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1. 发明申请

WO1996009820A1 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：WO1996009820A1
公开(公告)日：1996-04-04
申请号：PCT/US1995012284
申请日：1995-09-25
申请人： MERCK & CO., INC. , DeSOLMS, S., Jane , GRAHAM, Samuel, L.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/40
CPC分类号： C07D207/16
摘要： The present invention comprises dipeptide analogs that inhibit the farnesylation of Ras. These farnesyl-protein transferase inhibitors are characterized by the inclusion of a cyclic amine in the backbone of the dipeptide. 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Ras的法呢基化的二肽类似物。这些法呢基蛋白转移酶抑制剂的特征在于在二肽的主链中包含环胺。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。

2. 发明申请

WO1996010035A1 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：WO1996010035A1
公开(公告)日：1996-04-04
申请号：PCT/US1995012474
申请日：1995-09-27
申请人： MERCK & CO., INC. , ANTHONY, Neville, J. , deSOLMS, S., Jane , GRAHAM, Samuel, L. , STOKKER, Gerald, E. , WISCOUNT, Catherine, M. , CICCARONE, Terence, M.
发明人： MERCK & CO., INC.
IPC分类号： C07K05/06
CPC分类号： C07D401/06 , A61K38/00 , C07D207/28 , C07D403/06 , C07K5/0207 , C07K5/06026
摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogs 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：本发明包括通过体内法尼基化修饰的蛋白Ras的CAAX基序的类似物。这些CAAX类似物抑制法呢基蛋白转移酶。此外，这些CAAX类似物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。

3. 发明申请

WO1995009000A1 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：WO1995009000A1
公开(公告)日：1995-04-06
申请号：PCT/US1994010872
申请日：1994-09-26
申请人： MERCK & CO., INC. , DESOLMS, S., Jane , GIULIANI, Elizabeth, A. , GRAHAM, Samuel, L.
发明人： MERCK & CO., INC.
IPC分类号： A61K38/00
CPC分类号： C07K5/06034 , A61K38/00
摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogs differ from those previously described as inhibitors of Ras farnesyl 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：本发明包括通过体内法尼基化修饰的蛋白Ras的CAAX基序的类似物。这些CAAX类似物抑制Ras的法呢基化。此外，这些CAAX类似物与先前描述为Ras法呢基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。

4. 发明申请

WO02079147A3 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：WO02079147A3
公开(公告)日：2003-04-24
申请号：PCT/US0209213
申请日：2002-03-26
申请人： MERCK & CO INC , DESOLMS S JANE , SHAW ANTHONY W
发明人： DESOLMS S JANE , SHAW ANTHONY W
IPC分类号： A61P13/12 , A61P31/12 , A61P35/00 , C07D403/14 , A61K31/55 , A61K31/40 , A61K31/415 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/54 , C07D207/00 , C07D221/12 , C07D223/10 , C07D245/00 , C07D279/12 , C07D401/00 , C07D403/00 , C07D413/00
CPC分类号： C07D403/14
摘要： The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制异戊烯基 - 蛋白转移酶（FTase）和癌基因蛋白Ras的异戊烯化的化合物。本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。

5. 发明申请

WO2002078702A1 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：WO2002078702A1
公开(公告)日：2002-10-10
申请号：PCT/US2002/009208
申请日：2002-03-26
申请人： MERCK & CO., INC. , DESOLMS, S., Jane , SHAW, Anthony, W.
发明人： DESOLMS, S., Jane , SHAW, Anthony, W.
IPC分类号： A61K31/4178
CPC分类号： C07D403/04
摘要： The present invention is directed to compounds which inhibit a prenyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The compounds of the present invention comprise non-prodrug, non-thiol compounds that contain a spirocyclic pyrrolidinyl moiety. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting a prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制异戊烯基 - 蛋白转移酶（FTase）和癌基因蛋白Ras的法呢基化的化合物。本发明的化合物包含含有螺环吡咯烷基部分的非前体药物非硫醇化合物。本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和致癌基因蛋白Ras的异戊烯化的方法。

6. 发明申请

WO0034239A3 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：WO0034239A3
公开(公告)日：2000-09-08
申请号：PCT/US9929175
申请日：1999-12-07
申请人： MERCK & CO INC , DESOLMS S JANE , SHAW ANTHONY W
发明人： DESOLMS S JANE , SHAW ANTHONY W
IPC分类号： C07D498/18 , C07D273/02 , A61K31/55
CPC分类号： C07D498/18
摘要： The present invention is directed to compounds which inhibit prenyl-protein transferase and particularly, 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：本发明涉及抑制异戊烯基 - 蛋白转移酶，特别是癌基因蛋白Ras的法呢基化的化合物。本发明还涉及含有本发明化合物的化学治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。

7. 发明申请

WO1996031525A2 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：WO1996031525A2
公开(公告)日：1996-10-10
申请号：PCT/US1996003974
申请日：1996-03-25
申请人： MERCK & CO., INC. , deSOLMS, S., Jane
发明人： MERCK & CO., INC.
IPC分类号： C07K00/00
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0207
摘要： The present invention comprises analogs of the CA A X motif of the protein Ras that is modified by farnesylation in vivo. These CA A X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA A X analogs 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. The compounds of the instant invention also incorporate a cyclic amine moiety in the A position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译：本发明包括通过体内法尼基化修饰的蛋白Ras的CA 1 A 2 X基序的类似物。这些CA 1 A 2 X类似物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。此外，这些CA 1 A 2 X类似物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。本发明的化合物还在基序的A 2位上加入环胺部分。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。

8. 发明申请

WO1995009001A1 INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：法尼蛋白转移酶抑制剂
公开(公告)号：WO1995009001A1
公开(公告)日：1995-04-06
申请号：PCT/US1994011071
申请日：1994-09-29
申请人： MERCK & CO., INC. , DESOLMS, S., Jane , GARSKY, Victor, M. , GIULIANI, Elizabeth, A. , GOMEZ, Robert, P. , GRAHAM, Samuel, L. , STOKKER, Gerald, E. , WISCOUNT, Catherine, M.
发明人： MERCK & CO., INC.
IPC分类号： A61K38/00
CPC分类号： C07D213/82 , A61K38/00 , C07D207/28 , C07D233/64 , C07D233/90 , C07K5/0207 , C07K5/0821 , C07K5/0825 , C07K5/1024
摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogs differ from those previously described as inhibitors of Ras farnesyl 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：本发明涉及体内修饰的法尼基化Ras蛋白的CAAX序列的类似物。这些CAAX类似物抑制Ras的法尼基化，并且与先前描述为Ras法尼基转移酶抑制剂的那些不同，因为它们不包含硫醇部分。巯基的缺乏在改善动物中的药代动力学行为，预防硫醇相关的化学反应如自动氧化和与内源性硫醇形成二硫化物以及降低全身毒性方面具有独特优势。本发明还涉及含有这些法尼基转移酶抑制剂的化疗组合物及其制备方法。

9. 发明申请

WO1994009766A1 INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 审中-公开
标题翻译：法尼蛋白转移酶抑制剂
公开(公告)号：WO1994009766A1
公开(公告)日：1994-05-11
申请号：PCT/US1993010394
申请日：1993-10-28
申请人： MERCK & CO., INC. , DESOLMS, S., Jane , GRAHAM, Samuel, L. , WAI, John, Suiman
发明人： MERCK & CO., INC.
IPC分类号： A61K31/045
CPC分类号： C07D307/33 , C07C323/59
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和致癌基因蛋白的Ras的法呢基化的化合物，化学治疗以及包含此类化合物的组合物，以及抑制法呢基蛋白转移酶的方法和癌基因蛋白的法呢基化 RAS。

10. 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。

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