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41. 发明公开

EP1910312A1 QUADRATSÄUREDERIVATE II 审中-公开
标题翻译： QUADRATSÄUREDERIVATEII
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.

42. 发明公开

EP1817323A1 TETRAHYDROPYRANDERIVATE ALS ANTIDIABETIKA 审中-公开
标题翻译： TETRAHYDROPYRANDERIVATE ALS抗糖尿病药物
公开(公告)号：EP1817323A1
公开(公告)日：2007-08-15
申请号：EP05811335.8
申请日：2005-11-07
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , VAN AMSTERDAM, Christoph , BURGER, Christa , GREINER, Hartmut
IPC分类号： C07H15/203 , A61K31/706 , A61P3/10 , A61K31/7068
CPC分类号： C07H15/203
摘要： The invention relates to the novel compounds of formula (I) wherein T, E, R, R , R , R1, R2 and R2 are defined as in claim 1. The novel compounds are suitable as antidiabetics.

43. 发明授权

EP1202966B1 PIPERIDINALKOHOLE 有权
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

44. 发明公开

EP1140898A1 AMID- UND HARNSTOFFDERIVATE ALS 5-HT REUPTAKEINHIBITOREN UND ALS 5-HT1B/1D LIGANDEN 有权
标题翻译：酰胺，和脲衍生物作为5HT REUPTAKEINHIBITOREN AND AS 5HT 1B / 1D配体
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.

45. 发明公开

EP1140875A1 SULFONYLOXAZOLAMINE ALS THERAPEUTISCHE WIRKSTOFFE 审中-公开
标题翻译：磺酰氧胺唑啉ALS THERAPEUTISCHE WIRKSTOFFE
公开(公告)号：EP1140875A1
公开(公告)日：2001-10-10
申请号：EP99962190.7
申请日：1999-12-01
申请人： MERCK PATENT GmbH
发明人： GREINER, Hartmut , BARTOSZYK, Gerd , BÖTTCHER, Henning , BARNICKEL, Gerhard , CEZANNE, Bertram
IPC分类号： C07D263/48 , A61K31/42 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/24
CPC分类号： C07D263/48
摘要： The present invention relates to sulphonyloxazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, -(CH¿2?)n-Ar or alkenyl with 2-6 C atoms, R?1 and R2¿ together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF¿3?, NO2, Hal, OH, OA, NH2, NHA or NA2, A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br or I, n is 1 or 2 or the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
摘要翻译：本发明涉及通式（I）的磺酰基恶唑胺，其中R 1，R 2彼此独立地代表H，A， - （CH 2 2）n -Ar或具有2-6个C原子的烯基，R 1和R 2 A一起代表具有1-2个N，O和/或S原子的单核饱和杂环，Z代表H，A，CF 3，NO 2，Hal，OH，OA，NH 2，NHA或NA 2， Ar为Z-单取代或Z-二取代苯基，Hal为F，Cl，Br或I，n为1或2或其生理上可接受的盐或溶剂合物。所述磺酰恶唑胺用作治疗活性成分。本发明还涉及磺酰基恶唑胺作为治疗活性成分和/或用于制备抗中枢神经系统疾病的药物制剂的用途。本发明还涉及药物制剂及其制备。

46. 发明授权

EP2606034B1 PYRIMIDINDERIVATE ALS FAK INHIBITOREN 有权
标题翻译：嘧啶衍生物作为抑制剂FAK
公开(公告)号：EP2606034B1
公开(公告)日：2016-03-09
申请号：EP11743438.1
申请日：2011-07-19
申请人： Merck Patent GmbH
发明人： HEINRICH, Timo , ESDAR, Christina , GREINER, Hartmut
IPC分类号： C07D233/88 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/14 , C07D413/14 , A61K31/505 , A61P35/00
CPC分类号： C07D239/42 , C07D233/88 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12

47. 发明公开

EP2445916A1 ALKOXY-THIENOPYRIMIDINES AS TGF-BETA RECEPTOR KINASE MODULATORS 审中-公开
标题翻译：作为TGF-β受体激酶调节剂的烷氧基 - 噻吩并嘧啶
公开(公告)号：EP2445916A1
公开(公告)日：2012-05-02
申请号：EP10723928.7
申请日：2010-05-27
申请人： Merck Patent GmbH
发明人： HOELZEMANN, Guenter , DORSCH, Dieter , GREINER, Hartmut , AMENDT, Christiane , ZENKE, Frank
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04
摘要： Novel alkoxy-thienopyrimidine derivatives of formula (I) wherein R
1 and R
2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
摘要翻译：式（I）的新的烷氧基 - 噻吩并嘧啶衍生物（其中R 1和R 2具有根据权利要求1的含义）是TGF-β受体I激酶的抑制剂，尤其可用于治疗肿瘤。

48. 发明公开

EP2307425A1 IMIDAZOTHIADIAZOLES DERIVATIVES 有权
标题翻译：咪唑并噻唑衍生物
公开(公告)号：EP2307425A1
公开(公告)日：2011-04-13
申请号：EP09776906.1
申请日：2009-07-01
申请人： Merck Patent GmbH
发明人： HOELZEMANN, Guenter , GREINER, Hartmut , ROSSIGNOL, Emilie , SWINNEN, Dominique
IPC分类号： C07D513/04 , A61K31/433 , A61P35/00
CPC分类号： C07D513/04
摘要： Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R
1 and R
2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
摘要翻译：式（I）的新咪唑并[2,1-b] [1,3,4]噻二唑衍生物，其中R 1和R 2具有权利要求1的含义，是TGF-β受体I激酶的抑制剂，并且可以是除其他外用于治疗肿瘤。

49. 发明授权

EP0998474B1 PIPERAZIN-DERIVATE 失效
标题翻译：哌嗪衍生物
公开(公告)号：EP0998474B1
公开(公告)日：2007-02-07
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.

50. 发明授权

EP1228041B1 INDOLDERIVATE UND DEREN VERWENDUNG ALS 5HT2A LIGANDEN 有权
标题翻译：吲哚衍生物及其作为5HT2A配体的用途
公开(公告)号：EP1228041B1
公开(公告)日：2003-10-15
申请号：EP00954447.9
申请日：2000-07-07
申请人： MERCK PATENT GmbH
发明人： BÖTTCHER, Henning , MÄRZ, Joachim , GREINER, Hartmut , HARTING, Jürgen , BARTOSZYK, Gerd , SEYFRIED, Christoph , VAN AMSTERDAM, Christoph
IPC分类号： C07D209/12 , A61K31/404 , A61P43/00 , C07D403/06 , C07D409/06
CPC分类号： C07D209/12

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