotonin reuptake, especially for producing a medicament utilized as an anxiolytic, antidepressant, neuroleptic, and/or antihypertensive and/or for positively influencing obsessive-compulsive behavior (OCD), sleeping disorders, tardive dyskinesia, learning disorders, age-related memory defects, eating disorders such as bulimia, and/or sexual dysfunctions. The inventive compounds bond to the 5-HT1A receptor.

92. 发明公开

EP1611126A1 CHROMENONINDOLE 有权
公开(公告)号：EP1611126A1
公开(公告)日：2006-01-04
申请号：EP04718300.9
申请日：2004-03-08
申请人： Merck Patent GmbH
发明人： SCHIEMANN, Kai , BÖTTCHER, Henning , HEINRICH, Timo , HÖLZEMANN, Günter , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , LEIBROCK, Joachim , SEYFRIED, Christoph
IPC分类号： C07D405/12 , A61K31/495
CPC分类号： C07D405/12
摘要： The invention relates to the chromenone indole derivatives of formula (I), wherein R1, R2, R3, R, A and B are defined as in claim 1 and to the pharmaceutically useful prodrugs, derivatives, solvates, stereoisomers and salts thereof. The inventive substances have particular effects on the central nervous system, in particularly they are 5 HT reuptake inhibitors and 5 HTx agonists and/or antagonists. They are characterized by an especially good bioavailability and excellent inhibition of 5 HT reuptake.
摘要翻译：本发明涉及式（I）的苯并吡喃酮吲哚衍生物，其中R1，R2，R3，R，A和B如权利要求1中所定义，并涉及其药学上有用的前药，衍生物，溶剂合物，立体异构体和盐。本发明的物质对中枢神经系统具有特殊的作用，特别是它们是5HT再摄取抑制剂和5HTx激动剂和/或拮抗剂。它们具有特别良好的生物利用度和优异的5HT再摄取抑制作用。

93. 发明授权

EP1317430B1 (2-AZABICYCLO [2.2.1]HEPT-7-YL)METHANOL-DERIVATE ALS NIKOTINISCHE ACETYLCHOLINREZEPTOR AGONISTEN 有权
标题翻译：（2-氮杂双环[2.2.1]庚-7-基）甲醇衍生物作为烟碱乙酰胆碱受体激动剂
公开(公告)号：EP1317430B1
公开(公告)日：2005-05-18
申请号：EP01965274.2
申请日：2001-09-11
申请人： MERCK PATENT GmbH
发明人： SCHIEMANN, Kai , LEIBROCK, Joachim
IPC分类号： C07D209/52 , C07D401/12 , A61K31/403 , A61P25/00
CPC分类号： C07D401/12 , C07D209/52
摘要： The invention relates to substances of general formula (I), wherein X is selected from the following group: NH, NR4, O and S, R1 is selected from the following group: hydrogen, linear and branched, substituted and unsubstituted C¿1?-C10-alkyl groups, substituted and unsubstituted C5-C10-aryl groups, substituted and unsubstituted C4-C10-heteroaryl groups, acyl groups, thioacyl groups, carbonyl carboxy groups, N-organyl-substituted carbamoyl groups and organosulfonyl groups, R?2, R3¿, independently of each other, are chosen from the following group: C¿1?-C10-alkyl groups, C5-C12-aryl groups and C4-C12-heteroaryl groups, these groups being unsubstituted or having one or more substitutents which are chosen independently of each other from the following group: halogens, alkoxy groups, aryloxy groups, nitro groups, C1-C5-alkoxycarbonyl groups, alkyl or acyl groups and cyano groups, optionally substituted with fluorine, and R?4¿ is selected from the following group: hydrogen, linear and branched, substituted and unsubstituted C¿1?-C10-alkyl groups, substituted and unsubstituted C5-C10-aryl groups, substituted and unsubstituted C4-C10-heteroaryl groups, acyl groups, thioacyl groups, carbonyl carboxy groups, N-organyl-substituted carbamoyl groups and organosulfonyl groups; or a physiologically compatible salt thereof.

94. 发明公开

EP3183239A1 INDAZOLES 有权
标题翻译：吲唑
公开(公告)号：EP3183239A1
公开(公告)日：2017-06-28
申请号：EP15744882.0
申请日：2015-07-30
申请人： Merck Patent GmbH , Cancer Research Technology Ltd.
发明人： SCHIEMANN, Kai , MALLINGER, Aurélie
IPC分类号： C07D231/56 , C07D471/04 , A61K31/416 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/437 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K31/55 , C07D231/56 , C07D401/06 , C07D403/06
摘要： The invention provides novel substituted indazole compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
摘要翻译：本发明提供了式（I）的新型取代的吲唑化合物，其制备和用于治疗过度增殖性疾病如癌症，炎性或退行性疾病的用途。

95. 发明授权

EP2488504B1 SULFOXIDEDERIVATE ZUR BEHANDLUNG VON TUMOREN 有权
标题翻译： SULFOXIDEDERIVATE用于肿瘤的治疗
公开(公告)号：EP2488504B1
公开(公告)日：2016-07-06
申请号：EP10754433.0
申请日：2010-09-14
申请人： Merck Patent GmbH
发明人： SCHIEMANN, Kai , SCHULTZ, Melanie , STAEHLE, Wolfgang
IPC分类号： C07D249/18 , C07D263/58 , A61K31/4192 , A61K31/423 , A61P35/00
CPC分类号： C07D249/18 , C07D263/58

96. 发明授权

EP2807154B1 AZAHETEROCYCLIC COMPOUNDS 有权
标题翻译：氮杂 - 杂环CONNECTIONS
公开(公告)号：EP2807154B1
公开(公告)日：2015-12-23
申请号：EP13701200.1
申请日：2013-01-10
申请人： Merck Patent GmbH , Cancer Research Technology Ltd
发明人： SCHIEMANN, Kai , STIEBER, Frank , ESDAR, Christina
IPC分类号： C07D241/20 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D495/04 , A61K31/4965 , A61K31/497 , A61K31/416 , A61K31/4725 , A61P31/00
CPC分类号： C07D409/12 , A61K31/4965 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5415 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D495/04

97. 发明授权

EP2552914B1 BENZONAPHTHYRIDINAMINE ALS AUTOTAXIN-INHIBITOREN 有权
标题翻译： BENZONAPHTHYRIDINAMINE ALS抑制剂自分泌运动因子
公开(公告)号：EP2552914B1
公开(公告)日：2015-11-11
申请号：EP11706181.2
申请日：2011-02-28
申请人： Merck Patent GmbH
发明人： STAEHLE, Wolfgang , SCHULTZ, Melanie , SCHIEMANN, Kai
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00
CPC分类号： C07D471/04

98. 发明授权

EP2209777B1 THIAZOLDERIVATE ZUR BEHANDLUNG VON KREBS 有权
标题翻译：噻唑基癌症治疗
公开(公告)号：EP2209777B1
公开(公告)日：2015-07-29
申请号：EP08802403.9
申请日：2008-09-19
申请人： Merck Patent GmbH
发明人： SCHIEMANN, Kai , SCHULTZ, Melanie , BLAUKAT, Andree , KOBER, Ingo , STAEHLE, Wolfgang
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427 , A61P35/00
CPC分类号： C07D417/12 , C07D417/14

99. 发明公开

EP2742029A1 N-(BENZIMIMDAZOL-2-YL)-CYCLOPROPANE CARBOXAMIDES AS LYSOPHOSPHATIDIC ACID ANTAGONISTS 失效
标题翻译： N-（BENZIMIMDAZOL-2-YL）-CYCLOPROPAN CARBOXAMIDE ALS LYSOPHOSPHATIDINSUREURE ANTAGONISTS
公开(公告)号：EP2742029A1
公开(公告)日：2014-06-18
申请号：EP12733424.1
申请日：2012-07-07
申请人： Merck Patent GmbH
发明人： STAEHLE, Wolfgang , SCHULTZ, Melanie , SCHIEMANN, Kai
IPC分类号： C07D235/30 , A61K31/4184 , A61P29/00 , A61P35/00
CPC分类号： C07D473/00 , A61K31/416 , A61K31/4184 , A61K31/437 , A61K31/454 , A61K31/52 , C07D231/56 , C07D235/30 , C07D235/32 , C07D401/12 , C07D403/12 , C07D417/04 , C07D471/04
摘要： The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative inflammatory diseases, such as cancer, fibrosis or arthritis.

100. 发明授权

EP2414330B1 Piperidine and piperazine derivatives as autotaxin inhibitors 有权
标题翻译：哌啶和哌嗪衍生物作为抑制剂汽车出租车
公开(公告)号：EP2414330B1
公开(公告)日：2013-05-01
申请号：EP10707470.0
申请日：2010-03-03
申请人： Merck Patent GmbH
发明人： SCHIEMANN, Kai , SCHULTZ, Melanie , STAEHLE, Wolfgang
IPC分类号： C07D211/30 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/10 , A61K31/4427 , A61K31/4523 , A61P35/00 , A61P25/28 , A61P29/00 , A61P27/02 , A61P9/00
CPC分类号： C07D401/14 , A61K31/4545 , A61K31/496 , C07D211/26 , C07D211/30 , C07D249/18 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/10

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