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公开(公告)号:US5534537A
公开(公告)日:1996-07-09
申请号:US412830
申请日:1995-03-29
IPC分类号: C07C323/59 , C07D233/54 , C07D233/56 , A61K31/41 , C07D403/12
CPC分类号: C07D233/64 , C07C323/59
摘要: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors 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: 本发明包括含有适当取代的氨基烷基苯甲酰胺部分的拟肽化合物。 本化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 此外,法呢基蛋白转移酶抑制剂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。
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公开(公告)号:US5578629A
公开(公告)日:1996-11-26
申请号:US413137
申请日:1995-03-29
IPC分类号: C07C323/59 , C07D233/54 , C07D277/04 , C07C237/20 , C07C321/10 , C07C323/29 , C07D277/12
CPC分类号: C07D233/64 , C07C323/59
摘要: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors 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: 本发明包括含有适当取代的氨基烷基苯甲酰胺部分的拟肽化合物。 本化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 此外,法呢基蛋白转移酶抑制剂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。
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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。
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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.
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公开(公告)号:US5710171A
公开(公告)日:1998-01-20
申请号:US648330
申请日:1996-05-15
IPC分类号: A61K31/33 , A61K31/4164 , A61P13/12 , A61P31/10 , A61P31/12 , A61P35/00 , A61P43/00 , C07D233/54 , C07D233/61 , C07D233/64 , C07D521/00 , A61K31/415 , C07D233/56 , C07D233/60 , C07D403/02
CPC分类号: C07D233/64
摘要: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzene and analine analogs, further substituted with a second phenyl ring attached via a bond, a heteroatom linker or an aliphatic linker. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors 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: 本发明包括拟肽化合物,其包含适当取代的氨基烷基苯和分析物类似物,进一步被通过键连接的第二苯环,杂原子连接体或脂族连接体取代。 本发明化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 此外,法呢基蛋白转移酶抑制剂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。
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公开(公告)号:US5856326A
公开(公告)日:1999-01-05
申请号:US600728
申请日:1996-03-01
申请人: Neville J. Anthony , Terrence M. Ciccarone , Christopher J. Dinsmore , Robert P. Gomez , Theresa M. Williams , George D. Hartman
发明人: Neville J. Anthony , Terrence M. Ciccarone , Christopher J. Dinsmore , Robert P. Gomez , Theresa M. Williams , George D. Hartman
IPC分类号: C07D233/54 , C07D241/08 , C07D295/192 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , A61K31/495 , C07D241/04
CPC分类号: C07D233/64 , C07D241/08 , C07D295/192 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12
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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公开(公告)号:US5977134A
公开(公告)日:1999-11-02
申请号:US985320
申请日:1997-12-04
申请人: Terrence M. Ciccarone , Wasyl Halczenko , John H. Hutchinson , William C. Lumma, Jr. , Gerald E. Stokker , Craig A. Stump , Theresa M. Williams
发明人: Terrence M. Ciccarone , Wasyl Halczenko , John H. Hutchinson , William C. Lumma, Jr. , Gerald E. Stokker , Craig A. Stump , Theresa M. Williams
IPC分类号: C07D235/30 , C07D401/06 , C07D403/06 , C07D471/04 , C07D401/02 , A61K31/415 , A61K31/47
CPC分类号: C07D401/06 , C07D235/30 , C07D403/06 , 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:US5631280A
公开(公告)日:1997-05-20
申请号:US448865
申请日:1995-05-24
申请人: Terrence M. Ciccarone , Christopher J. Dinsmore , Gerald E. Stokker , John S. Wai , Theresa M. Williams
发明人: Terrence M. Ciccarone , Christopher J. Dinsmore , Gerald E. Stokker , John S. Wai , Theresa M. Williams
IPC分类号: C07D521/00 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61P35/00 , A61P43/00 , C07C323/25 , C07C323/60 , C07D209/08 , C07D209/46 , C07D209/44
CPC分类号: C07C323/25 , C07C323/60 , C07D209/08 , C07D209/46 , C07C2102/10
摘要: The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. 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: 本发明包括含有合适的苯胺和氨基烷基苯部分的拟肽化合物。 本发明化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 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。
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公开(公告)号:US5527819A
公开(公告)日:1996-06-18
申请号:US488957
申请日:1995-06-07
申请人: Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
发明人: Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
IPC分类号: C07D209/12 , C07D209/30 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12 , C07D521/00 , A61K31/40
CPC分类号: C07D231/12 , C07D209/12 , C07D209/30 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12
摘要: Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译: 新型吲哚化合物抑制HIV逆转录酶,可用于预防或治疗艾滋病毒和艾滋病感染,作为化合物,药学上可接受的盐,药物组合物成分,无论是否与其他抗病毒药物结合使用,抗感染药物 ,免疫调节剂,抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号:US20130210804A1
公开(公告)日:2013-08-15
申请号:US13880171
申请日:2011-10-20
申请人: Neville J. Anthony , Robert P. Gomez , Jing Li , Swati P. Mercer , Anthony J. Roecker , Craig A. Stump , Theresa M. Williams
发明人: Neville J. Anthony , Robert P. Gomez , Jing Li , Swati P. Mercer , Anthony J. Roecker , Craig A. Stump , Theresa M. Williams
IPC分类号: C07D513/04 , C07D498/04 , C07D471/14 , C07D471/04
CPC分类号: C07D513/04 , C07D471/04 , C07D471/14 , C07D498/04
摘要: The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译: 本发明涉及三环化合物,其是代谢型谷氨酸受体,特别是mGluR5受体的正性变构调节剂,其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病症以及涉及代谢型谷氨酸受体的疾病 。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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