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公开(公告)号:US5294627A
公开(公告)日:1994-03-15
申请号:US936708
申请日:1992-08-27
IPC分类号: A61K45/06 , C07D493/08 , H61K31/335 , H61K31/38
CPC分类号: C07D493/08 , A61K45/06
摘要: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds 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.
摘要翻译: 结构式(I)化合物通过定向生物合成制备。 这些化合物是角鲨烯合成酶抑制剂,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。
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公开(公告)号:US5221625A
公开(公告)日:1993-06-22
申请号:US818936
申请日:1992-01-10
申请人: Shieh-Shung T. Chen , Raymond F. White , Georgette Dezeny , Brian R. Petuch , George M. Garrity , Byron H. Arison , Amy M. Bernick
发明人: Shieh-Shung T. Chen , Raymond F. White , Georgette Dezeny , Brian R. Petuch , George M. Garrity , Byron H. Arison , Amy M. Bernick
IPC分类号: C12P17/16
CPC分类号: C12P17/16 , Y10S435/899
摘要: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6963) ATCC No. 55230. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
摘要翻译: 描述了在新型发酵条件下利用新型微生物Streptomyces sp。生产新的免疫抑制剂,FR-900520的C-19 / C-22环状半缩酮(化合物I)生物转化类似物的方法。 (Merck Culture Collection MA6963)ATCC No.55530。大环内酯类免疫抑制剂可用于预防异种器官移植的人宿主排斥反应。 骨髓,肝,肺,肾和心脏移植。
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公开(公告)号:US5070015A
公开(公告)日:1991-12-03
申请号:US597604
申请日:1990-10-15
IPC分类号: C12P19/62
CPC分类号: C12P19/623 , Y10S435/839 , Y10S435/897
摘要: Incubation of 13-deoxy ivermectin aglycone with a species of B. subtilis and of S. griseus results in the production of 13-.beta. ivermectin monoglucopyranoside as the major product and of 5-.beta. ivermectin monoglucopyranoside as the minor product.
摘要翻译: 13-脱氧伊维菌素糖苷配基与一种枯草芽孢杆菌和灰泥灰霉菌的融合导致13-β-伊维菌素单吡喃葡萄糖苷作为主要产物和5-β伊维菌素单吡喃葡萄糖苷作为次要产物的产生。
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4.
公开(公告)号:US5302604A
公开(公告)日:1994-04-12
申请号:US957316
申请日:1992-10-06
申请人: Kevin M. Byrne , Shieh-Shung T. Chen , Louis Kaplan , John G. MacConnell , Brian R. Petuch , Raymond F. White , Byron H. Arison
发明人: Kevin M. Byrne , Shieh-Shung T. Chen , Louis Kaplan , John G. MacConnell , Brian R. Petuch , Raymond F. White , Byron H. Arison
IPC分类号: A61K45/06 , C07D493/08 , A61K31/38 , A61K31/44
CPC分类号: C07D493/08 , A61K45/06
摘要: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.
摘要翻译: 结构式(I)化合物通过定向生物合成制备。 这些化合物是角鲨烯合成酶抑制剂,因此可用作胆固醇降低剂,抗真菌剂和癌症治疗剂。
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5.
公开(公告)号:US5250422A
公开(公告)日:1993-10-05
申请号:US880870
申请日:1992-05-11
CPC分类号: C07H19/01 , C12P19/623
摘要: Incubation of 13.beta.-hydroxy ivermectin aglycone with a species of Bacillus subtilis or the incubation of 13-deoxy ivermectin aglycone with a mixed culture of a species of Bacillus subtilis and of Streptomyces griseus results in the production of 13-.beta. ivermectin monoglucopyranoside as the major product and of 5-.beta. ivermectin monoglucopyranoside as the minor product.
摘要翻译: 将13个β-羟基伊维菌素糖苷配基与一种枯草芽孢杆菌的孵育或13-脱氧伊维菌素糖苷配基与枯草芽孢杆菌和灰色链霉菌的混合培养物的孵育导致13-β-伊维菌素单吡喃葡萄糖苷的生产作为主要 产品和5-β伊维菌素单吡喃葡萄糖苷作为次要产品。
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公开(公告)号:US5210030A
公开(公告)日:1993-05-11
申请号:US542849
申请日:1990-06-25
IPC分类号: C07D498/18 , C12P17/16 , C12P17/18
CPC分类号: C07D498/18 , C12P17/188
摘要: Described is a new process for selectively acylating FK-506 type immunosuppressant macrolides, including immunomycin (FK-520), in the C-32 position, under novel conditions utilizing an immobilized lipase enzyme, an acyl donor, and a dry, non hydroxylic organic solvent. The enzyme is absorbed onto a solid support and the enzyme/support catalyzes the C-32 acylation. The enzyme/support complex can then be filtered from the reaction mixture and, recycled for use.
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公开(公告)号:US5198421A
公开(公告)日:1993-03-30
申请号:US691606
申请日:1991-04-26
CPC分类号: C12P9/00 , C07F9/091 , C07F9/117 , C07F9/6533 , C07F9/65527 , C07H19/01 , C07K7/56 , A61K38/00 , Y10S435/939 , Y10S930/27
摘要: There is disclosed a monophosphorylated cyclic lipopeptide compound obtained by biophosphorylating a cyclic lipopeptide related to echinocandins and having a peptide skeleton bearing several hydroxy groups wherein in the phosphorylated cyclic lipopeptide, the phosphate group is attached to the hydroxy group of the 4-hydroxyproline component of the lipopeptide. The compounds are useful for the control of fungi and parasites.
摘要翻译: 公开了通过生物磷酸化与棘白菌素相关的环状脂肽并具有多个羟基的肽骨架获得的单磷酸化环状脂肽化合物,其中磷酸化环状肽中磷酸基与4-羟基脯氨酸成分的羟基连接 脂肽。 这些化合物可用于控制真菌和寄生虫。
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公开(公告)号:US5219985A
公开(公告)日:1993-06-15
申请号:US607430
申请日:1990-10-31
申请人: Brian R. Petuch , Byron H. Arison
发明人: Brian R. Petuch , Byron H. Arison
摘要: A compound having the formula ##STR1## and a method of obtaining said compound is described. The compound has antifungal properties.
摘要翻译: 描述了具有式“IMAGE”的化合物和获得所述化合物的方法。 该化合物具有抗真菌性质。
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公开(公告)号:US4997849A
公开(公告)日:1991-03-05
申请号:US370481
申请日:1989-06-23
申请人: Brian R. Petuch , Byron H. Arison
发明人: Brian R. Petuch , Byron H. Arison
IPC分类号: C07C59/54 , C07C69/732 , C07D309/30
CPC分类号: C07C69/732 , C07C59/54 , C07D309/30 , Y10S514/824
摘要: Compounds of formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
摘要翻译: 式(I)和(II)的化合物:HMG-CoA还原酶抑制剂。
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