公开(公告)号：EP1611122B1

公开(公告)日：2007-06-13

申请号：EP04718926.1

申请日：2004-03-10

申请人： Merck Patent GmbH

发明人： SCHADT, Oliver ,  ARLT, Michael ,  FINSINGER, Dirk ,  SCHIEMANN, Kai ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D401/04 ,  C07D231/10 ,  A61K31/435

CPC分类号： C07D231/12 ,  C07D231/40 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14

摘要： The invention relates to compounds of formula (I), in addition to their salts and solvates. In said formula, X, R1, R2, R3, R4 and R5 are defined as cited in claim (1). Said compounds are suitable for use as ligands of 5 HT receptors.

公开(公告)号：EP1569930B1

公开(公告)日：2007-01-03

申请号：EP03779945.9

申请日：2003-11-17

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  CRASSIER, Helene ,  BÖTTCHER, Henning ,  HEINRICH, Timo ,  SCHIEMANN, Kai ,  LEIBROCK, Joachim ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D417/12 ,  A61K31/433 ,  A61K31/4245 ,  A61P43/00 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D417/12

摘要： The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above.

公开(公告)号：EP1626967A1

公开(公告)日：2006-02-22

申请号：EP04718277.9

申请日：2004-03-08

申请人： Merck Patent GmbH

发明人： SCHIEMANN, Kai ,  ACKERMANN, Karl-August ,  ARLT, Michael ,  FINSINGER, Dirk ,  SCHADT, Oliver ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D401/04 ,  A61K31/415 ,  A61P25/28

CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D231/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D409/06 ,  C07D409/10 ,  C07D413/12 ,  C07D451/06 ,  C07D453/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/08

摘要： The invention relates to the compounds of formula (I) and the salts and solvates thereof, wherein X, R1, R2, R3, R4 and R5 are defined as in claim 1. The inventive compounds are suitable as ligands of 5 HT receptors.

摘要翻译： 本发明涉及式（I）化合物及其盐和溶剂化物，其中X，R 1，R 2，R 3，R 4和R 5如权利要求1中所定义。本发明化合物适合作为5HT受体的配体。

公开(公告)号：EP1592687A1

公开(公告)日：2005-11-09

申请号：EP04701298.4

申请日：2004-01-10

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  BÖTTCHER, Henning ,  SCHIEMANN, Kai ,  HEINRICH, Timo ,  LEIBROCK, Joachim ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D405/12 ,  A61K31/40 ,  A61P25/18

CPC分类号： C07D405/12

摘要： The invention relates to novel benzofurane derivatives of formula (I) wherein R1, R2, X, Y, Z and m have the designations cited in patent claim 1. Said compounds have a strong affinity towards 5-HT1A receptors, inhibit the resumption of serotonin, have serotonin-agonistic and serotonin-antagonistic characteristics, and are suitable for using as antidepressants, anxiolytics, antipsychotics, neuroleptics and/or antihypertonics.

公开(公告)号：EP1366039B1

公开(公告)日：2005-09-07

申请号：EP01273302.8

申请日：2001-12-24

申请人： Merck Patent GmbH

发明人： BÖTTCHER, Henning ,  BARTOSZYK, Gerd ,  HARTING, Jürgen ,  VAN AMSTERDAM, Christoph ,  SEYFRIED, Christoph

IPC分类号： C07D403/06 ,  A61K31/495 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D215/48 ,  A61K31/495 ,  C07D217/26

公开(公告)号：EP1140898B1

公开(公告)日：2002-08-28

申请号：EP98966851.2

申请日：1998-12-22

申请人： MERCK PATENT GmbH

发明人： MATZEN, Lisa ,  BÖTTCHER, Henning ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  HARTING, Jürgen ,  RAUTENBERG, Wilfried

IPC分类号： C07D401/04 ,  A61K31/40 ,  C07D401/06 ,  C07D209/14 ,  C07D401/14 ,  C07D209/16

CPC分类号： C07D401/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/06 ,  C07D401/14

公开(公告)号：EP1497279B1

公开(公告)日：2011-03-09

申请号：EP03720455.9

申请日：2003-04-11

申请人： Merck Patent GmbH

发明人： SCHADT, Oliver ,  BÖTTCHER, Henning ,  LEIBROCK, Joachim ,  SCHIEMANN, Kai ,  HEINRICH, Timo ,  HÖLZEMANN, Günter ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D401/06 ,  A61K31/404 ,  A61P43/00 ,  C07D405/12 ,  C07D209/42 ,  C07D471/04 ,  C07D417/12 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D231/12 ,  C07D209/42 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The invention relates to substituted indoles of formula (I) and to their physiologically safe derivatives and salts, wherein R1, D, E, R12, p, X1, E, G, X2 and Z have the meanings as cited in Claim 1. These substituted indoles and their physiologically safe derivatives and salts have particular effects on the central nervous system, above all, effects that inhibit 5HT-resumption and 5 HTx-agonistic and/or antagonistic effects and, in particular, serotonin, agonistic and antagonistic properties, and can be used as antipsychotics, antidepressants, anxiolytics and/or antihypertensives. These compositions can also be used as excitatory amino acid antagonists for fighting neurodegenerative diseases including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease or Huntington's disease, cerebral ischemias, infarcts or psychoses.

公开(公告)号：EP1817323A1

公开(公告)日：2007-08-15

申请号：EP05811335.8

申请日：2005-11-07

申请人： Merck Patent GmbH

发明人： MEDERSKI, Werner ,  VAN AMSTERDAM, Christoph ,  BURGER, Christa ,  GREINER, Hartmut

IPC分类号： C07H15/203 ,  A61K31/706 ,  A61P3/10 ,  A61K31/7068

CPC分类号： C07H15/203

摘要： The invention relates to the novel compounds of formula (I) wherein T, E, R, R , R , R1, R2 and R2 are defined as in claim 1. The novel compounds are suitable as antidiabetics.

公开(公告)号：EP1562596B1

公开(公告)日：2006-08-30

申请号：EP03811744.6

申请日：2003-10-30

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  SCHIEMANN, Kai ,  HEINRICH, Timo ,  BÖTTCHER, Henning ,  LEIBROCK, Joachim ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： A61K31/4439 ,  A61K31/4709 ,  C07D401/12

CPC分类号： C07D401/12

摘要： The invention relates to novel derivatives of indole of a formula (I) wherein X, Y, R1, R1', m and n are as defined in a first claim. Said compounds exhibit a high affinity with respect to the receptors 5-HT1A and a partial affinity with respect to the receptors 5-HT1D. The compounds inhibit the recapture of serotonin, exhibit agonistic and antagonistic properties with respect to said serotonin and can be used as antidepressant and anxiolitic and for curing neurogenerative disorders.

公开(公告)号：EP1633742A1

公开(公告)日：2006-03-15

申请号：EP04734520.2

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 ,  C07D405/14 ,  A61K31/4045 ,  A61P25/00

CPC分类号： C07D405/12 ,  C07D405/14

摘要： The invention relates to compounds of formula (I) used for producing drugs for treating diseases related to a serotonin receptor and/or a serotonin reabsorption, in particular for producing drugs like anxiolitic, antidepressive, neuroleptic and/or antihypertensive drugs and/or for positively influencing obsessional compulsive troubles, sleep disorders, tardive dyskinesia, learning troubles, gerontal memory loss, eating disorders such as bulimia and/or irritable bowel syndrome and/or sexual function troubles. Said compounds are associated with to a 5-HT1A receptor.

摘要翻译： 本发明涉及用于生产用于治疗与5-羟色胺受体和/或5-羟色胺再吸收相关的疾病的药物，特别是用于生产类似抗焦虑药，抗抑郁药，精神安定药和/或抗高血压药的药物和/或用于治疗 影响强迫症，睡眠障碍，迟发性运动障碍，学习困难，老年记忆丧失，进食障碍如贪食症和/或肠易激综合征和/或性功能障碍。 所述化合物与5-HT1A受体结合。