公开(公告)号：US06248756B1

公开(公告)日：2001-06-19

申请号：US09248883

申请日：1999-02-11

申请人： Neville J. Anthony ,  Christopher Dinsmore ,  Robert P. Gomez ,  John H. Hutchinson ,  John S. Wai ,  Theresa M. Williams ,  Ian M. Bell ,  Mark W. Embrey ,  Thorsten E. Fisher

发明人： Neville J. Anthony ,  Christopher Dinsmore ,  Robert P. Gomez ,  John H. Hutchinson ,  John S. Wai ,  Theresa M. Williams ,  Ian M. Bell ,  Mark W. Embrey ,  Thorsten E. Fisher

IPC分类号： A61K314468

CPC分类号： C07D401/06 ,  C07D211/62 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferas (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： 本发明涉及抑制法尼基蛋白转移（Fatease-protein transferas，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。

公开(公告)号：US5891889A

公开(公告)日：1999-04-06

申请号：US831308

申请日：1997-04-01

申请人： Neville J. Anthony ,  Robert P. Gomez ,  John S. Wai ,  Mark W. Embrey ,  Thorsten E. Fisher

发明人： Neville J. Anthony ,  Robert P. Gomez ,  John S. Wai ,  Mark W. Embrey ,  Thorsten E. Fisher

IPC分类号： C07D211/62 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D401/08 ,  A61K31/445

CPC分类号： C07D401/06 ,  C07D211/62 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

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.

公开(公告)号：US06921759B2

公开(公告)日：2005-07-26

申请号：US09973853

申请日：2001-10-10

申请人： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa Egbertson ,  John S. Wai ,  Linghang Zhuang ,  Mark Embrey ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  James P. Guare ,  Thorsten E. Fisher ,  Samson M. Jolly ,  Michelle S. Kuo ,  Debra S. Perlow ,  Jennifer J. Bennett ,  Timothy W. Funk

发明人： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa Egbertson ,  John S. Wai ,  Linghang Zhuang ,  Mark Embrey ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  James P. Guare ,  Thorsten E. Fisher ,  Samson M. Jolly ,  Michelle S. Kuo ,  Debra S. Perlow ,  Jennifer J. Bennett ,  Timothy W. Funk

IPC分类号： A61K31/4375 ,  A61K31/47 ,  A61K31/4985 ,  A61K31/541 ,  A61K31/554 ,  A61P31/12 ,  A61P31/18 ,  C07D20060101 ,  C07D215/48 ,  C07D221/00 ,  C07D241/00 ,  C07D471/00 ,  C07D471/04 ,  C07D471/16 ,  C07D487/00 ,  C07D519/00 ,  A61P31/00 ,  C07D471/02

CPC分类号： C07D471/04

摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 描述了包括某些喹啉羧酰胺和萘啶甲酰胺衍生物的氮杂和多氮萘基甲酰胺衍生物。 这些化合物是HIV整合酶和HIV复制抑制剂的抑制剂，并且可用于预防或治疗HIV感染和治疗AIDS，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，任选地与其它组合 抗病毒药，免疫调节剂，抗生素或疫苗。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

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：US06919351B2

公开(公告)日：2005-07-19

申请号：US10399083

申请日：2001-10-09

申请人： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa S. Egbertson ,  John S. Wai ,  Jennifer J. Bennett

发明人： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa S. Egbertson ,  John S. Wai ,  Jennifer J. Bennett

IPC分类号： A61K31/4375 ,  A61K31/44 ,  A61K31/444 ,  A61K31/47 ,  A61K31/495 ,  A61K31/50 ,  A61K31/502 ,  A61K31/54 ,  A61K31/541 ,  A61K45/00 ,  A61K45/06 ,  A61P31/00 ,  A61P31/18 ,  A61P37/02 ,  A61P43/00 ,  C07D401/12 ,  C07D471/04 ,  C07D519/00 ,  A61K31/5415 ,  C07D417/12

CPC分类号： C07D471/04 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61K31/50 ,  A61K31/54 ,  A61K45/06 ,  C07D401/12

摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 包括某些喹啉羧酰胺和萘啶甲酰胺衍生物的氮杂和多氮萘甲酰胺衍生物被描述为HIV整合酶的抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，任选地与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

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.

公开(公告)号：US06841558B2

公开(公告)日：2005-01-11

申请号：US10398988

申请日：2001-10-09

申请人： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Jennifer J. Bennett

发明人： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Jennifer J. Bennett

IPC分类号： A61K31/4375 ,  A61P31/18 ,  A61P43/00 ,  C07D471/04 ,  C07D471/02

CPC分类号： C07D471/04

摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating, or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 包括某些喹啉羧酰胺和萘啶甲酰胺衍生物的氮杂和多氮萘甲酰胺衍生物被描述为HIV整合酶的抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，任选地与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合。 还描述了预防，治疗或延迟AIDS发病的方法以及预防或治疗HIV感染的方法。

公开(公告)号：US5854264A

公开(公告)日：1998-12-29

申请号：US826251

申请日：1997-03-27

申请人： Neville J. Anthony ,  Robert P. Gomez

发明人： Neville J. Anthony ,  Robert P. Gomez

IPC分类号： C07D401/10 ,  C07D403/10 ,  A61K31/44

CPC分类号： C07D401/10 ,  C07D403/10

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.

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：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。