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31. 发明授权

US5703241A Inhibitor 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：US5703241A
公开(公告)日：1997-12-30
申请号：US729265
申请日：1996-10-10
申请人： S. Jane deSolms , Samuel L. Graham
发明人： S. Jane deSolms , Samuel L. Graham
IPC分类号： A61K38/00 , C07K5/06 , A61K31/415 , C07D403/02
CPC分类号： C07K5/06026 , A61K38/00
摘要： The present invention comprises an analog of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. This CA.sub.1 A.sub.2 X analog inhibits the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, this CA.sub.1 A.sub.2 X analog differs from most compounds previously described as inhibitors of farnesyl-protein transferase in that it does 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 compound of the instant invention also incorporates a cyclic amine moiety in the A.sup.1 position of the motif. Further contained in this invention are chemotherapeutic compositions containing this farnesyl transferase inhibitor and methods for its 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。该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，该CA1A2X类似物与先前描述为法呢基 - 蛋白转移酶抑制剂的大多数化合物不同，因为其不具有硫醇部分。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A1位置加入环胺部分。本发明还包含含有该法呢基转移酶抑制剂的化疗组合物及其生产方法。

32. 发明授权

US5686472A 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：US5686472A
公开(公告)日：1997-11-11
申请号：US143943
申请日：1993-10-27
申请人： Neville J. Anthony , S. Jane deSolms , Ta Jyh Lee, deceased
发明人： Neville J. Anthony , S. Jane deSolms , Ta Jyh Lee, deceased
IPC分类号： A61K31/195 , A61K31/215 , A61K31/365 , A61P35/00 , A61P35/02 , A61P43/00 , C07C323/25 , C07C323/52 , C07C323/56 , C07C323/57 , C07C323/58 , C07C323/59 , C07D307/33 , C07D213/28 , A61K31/41 , C07C381/00 , C07C729/00
CPC分类号： C07D307/33 , C07C323/25 , C07C323/56 , 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（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。

33. 发明授权

US5661161A 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：US5661161A
公开(公告)日：1997-08-26
申请号：US527972
申请日：1995-09-14
申请人： Neville J. Anthony , Terrence M. Ciccarone , S. Jane deSolms , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
发明人： Neville J. Anthony , Terrence M. Ciccarone , S. Jane deSolms , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
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 , C07D207/16
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 antoxidation 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体内的药代动力学行为方面提供独特的优势，预防硫醇依赖的化学反应，如用内源性硫醇快速无毒化和二硫化物形成，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。

34. 发明授权

US5504115A 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：US5504115A
公开(公告)日：1996-04-02
申请号：US267088
申请日：1994-06-28
申请人： Albert A. Deana, deceased , S. Jane deSolms , Samuel L. Graham , Robert L. Smith
发明人： Albert A. Deana, deceased , S. Jane deSolms , Samuel L. Graham , Robert L. Smith
IPC分类号： C07D235/24 , A61K31/165 , A61K31/415 , A61K31/4184 , A61P3/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07C233/06 , C07C323/25 , C07C323/60 , C07K5/06 , A61K31/16 , C07C237/06
CPC分类号： C07C323/25 , C07K5/0606
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。

35. 发明授权

US5340828A Inhibitors of farnesyl protein transferase 失效
公开(公告)号：US5340828A
公开(公告)日：1994-08-23
申请号：US768798
申请日：1991-09-30
申请人： Samuel L. Graham , S. Jane deSolms
发明人： Samuel L. Graham , S. Jane deSolms
IPC分类号： A61K38/55 , A61K38/00 , A61P35/00 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/10 , C07K5/103 , C12N9/99 , A61K31/44 , A61K31/195 , A61K31/415
CPC分类号： C07K5/06034 , C07K5/0808 , A61K38/00
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.

36. 发明授权

US5238922A Inhibitors of farnesyl protein transferase 失效
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：US5238922A
公开(公告)日：1993-08-24
申请号：US770078
申请日：1991-09-30
申请人： Samuel L. Graham , S. Jane deSolms , Victor M. Garsky
发明人： Samuel L. Graham , S. Jane deSolms , Victor M. Garsky
IPC分类号： A61K38/55 , A61K38/00 , A61P35/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/083 , C07K5/087 , C07K5/10
CPC分类号： C07K5/0808 , C07K5/0207 , C07K5/06078 , A61K38/00
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.

37. 发明授权

US4755612A Intermediate compounds resulting from method for forming a dihydrogen-phosphate inositol 失效
标题翻译：由形成磷酸二氢磷酸肌醇的方法得到的中间体化合物
公开(公告)号：US4755612A
公开(公告)日：1988-07-05
申请号：US75164
申请日：1987-07-20
申请人： Joseph P. Vacca , S. Jane deSolms
发明人： Joseph P. Vacca , S. Jane deSolms
IPC分类号： C07F9/117 , C07F9/655 , C07D317/46
CPC分类号： C07F9/65517 , C07F9/117
摘要： This invention relates to novel intermediate compounds resulting from a method for forming a dihydrogen-phosphate inositol from a protected or unprotected inositol that comprises at least two vicinal trans hydroxy groups that are unprotected. This method results in each of the unprotected hydroxy groups of the inositol, which can contain from two to six unprotected hydroxy groups, being converted to a dihydrogen-phosphate group and each protected group being converted to a free hydroxy group. The method permits one to make such compounds in very few steps and in very high yields.
摘要翻译：本发明涉及由保护或未保护的肌醇形成磷酸二氢肌醇的方法得到的新型中间体化合物，其包含至少两个未被保护的邻位反式羟基。该方法导致肌醇中的每个未保护的羟基，其可以含有2-6个未被保护的羟基，被转化为磷酸二氢基，每个被保护基被转化为游离羟基。该方法允许以非常少的步骤和非常高的产率制备这些化合物。

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