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61. 发明公开

EP1597244A1 ETHYNYLDERIVATE ALS FAKTOR XA-INHIBITOREN 有权
标题翻译： ETHYNYLDERIVATE AS Xa因子抑制剂
公开(公告)号：EP1597244A1
公开(公告)日：2005-11-23
申请号：EP04706669.1
申请日：2004-01-30
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , TSAKLAKIDIS, Christos , DORSCH, Dieter , CEZANNE, Bertram , GLEITZ, Johannes , VAN AMSTERDAM, Christoph
IPC分类号： C07D265/32 , C07D213/64 , C07F9/40 , C07D233/46 , A61K31/5377 , A61K31/5375 , A61P7/02 , C07D401/12 , C07D403/12
CPC分类号： C07D213/64 , C07D233/46 , C07D265/32 , C07D401/12 , C07D403/12 , C07F9/6533
摘要： The invention relates to novel compounds of formula (I), wherein R1, R2, R3, X and Y have the meanings as cited in Patent Claim 1. The compounds are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.

62. 发明公开

EP1549304A1 HETEROZYKLISCHE AMIDE UND IHRE VERWENDUNG IN DER BEHANDLUNG VON THROMBOEMBOLISCHEN ERKRANKUNGEN UND TUMOREN 审中-公开
标题翻译：杂环酰胺它们在肿瘤和疾病血栓栓塞治疗的
公开(公告)号：EP1549304A1
公开(公告)日：2005-07-06
申请号：EP03750577.3
申请日：2003-09-18
申请人： MERCK PATENT GmbH
发明人： DORSCH, Dieter , CEZANNE, Bertram , MEDERSKI, Werner , TSAKLAKIDIS, Christos , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： A61K31/17 , A61K31/381 , A61K31/5377 , C07D413/12
CPC分类号： C07D409/12 , C07D333/36 , C07D409/14 , C07D413/12
摘要： The invention relates to novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meanings as cited in Patent Claim 1. These compounds are inhibitors of coagulation factor Xa and can be used for the prevention and/or treatment of thromboembolic diseases and for treating tumors.

63. 发明公开

EP1501814A1 SEMICARBAZIDDERIVATE ZUR BEKÄMPFUNG VON THROMBOEMBOLISCHEN KRANKHEITEN 审中-公开
标题翻译： SEMICARBAZIDDERIVATE抵抗疾病血栓栓塞
公开(公告)号：EP1501814A1
公开(公告)日：2005-02-02
申请号：EP03724967.9
申请日：2003-04-07
申请人： MERCK PATENT GmbH
发明人： MEDERSKI, Werner , TSAKLAKIDIS, Christos , CEZANNE, Bertram , DORSCH, Dieter , BARNES, Christopher , GLEITZ, Johannes
IPC分类号： C07D295/135 , C07D265/32 , C07D213/64 , C07D237/14 , C07D207/26 , C07D241/08 , C07D263/22 , C07D223/10 , C07D453/06 , C07D211/76 , A61K31/445 , A61K31/5375 , A61P7/02
CPC分类号： C07D207/26 , C07D211/76 , C07D213/64 , C07D223/10 , C07D237/14 , C07D241/08 , C07D263/22 , C07D265/32 , C07D295/135 , C07D453/06
摘要： The invention relates to novel compounds of formula (I), wherein R, R1, R1', X and T have the meaning given in patent claim 1. Said novel compounds are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.

64. 发明公开

EP1490056A1 N-'4-(2-IMINO-PYRROLIDIN-1-YL)PHENYL)-ACETEMID-UND ENTSPRECHENDE PIPERIDINDERIVATE ALS FAKTOR XA INHIBITOREN ZUR BEHANDLUNG VON THROMBOEMBOLISCHEN ERKRANKUNGEN 有权
标题翻译：的N- '4-（2-亚氨基吡咯烷-1-基）苯基）-ACETEMID和适当的哌啶作为因子Xa抑制剂用于治疗疾病的血栓栓塞于治疗
公开(公告)号：EP1490056A1
公开(公告)日：2004-12-29
申请号：EP03709758.1
申请日：2003-03-07
申请人： MERCK PATENT GmbH
发明人： CEZANNE, Bertram , DORSCH, Dieter , MEDERSKI, Werner , TSAKLAKIDIS, Christos , BARNES, Christopher , GLEITZ, Johannes
IPC分类号： A61K31/402 , A61K31/451 , C07D207/22 , C07D211/72 , C07D401/12 , C07D453/06
CPC分类号： C07D401/12 , C07D207/22 , C07D207/24 , C07D211/72 , C07D403/12 , C07D413/12 , C07D453/06
摘要： The invention relates to novel compounds of formula (I) wherein D, M, W, X, Y, T and R1 have the designation cited in patent claim 1. According to the invention, said compounds are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or treatment of thromboembolic diseases and for the treatment of tumours.

65. 发明公开

EP1368341A1 PHENYL DERIVATIVES 3 审中-公开
标题翻译： PHENYL DERIVATE
公开(公告)号：EP1368341A1
公开(公告)日：2003-12-10
申请号：EP02718165.0
申请日：2002-02-27
申请人： MERCK PATENT GmbH
发明人： DORSCH, Dieter , CEZANNE, Bertram , MEDERSKI, Werner , TSAKLAKIDIS, Christos , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： C07D401/12 , C07D211/76 , A61K31/4412 , A61P7/02
CPC分类号： C07D401/12 , C07D211/76 , C07D471/04 , Y02P20/55
摘要： Novel compounds of the formula (I) formula (I) in which W, E, X, Y, T, R1, R?2, R2', and R2''¿ are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.

66. 发明公开

EP1318984A1 4-AMINO-QUINAZOLINES 审中-公开
标题翻译： 4-氨基CHINAZOLINE
公开(公告)号：EP1318984A1
公开(公告)日：2003-06-18
申请号：EP01974258.4
申请日：2001-09-17
申请人： MERCK PATENT GmbH
发明人： MEDERSKI, Werner , DEVANT, Ralf , BARNICKEL, Gerhard , BERNOTAT-DANIELOWSKI, Sabine , VICKERS, James , CEZANNE, Bertram , DHANOA, Daljit , ZHAO, Bao-Ping , RINKER, James , PLAYER, Mark, R. , JAEGER, Edward , SOLL, Richard
IPC分类号： C07D239/94 , C07D239/95 , C07D403/12 , C07D405/12 , C07D409/14 , C07D401/12 , C07D409/04 , A61K31/517 , A61P9/10
CPC分类号： C07D239/94 , C07D239/95 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/14
摘要： Quinazolines of the formula (I) in which R, R?1, R2, R3, R4¿ and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein lbIX antagonists.

67. 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。

68. 发明授权

EP1966211B1 TRIAZOLDERIVATE 有权
标题翻译：三唑衍生物
公开(公告)号：EP1966211B1
公开(公告)日：2012-12-26
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 , C07D471/14 , A61K31/55 , A61K31/38 , A61P35/00
CPC分类号： C07D513/04 , C07D471/14 , C07D487/04

69. 发明授权

EP1585730B1 CARBONSÄUREAMIDDERIVATE UND IHRE VERWENDUNG ALS FAKTOR XA INHIBITOREN 有权
标题翻译：甲酰胺及其作为Xa因子抑制剂
公开(公告)号：EP1585730B1
公开(公告)日：2011-03-09
申请号：EP04700684.6
申请日：2004-01-08
申请人： Merck Patent GmbH
发明人： DORSCH, Dieter , CEZANNE, Bertram , MEDERSKI, Werner , TSAKLAKIDIS, Christos , GLEITZ, Johannes , VAN AMSTERDAM, Christoph
IPC分类号： C07D213/64 , C07D241/18 , C07D265/32 , C07D265/06 , C07D265/10 , C07F9/09 , A61K31/4412 , A61K31/5375 , A61K31/4965 , A61P7/00 , A61P9/00
CPC分类号： C07D213/64 , C07D241/18 , C07D265/06 , C07D265/10 , C07D265/32 , C07F9/581 , C07F9/591 , C07F9/650958 , C07F9/653 , C07F9/6533
摘要： The invention relates to the novel compounds of formula (I), wherein R1, D, X, W, Y and T are defined as in claim 1, for example (II). The novel compounds inhibit coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.

70. 发明授权

EP1720844B1 PYRROLIDIN-1,2-DICARBONSÄURE-1-(PHENYLAMID)-2-(4-(3-OXO-MORPHOLIN-4-YL)-PHENYLAMID) DERIVATE UND VERWANDTE VERBINDUNGEN ALS INHIBITOREN DES KOAGULATIONSFAKTORS XA ZUR BEHANDLUNG VON THROMBOEMBOLISCHEN ERKRANKUNGEN 有权
标题翻译：吡咯烷-1,2-二羧酸1-（苯基氨基）-2-（4-（3-氧代 - 吗啉-4-基）-PHENYLAMID）作为凝血因子的抑制剂衍生物和相关化合物XA治疗血栓栓塞性病症的
公开(公告)号：EP1720844B1
公开(公告)日：2009-04-29
申请号：EP04718299.3
申请日：2004-03-08
申请人： Merck Patent GmbH
发明人： TSAKLAKIDIS, Christos , DORSCH, Dieter , MEDERSKI, Werner , CEZANNE, Bertram , GLEITZ, Johannes
IPC分类号： C07D265/32
CPC分类号： C07D413/12 , C07D207/16 , C07D207/27 , C07D211/60 , C07D211/76 , C07D213/64 , C07D213/68 , C07D223/10 , C07D241/18 , C07D265/08 , C07D265/32 , C07D267/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/02 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08
摘要： The invention relates to the compounds of formula (I), wherein W represents N, CR3, or a sp2 hybridized C atom, E, together with W, represents a 3- to 7-membered saturated carbocylic or heterocyclic ring having 0 to 3 N atoms, 0 to 2 O atoms and/or 0 to 2 S atoms, which ring may contain a double bond, D represents a mononuclear or binuclear unsubstituted aromatic carbocycle or heterocycle having 0 to 4 N atoms, O atoms and/or S atoms or being monosubstituted or polysubstituted by Hal, A, OR3, N(R3)2, NO2, CN, COOR3 or CON(R3)2, G represents -[C(R4)2]n-, -[C(R4)2]nNR3-, -[C(R4)2]nO-, -[C(R4)2]nS- or -[C(R4)=C(R4)]n-, X represents -[C(R4)2]nCONR3[C(R4)2]n-, -[C(R4)2]nNR3CO[C(R4)2]n-, -[C(R4)2]nNR3[C(R4)2]n-, -[C(R4)2]nO[C(R4)2]n-, -[C(R4)2]nCO[C(R4)2]n- or -[C(R4)2]nCOO[C(R4)2]n-, Y represents alkylene, cycloalkylene, Het-diyl or Ar-diyl, T represents a mononuclear or binuclear saturated or unsaturated carbocycle or heterocycle having 0 to 4 N atoms, O atoms and/or S atoms, which is monosubstituted or polysubstituted by =O, =S, =NR3, =N-CN, =N-NO2, =NOR3, =NCOR3, =NCOOR3, =NOCOR3 and which may further be monosubstituted, disubstituted or trisubstituted by R3, Hal, A,-[C(R4)2]n, -Ar, -[C(R4)2]n-het, -[C(R4)2]n-cycloalkyl, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 and/or S(O)nA, and R1 and R2 are defined as in claim 1. The inventive compounds inhibit coagulation factor Xa and can be used in the prophylaxis and/or therapy of thrombo-embolic diseases and for treating tumors.

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