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公开(公告)号：US5858738A
公开(公告)日：1999-01-12
申请号：US964081
申请日：1997-11-04
申请人： Russell B. Lingham , Jon David Polishook , Ali Shafiee , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink
发明人： Russell B. Lingham , Jon David Polishook , Ali Shafiee , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink
CPC分类号： C12R1/645 , C07C69/757 , C12P7/62
摘要： Natural products such as certain ermophilane sesquiterpenoids and derivatives thereof are described. These compounds are useful in the inhibition of HIV integrase, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The fungal culture MF6254, Xylaria sp. (ATCC 74397) is also described and disclosed.
摘要翻译： 描述天然产物如某些ermophilane倍半萜类及其衍生物。 这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，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，免疫调节剂，抗生素或其他抗生素组合使用 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。 真菌培养物MF6254，Xylaria sp。 （ATCC 74397）也被描述和公开。
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公开(公告)号：US6110716A
公开(公告)日：2000-08-29
申请号：US18684
申请日：1998-02-04
申请人： Russell B. Lingham , Ali Shafiee , Keith C. Silverman , Ana M. Teran , Sheo Bux Singh , Deborah L. Zink
发明人： Russell B. Lingham , Ali Shafiee , Keith C. Silverman , Ana M. Teran , Sheo Bux Singh , Deborah L. Zink
IPC分类号： A61K31/335 , A61K31/352 , A61K31/365 , C07D311/92 , C07D407/04 , C12P17/16 , A61K31/35 , C07D311/78 , C07D321/10
CPC分类号： C07D407/04 , A61K31/335 , A61K31/352 , A61K31/365 , C07D311/92 , C12P17/162
摘要： Natural products such as certain chaetochromins are described. These compounds are useful in the inhibition of HIV integrase, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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公开(公告)号：US06403347B1
公开(公告)日：2002-06-11
申请号：US09355692
申请日：1999-10-25
申请人： Gerald F. Bills , Russell B. Lingham , Ali Shafiee , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink , Fernando Pelaez , Ana M. Teran
发明人： Gerald F. Bills , Russell B. Lingham , Ali Shafiee , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink , Fernando Pelaez , Ana M. Teran
IPC分类号： A61K3135
CPC分类号： A61K31/35
摘要： Natural products such as certain chaetochromins are described. These compounds are useful in the inhibition of HIV integrase, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 描述了天然产物，如某些chaetochromins。 这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，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，免疫调节剂，抗生素或其他抗生素组合使用 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：US6124327A
公开(公告)日：2000-09-26
申请号：US123180
申请日：1998-07-27
IPC分类号： C07C69/88 , C12P7/62 , C07C69/84 , A61K31/235
摘要： Natural products such as certain dimerized hydroxyphenylundecanes are described. These compounds are useful in the inhibition of HIV integrase, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 描述了某些二聚羟基苯基十一烷等天然产物。 这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，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，免疫调节剂，抗生素或其他抗生素组合使用 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：US5703067A
公开(公告)日：1997-12-30
申请号：US435047
申请日：1995-05-08
申请人： Hiranthi Jayasuriya , Russell B. Lingham , Fernando Pelaez , Manuel Sanchez , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink
发明人： Hiranthi Jayasuriya , Russell B. Lingham , Fernando Pelaez , Manuel Sanchez , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink
IPC分类号： A61K31/575 , C07J9/00 , C07J17/00
CPC分类号： A61K31/573 , A61K31/575 , C07J17/00 , C07J9/00
摘要： The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer. The compounds of this invention have the following structure: ##STR1##
摘要翻译： 本发明涉及抑制法呢基蛋白转移酶（FPTase）的甾族化合物或萜类化合物。 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和治疗癌症的方法。 本发明的化合物具有以下结构：
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公开(公告)号：US5789438A
公开(公告)日：1998-08-04
申请号：US924557
申请日：1997-09-05
申请人： Sheo B. Singh , Russell B. Lingham , Keith C. Silverman , Deborah L. Zink , Isabel Martin , Fernando Pelaez , Manuel Sanchez
发明人： Sheo B. Singh , Russell B. Lingham , Keith C. Silverman , Deborah L. Zink , Isabel Martin , Fernando Pelaez , Manuel Sanchez
IPC分类号： C07D311/78 , C07D493/04 , A61K31/365 , C07D493/06
CPC分类号： C07D493/04 , C07D311/78
摘要： The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
摘要翻译： 本发明涉及抑制法呢基蛋白转移酶（FPTase）的甾族化合物或萜类化合物。 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和治疗癌症的方法。
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公开(公告)号：US5663193A
公开(公告)日：1997-09-02
申请号：US682248
申请日：1996-07-17
申请人： Carmen Cascales , Russell B. Lingham , Fernando Pelaez , Jon D. Polishook , Keith C. Silverman , Sheo B. Singh , Deborah L. Zink
发明人： Carmen Cascales , Russell B. Lingham , Fernando Pelaez , Jon D. Polishook , Keith C. Silverman , Sheo B. Singh , Deborah L. Zink
IPC分类号： C07D493/04 , A61K31/535
CPC分类号： C07D493/04 , Y10S514/908
摘要： The present invention is directed to non-peptide compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention also relates to the process for the preparation of a compound of this invention by cultivating a culture of Phoma sp. 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（FPTase）和致癌基因蛋白Ras的法呢基化的非肽化合物。 本发明还涉及通过培养Phoma sp。培养物来制备本发明化合物的方法。 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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8.发明授权Inhibitor compounds of farnesyl-protein transferase and chemotherapeutic compositions containing the same, produced by strain ATCC 55532 失效法呢基蛋白转移酶的抑制剂化合物和含有该化合物的化学治疗组合物，由ATCC 55532
公开(公告)号：US5627057A
公开(公告)日：1997-05-06
申请号：US611700
申请日：1996-03-06
申请人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary Nallin-Omstead , Keith C. Silverman , Deborah L. Zink
发明人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary Nallin-Omstead , Keith C. Silverman , Deborah L. Zink
IPC分类号： A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , C12N1/20 , C12P1/06 , C12P33/00
CPC分类号： C12R1/045 , A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , Y10S435/822
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) 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. Furthermore, Actinoplanes sp. ATCC 55532 and Streptomces sp. ATCC 55550 are microorganisms which are capable of producing the disclosed compounds which are classified as carboxylic acid esters. In addition a method for preparing the compounds is disclosed which includes cultivating strain ATCC 55532 or strain ATCC 55550. The strains are independently capable of producing the carboxylic acid ester compounds.
摘要翻译： 本发明涉及抑制法呢基蛋白转移酶（FPTase）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。 此外，Actinoplanes sp。 ATCC 55532和Streptomces sp。 ATCC 55550是能够产生被分类为羧酸酯的公开化合物的微生物。 此外，公开了制备化合物的方法，其包括培养菌株ATCC 55532或菌株ATCC 55550.菌株独立地能够产生羧酸酯化合物。
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公开(公告)号：US5510371A
公开(公告)日：1996-04-23
申请号：US254228
申请日：1994-06-06
申请人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary N. Omstead , Keith C. Silverman , Deborah L. Zink
发明人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary N. Omstead , Keith C. Silverman , Deborah L. Zink
IPC分类号： A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , A61K31/335
CPC分类号： C12R1/045 , A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , Y10S435/822
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) 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：US5420157A
公开(公告)日：1995-05-30
申请号：US808124
申请日：1991-12-16
IPC分类号： A61K31/19 , A61K31/23 , A61P35/00 , A61P43/00 , C07C57/13 , C07C57/155 , C07C69/347 , C07C69/602 , C12N9/99 , C12P7/26 , C12P7/44 , C12P17/04 , C12R1/01 , A01N43/32 , C07D307/02 , C07D307/34
CPC分类号： C12R1/645 , C07C57/13 , C07C69/602 , C12P17/04 , C12P7/44
摘要： This invention relates to pharmaceutical compounds of structural formulae (I) and (II): ##STR1## and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.
摘要翻译： 本发明涉及结构式（I）和（II）的药物化合物：利用这些化合物抑制法呢基蛋白转移酶和癌基因蛋白法尼基化的组合物和方法Ras 。
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