公开(公告)号：EP1202966A1

公开(公告)日：2002-05-08

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

摘要： The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT¿2A? antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).

摘要翻译： 本发明涉及式（I）的化合物，其中R1，R2和A具有权利要求1中给出的含义，是有效的5-HT2A 拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经疾病，记忆障碍，帕金森病，肌萎缩侧索硬化症，阿尔茨海默氏病，亨廷顿舞蹈病，食欲紊乱如神经性贪食症和神经性厌食症，月经前期综合征和/ 强迫症（OCD）。

公开(公告)号：EP0885196A1

公开(公告)日：1998-12-23

申请号：EP97900586.0

申请日：1997-01-10

申请人： MERCK PATENT GmbH

发明人： ACKERMANN, Karl-August ,  GOTTSCHLICH, Rudolf ,  HÖLZEMANN, Günter ,  LEIBROCK, Joachim ,  RAUTENBERG, Wilfried ,  SEYFRIED, Christoph

IPC分类号： A61K31 ,  A61P25 ,  C07D215 ,  C07D401

CPC分类号： C07D215/22 ,  C07D401/10

摘要： The invention relates to chinoline-2-(1H)-ones derivatives of the formula (I), in which R?1, R2 and R3¿ are each independently H, Hal, A or OA; R4 is H, -(CH¿2?)m-NR?6R7, R5¿ is H, -(CH¿2?)n-NR?6R7, R6¿ is H, A or together with R7-(CH2)4 or -(CH2)5-; R7 is H, A or (CH¿2?)m- with a bond for an identical or adjacent ring B or D or together with R?6-(CH¿2)4- or -(CH2)5-; X is -CHR?5-, -NR5¿-, -O-, -S-; A is alkyl with 1 to 6 C-atoms; Hal is F, Cl, Br or I; m is 1 to 3; and n is 0 to 3, at least one of the two radicals R4 or R5 having the meaning -(CH¿2?)m-NR?6R7¿ or -(CH¿2?)n-NR?6R7¿. The invention also relates to the salts and solvates of said derivatives, and the use of said compounds and the biocompatible salts for the treatment of neurodegenerative changes in functions of the central nervous system.

公开(公告)号：EP1682548B1

公开(公告)日：2009-09-23

申请号：EP04790407.3

申请日：2004-10-14

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  CRASSIER, Helene ,  ACKERMANN, Karl-August ,  STÄHLE, Wolfgang ,  JONCZYK, Alfred ,  RAUTENBERG, Wilfried ,  MITJANS, Francesc ,  ROSELL-VIVES, Elisabet ,  ADAN, Jaume ,  SOLER RIERA, Marta

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The invention relates to compounds of formula (I) wherein R1, R2 , R3 , R4 , R5, R6 , R7 , R8, R9, X and X' have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumours.

公开(公告)号：EP1651626A1

公开(公告)日：2006-05-03

申请号：EP04763077.7

申请日：2004-07-02

申请人： Merck Patent GmbH

发明人： HÖLZEMANN, Günter ,  ACKERMANN, Karl-August ,  STÄHLE, Wolfgang ,  JONCZYK, Alfred ,  RAUTENBERG, Wilfried ,  MITJANS, Francesc ,  ROSELL-VIVES, Elisabet ,  ADAN, Jaume ,  SOLER, Marta ,  CRASSIER, Helene

IPC分类号： C07D285/14 ,  C07D213/81 ,  C07D213/70 ,  C07D319/18 ,  C07D277/64 ,  C07D307/86 ,  C07D317/64 ,  C07D213/69 ,  C07D235/32 ,  C07D471/04 ,  C07D209/08 ,  A61P35/00 ,  A61K31/435 ,  A61K31/4745 ,  A61K31/4184

CPC分类号： C07D213/69 ,  C07D209/08 ,  C07D213/70 ,  C07D213/81 ,  C07D235/32 ,  C07D277/64 ,  C07D277/82 ,  C07D285/14 ,  C07D307/86 ,  C07D317/64 ,  C07D319/18 ,  C07D471/04

摘要： The invention relates to novel urea derivatives which inhibit tyrosinkinases, especially TIE-2, and Raf kinases and which are used in the treatment of tumors.

公开(公告)号：EP1073634B1

公开(公告)日：2005-08-31

申请号：EP99923421.4

申请日：1999-04-16

申请人： Merck Patent GmbH

发明人： BATHE, Andreas ,  HELFERT, Bernd ,  ACKERMANN, Karl-August ,  GOTTSCHLICH, Rudolf ,  STEIN, Ingeborg ,  BUDAK, Jens

IPC分类号： C07D207/12 ,  A61K31/40 ,  C07B43/06 ,  C07B35/02

CPC分类号： C07B35/02 ,  A61K31/40 ,  C07B43/06 ,  C07D207/12 ,  Y02P20/55

摘要： The invention relates to a new method for producing N-methyl-N- [(1S)- 1-phenyl-2- ((3S)-3- hydroxypyrrolidine- 1-yl)ethyl]- 2,2-diphenyl acetamide or N-methyl- N-[(1R)- 1-phenyl-2- ((3R)-3- hydroxypyrrolidine- 1-yl)ethyl]- 2,2-diphenyl acetamide and to the new compounds N-methyl- N-[(1S)- 1-phenyl- 2-((3S)- 3-hydroxypyrrolidine- 1-yl)- ethane] and N-methyl-N- [(1R)- 1-phenyl-2- ((3R)-3- hydroxypyrrolidine- 1-yl)- ethane] produced as intermediate products.

公开(公告)号：EP1246803A1

公开(公告)日：2002-10-09

申请号：EP01905650.6

申请日：2001-01-05

申请人： MERCK PATENT GmbH

发明人： ACKERMANN, Karl-August ,  BÖTTCHER, Henning ,  PRÜCHER, Helmut ,  VAN AMSTERDAM, Christoph ,  SEYFRIED, Christoph ,  GREINER, Hartmut ,  BARTOSZYK, Gerd ,  HARTING, Jürgen

IPC分类号： C07D215/36 ,  C07D295/22 ,  C07D333/34 ,  C07D285/14 ,  C07D307/91 ,  C07D333/62 ,  C07D271/12 ,  C07D209/08 ,  C07D213/70 ,  C07D513/04 ,  C07D233/84 ,  C07D401/04 ,  C07D217/02 ,  C07D401/12 ,  C07D211/54

CPC分类号： C07D213/70 ,  C07D209/08 ,  C07D211/54 ,  C07D217/02 ,  C07D233/84 ,  C07D271/12 ,  C07D285/14 ,  C07D295/26 ,  C07D307/91 ,  C07D333/34 ,  C07D333/62 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： The invention relates to compounds of formula (I), wherein R1, R2, X, Y and alk are defined as per claim 1, are potent 5-HT¿2A? antagonists and are suitable for treating psychosis, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, such as bulimia and anorexia nervosa, premenstrual syndrome and/or for positively influencing compulsive behaviour (obsessive-compulsive disorder, OCD).