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公开(公告)号:US5431896A
公开(公告)日:1995-07-11
申请号:US923025
申请日:1992-07-30
IPC分类号: C12P17/16 , A61K31/445 , A61P37/00 , A61P37/06 , C07D498/18 , C07H19/01 , C12P17/18 , C12P19/44 , C12R1/55 , A61K35/00 , A61K31/395 , C07D498/16 , C07F7/04
CPC分类号: C07H19/01 , C12P19/445 , Y10S435/898
摘要: Described is a new immunosuppressant, L-687,819, a C-31 demethylated derivative of L-683,795 (FK-523), produced under fermentation conditions utilizing the new mutant microorganism, Streptomyces hygroscopicus subsp. ascomyceticus (Merck Culture Collection MA 6646) ATCC No. 53855, being a blocked mutant of Streptomyces hygroscopicus subsp. ascomyceticus (MA 6475) ATCC No. 14891. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
摘要翻译: 描述了一种新的免疫抑制剂L-687,819,L-683,795(FK-523)的C-31去甲基化衍生物,其在使用新的突变微生物,吸水链霉菌Subsp。 子囊菌纲(Merck Culture Collection MA 6646)ATCC No.53855是吸水链霉菌亚种的阻断突变体。 子囊菌纲(MA 6475)ATCC No.14891。大环内酯类免疫抑制剂可用于防止外来器官移植物的人宿主排斥。 骨髓和心脏移植。
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公开(公告)号:US5252471A
公开(公告)日:1993-10-12
申请号:US848573
申请日:1992-03-09
申请人: Kevin M. Byrne , Louis Kaplan , Mary N. Omstead
发明人: Kevin M. Byrne , Louis Kaplan , Mary N. Omstead
IPC分类号: A61K45/06 , C07D493/08 , C12P17/18 , C12N1/14
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 useful as cholesterol-lowering agents.
摘要翻译: 结构式(I)化合物通过定向生物合成制备。 这些化合物是可用作降胆固醇剂的角鲨烯合成酶抑制剂。
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公开(公告)号:US5318895A
公开(公告)日:1994-06-07
申请号:US956716
申请日:1992-10-05
IPC分类号: C12Q1/02 , C12Q1/18 , C07D498/00 , C12N1/00
CPC分类号: C12R1/685 , C12Q1/025 , Y10S435/911 , Y10S435/913 , Y10S435/917
摘要: Disclosed are new Aspergillus niger mutants which can be used for identifying active FK-506/ rapamycin type, or cyclosporin A type inununosuppressants in a broth, natural product extract, or composition exhibiting inununosuppressant activity. Specifically disclosed are the new mutants, ATCC No. 74085 (MF 5659), which is sensitive to FK-506 and rapamycin but resistant to cyclosporin A; ATCC No. 74086 (MF 5659) which is resistant to FK-506, cyclosporin A and rapamycin; and ATCC No. 74087 (MF 5661) which is resistant to FK-506 and rapamycin, but sensitive to cyclosporin A.
摘要翻译: 公开了可以用于鉴定活性FK-506 /雷帕霉素类型的新型黑曲霉突变体,或在肉汤,天然产物提取物或具有抑制剂活性的组合物中的环孢菌素A型抑制剂。 具体公开的是新的突变体ATCC No. 74085(MF5659),其对FK-506和雷帕霉素敏感,但对环孢菌素A具有抗性; 对抗FK-506,环孢菌素A和雷帕霉素的ATCC No.74086(MF5659); 和对抗FK-506和雷帕霉素但对环孢菌素A敏感的ATCC No.74087(MF5661)。
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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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公开(公告)号:US5834260A
公开(公告)日:1998-11-10
申请号:US914998
申请日:1997-08-20
申请人: Kevin M. Byrne , Arlene M. Dahl , Anne Dombrowski , Joyce A. Greene , John G. Ondeyka , Dan A. Ostlind , Sheo Bux Singh , Diane M. Vesey
发明人: Kevin M. Byrne , Arlene M. Dahl , Anne Dombrowski , Joyce A. Greene , John G. Ondeyka , Dan A. Ostlind , Sheo Bux Singh , Diane M. Vesey
IPC分类号: C12P17/10 , A01N45/00 , A61K31/403 , A61K31/407 , A61P33/00 , C07D209/70 , C07D209/80 , C07D209/94 , C07D491/04 , C07D491/052 , C07D491/14 , C07D491/153 , C07D491/16 , C07D491/22 , C12N1/14 , C12P17/16 , C12P17/18 , C12R1/645 , C07D209/62 , C07D491/048
CPC分类号: C07D209/80 , C07D209/70 , C07D491/04 , C07D491/14 , C12P17/10 , C12P17/18 , C12R1/645 , Y10S435/911
摘要: Novel compounds isolated from the fermentation of producing cultures of Nodulisporium sp. are antiparasitic and insecticidal agents.
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公开(公告)号:US5945317A
公开(公告)日:1999-08-31
申请号:US157862
申请日:1998-09-21
申请人: Kevin M. Byrne , Arlene M. Dahl , Anne Dombrowski , Joyce A. Greene , John G. Ondeyka , Dan A. Ostlind , Sheo Bux Singh , Diane M. Vesey
发明人: Kevin M. Byrne , Arlene M. Dahl , Anne Dombrowski , Joyce A. Greene , John G. Ondeyka , Dan A. Ostlind , Sheo Bux Singh , Diane M. Vesey
IPC分类号: C12P17/10 , A01N45/00 , A61K31/403 , A61K31/407 , A61P33/00 , C07D209/70 , C07D209/80 , C07D209/94 , C07D491/04 , C07D491/052 , C07D491/14 , C07D491/153 , C07D491/16 , C07D491/22 , C12N1/14 , C12P17/16 , C12P17/18 , C12R1/645 , C07D209/62 , C07D491/048
CPC分类号: C07D209/80 , C07D209/70 , C07D491/04 , C07D491/14 , C12P17/10 , C12P17/18 , C12R1/645 , Y10S435/911
摘要: Novel compounds isolated from the fermentation of producing cultures of Nodulisporium sp. are antiparasitic and insecticidal agents.
摘要翻译: 从产生Nodulisporium sp。培养物的发酵中分离的新型化合物。 是抗寄生虫剂和杀虫剂。
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