公开(公告)号：EP1761482A1

公开(公告)日：2007-03-14

申请号：EP05750905.1

申请日：2005-06-06

申请人： Merck Patent GmbH

发明人： GERICKE, Rolf ,  DORSCH, Dieter ,  MEDERSKI, Werner ,  BEIER, Norbert ,  LANG, Florian

IPC分类号： C07C251/86 ,  C07D295/12 ,  C07C309/66 ,  C07C311/48 ,  C07C323/48 ,  C07C309/46 ,  A61K31/15 ,  A61P9/00 ,  A61P3/10 ,  A61P35/00

CPC分类号： C07C251/86 ,  C07D295/135

摘要： The invention relates to the novel ortho-substituted (3-hydroxyphenyl)-acetic acid benzylidene hydrazides of formula (I), wherein R1 to R9 are defined as in claim 1. Said novel compounds are SGK inhibitors and can be used in the treatment of SGK-relates diseases and disorders such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonary hypertension, cardiovascular diseases and renal diseases, and generally for any kind of fibroses and inflammatory processes.

公开(公告)号：EP1720844A2

公开(公告)日：2006-11-15

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.

公开(公告)号：EP1608645A1

公开(公告)日：2005-12-28

申请号：EP04718641.6

申请日：2004-03-09

申请人： Merck Patent GmbH

发明人： MEDERSKI, Werner ,  TSAKLAKIDIS, Christos ,  DORSCH, Dieter ,  CEZANNE, Bertram ,  GLEITZ, Johannes

IPC分类号： C07D413/12 ,  C07D401/12 ,  C07D453/06 ,  C07D403/12 ,  C07C275/26 ,  A61K31/5377 ,  A61K31/4155 ,  A61K31/4748 ,  A61P7/02

CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D453/06

摘要： The invention relates to novel compounds of formula (I), where R, R1, R2 and R3 have the meanings given in claim 1, which are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

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.

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.

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.

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.

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.

公开(公告)号：EP1311476A1

公开(公告)日：2003-05-21

申请号：EP01960693.8

申请日：2001-08-21

申请人： MERCK PATENT GmbH

发明人： MEDERSKI, Werner ,  JURASZYK, Horst ,  DORSCH, Dieter ,  TSAKLAKIDIS, Christos ,  GLEITZ, Johannes ,  BARNES, Christopher

IPC分类号： C07C311/47 ,  C07C317/42 ,  C07C333/04 ,  C07D211/46 ,  C07D213/30 ,  C07D257/04 ,  C07D295/08 ,  C07D317/40 ,  A61K31/175 ,  A61K31/18 ,  A61P9/00 ,  A61P35/00

CPC分类号： C07D213/30 ,  C07C311/47 ,  C07C317/42 ,  C07C333/04 ,  C07C2601/14 ,  C07D211/46 ,  C07D257/04 ,  C07D295/088 ,  C07D317/40

摘要： The invention relates to semicarbicides of the general formula (I), wherein R?1, R2, R3, R4¿ and I are defined as in claim 1. The compounds of formula (I) can be used as active ingredients for medicaments in human and veterinary medicine, especially for combating and preventing thromboembolic diseases such as thrombosis, myocardial infarction, arteriosclerosis, inflammations, apoplexy, angina pectoris, restenosis after angioplasty, intermittent claudication, tumors, tumor diseases and/or tumor metastases.

摘要翻译： 本发明涉及通式I的氨基脲，其中R 1，R 2，R 3，R 4和I具有权利要求1所示的含义。式I化合物可以用作药物 人和兽医学中的活性化合物，特别是用于控制和预防血栓形成障碍如血栓形成，心肌梗死，动脉硬化，炎症，中风，心绞痛，血管成形术后的再狭窄和间歇性跛行。

公开(公告)号：EP1076643A1

公开(公告)日：2001-02-21

申请号：EP99920646.9

申请日：1999-04-12

申请人： MERCK PATENT GmbH

发明人： GANTE, Joachim DI ,  DORSCH, Dieter ,  JURASZYK, Horst ,  MEDERSKI, Werner ,  WURZIGER, Hanns ,  BUCHSTALLER, Hans-Peter ,  BERNOTAT-DANIELOWSKI, Sabine ,  MELZER, Guido

IPC分类号： C07C257/18 ,  C07C279/22 ,  A61K31/155

CPC分类号： C07C257/18 ,  C07C279/22

摘要： The invention relates to novel compounds of formula (I), wherein X, R?1, R2, R3, R4 and R5¿ have the meanings cited in Patent Claim No. 1. Said compounds are inhibitors of the coagulation factor Xa and can be used for prophylaxis and/or for treating thromboembolic disorders.