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公开(公告)号:EP0547670A3
公开(公告)日:1993-08-25
申请号:EP92203807.0
申请日:1992-12-08
申请人: MERCK & CO. INC.
发明人: Singh, Sheo Bux , Bills, Gerald F. , Lingham, Russell B. , Silverman, Keith C. , Zink, Deborah L.
IPC分类号: C07C57/13 , A61K31/19 , C07C211/00
CPC分类号: C12P7/6427 , C07C57/13 , C07C69/602 , C12P7/6436 , C12P17/04
摘要: This invention relates to pharmaceutical compounds of structural formula (I):
and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.-
公开(公告)号:EP0478061A1
公开(公告)日:1992-04-01
申请号:EP91202395.9
申请日:1991-09-18
申请人: MERCK & CO. INC.
发明人: Bills, Gerald F. , Ondeyka, John G. , Hensens, Otto D. , Zink, Deborah L. , Koupal, Lawrence , Lingham, Russell B.
IPC分类号: C07D209/70 , A61K31/40
CPC分类号: C07D209/76 , C12P17/10
摘要: An antiviral agent produced by Hypoxylon fragiforme and having the structure:
is described. The product has high activity as an HIV protease enzyme inhibitor and is useful in the treatment of diseases in which control of HIV protease activity is desirable.摘要翻译: 描述了由Hypoxylon fragiforme生产并具有以下结构的抗病毒剂:
。 该产品作为HIV蛋白酶抑制剂具有高活性,并且可用于治疗其中需要控制HIV蛋白酶活性的疾病。 -
公开(公告)号:EP0547670A2
公开(公告)日:1993-06-23
申请号:EP92203807.0
申请日:1992-12-08
申请人: MERCK & CO. INC.
发明人: Singh, Sheo Bux , Bills, Gerald F. , Lingham, Russell B. , Silverman, Keith C. , Zink, Deborah L.
IPC分类号: C07C57/13 , A61K31/19 , C07C211/00
CPC分类号: C12P7/6427 , C07C57/13 , C07C69/602 , C12P7/6436 , C12P17/04
摘要: This invention relates to pharmaceutical compounds of structural formula (I):
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)的药物化合物:
以及利用这些化合物抑制法呢基蛋白转移酶和致癌基因蛋白Ras的法呢基化的组合物和方法。 -
公开(公告)号:EP0480624A1
公开(公告)日:1992-04-15
申请号:EP91309028.8
申请日:1991-10-02
申请人: MERCK & CO. INC.
发明人: Treiber, Lazslo R. , Lingham, Russell B. , Arison, Byron H. , Colwell, Lawrence F., Jr. , Dezeny, Georgette , Kohl, Nancy E.
IPC分类号: C07D295/088 , C12P17/14
CPC分类号: C07D295/088 , C12P17/14
摘要: A novel dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces . It inhibits HIV protease, and is useful in the prevention or treatment of infection by DIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventinp or treating infection by DIV are also described.
摘要翻译: 新型二肽等排物是与Streptomyces培养物孵育后的生物转化产物。 它可以抑制HIV蛋白酶,并且可用作预防或治疗DIV的感染和治疗AIDS,无论作为化合物,药学上可接受的盐,药物组合物成分,无论是作为前药还是作为与其它抗病毒药物的组合, 抗感染药,免疫调节剂,抗生素或疫苗。 还描述了治疗AIDS的方法和预防或治疗DIV感染的方法。
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公开(公告)号:EP0547671A2
公开(公告)日:1993-06-23
申请号:EP92203808.8
申请日:1992-12-08
申请人: MERCK & CO. INC.
发明人: Singh, Sheo Bux , Bills, Gerald F. , Lingham, Russell B. , Silverman, Keith C. , Zink, Deborah L.
IPC分类号: C07C57/13 , A61K31/19 , C07C211/00
CPC分类号: C12R1/645 , C07C57/13 , C07C69/602 , C12P7/44 , C12P17/04
摘要: This invention relates to pharmaceutical compounds of structural formulae (I) and (II):
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:< CHEM>以及利用这些化合物抑制法呢基蛋白转移酶和致癌基因蛋白Ras的法呢基化的组合物和方法。
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公开(公告)号:EP0480711A1
公开(公告)日:1992-04-15
申请号:EP91309292.0
申请日:1991-10-09
申请人: MERCK & CO. INC.
发明人: Treiber, Laszlo R. , Dezeny, Georgette , Colwell, Lawrence F. , Lingham, Russell B. , Arison, Byron H. , Thompson, Wayne J. , Balani, Suresh Kumar
IPC分类号: C07C271/22 , C12P13/02
CPC分类号: C07C271/22 , C12P13/02
摘要: A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces . It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a 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: 二肽等体积是与Streptomyces培养物孵育后的生物转化产物。 它抑制HIV蛋白酶,并且可用作预防或治疗HIV感染和治疗艾滋病,作为化合物,药学上可接受的盐,药物组合物成分,无论作为前药或与其它抗病毒药物的组合, 抗感染药,免疫调节剂,抗生素或疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。
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公开(公告)号:EP0547671A3
公开(公告)日:1993-08-25
申请号:EP92203808.8
申请日:1992-12-08
申请人: MERCK & CO. INC.
发明人: Singh, Sheo Bux , Bills, Gerald F. , Lingham, Russell B. , Silverman, Keith C. , Zink, Deborah L.
IPC分类号: C07C57/13 , A61K31/19 , C07C211/00
CPC分类号: C12R1/645 , C07C57/13 , C07C69/602 , C12P7/44 , C12P17/04
摘要: This invention relates to pharmaceutical compounds of structural formulae (I) and (II):
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:以及使用这些化合物抑制法尼基蛋白转移酶和癌基因蛋白Ras的法尼基化的组合物和治疗方法。
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公开(公告)号:EP0526936A3
公开(公告)日:1993-05-05
申请号:EP92202300.7
申请日:1992-07-25
申请人: MERCK & CO. INC.
发明人: Meinz, Maria Sandrino , Pelaez, Fernando , Omstead, Mary Nallin , Milligan, James A. , Diez, Maria Teresa , Onishi, Janet C. , Bergstrom, James D. , Jenkins, Rosalind F. , Harris, Guy H. , Jones, E. Tracy Turner , Huang, Leeyuan , Kong, Yu Lin , Lingham, Russell B. , Zink, Deborah
IPC分类号: C07C235/76 , C07D209/20 , A61K31/195 , A61K31/405 , C07C211/10 , C07C215/12 , C07C279/14
CPC分类号: C12P13/04 , C07C235/76 , C07D209/20
摘要: This invention relates to compounds of structural formula (I): which are squalene synthase inhibitors and thus useful as cholesterol lowering agents, and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).
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公开(公告)号:EP0526936A2
公开(公告)日:1993-02-10
申请号:EP92202300.7
申请日:1992-07-25
申请人: MERCK & CO. INC.
发明人: Meinz, Maria Sandrino , Pelaez, Fernando , Omstead, Mary Nallin , Milligan, James A. , Diez, Maria Teresa , Onishi, Janet C. , Bergstrom, James D. , Jenkins, Rosalind F. , Harris, Guy H. , Jones, E. Tracy Turner , Huang, Leeyuan , Kong, Yu Lin , Lingham, Russell B. , Zink, Deborah
IPC分类号: C07C235/76 , C07D209/20 , A61K31/195 , A61K31/405 , C07C211/10 , C07C215/12 , C07C279/14
CPC分类号: C12P13/04 , C07C235/76 , C07D209/20
摘要: This invention relates to compounds of structural formula (I):
which are squalene synthase inhibitors and thus useful as cholesterol lowering agents, and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).摘要翻译: 本发明涉及结构式(I)的化合物:作为角鲨烯合成酶抑制剂的
,因此可用作胆固醇降低剂和抗真菌剂。 这些化合物也是法呢基蛋白转移酶的抑制剂和致癌基因蛋白Ras的法呢基化,因此可用于治疗癌症。 本发明还涉及获得结构式(I)化合物的方法。
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