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.

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。

公开(公告)号：EP1597244A1

公开(公告)日：2005-11-23

申请号：EP04706669.1

申请日：2004-01-30

申请人： Merck Patent GmbH

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

IPC分类号： C07D265/32 ,  C07D213/64 ,  C07F9/40 ,  C07D233/46 ,  A61K31/5377 ,  A61K31/5375 ,  A61P7/02 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D213/64 ,  C07D233/46 ,  C07D265/32 ,  C07D401/12 ,  C07D403/12 ,  C07F9/6533

摘要： The invention relates to novel compounds of formula (I), wherein R1, R2, R3, X and Y have the meanings as cited in Patent Claim 1. The compounds are inhibitors of 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：EP1448201A2

公开(公告)日：2004-08-25

申请号：EP02781293.2

申请日：2002-10-28

申请人： Merck Patent GmbH

发明人： VAN AMSTERDAM, Christoph ,  SEDMAN, Ewen ,  BARTOSZYK, Gard ,  HELLMANN, Jürgen ,  VON LANDENGERB

IPC分类号： A61K31/495 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28

CPC分类号： A61K31/496

摘要： The invention relates to the use of compounds of formula (I), wherein R?1, R2, R4 and R5¿ have the designations cited in patent claim 1, and to the physiologically acceptable salts and solvates of said compounds, for the treatment of obesity, sub-types of anxiety, sub-types of schizophrenia and types of dementia of various origins.

公开(公告)号：EP1202966B1

公开(公告)日：2004-06-09

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

公开(公告)号：EP1140898A1

公开(公告)日：2001-10-10

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

摘要： The invention relates to amide and urea derivatives of formula (I): R1-(CH2)n-(Y)q-(Z)r-CO-NH-R2, wherein R1, n, Y, q, Z, r and R¿2? have the meanings indicated in claim 1. Said derivatives are potent 5-HT1B/1D antagonists and 5-HT-reuptake inhibitors and are useful for the treatment and the prophylaxis of anxiety conditions, depressions, schizophrenia, obsessive ideas, tardive dyskinesias, impairment of the learning faculty, age-related memory disorders, for positively influencing obsessive-compulsive disorders (OCD), and in treating and controlling the consequences of cerebral infarctions such as strokes and cerebral ischemias.

公开(公告)号：EP1585730B1

公开(公告)日：2011-03-09

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：EP1611107B1

公开(公告)日：2010-08-18

申请号：EP04718264.7

申请日：2004-03-08

申请人： Merck Patent GmbH

发明人： SCHIEMANN, Kai ,  SCHADT, Oliver ,  VAN AMSTERDAM, Christoph ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D231/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/4155 ,  A61P25/18

CPC分类号： C07D231/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14

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

公开(公告)号：EP1611126B1

公开(公告)日：2009-10-28

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

公开(公告)号：EP1562939B1

公开(公告)日：2009-01-21

申请号：EP03776875.1

申请日：2003-10-30

申请人： Merck Patent GmbH

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

IPC分类号： C07D413/12 ,  C07D265/32 ,  C07D409/12 ,  A61K31/5377 ,  A61P7/02 ,  A61P9/00 ,  A61P35/00

CPC分类号： C07D409/12 ,  C07D265/32 ,  C07D413/12

摘要： The invention relates to novel compounds of formula (I) wherein D, W, X, Y, T, m and R1 have the designations cited in patent claim 1. Said novel compounds are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or treatment of thromboembolic diseases and for the treatment of tumours.