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：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：EP1425008B1

公开(公告)日：2006-10-04

申请号：EP02767352.4

申请日：2002-08-09

申请人： Merck Patent GmbH

发明人： BARTOSZYK, Gerd ,  RUSS, Hermann ,  SEYFRIED, Christoph ,  BÖTTCHER, Henning ,  BOKEL, Heinz-Hermann ,  SCHMID-GROSSMANN, Uschi

IPC分类号： A61K31/353 ,  A61K31/195 ,  A61P25/14 ,  A61P25/16

CPC分类号： A61K31/353

摘要： Substituted aminomethyl chromans, one of their optical isomers or pharmaceutically acceptable salts, used for the manufacture of a medicament for the treatment of adverse effects of anti-Parkinsonian drugs in extrapyramidal movement disorders and/or for the manufacture of a medicament for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics. A preferred compound is (-)-(R)-2-{4-[[3,4-dihydro-2H-benzopyran-2-yl)-methyl!amino!butyl}-1,2-benzoisothiazol-3-(2H)-on-1,1-dioxide or a physiologically acceptable salt thereof.

公开(公告)号：EP1572640A1

公开(公告)日：2005-09-14

申请号：EP03780043.0

申请日：2003-11-25

申请人： Merck Patent GmbH

发明人： WIESNER, Matthias ,  SEYFRIED, Christoph

IPC分类号： C07D207/12 ,  A61K31/40

CPC分类号： C07D207/12

摘要： The invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidine-1-yl)-ethyl]-2,2-diphenyl acetamide comprising covalently bonded acids and to the salts, solvates and prodrugs of said derivatives. The invention also relates to the use of the derivatives as medicaments, to their use for producing a medicament and for producing a pharmaceutical composition, to a method for producing said pharmaceutical compositions, to pharmaceutical compositions obtained by said method and to a method for treating diseases, comprising the administration of the aforementioned pharmaceutical composition.

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：EP0964863B1

公开(公告)日：2003-05-21

申请号：EP98909397.6

申请日：1998-02-06

申请人： MERCK PATENT GmbH

发明人： BÖTTCHER, Henning ,  PRÜCHER, Helmut ,  GREINER, Helmut ,  BARTOSZYK, Gerd ,  SEYFRIED, Christoph

IPC分类号： C07D413/14 ,  A61K31/445 ,  C07D491/056

CPC分类号： C07D413/14

摘要： The invention relates to novel oxazolidine derivatives of formula (I), wherein R?1, R2 and R3¿ have the meaning cited in Claim 1. The invention further relates to the salts thereof and to a method for the production of the inventive compounds. The compounds of formula (I) act as 5-HT¿2A? antagonists having a reuptake-inhibiting, antidepressant or anxiolytic effect and can be used in the production of medicaments.

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：EP0998474A1

公开(公告)日：2000-05-10

申请号：EP98938671.9

申请日：1998-06-29

申请人： MERCK PATENT GmbH

发明人： BÖTTCHER, Henning ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  SEYFRIED, Christoph

IPC分类号： C07D405/12 ,  A61K31/495

CPC分类号： C07D405/12

摘要： The invention relates to piperazine derivatives of formula (I), wherein R1, m, k and R2 have the meaning given in Claim 1. Said piperazine derivatives are potent 5-HT¿1A? agonists, have 5-HT-re-uptake inhibiting effects and are suitable for treating and preventing anxiety states, depression, schizophrenia, obsessive thoughts, tardive dyskensia, learning impairments and memory disturbances caused by age, for positively influencing compulsive behaviour, and for treating and combating the effects of cerebral infarctions, such as strokes and cerebral ischaemia.