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91. 发明专利

CA2829287C PYRIDO [2,3-B] PYRAZINE DERIVATIVES AND THEIR THERAPEUTICAL USES 未知
公开(公告)号：CA2829287C
公开(公告)日：2019-12-17
申请号：CA2829287
申请日：2012-02-13
申请人： MERCK PATENT GMBH
发明人： DORSCH DIETER , JONCZYK ALFRED , HOELZEMANN GUENTER , AMENDT CHRISTIANE , ZENKE FRANK
IPC分类号： C07D471/04 , A61K31/5025 , A61P35/00
摘要： The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

92. 发明专利

CA2804285C BIPYRIDYL DERIVATIVES USEFUL FOR THE TREATMENT OF KINASE - INDUCED DISEASES 未知
公开(公告)号：CA2804285C
公开(公告)日：2019-05-14
申请号：CA2804285
申请日：2011-06-07
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , DORSCH DIETER , JONCZYK ALFRED , ZENKE FRANK , AMENDT CHRISTIANE
IPC分类号： C07D213/74 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P25/00 , A61P29/00 , A61P35/00 , C07D401/14 , C07D471/04
摘要： The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

93. 发明专利

CA2803665C 2,4- DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER 未知
公开(公告)号：CA2803665C
公开(公告)日：2019-03-05
申请号：CA2803665
申请日：2011-05-31
申请人： MERCK PATENT GMBH
发明人： DORSCH DIETER , JONCZYK ALFRED , HOELZEMANN GUENTER , AMENDT CHRISTIANE , ZENKE FRANK
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00 , C07D519/00
摘要： The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

94. 发明专利

AU2010314518B2 Heteroarylaminoquinolines as TGF-beta receptor kinase inhibitors 未知
公开(公告)号：AU2010314518B2
公开(公告)日：2016-04-21
申请号：AU2010314518
申请日：2010-10-12
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , AMENDT CHRISTIANE , ZENKE FRANK
IPC分类号： C07D401/12 , A61K31/4706 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D471/04
摘要： Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

95. 发明专利

CY1112947T1 ΠΑΡΑΓΩΓΑ ΠΥΡΡΟΛΗΣ ΚΑΤΑΛΛΗΛΑ ΓΙΑ ΤΗΝ ΘΕΡΑΠΕΙΑ ΠΟΛΛΑΠΛΑΣΙΑΣΤΙΚΩΝ ΑΣΘΕΝΕΙΩΝ 未知
公开(公告)号：CY1112947T1
公开(公告)日：2016-04-13
申请号：CY121100678
申请日：2012-07-31
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： C07D401/12 , C07D207/32 , C07D207/337
摘要： Ενώσειςτουτύπου (Ι), στονοποίονΧ, Υ, ΖκαιΑr έχουντησημασίαπουδίνεταιστηναξίωση (1), είναιαναστολείςτης Raf-κινάσηςκαιμπορούνμεταξύάλλωνναχρησιμοποιηθούνγιατηνθεραπείαόγκων.

96. 发明专利

NZ603456A 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer 未知
公开(公告)号：NZ603456A
公开(公告)日：2014-08-29
申请号：NZ60345611
申请日：2011-05-31
申请人： MERCK PATENT GMBH
发明人： AMENDT CHRISTIANE , DORSCH DIETER , JONCZYK ALFRED , HOELZEMANN GUENTER , ZENKE FRANK
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00 , C07D519/00
摘要： 603456 Disclosed are [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumours. Examples of compounds of formula (I) include: 2-(5-Chloro-2-fluorophenyl)-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)-[1,8]naphthyridine formate; 2-(5-Chloro-2-fluorophenyl)-4- isoquinolin-5-yl-[1,8]naphthyridine and 2-(6-Methylpyridin-2-yl)-4-[2,6]naphthyridin-1-yl-[1,8]naphthyridine. Also disclosed are processes for preparing a compound of formula (I), compositions comprising compounds of formula (I) and the use of compounds of formula (I) in the manufacture of a medicament for treating cancer, carcinomas, tumours and hyperproliferative disorders.

97. 发明专利

CA2531859C BENZIMIDAZOLE DERIVATIVES AS RAF KINASE INHIBITORS 未知
公开(公告)号：CA2531859C
公开(公告)日：2013-08-06
申请号：CA2531859
申请日：2004-06-15
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , FINSINGER DIRK , WIESNER MATTHIAS , BURGDORF LARS , AMENDT CHRISTIANE , GRELL MATTHIAS , SIRRENBERG CHRISTIAN , ZENKE FRANK
IPC分类号： C07D401/12 , A61K31/4439 , A61P35/00
摘要： The present invention relates to a benzimidazole derivative of formula I: (see formula I) wherein: R6 and R7 are independently H or A, A is alkyl, Ar2 is independently phenyl, pyridinyl or pyrimidyl, R8 is alkyl, alkoxy or perhaloalkyl comprising 1 to 4 carbon atoms, Hal, CH2Hal, CH(Hal)2, NO2 or (CH2)n CN, R9 and R10 are independently H, A, cycloalkyl comprising 3 to 7 carbon atoms, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)n CN, (CH2)n NR11R12, (CH2)n OR11, (CH2)n O(CH2)k NR11R12, (CH2)n COOR12, (CH2),CONR11R12, (CH2)n NR11COR13, (CH2)n NR11CONR11R12, (CH2)n NR11SO2A, (CH2)n SO2NR11R12, (CH2)n S(O)n R13, (CH2)n OC(O)R13, (CH2)n COR13, (CH2)n SR11, CH=N-OA, CH2CH=N-OA, (CH2)n NHOA, (CH2)n CH=N-R11, (CH2)n OC(O)n R11R12, (CH2)n NR11COOR12, (CH2)n N(R11)CH2CH2OR13, (CH2)n N(R11)CH2CH2OCF3, (CH2)n N(R11)C(R13)HCOOR12, C(R13)HCOR12, (CH2)n N(R11)CH2CH2N(R12)CH2COOR12, (CH2)n N(R11)CH2CH2NR11R12, CH=CHCOOR11, CH=CHCH2NR11R12, CH=CHCH2NR11R12, CH=CHCH2OR13, (CH2)n N(COOR11)COOR12, (CH2)n N(CONH2)COOR11, (CH2)n N(CONH2)CONH2, (CH2)n N(CH2COOR11)COOR12, (CH2)n N(CH2CONH2)COOR11, (CH2)n N(CH2CONH2)CONH2, (CH2)n CHR13COR11, (CH2)n CHR13COOR11, (CH2)n CHR13CH2OR14, (CH2)n OCN or (CH2)n NCO, wherein R11 and R12 are independently H, A, (CH2)m Ar3 or (CH2)m Het, or in NR11R12, R11 and R12 form, together with the N-atom they are bound to, a 5-, 6- or 7-membered heterocyclus, R13 and R14 are independently H, Hal, A, (CH2)m Ar4 or (CH2)m Het, Ar3 and Ar4 are independently optionally substituted aromatic hydrocarbon residues comprising 5 to 12 carbon atoms, Het is an optionally substituted saturated, unsaturated or aromatic heterocyclic residue, k, m and n are independently 0, 1, 2, 3, 4, or 5, X is S, CH2 or O, Y is O, S or NR21, R21 is independently selected from the meanings given for R13, R14 and p and r are independently 0, 1, 2, 3, 4 or 5, q is 0, 1, 2, 3 or 4, u is 0, 1, 2 or 3, and Hal is independently F, CI, Br or I; or a physiologically acceptable salt or solvate thereof. The compound is useful as an inhibitor of one or more kinases. Accordingly, the compound is useful for the treatment of diseases mediated by one or more kinase pathways, preferably by the raf kinase pathway, especially cancers.

98. 发明专利

AU2008314245B2 5-cyano-thienopyridines for the treatment of tumors 未知
公开(公告)号：AU2008314245B2
公开(公告)日：2013-07-18
申请号：AU2008314245
申请日：2008-09-19
申请人： MERCK PATENT GMBH
发明人： HILLERTZ PER , GRAEDLER ULRICH , AMENDT CHRISTIANE , MUSIL DJORDJE , GREINER HARTMUT , HOELZEMANN GUENTER
IPC分类号： C07D495/04 , A61K31/4365 , A61P35/00 , A61P35/02
摘要： The invention relates to novel 5-cyano-thienopyridines of the formula (I) where

99. 发明专利

ZA201207133B HETARYLAMINONONAPHTHYRIDINES 未知
公开(公告)号：ZA201207133B
公开(公告)日：2013-05-29
申请号：ZA201207133
申请日：2012-09-21
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , ZENKE FRANK , DORSCH DIETER , AMENDT CHRISTIANE
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
摘要： Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

100. 发明专利

CA2611889C SUBSTITUTED TETRAHYDROQUINOLINES 未知
公开(公告)号：CA2611889C
公开(公告)日：2013-05-14
申请号：CA2611889
申请日：2006-05-17
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , EMDE ULRICH , FINSINGER DIRK , AMENDT CHRISTIANE , HEISS NINA , ZENKE FRANK
IPC分类号： C07D491/04 , A61K31/4355 , A61K31/436 , A61K31/4375 , A61K31/4706 , A61K31/4709 , A61P35/00 , C07D215/42 , C07D401/04 , C07D471/04
摘要： Compounds of the formula (I), (see formula I) in which W, R, R1, R2, R3, R6 and R7 have the meanings indicated in claim 1 can be employed inter alia for the treatment of tumors.

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