公开(公告)号：US5972984A

公开(公告)日：1999-10-26

申请号：US960248

申请日：1997-10-29

申请人： Neville J. Anthony ,  Jeffrey M. Bergman ,  S. Jane deSolms ,  Chrisopher J. Dinsmore ,  Robert P. Gomez ,  Suzanne C. MacTough ,  Kelly M. Solinsky ,  Theresa M. Williams

发明人： Neville J. Anthony ,  Jeffrey M. Bergman ,  S. Jane deSolms ,  Chrisopher J. Dinsmore ,  Robert P. Gomez ,  Suzanne C. MacTough ,  Kelly M. Solinsky ,  Theresa M. Williams

IPC分类号： C07D233/54 ,  C07D401/14 ,  C07D403/06 ,  C07D403/02 ,  A61K31/40 ,  A61K31/415

CPC分类号： C07D233/64 ,  C07D401/14 ,  C07D403/06

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。

公开(公告)号：US5756528A

公开(公告)日：1998-05-26

申请号：US652055

申请日：1996-05-23

申请人： Neville J. Anthony ,  Jeffrey M. Bergman ,  Chrisopher J. Dinsmore ,  Robert P. Gomez ,  Suzanne C. MacTough ,  Kelly M. Solinsky ,  Theresa M. Williams

发明人： Neville J. Anthony ,  Jeffrey M. Bergman ,  Chrisopher J. Dinsmore ,  Robert P. Gomez ,  Suzanne C. MacTough ,  Kelly M. Solinsky ,  Theresa M. Williams

IPC分类号： C07D233/54 ,  C07D233/61 ,  C07D401/14 ,  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.

公开(公告)号：US6080870A

公开(公告)日：2000-06-27

申请号：US155663

申请日：1998-10-01

申请人： Neville J. Anthony ,  Robert P. Gomez ,  Gerald E. Stokker ,  John S. Wai ,  Theresa M. Williams ,  Wasyl Halczenko ,  John H. Hutchinson ,  Steven D. Young ,  Kelly M. Solinsky

发明人： Neville J. Anthony ,  Robert P. Gomez ,  Gerald E. Stokker ,  John S. Wai ,  Theresa M. Williams ,  Wasyl Halczenko ,  John H. Hutchinson ,  Steven D. Young ,  Kelly M. Solinsky

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/66 ,  C07D233/70 ,  C07D403/10 ,  C07D403/14 ,  C07D233/30 ,  A61K31/4164 ,  A61K31/4174 ,  C07D233/32

CPC分类号： C07D233/56 ,  C07D233/64 ,  C07D233/70 ,  C07D403/10 ,  C07D403/14

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.

摘要翻译： PCT No.PCT / US97 / 05383 Sec。 371日期：1998年10月1日 102（e）1998年10月1日PCT PCT 1997年4月1日PCT公布。 第WO97 / 36875号公报 日期1997年10月9日本发明涉及抑制法尼基蛋白转移酶（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。

公开(公告)号：US5939557A

公开(公告)日：1999-08-17

申请号：US823919

申请日：1997-03-25

申请人： Neville J. Anthony ,  Robert P. Gomez ,  Kelly M. Solinsky

发明人： Neville J. Anthony ,  Robert P. Gomez ,  Kelly M. Solinsky

IPC分类号： C07D233/54 ,  C07D233/70 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

CPC分类号： C07D233/56 ,  C07D233/64 ,  C07D233/70 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

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.