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12. 发明专利

CA2348391C CHROMENONE AND CHROMANONE DERIVATIVES AS INTEGRIN INHIBITORS 未知
公开(公告)号：CA2348391C
公开(公告)日：2009-09-29
申请号：CA2348391
申请日：1999-10-14
申请人： MERCK PATENT GMBH
发明人： FITTSCHEN CLAUS , MARZ JOACHIM , GOODMAN SIMON , RADDATZ PETER , WIESNER MATTHIAS
IPC分类号： C07D405/12 , A61K31/352 , A61K31/353 , A61K31/4178 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , A61P21/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D233/66 , C07D311/22 , C07D311/24
摘要： The invention relates to compounds having formula (I), wherein R1, R2, R3, R4, R5, R7, R8, R11, Z, m and n have the meaning cited in claim 1, and to the physiologically acceptable salts and solvates which can be used as integrin inhibitors, especially in the prophylaxis and treatment of circulatory diseases, in case of thrombosis, myocardial infarction, coronary heart diseases, arteriosclerosis, osteoporosis, pathologic processes caused or propagated by angiogenesis and in tumor therapy.

13. 发明专利

ES2311120T3 DERIVADOS DE GLICINAMIDA COMO INHIBIDORES DE QUINASA-RAF. 未知
公开(公告)号：ES2311120T3
公开(公告)日：2009-02-01
申请号：ES03790841
申请日：2003-07-31
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , WIESNER MATTHIAS , SCHADT OLIVER , AMENDT CHRISTIANE , ZENKE FRANK , SIRRENBERG CHRISTIAN
IPC分类号： A61K31/4409 , C07D213/64 , A61K31/4406 , A61K31/4427 , A61K31/4439 , A61P3/00 , A61P7/02 , A61P9/10 , A61P13/08 , A61P13/12 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/06 , A61P43/00 , C07D213/65 , C07D213/68 , C07D213/807 , C07D413/12
摘要： Derivados de glicinamida de fórmula II (Ver fórmula) donde Ar 1 se selecciona entre fenilo y oxazolilo, Ar 2 es piridinilo, R 8 , R 9 y R 10 se seleccionan independientemente del grupo que consiste en H, A, cicloalquilo de 3 a 7 átomos de carbono, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)nCN, (CH2)nNR 11 R 12 , (CH2)nOR 11 , (CH2)nO(CH2)k NR 11 R 12 , (CH2)nCOOR 12 , (CH2)nCONR 11 R 12 , (CH2)nNR 11 COR 13 , (CH2)nNR 11 CONR 11 R 12 , (CH2)nNR 11 SO2A, (CH2)nSO2NR 11 R 12 , (CH2)nS(O)uR 13 , (CH2)nOC(O)R 13 , (CH2)nCOR 13 , (CH2)nSR 11 , CH=N-OA, CH2CH=N-OA, (CH2)nNHOA, (CH2)nCH=N-R 11 , (CH2)nOC(O)NR 11 R 12 , (CH2)nNR 11 COOR 12 , (CH2)nN(R 11 )CH2CH2 OR 13 , (CH2)nN(R 11 )CH2CH2OCF3, (CH2)nN(R 11 )C(R 13 )HCOOR 12 , C(R 13 )HCOR 12 , (CH2)nN(R 11 )CH2CH2N (R 12 )CH2COOR 12 , (CH2)nN(R 11 )CH2CH2NR 11 R 12 , CH=CHCOOR 11 , CH=CHCH2NR 11 R 12 , CH=CHCH2NR 11 R 12 , CH=CHCH2OR 13 , (CH2)nN(COOR 11 )COOR 12 , (CH2)nN(CONH2)COOR 11 , (CH2)nN(CONH2)CONH2, (CH2)nN(CH2COOR 11 )COOR 12 , (CH2)nN(CH2CONH2)COOR 11 , (CH2)nN(CH2CONH2)CONH2, (CH2)nCHR 13 COR 11 , (CH2)nCHR 13 COOR 11 , (CH2)nCHR 13 CH2OR 14 , (CH2)nOCN y (CH2)nNCO, donde R 11 , R 12 se seleccionan independientemente del grupo que consiste en H, A, (CH2)mAr 3 y (CH2)mHet, o en NR 11 R 12 , R 11 y R 12 forman, junto con el átomo de N al que están enlazados, un heterociclo de 5, 6 o 7 miembros que contiene opcionalmente 1 o 2 heteroátomos adicionales, que pueden ser N, O y S, R 13 , R 14 se seleccionan independientemente del grupo que consiste en H, A, (CH2)mAr 4 y (CH2)mHet, A se selecciona del grupo que consiste en alquilo, alquenilo, cicloalquilo, alquilencicloalquilo, alcoxi y alcoxialquilo, Ar 3 , Ar 4 son residuos hidrocarbonados aromáticos de 5 a 12 átomos de carbono, preferiblemente de 1 a 10, independientes el uno del otro, y opcionalmente pueden estar sustituidos con uno o varios sustituyentes, seleccio-nados del grupo que consiste en A, Hal, NO2, CN, OR 15 , NR 15 R 16 , COOR 15 , CONR 15 R 16 , NR 15 COR 16 , NR 15 CONR 15 R 16 , NR 16 SO2A, COR 15 , SO2R 15 R 16 , S(O)uA y OOCR 15 , Het es un residuo heterocíclico saturado, insaturado o aromático que opcionalmente puede estar sustituido por uno o varios sustituyentes, seleccionados del grupo que consiste en A, Hal, NO2, CN, OR 15 , NR 15 R 16 , COOR 15 , CONR 15 R 16 , NR 15 COR 16 , NR 15 CONR 15 R 16 , NR 16 SO2A, COR 15 , SO2R 15 R 16 , S(O)uA y OOCR 15 , R 15 , R 16 se seleccionan independientemente del grupo que consiste en H, A, (CH2)mAr 5 , donde Ar 6 es un hidrocarburo aromático de 5 o 6 miembros que opcionalmente puede sustituirse con uno o varios sustituyentes seleccionados del grupo que consiste en metilo, etilo, propilo, 2-propilo, ter-butilo, Hal, CN, OH, NH2 y CF3, n, m son...

14. 发明专利

CA2161857C OXAZOLIDINONE DERIVATIVES AS ADHESION RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2161857C
公开(公告)日：2007-10-09
申请号：CA2161857
申请日：1995-10-31
申请人： MERCK PATENT GMBH
发明人： GANTE JOACHIM , JURASZYK HORST , RADDATZ PETER , WURZIGER HANNS , FITTSCHEN CLAUS , WIESNER MATTHIAS , BERNOTAT-DANIELOWSKI SABINE , MELZER GUIDO
IPC分类号： C07D263/24 , A61K31/42 , A61K31/421 , A61K31/445 , A61K31/495 , A61K31/496 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P13/12 , A61P15/00 , A61P19/08 , A61P19/10 , A61P35/00 , A61P43/00 , C07D413/02 , C07D413/04 , C07D413/06 , C07D413/10
摘要： Compounds of the formula I (see formula I) wherein R1, R2 and R3 have the meanings indicated, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, ischaemias, inflammations, arteriosclerosis and osteolytic disorders.

15. 发明专利

AU2001231664B2 Indol-3-yl derivatives 未知
公开(公告)号：AU2001231664B2
公开(公告)日：2006-02-23
申请号：AU2001231664
申请日：2001-01-05
申请人： MERCK PATENT GMBH
发明人： GOTTSCHLICH RUDOLF , WIESNER MATTHIAS , GOODMAN SIMON
IPC分类号： C07D401/06 , C07D401/12 , A61K31/404 , A61K31/405 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/506 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D209/20 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/06 , C07D417/14
摘要： Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in Patent claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.

17. 发明专利

CA2557359A1 SEMICARBAZIDE DERIVATIVES AS KINASE INHIBITORS 未知
公开(公告)号：CA2557359A1
公开(公告)日：2005-09-09
申请号：CA2557359
申请日：2005-02-14
申请人： MERCK PATENT GMBH
发明人： ZENKE FRANK , GRELL MATTHIAS , SIRRENBERG CHRISTIAN , AMENDT CHRISTIANE , WIESNER MATTHIAS , BUCHSTALLER HANS-PETER , STIEBER FRANK , FINSINGER DIRK
IPC分类号： C07D213/68 , A61K31/4409 , A61P19/02 , C07D213/81 , C07D401/12

18. 发明专利

DK1411926T3 未知
公开(公告)号：DK1411926T3
公开(公告)日：2005-08-29
申请号：DK02748841
申请日：2002-07-03
申请人： MERCK PATENT GMBH
发明人： BENDER HANS MARKUS , HAUNSCHILD JUTTA , LANG ULRICH , WIESNER MATTHIAS , FRIEDLANDER MARTIN
IPC分类号： A61K9/10 , A61K31/335 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/38 , A61K31/395 , A61K31/405 , A61K31/4178 , A61K31/4184 , A61K31/4433 , A61K31/4439 , A61K31/538 , A61K38/00 , A61K38/12 , A61K45/00 , A61K47/34 , A61P27/02 , A61K31/35
摘要： Methods for the treatment of a disease of the eye of a patient comprising injecting into the vitreous body of the eye a composition comprising a therapeutically effective amount of an alphavbeta3 and/or alphavbeta5 inhibitor sufficient to inhibit angiogenesis and inhibit neovascularization in the treated eye. The alphavbeta3 and/or alphavbeta5 inhibitor being a compound of formula II: as defined herein or a physiologically acceptable salt thereof.

19. 发明专利

DE10354060A1 未知
公开(公告)号：DE10354060A1
公开(公告)日：2005-06-02
申请号：DE10354060
申请日：2003-11-19
申请人： MERCK PATENT GMBH
发明人： FINSINGER DIRK , BUCHSTALLER HANS-PETER , BURGDORF LARS , WIESNER MATTHIAS , AMENDT CHRISTIANE , GRELL MATTHIAS , SIRRENBERG CHRISTIAN , ZENKE FRANK
IPC分类号： C07D207/32 , C07D207/337 , C07D401/12 , A61K31/4439 , A61P35/00 , A61P17/00 , A61P19/00 , A61P31/00 , A61P13/00 , A61P37/00
摘要： Compounds of the formula (I), in which X, Y, Z and Ar have the meanings indicated in claim 1, are inhibitors of Raf kinase and can be employed, inter alia, for the treatment of tumours

20. 发明专利

AT293620T 未知
公开(公告)号：AT293620T
公开(公告)日：2005-05-15
申请号：AT01903624
申请日：2001-01-05
申请人： MERCK PATENT GMBH
发明人： GOODMAN SIMON , GOTTSCHLICH RUDOLF , WIESNER MATTHIAS
IPC分类号： C07D401/06 , A61K31/404 , A61K31/405 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/506 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D209/20 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/06 , C07D417/14
摘要： Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in Patent claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.

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