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31. 发明申请

WO1996039137A1 INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：WO1996039137A1
公开(公告)日：1996-12-12
申请号：PCT/US1996008740
申请日：1996-06-03
申请人： MERCK & CO., INC. , ANTHONY, Neville, J. , SOLINSKY, Kelly, M. , GOMEZ, Robert, P. , WILLIAMS, Theresa, M. , BERGMAN, Jeffrey, M. , DeSOLMS, S., Jane , DINSMORE, Christopher, J. , MacTOUGH, Suzanne, C.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/415
CPC分类号： C07D233/64 , C07D401/14
摘要： The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译：本发明包括抑制法呢基蛋白转移酶的低分子量肽基化合物。此外，这些化合物不同于先前描述为法呢基 - 蛋白转移酶抑制剂的单或二肽类似物，因为它们不具有硫醇部分。缺乏硫醇在改善动物药代动力学行为方面提供独特的优势，防止硫醇依赖的化学反应，如快速自身氧化和内源性硫醇形成二硫键，并减少全身毒性。本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。

32. 发明申请

WO1996037204A1 INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：WO1996037204A1
公开(公告)日：1996-11-28
申请号：PCT/US1996007260
申请日：1996-05-20
申请人： MERCK & CO., INC. , DINSMORE, Christopher, J. , WILLIAMS, Theresa, M. , MacTOUGH, Suzanne, C. , STOKKER, Gerald, E.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/41
CPC分类号： C07D233/64
摘要： The present invention comprises peptidomimetic compounds which comprises a suitably substituted aminoalkylbenzene and analine analogs, further substituted with a second phenyl ring attached via a bond, a heteroatom linker or an aliphatic linker. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译：本发明包括拟肽化合物，其包含适当取代的氨基烷基苯和分析物类似物，进一步被经由键连接的第二苯环，杂原子接头或脂族连接体取代。本发明化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。此外，法呢基蛋白转移酶抑制剂与先前描述为法呢基蛋白转移酶抑制剂的不同之处在于它们不具有硫醇部分。缺乏硫醇在改善动物药代动力学行为方面提供独特的优势，防止硫醇依赖的化学反应，如快速自身氧化和内源性硫醇形成二硫键，并减少全身毒性。本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。

33. 发明申请

WO1996030343A1 INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：WO1996030343A1
公开(公告)日：1996-10-03
申请号：PCT/US1996004019
申请日：1996-03-25
申请人： MERCK & CO., INC. , ANTHONY, Neville, J. , CICCARONE, Terrence, M. , GOMEZ, Robert, P. , HUTCHINSON, John, H. , WILLIAMS, Theresa, M. , DINSMORE, Christopher, J. , STOKKER, Gerald, E.
发明人： MERCK & CO., INC.
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07D241/08 , C07D295/192 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制法呢基蛋白转移酶（FTase）和致癌基因蛋白Ras的法呢基化的化合物。本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。

34. 发明申请

WO1996030014A1 INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：WO1996030014A1
公开(公告)日：1996-10-03
申请号：PCT/US1996003958
申请日：1996-03-25
申请人： MERCK & CO., INC. , CICCARONE, Terrence, M. , WILLIAMS, Theresa, M. , DINSMORE, Christopher, J. , STOKKER, Gerald, E. , WAI, John, S.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/405
CPC分类号： C07C323/25 , C07C323/60 , C07C2602/10 , C07D209/08 , C07D209/46
摘要： The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译：本发明包括含有合适的苯胺和氨基烷基苯部分的拟肽化合物。本发明化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。

35. 发明申请

WO2013040863A1 CYCLOALKYLNITRILE PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：作为甘薯激酶抑制剂的环丙基鸟氨酸羧酰胺
公开(公告)号：WO2013040863A1
公开(公告)日：2013-03-28
申请号：PCT/CN2012/001291
申请日：2012-09-21
申请人： MERCK SHARP & DOHME CORP. , BRUBAKER, Jason , DINSMORE, Christopher J. , HOFFMAN, Dawn Marie , JUNG, Joon , LIU, Duan , PETERSON, Scott , SIU, Tony , TORRES, Luis E. , ZHANG, Hongjun , WEI, Zhongyong , SHI, Feng
发明人： BRUBAKER, Jason , DINSMORE, Christopher J. , HOFFMAN, Dawn Marie , JUNG, Joon , LIU, Duan , PETERSON, Scott , SIU, Tony , TORRES, Luis E. , ZHANG, Hongjun , WEI, Zhongyong , SHI, Feng
IPC分类号： C07D231/10 , A61K31/415 , A61P37/00 , A61P35/00
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Cycloalkylnitrile pyrazole carboxamides as JAK inhibitors useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer are provided.
摘要翻译：提供了可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症的环烷基腈吡唑甲酰胺作为JAK抑制剂。

36. 发明申请

WO2012145471A1 INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR INHIBITORS 审中-公开
标题翻译：胰岛素样生长因子-1受体抑制剂
公开(公告)号：WO2012145471A1
公开(公告)日：2012-10-26
申请号：PCT/US2012/034188
申请日：2012-04-19
申请人： MERCK SHARP & DOHME CORP. , PIRAMAL HEALTHCARE LTD. , BALACHANDRAN, Sarala , DINSMORE, Christopher, J. , ROYCHOWDHURY, Abhijit , SHARMA, Rajiv , VISHWAKARMA, Ram Asrey
发明人： BALACHANDRAN, Sarala , DINSMORE, Christopher, J. , ROYCHOWDHURY, Abhijit , SHARMA, Rajiv , VISHWAKARMA, Ram Asrey
IPC分类号： C07D413/12 , C07D413/14 , A61K31/5377 , A61P35/00
CPC分类号： C07D413/14 , A61K31/5377 , A61K45/06 , C07D413/12
摘要： The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharrnaceuticaUy acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译：本发明涉及能够抑制，调节和/或调节胰岛素样生长因子I受体和胰岛素受体的化合物。本发明的化合物具有包含磺酰基吲哚部分的核心结构。本发明还涉及这些化合物的药物可接受的盐，水合物和立体异构体。

37. 发明申请

WO0160458A3 INHIBITORS OF PRENYL-PROTEIN TRANSFERASE 审中-公开
标题翻译： PRENYL-PROTEIN TRANSFERASE的抑制剂
公开(公告)号：WO0160458A3
公开(公告)日：2009-06-04
申请号：PCT/US0105096
申请日：2001-02-15
申请人： MERCK & CO INC , DINSMORE CHRISTOPHER J , BERGMAN JEFFREY M
发明人： DINSMORE CHRISTOPHER J , BERGMAN JEFFREY M
IPC分类号： A61K31/495 , A61K31/50 , A61K31/55 , A61P31/12 , A61P35/00 , C07D233/24 , C07D243/08 , C07D401/00 , C07D403/00 , C07D417/00
CPC分类号： C07D233/24
摘要： The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
摘要翻译：本发明包括抑制异戊烯基 - 蛋白转移酶的含哌嗪化合物，包括法呢基 - 蛋白转移酶和er牛鞭毛蛋白转移酶I型。这样的治疗化合物可用于治疗癌症。

38. 发明申请

WO2007002254A3 BENZOCYCLOHEPTAPYRIDINES AS INHIBITORS OF THE RECEPTOR TYROSINE KINASE MET 审中-公开
标题翻译：作为受体酪氨酸激酶的抑制剂的苄基胆碱酯酶
公开(公告)号：WO2007002254A3
公开(公告)日：2007-05-18
申请号：PCT/US2006024247
申请日：2006-06-22
申请人： MERCK & CO INC , DINSMORE CHRISTOPHER J , ORTEGA GABARDA ANA ESTHER , GUERIN DAVID J , JEWELL JAMES P , KATZ JASON D , LIM JONGWON , MACHACEK MICHELLE R , OTTE RYAN D , YOUNG JONATHAN R
发明人： DINSMORE CHRISTOPHER J , ORTEGA GABARDA ANA ESTHER , GUERIN DAVID J , JEWELL JAMES P , KATZ JASON D , LIM JONGWON , MACHACEK MICHELLE R , OTTE RYAN D , YOUNG JONATHAN R
IPC分类号： C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/10 , C07F7/08
CPC分类号： C07D471/04 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07D491/10 , C07D491/113 , C07F7/1856
摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译：本发明涉及用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病和用于抑制受体酪氨酸激酶MET的5H-苯并[4,5]环庚并[1,2-b]吡啶化合物。本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

39. 发明申请

WO2007050383A2 TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO2007050383A2
公开(公告)日：2007-05-03
申请号：PCT/US2006/040667
申请日：2006-10-18
申请人： MERCK & CO., INC. , DINSMORE, Christopher, J. , ORTEGA GABARDA, Ana Esther , LIM, Jongwon , MACHACEK, Michelle, R. , NORTHRUP, Alan, B. , YOUNG, Jonathan, R.
发明人： DINSMORE, Christopher, J. , ORTEGA GABARDA, Ana Esther , LIM, Jongwon , MACHACEK, Michelle, R. , NORTHRUP, Alan, B. , YOUNG, Jonathan, R.
IPC分类号： A61K31/551
CPC分类号： C07D471/04
摘要： The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译：本发明涉及咪唑并[1,2-a]嘧啶衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及用于抑制受体酪氨酸激酶MET。本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

40. 发明申请

WO2007002258A2 TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO2007002258A2
公开(公告)日：2007-01-04
申请号：PCT/US2006024256
申请日：2006-06-22
申请人： MERCK & CO INC , DINSMORE CHRISTOPHER J , JEWELL JAMES P , KATZ JASON D , MACHACEK MICHELLE R , OTTE RYAN D , YOUNG JONATHAN R
发明人： DINSMORE CHRISTOPHER J , JEWELL JAMES P , KATZ JASON D , MACHACEK MICHELLE R , OTTE RYAN D , YOUNG JONATHAN R
CPC分类号： C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译：本发明涉及可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病和用于抑制受体酪氨酸激酶MET的5H-苯并[4,5]环庚并[1,2-b]吡啶衍生物。本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

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