公开(公告)号：EP1966211A1

公开(公告)日：2008-09-10

申请号：EP06818796.2

申请日：2006-11-24

申请人： Merck Patent GmbH

发明人： CEZANNE, Bertram ,  AMENDT, Christiane ,  GREINER, Hartmut ,  GRAEDLER, Ulrich ,  HOELZEMANN, Guenter

IPC分类号： C07D487/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/38 ,  A61P35/00

CPC分类号： C07D513/04 ,  C07D471/14 ,  C07D487/04

摘要： Novel triazole derivatives, inhibitors of TGF-beta receptor I kinase, of application, amongst other things, to the treatment of tumours.

公开(公告)号：EP1891008A1

公开(公告)日：2008-02-27

申请号：EP06753563.3

申请日：2006-05-11

申请人： Merck Patent GmbH

发明人： BURGDORF, Lars, Thore ,  BRUGE, David ,  GREINER, Hartmut ,  KORDOWICZ, Maria ,  SIRRENBERG, Christian ,  ZENKE, Frank

IPC分类号： C07D209/34 ,  A61K31/404 ,  A61P9/00 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07D209/34

摘要： The present invention relates to oxindoles of the formula (I), their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition.

公开(公告)号：EP1874769A1

公开(公告)日：2008-01-09

申请号：EP06723838.6

申请日：2006-03-30

申请人： Merck Patent GmbH

发明人： HEINRICH, Timo ,  BLAUKAT, Andree ,  STAEHLE, Wolfgang ,  GREINER, Hartmut ,  KORDOWICZ, Maria

IPC分类号： C07D471/04 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The invention relates to compounds of formula (I), to their production and to their use for producing a medicament for treating diseases, particularly tumors and/or diseases in whose origin or progression kinases are involved.

公开(公告)号：EP1799669A1

公开(公告)日：2007-06-27

申请号：EP05789864.5

申请日：2005-10-06

申请人： Merck Patent GmbH

发明人： STIEBER, Frank ,  JONCZYK, Alfred ,  HOELZEMANN, Guenter ,  BUCHSTALLER, Hans-Peter ,  BURGDORF, Lars, Thore ,  RAUTENBERG, Wilfried ,  GREINER, Hartmut

IPC分类号： C07D401/12 ,  C07D471/04 ,  C07D403/12 ,  C07D413/12 ,  C07D471/10 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D471/10

摘要： The present invention relates to heterocyclic substituted bisarylurea derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

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：EP1233963A2

公开(公告)日：2002-08-28

申请号：EP00990614.0

申请日：2000-11-24

申请人： MERCK PATENT GmbH

发明人： GERICKE, Rolf ,  BÖTTCHER, Henning ,  GASSEN, Michael ,  GREINER, Hartmut

IPC分类号： C07D413/04 ,  C07D263/48 ,  C07D213/81 ,  C07D213/82 ,  C07D333/38 ,  C07D307/68 ,  A61K31/422 ,  A61P25/00

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D307/68 ,  C07D333/38 ,  C07D413/04

摘要： The invention relates to compounds of the general formula (I), wherein R1 and R2 independently of one another represent H, -R6, C3-C8-cycloalkyl, -(CH2)n-R7, -(CH2)n-O-R6, -(CH2)n-NH2, -(CH2)n-NHR6, -(CH2)-N(R6)2, C2-C6-alkenyl or optionally together form a mononuclear saturated heterocycle with one or two nitrogen, oxygen and/or sulphur atoms; R3 and R4 independently of one another represent H, -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, or -N(R6)2; R5 represents a 5- or 6-member, saturated or unsaturated heterocycle with one or two nitrogen, oxygen and/or sulphur atoms, which is optionally monosubstituted or disubstituted by -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, or -N(R6)2; and R6 represents C1-C6-alkyl; R7 together with R3 and/or R4 represents substituted phenyl, n represents 0 to 2. The invention also relates to the physiologically safe salts or solvates of said compounds and to the use of the compounds of the general formula (I) as medicaments.

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.