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1.发明授权
公开(公告)号：US5087702A
公开(公告)日：1992-02-11
申请号：US647945
申请日：1991-01-30
IPC分类号： C07D471/04 , C12P17/18
CPC分类号： C12P17/182 , C07D471/04
摘要： Fermentation of the microorganism Streptomyces sp. (MA6750) ATCC No. 55042 in the presence of the Angiotensin II (A II) receptor antagonist of the following structure: ##STR1## yields an analog having a shikimate sugar-like moiety attached to the tetrazole, the said analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II angatonists.
摘要翻译： 微生物发酵链霉菌Streptomyces sp。 （MA6750）ATCC No.55042在存在下列结构的血管紧张素II（AII）受体拮抗剂的情况下：产生具有连接于四唑的眨眼糖基部分的类似物，所述类似物也是 可用于治疗高血压和充血性心力衰竭的II拮抗剂和已知对A II血管炎症反应的其他适应症。
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2.发明授权
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：US5290772A
公开(公告)日：1994-03-01
申请号：US899235
申请日：1992-06-16
CPC分类号： C12R1/01 , C07H19/01 , C12P17/188
摘要： Described is a process for producing an immunosuppressant, "demethimmunomycin" (L-683,7411) a C-31 demethylated analog of L-683,590 under fermentation conditions utilizing the microorganism, Actinoplanacete sp, (Merck Culture Collection MA 6559) ATCC No. 53771. 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： 描述了在使用微生物Actinoplanacete sp（Merck Culture Collection MA 6559）ATCC No.53771的发酵条件下生产免疫抑制剂“demethimmunomycin”（L-683,71411）L-683,590的C-31去甲基化类似物的方法 大环内酯类免疫抑制剂可用于预防外来器官移植的人宿主排斥反应 骨髓和心脏移植。
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公开(公告)号：US5268370A
公开(公告)日：1993-12-07
申请号：US872741
申请日：1992-04-22
IPC分类号： C07D498/18 , C07H19/01 , C12P17/18 , C12P19/44 , A61K31/33 , C07D498/16
CPC分类号： C07D498/18 , C07H19/01 , C12P17/188 , C12P19/445
摘要： Described is a new immunosuppressant, L-683,519, a monodemethylated rearranged derivative of L-679,934, (FK-506) produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Culture Collection MA 6474) ATCC No. 53828. 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-683,519，L-679,934的单甲基化重排的衍生物（FK-506），其在使用微生物，不明的放线菌（Merck Culture Collection MA 6474）ATCC No.58288的发酵条件下产生。大环内酯类免疫抑制剂是 可用于预防人体宿主排斥外来器官移植物，例如 骨髓和心脏移植。
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公开(公告)号：US5252612A
公开(公告)日：1993-10-12
申请号：US905075
申请日：1992-06-24
IPC分类号： C07D498/18 , C07H19/01 , C12P1/06 , A61K35/00
CPC分类号： C07D498/18 , C07H19/01 , C12P1/06
摘要： Described is a new immunosuppressant, L-683,756, a bisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. 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-683,756，L-683,590的双脱甲基化环重排衍生物，其在使用微生物Actinoplanacete sp。 （Merck Culture Collection MA 6559）ATCC No.53771.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。 骨髓和心脏移植。
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公开(公告)号：US4981792A
公开(公告)日：1991-01-01
申请号：US213063
申请日：1988-06-29
IPC分类号： A61K31/395 , A61K35/74 , A61P37/06 , C07D213/50 , C07D213/79 , C07D493/18 , C07D498/18 , C07G99/00 , C07H19/01 , C12P17/18 , C12R1/01
CPC分类号： C07D493/18 , C07H19/01 , C12P17/18 , Y10S435/827
摘要： Described is a process for producing a new immunosuppressant, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934 under novel fermentation conditions utilizing the microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in prevent human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
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公开(公告)号：US5202258A
公开(公告)日：1993-04-13
申请号：US847873
申请日：1992-03-09
申请人： Shieh-Shung T. Chen , Byron H. Arison , George M. Garrity , Edward S. Inamine , Sagrario Mochales , Linda S. Wicker
发明人： Shieh-Shung T. Chen , Byron H. Arison , George M. Garrity , Edward S. Inamine , Sagrario Mochales , Linda S. Wicker
CPC分类号： C12R1/045 , Y10S436/827
摘要： Described is a new microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The microorganism acts as a demethylating agent and can produce the new immunosuppressants, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934, and "demethimmunomycin" (L-683,742) a C-31 demethylated analog of L-683,590, under novel fermentation conditions. These macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
摘要翻译： 描述了一种新的微生物Actinoplanacete sp。（Merck Culture Collection MA 6559）ATCC No.53771.微生物作为去甲基化剂，可以产生新的免疫抑制剂“吗啡霉素”（L-682,993）C-31去甲基化的类似物 的L-679,934和“demethimmunomycin”（L-683,742）L-683,590的C-31去甲基化类似物，在新的发酵条件下。 这些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。 骨髓和心脏移植。
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公开(公告)号：US4975372A
公开(公告)日：1990-12-04
申请号：US297631
申请日：1989-01-13
IPC分类号： C12P17/18 , A61K31/445 , A61P37/00 , A61P37/02 , A61P37/04 , A61P37/06 , C07D498/18 , C07H19/01 , C12P1/06 , C12R1/01
CPC分类号： C07D498/18 , C07H19/01 , C12P1/06 , Y10S435/826
摘要： Described is a new immunosuppressant, L-685,487, a monodemethylated rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Cultrue Collection MA 6474) ATCC No. 53828. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
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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：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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