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21. 发明授权

US06316436B1 Inhibitors of prenyl-protein transferase 失效
标题翻译：异戊烯基蛋白转移酶的抑制剂
公开(公告)号：US06316436B1
公开(公告)日：2001-11-13
申请号：US09455627
申请日：1999-12-07
申请人： S. Jane deSolms , Anthony W. Shaw
发明人： S. Jane deSolms , Anthony W. Shaw
IPC分类号： A61K3155
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。

22. 发明授权

US5932590A Inhibitors of farnesyl-protein transferase 失效
公开(公告)号：US5932590A
公开(公告)日：1999-08-03
申请号：US985337
申请日：1997-12-04
申请人： Terrence M. Ciccarone , S. Jane deSolms
发明人： Terrence M. Ciccarone , S. Jane deSolms
IPC分类号： C07D401/06 , C07D401/12 , C07D401/14 , C07D217/20 , A61K31/47
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14
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.

23. 发明授权

US5624936A Inhibitors of farnesyl-protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US5624936A
公开(公告)日：1997-04-29
申请号：US600792
申请日：1996-02-13
申请人： S. Jane deSolms
发明人： S. Jane deSolms
IPC分类号： A61K38/00 , C07K5/078 , C07D401/06 , A61K31/47
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention comprises analogs of the CA.sup.1 A.sup.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sup.1 A.sup.2 X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA.sup.1 A.sup.2 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.sup.2 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CA1A2X基序的类似物。这些CA1A2X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CA1A2X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A2位置加入环胺部分。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。

24. 发明授权

US06566385B2 Inhibitors of prenyl-protein transferase 失效
公开(公告)号：US06566385B2
公开(公告)日：2003-05-20
申请号：US09757217
申请日：2001-01-09
申请人： S. Jane deSolms , Gerald E. Stokker , Anthony W. Shaw
发明人： S. Jane deSolms , Gerald E. Stokker , Anthony W. Shaw
IPC分类号： A61K314178
CPC分类号： C07D405/04 , C07D413/04
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase 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.

25. 发明授权

US06054466A Inhibitors of farnesyl-protein transferase 失效
公开(公告)号：US06054466A
公开(公告)日：2000-04-25
申请号：US195578
申请日：1998-11-18
申请人： Terrence M. Ciccarone , S. Jane deSolms
发明人： Terrence M. Ciccarone , S. Jane deSolms
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
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.

26. 发明授权

US5627202A Inhibitors of farnesyl-protein transferase 失效
公开(公告)号：US5627202A
公开(公告)日：1997-05-06
申请号：US600794
申请日：1996-02-13
申请人： S. Jane deSolms
发明人： S. Jane deSolms
IPC分类号： A61K38/00 , C07K5/078 , C07D401/06 , A61K31/415
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention comprises analogs of the CA.sup.1 A.sup.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sup.1 A.sup.2 X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA.sup.1 A.sup.2 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.sup.2 position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

27. 发明授权

US5872135A Inhibitors of farnesyl-protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US5872135A
公开(公告)日：1999-02-16
申请号：US824936
申请日：1997-03-26
申请人： S. Jane deSolms
发明人： S. Jane deSolms
IPC分类号： A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K38/00 , A61P9/00 , A61P9/10 , A61P31/00 , A61P43/00 , C07D207/28 , C07D401/06 , C07D403/06 , C07K5/02 , C07K5/06 , C07K5/08 , A61K31/445 , C07D211/32 , C07D211/60
CPC分类号： C07D401/06 , C07D207/28 , C07D403/06 , C07K5/0207 , C07K5/06026 , 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 farnesyl-protein transferase. Furthermore, these CAAX analogues 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。

28. 发明授权

US5491164A Inhibitors of farnesyl-protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US5491164A
公开(公告)日：1996-02-13
申请号：US315151
申请日：1994-09-29
申请人： S. Jane deSolms , Samuel J. Graham
发明人： S. Jane deSolms , Samuel J. Graham
IPC分类号： C07D217/22 , A61K31/40 , A61K31/401 , A61K31/445 , A61K31/451 , A61K31/47 , A61K31/472 , A61P35/00 , A61P43/00 , C07D207/16 , C07D211/60 , A61K38/05 , C07D207/06 , C07D207/08 , C07D207/09
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。

29. 发明授权

US06413964B1 Inhibitors of prenyl-protein transferase 失效
标题翻译：异戊烯基蛋白转移酶的抑制剂
公开(公告)号：US06413964B1
公开(公告)日：2002-07-02
申请号：US09757213
申请日：2001-01-09
申请人： S. Jane deSolms , Suzanne C. MacTough , Anthony W. Shaw
发明人： S. Jane deSolms , Suzanne C. MacTough , Anthony W. Shaw
IPC分类号： A61K3155
CPC分类号： C07D515/08
摘要： The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase 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：本发明涉及式A的拟肽大环化合物：其中W是杂环，V是杂环或芳基，Z1是适当取代的芳基或杂环部分。本发明化合物抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化。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。

30. 发明授权

US06350755B1 Inhibitors of prenyl-protein transferase 失效
标题翻译：异戊烯基蛋白转移酶的抑制剂
公开(公告)号：US06350755B1
公开(公告)日：2002-02-26
申请号：US09757218
申请日：2001-01-09
申请人： S. Jane deSolms , Anthony W. Shaw
发明人： S. Jane deSolms , Anthony W. Shaw
IPC分类号： A61P3500
CPC分类号： C07D498/18 , C07D515/18
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase 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 - 蛋白转移酶和致癌基因蛋白Ras的异戊烯化的拟肽大环化合物。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。

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