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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：US4696925A
公开(公告)日：1987-09-29
申请号：US695113
申请日：1985-01-25
IPC分类号： A61K31/55 , A61P1/00 , C07D487/04 , C07D487/22 , C07D519/00 , C12P17/18 , C12R1/66
CPC分类号： C07D487/04 , C12P17/182 , C12R1/66 , Y10S435/913
摘要： Products of Aspergillus alliaceus fermentation having cholecystokinin (CCK) antagonist activity, their preparation and use are disclosed.
摘要翻译： 公开了具有胆囊收缩素（CCK）拮抗剂活性的连翘曲霉的发酵产物及其制备和应用。
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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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4.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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公开(公告)号：US4766112A
公开(公告)日：1988-08-23
申请号：US857670
申请日：1986-04-30
IPC分类号： A23K20/195 , C07H19/01 , C12P19/62 , A61K31/71 , C07H17/08
CPC分类号： C07H19/01 , A23K20/195 , C12P19/623 , C12R1/365
摘要： There are disclosed macrolides isolated from the fermentation broth, with avermectin Bla, avermectin Blb or 22,23-dihydro avermectin Bla as a substrate, of a known microorganism identified as MA-6181. The structure of the novel compounds isolated from the microorganism are presented based upon analytical studies. The compounds are highly potent antiparasitic, insecticidal, and anthelmintic agents. Compositions for such uses are also disclosed.
摘要翻译： 公开了从发酵液中分离出的大环内酯类，其中以除虫菌素Bla，阿维菌素B1b或22,23-二氢阿凡曼菌素Bla作为底物，鉴定为MA-6181。 基于分析研究提出了从微生物中分离的新化合物的结构。 这些化合物是非常有效的抗寄生虫，杀虫剂和驱肠剂。 还公开了用于此类用途的组合物。
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6.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：US5116870A
公开(公告)日：1992-05-26
申请号：US533744
申请日：1990-06-06
申请人： Robert L. Smith , Wasyl Halczenko , George D. Hartman , Gerald E. Stokker , Edward S. Inamine , Otto D. Hensens , David R. Houck , Ta J. Lee
发明人： Robert L. Smith , Wasyl Halczenko , George D. Hartman , Gerald E. Stokker , Edward S. Inamine , Otto D. Hensens , David R. Houck , Ta J. Lee
IPC分类号： C07D309/30 , C12P7/62 , C12P17/06
CPC分类号： C12R1/365 , C07D309/30 , C12P17/06 , C12P7/62 , Y10S514/824
摘要： Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##
摘要翻译： 新型3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂可用作抗高胆固醇血症药，并由以下一般结构式（II）表示：
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8.发明授权
公开(公告)号：US4997755A
公开(公告)日：1991-03-05
申请号：US181877
申请日：1988-04-14
CPC分类号： C12R1/365 , C07D309/30 , C12P17/06 , C12P7/62 , Y10S435/872
摘要： A microbiological process is described for the preparation of 6-desmethyl-6-.beta.-hydroxymethyl and 6-desmethyl-6-.beta.-carboxylovastatin derivatives and 8-acyl analogs thereof.
摘要翻译： 描述了用于制备6-去甲基-6β-羟基甲基和6-去甲基-6β-羧基伐昔他汀衍生物及其8-酰基类似物的微生物过程。
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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：US4666937A
公开(公告)日：1987-05-19
申请号：US830333
申请日：1986-02-20
IPC分类号： C07D493/22 , A01N43/90 , A23K1/16 , A61K31/365 , A61P33/10 , C07H19/01 , C12P17/08 , C12P17/18 , C12P19/44 , C12R1/645
CPC分类号： C07H19/01 , A01N43/90 , C12P17/08 , C12P19/445 , Y10S435/822
摘要： There are disclosed novel compounds which are derived from 22,23-dihydro avermectin Bla aglycone, 13-deoxy-22,23 dihydro overmectin Bla aglycone and 13-deoxy-22,23-dihydro overmectin Blb aglycone. The six compounds are hydroxy adducts of the substrate avermectin compound at the 12a, 24, 24a, 26, 26a and 27 positions. The hydroxy adducts are prepared by incubating the substrate with the microorganism Cunninghamella blakesleeana and isolating the hydroxy adducts from the fermentation broth. The compounds are highly potent antiparasitic, insecticidal and anthelmintic agents.
摘要翻译： 公开了衍生自22,23-二氢阿凡曼菌素Bla糖苷配基，13-脱氧-22,23二氢过表单素Bla糖苷配基和13-脱氧-22,23-二氢过度连接素Blb糖苷配基的新化合物。 六种化合物是在12a，24,24a，26，26a和27位置的基质阿维菌素化合物的羟基加合物。 羟基加合物通过将底物与微生物Cunninghamella blakesleeana孵育并从发酵液中分离羟基加合物来制备。 这些化合物是高度有效的抗寄生虫，杀虫剂和驱肠剂。
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