公开(公告)号：EP1293503A1

公开(公告)日：2003-03-19

申请号：EP01930192.8

申请日：2001-05-17

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  Merck Patent GmbH

发明人： TOBE, Takahiko ,  SUGANE, Takashi ,  HAMAGUCHI, Wataru ,  SHIMADA, Itsuro ,  MAENO, Kyoichi ,  MIYATA, Junji ,  KIMIZUKA, Tetsuya ,  SUZUKI, Takeshi ,  KOHARA, Atsuyuki ,  MORITA, Takuma ,  ARLT, Michael ,  GREINER, Hartmut

IPC分类号： C07D249/08 ,  C07D249/12 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  C07D405/12 ,  C07D405/04 ,  A61K31/41

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

摘要翻译： 本发明涉及具有活性抑制甘氨酸转运体并用作药物的三唑衍生物和新的三唑衍生物。 本发明的三唑衍生物具有优异的抑制甘氨酸转运蛋白的活性，可用作痴呆，精神分裂症，认知障碍或涉及各种疾病如阿尔茨海默病，帕金森病或亨廷顿病等的认知障碍或痉挛的治疗剂 涉及诸如神经变性疾病和脑血管障碍等疾病。 特别地，药物对于改善痴呆等的学习障碍是有用的。

公开(公告)号：EP2197886A1

公开(公告)日：2010-06-23

申请号：EP08802398.1

申请日：2008-09-19

申请人： Merck Patent GmbH

发明人： HOELZEMANN, Guenter ,  GRAEDLER, Ulrich ,  GREINER, Hartmut ,  AMENDT, Christiane ,  MUSIL, Djordje ,  HILLERTZ, Per

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P35/00 ,  A61P35/02

CPC分类号： C07D495/04

摘要： The invention relates to novel 5-cyano-thienopyridines of the formula (I) where R1, R2, and R3 have the meanings designated in Claim 1. Said 5-cyano-thienopyridines are inhibitors of TGF beta receptor kinase and may be used, among other things, for the treatment of tumors.

公开(公告)号：EP1720846A1

公开(公告)日：2006-11-15

申请号：EP05701263.5

申请日：2005-01-31

申请人： Merck Patent GmbH

发明人： BURGDORF, Lars ,  BUCHSTALLER, Hans-Peter ,  STIEBER, Frank ,  ANZALI, Soheila ,  AMENDT, Christiane ,  GREINER, Hartmut ,  GRELL, Matthias ,  SIRRENBERG, Christian ,  ZENKE, Frank

IPC分类号： C07D285/135 ,  C07D417/06 ,  C07D417/12 ,  A61K31/4439 ,  A61K31/433

CPC分类号： C07D285/135 ,  C07D417/06 ,  C07D417/12

摘要： The invention relates to the use of compounds of formula (I) where Art, Ar2 and Z have the meanings given in claim 1, for the prophylaxis and/or treatment of diseases in which the inhibition, regulation and/or modulation of signal transduction of kinases, in particular of RAF kinases plays a role.

摘要翻译： 本发明涉及式（I）化合物（其中Ar 1，Ar 2和Z具有权利要求1中给出的含义）用于预防和/或治疗其中抑制，调节和/或调节 激酶，特别是RAF激酶起作用。

公开(公告)号：EP1140898B1

公开(公告)日：2002-08-28

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

公开(公告)号：EP0898569A1

公开(公告)日：1999-03-03

申请号：EP97920673.0

申请日：1997-04-14

申请人： MERCK PATENT GmbH

发明人： MÄRZ, Joachim ,  BÖTTCHER, Henning ,  DEVANT, Ralf ,  GREINER, Hartmut ,  BARTOSZYK, Gerd ,  HARTING, Jürgen ,  SEYFRIED, Christoph ,  BENGT, Ronny, Andersson ,  HANSSON, Lars, Olov ,  SONESSON, Clas, Ake ,  STJERNLÖF, Nils, Peter

IPC分类号： C07D211 ,  A61K31 ,  A61P25 ,  A61P43 ,  C07D207 ,  C07D401 ,  C07D403 ,  C07D405

CPC分类号： C07D401/12 ,  A61K9/19 ,  A61K9/2018 ,  A61K9/2059 ,  C07D401/14 ,  C07D405/14

摘要： The invention relates to novel piperidine and pyrrolidine derivatives of formula (I) in which R?1, R2, R3¿, k, l, m and n have the meanings indicated in Claim 1, and their salts, novel intermediates and processes for the preparation of the compounds according to the invention. The compounds of formula (I) act as 5-HT¿1A? receptor antagonists and exhibit 5-HT reuptake-inhibiting actions and can be used for the production of medicaments.

公开(公告)号：EP0879234A1

公开(公告)日：1998-11-25

申请号：EP97901049.0

申请日：1997-01-17

申请人： MERCK PATENT GmbH

发明人： BÖTTCHER, Henning ,  MÄRZ, Joachim ,  BARTOSZYK, Gerd ,  GREINER, Hartmut ,  HARTING, Jürgen ,  SEYFRIED, Christoph

IPC分类号： A61K31 ,  A61P25 ,  C07D401

CPC分类号： C07D401/14

摘要： The invention concerns new 1-pyrazol-3-yl-ethyl-4-indol-3-piperidine derivatives of formula (I) where R1 is H or A; R2 is H, a phenyl substituted 1 to 3 times by Hal, NO¿2?, CON(R?4)¿2, SO2N(R4)2, cyanogen, A or R4-O; R3 is H, Hal, A, A-O-, amino, cyanogen, carboxamide, NO¿2?, SO2N(R?4)¿2; R4 is H or A; A is (C¿1?-C6)alkyl or (C1-C6)alkyl containing one to three times substituted by fluorine; Hal is F, Cl, Br or J. The invention also concerns the salts of said derivatives. It has been shown that these compounds have an interesting pharmaceutical activity.

公开(公告)号：EP1966212B1

公开(公告)日：2015-05-13

申请号：EP06829158.2

申请日：2006-11-28

申请人： Merck Patent GmbH

发明人： SCHULTZ, Melanie ,  BURGDORF, Lars, Thore ,  FINSINGER, Dirk ,  BLAUKAT, Andree ,  GREINER, Hartmut ,  ESDAR, Christina

IPC分类号： C07D487/04 ,  A61K31/5517 ,  A61P35/00

CPC分类号： C07D487/04

公开(公告)号：EP1891008B1

公开(公告)日：2010-06-30

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：EP2111403A1

公开(公告)日：2009-10-28

申请号：EP07818574.1

申请日：2007-09-29

申请人： Merck Patent GmbH

发明人： HOELZEMANN, Guenter ,  GREINER, Hartmut ,  AMENDT, Christiane

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

CPC分类号： C07D487/04

摘要： Novel triaza-benzo[e]azulene derivatives of the formula (I) in which R1, R2 and R3 are each as defined in claim 1 are inhibitors of TGF-beta receptor kinase, and can be used, inter alia, for the treatment of tumors.

公开(公告)号：EP1910312A1

公开(公告)日：2008-04-16

申请号：EP06762312.4

申请日：2006-06-30

申请人： Merck Patent GmbH

发明人： MEDERSKI, Werner ,  EMDE, Ulrich ,  BARNICKEL, Gerhard ,  ZENKE, Frank ,  GREINER, Hartmut ,  STIEBER, Frank

IPC分类号： C07D235/06 ,  C07D231/56 ,  C07D209/80 ,  C07D513/04 ,  C07D471/04 ,  C07D307/82 ,  C07D277/64 ,  A61K31/343 ,  A61K31/4188 ,  A61P35/00

CPC分类号： C07D209/80 ,  C07D231/56 ,  C07D235/04 ,  C07D235/06 ,  C07D249/18 ,  C07D277/62 ,  C07D277/64 ,  C07D307/82 ,  C07D471/04 ,  C07D513/04

摘要： The invention relates to compounds of formula (I), wherein R, X, X' and R2, R2', R2', R3 ', R2'' and R7 have the significances specified in claim 1, wherein said compounds are embodied in the form of CHK1- CHK2- and SGK kinase inhibitors and can be used, inter alia, for treating cancer.