公开(公告)号：EP1592687B1

公开(公告)日：2008-06-04

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：EP1585730A1

公开(公告)日：2005-10-19

申请号：EP04700684.6

申请日：2004-01-08

申请人： Merck Patent GmbH

发明人： DORSCH, Dieter ,  CEZANNE, Bertram ,  MEDERSKI, Werner ,  TSAKLAKIDIS, Christos ,  GLEITZ, Johannes ,  VAN AMSTERDAM, Christoph

IPC分类号： C07D213/64 ,  C07D241/18 ,  C07D265/32 ,  C07D265/06 ,  C07D265/10 ,  C07F9/09 ,  A61K31/4412 ,  A61K31/5375 ,  A61K31/4965 ,  A61P7/00 ,  A61P9/00

CPC分类号： C07D213/64 ,  C07D241/18 ,  C07D265/06 ,  C07D265/10 ,  C07D265/32 ,  C07F9/581 ,  C07F9/591 ,  C07F9/650958 ,  C07F9/653 ,  C07F9/6533

摘要： The invention relates to the novel compounds of formula (I), wherein R1, D, X, W, Y and T are defined as in claim 1, for example (II). The novel compounds inhibit coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.

公开(公告)号：EP1562596A1

公开(公告)日：2005-08-17

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：EP1545531A1

公开(公告)日：2005-06-29

申请号：EP03775144.3

申请日：2003-09-03

申请人： MERCK PATENT GmbH

发明人： BARTOSZYK, Gerd ,  VAN AMSTERDAM, Christoph

IPC分类号： A61K31/496 ,  A61P25/20

CPC分类号： A61K31/496

摘要： The invention relates to the use of 5-HT2 receptor antagonists for producing a medicament which extends non-REM sleep and REM sleep.

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

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).

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.

公开(公告)号：EP1594864B1

公开(公告)日：2008-10-22

申请号：EP04703167.9

申请日：2004-01-19

申请人： Merck Patent GmbH

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

IPC分类号： C07D405/12 ,  A61K31/404 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D405/12

摘要： The invention relates to novel benzofuran oxyethylamines of formula (I), wherein R1, R2, R3, R4, m and n have the meanings as cited in Patent Claim No. 1, which have a strong affinity to the 5 HT1A receptors and/or 5HT1D receptors. The compounds inhibit the reuptake of serotonin, exhibit serotonin-agonistic and serotonin-antagonistic properties and are suited for use antidepressant drugs, anxiolytic drugs, antipsychotic drugs, neuroleptic drugs and/or antihypertonic drugs.

公开(公告)号：EP1611094B1

公开(公告)日：2007-06-20

申请号：EP04718288.6

申请日：2004-03-08

申请人： Merck Patent GmbH

发明人： SCHADT, Oliver ,  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 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14

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, R5 and R6 are defined as cited in claim 1. Said compounds are suitable for use as ligands of 5 HT receptors.

摘要翻译： 本发明涉及式（I）化合物，除了它们的盐和溶剂化物。 在所述式中，X，R1，R2，R3，R4，R5和R6如权利要求1中所定义。所述化合物适合用作5HT受体的配体。

公开(公告)号：EP1572685B1

公开(公告)日：2007-01-03

申请号：EP03782241.8

申请日：2003-11-27

申请人： Merck Patent GmbH

发明人： HEINRICH, Timo ,  BÖTTCHER, Henning ,  SCHIEMANN, Kai ,  HÖLZEMANN, Günter ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  SEYFRIED, Christoph ,  BRUNET, Michel ,  ZEILLER, Jean ,  BERTHELON, Jean

IPC分类号： C07D405/12 ,  A61K31/404 ,  A61P25/00

CPC分类号： C07D405/12

摘要： Disclosed are benzodioxepins of formula (I) and the physiologically acceptable salts and solvates thereof, R1, R2, R3, R4, A, B, a, and b having the meanings indicated in claim 1. Said benzodioxepins are ligands of the 5HT1A receptors and/or 5HT4 receptors while greatly inhibiting serotonin reuptake. The inventive benzodioxepins can be used for the treatment and prophylaxis of different diseases.