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公开(公告)号：US5652257A
公开(公告)日：1997-07-29
申请号：US526244
申请日：1995-09-21
申请人： Neville J. Anthony , S. Jane deSolms , Robert P. Gomez , Samuel L. Graham , John H. Hutchinson , Gerald E. Stokker
发明人： Neville J. Anthony , S. Jane deSolms , Robert P. Gomez , Samuel L. Graham , John H. Hutchinson , Gerald E. Stokker
IPC分类号： A61K38/00 , C07D233/54 , C07K5/02 , C07K5/06 , C07K5/062 , A61K31/415 , C07D233/02 , C07D233/04 , C07D233/30
CPC分类号： C07D233/64 , C07K5/0205 , 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 the farnesylation of Ras. Furthermore, these CAAX analogues 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。
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公开(公告)号：US5571835A
公开(公告)日：1996-11-05
申请号：US315059
申请日：1994-09-29
IPC分类号： C12N9/99 , A61K31/40 , A61K38/00 , A61K38/55 , A61P35/00 , A61P43/00 , C07D207/08 , C07D207/09 , C07K5/02 , C07K5/065
CPC分类号： C07D207/09 , C07K5/06078 , A61K38/00
摘要： The present invention comprises analogs of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sub.1 A.sub.2 X analogs inhibit the farnesylation of Ras. Furthermore, these CA.sub.1 A.sub.2 X analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they have a prolyl like moiety in the A.sub.1 position. 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Ras的法呢基化。 此外，这些CA1A2X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在A1位置具有脯氨酰类似的部分。 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。
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公开(公告)号：US5480893A
公开(公告)日：1996-01-02
申请号：US242575
申请日：1994-05-13
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 , A61K31/415 , C07D313/04
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.
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公开(公告)号：US5468733A
公开(公告)日：1995-11-21
申请号：US130032
申请日：1993-09-30
IPC分类号： C12N9/99 , A61K31/40 , A61K31/415 , A61K31/4166 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/445 , A61K38/00 , A61K38/55 , A61P35/00 , C07D207/12 , C07D211/76 , C07D233/32 , C07D263/14 , C07D277/14 , C07D279/06 , C07K5/06 , C07K5/083 , C07D207/24 , C07D211/40
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 analogues 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。
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公开(公告)号：US5352705A
公开(公告)日：1994-10-04
申请号：US905927
申请日：1992-06-26
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.
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公开(公告)号：US06297239B1
公开(公告)日：2001-10-02
申请号：US09167180
申请日：1998-10-06
申请人： S. Jane deSolms , John H. Hutchinson , Anthony W. Shaw , Samuel L. Graham , Terrence M. Ciccarone
发明人： S. Jane deSolms , John H. Hutchinson , Anthony W. Shaw , Samuel L. Graham , Terrence M. Ciccarone
IPC分类号： A61K314174
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/90 , C07D249/08 , C07D401/12
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 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。 本发明还涉及含有本发明化合物的化学治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的异戊烯基化的方法。
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公开(公告)号：US06284755B1
公开(公告)日：2001-09-04
申请号：US09456153
申请日：1999-12-07
申请人： S. Jane deSolms , Samuel L. Graham , Anthony W. Shaw , Terrence M. Ciccarone , Gerald E. Stokker
发明人： S. Jane deSolms , Samuel L. Graham , Anthony W. Shaw , Terrence M. Ciccarone , Gerald E. Stokker
IPC分类号： A01N4346
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04
摘要： The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-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 - 蛋白质转移酶，特别是法呢基蛋白转移酶（Ftase）的酪蛋白-2-酮化合物和致癌基因蛋白Ras的异戊烯基化。 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。
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公开(公告)号：US5939439A
公开(公告)日：1999-08-17
申请号：US995744
申请日：1997-12-22
申请人： Neville J. Anthony , Samuel L. Graham , Lekhanh O. Tran , Ian M. Bell , S. Jane deSolms , Robert P. Gomez , Michelle Sparks Kuo , William C. Lumma, Jr. , Debra S. Perlow , Anthony W. Shaw , John S. Wai , Steven D. Young
发明人： Neville J. Anthony , Samuel L. Graham , Lekhanh O. Tran , Ian M. Bell , S. Jane deSolms , Robert P. Gomez , Michelle Sparks Kuo , William C. Lumma, Jr. , Debra S. Perlow , Anthony W. Shaw , John S. Wai , Steven D. Young
IPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D417/14 , C07D471/04 , C07D401/04 , A61K31/44
CPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D417/14 , 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.
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公开(公告)号：US5576293A
公开(公告)日：1996-11-19
申请号：US314987
申请日：1994-09-29
申请人： S. Jane deSolms , Victor M. Garsky , Elizabeth A. Giuliani , Robert P. Gomez , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
发明人： S. Jane deSolms , Victor M. Garsky , Elizabeth A. Giuliani , Robert P. Gomez , Samuel L. Graham , Gerald E. Stokker , Catherine M. Wiscount
IPC分类号： C07D233/64 , A61K31/35 , A61K31/351 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K38/00 , A61K38/55 , A61P35/00 , A61P43/00 , C07D207/28 , C07D209/18 , C07D211/76 , C07D213/82 , C07D233/54 , C07D233/90 , C07D277/20 , C07D277/56 , C07D309/30 , C07D405/12 , C07D409/12 , C07K5/02 , C07K5/097 , C07K5/117 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07D213/82 , C07D207/28 , C07D233/64 , C07D233/90 , C07K5/0207 , C07K5/0821 , C07K5/0825 , C07K5/1024 , 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 analogues 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.
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公开(公告)号：US5817678A
公开(公告)日：1998-10-06
申请号：US749254
申请日：1996-11-15
IPC分类号： C07D233/24 , C07D401/12 , A61K31/445
CPC分类号： C07D233/24 , C07D401/12
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.
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