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公开(公告)号：US5006466A
公开(公告)日：1991-04-09
申请号：US426836
申请日：1989-10-26
CPC分类号： C12R1/58 , C07K5/06139 , C12P17/188 , A61K38/00 , Y10S435/886 , Y10S435/902
摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.
摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 弗吉尼亚霉素M1和式I，III和IV的类似物是通过控制好氧发酵链霉菌链霉菌ATCC No.55327产生的，而式II的类似物是通过化学合成制备的。
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公开(公告)号：US4859690A
公开(公告)日：1989-08-22
申请号：US934212
申请日：1986-11-21
CPC分类号： C12R1/58 , C07K5/06139 , C12P17/188 , A61K38/00
摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527. The analog of Formula II is produced by chemical synthesis.
摘要翻译： （I）图像（III）（IV）维他命霉素M1和类似物I -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 维生素霉素M1和式I，III和IV的类似物是通过控制好氧发酵的链霉菌链霉菌ATCC No.55327产生的。式II的类似物是通过化学合成制备的。
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公开(公告)号：US5137900A
公开(公告)日：1992-08-11
申请号：US644755
申请日：1991-01-23
CPC分类号： C07K5/06182 , A61K31/42 , A61K38/00
摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527. The analog of Formula II is produced by chemical synthesis.
摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 维生素霉素M1和式I，III和IV的类似物是通过控制好氧发酵的链霉菌链霉菌ATCC No.55327产生的。式II的类似物是通过化学合成制备的。
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4.发明授权Compositions having fermentation analogs of virginiamycin M.sub.1 as active ingredient 失效具有维吉尼亚霉素M1的发酵类似物作为有效成分的组合物
公开(公告)号：US4894370A
公开(公告)日：1990-01-16
申请号：US173342
申请日：1988-03-25
CPC分类号： C12R1/58 , C07K5/06139 , C12P17/188 , A61K38/00
摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.
摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 弗吉尼亚霉素M1和式I，III和IV的类似物是通过控制好氧发酵链霉菌链霉菌ATCC No.55327产生的，而式II的类似物是通过化学合成制备的。
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5.发明授权Fermentation analogs of Virginiamycin M.sub.1 to treat panic and anxiety disorder 失效VIRGINIAMYCIN M1的发酵模拟物治疗神经性和恶性疾病
公开(公告)号：US5189050A
公开(公告)日：1993-02-23
申请号：US709676
申请日：1991-06-03
申请人： Roger M. Freidinger , Mark G. Bock , Yiu-Kuen T. Lam , Raymond S. Chang , Otto D. Hensens , Cheryl D. Schwartz , Deborah L. Zink
发明人： Roger M. Freidinger , Mark G. Bock , Yiu-Kuen T. Lam , Raymond S. Chang , Otto D. Hensens , Cheryl D. Schwartz , Deborah L. Zink
IPC分类号： A61K31/42 , A61K38/00 , A61P25/00 , A61P25/20 , A61P25/30 , A61P27/02 , A61P35/00 , C07D498/18 , C07K5/078 , C12P17/18 , C12R1/58
CPC分类号： C07K5/06182 , A61K38/00
摘要： Pharmaceutical compositions containing Virginiamycin M.sub.1 having the Formula: ##STR1## and Virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
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公开(公告)号：US4762923A
公开(公告)日：1988-08-09
申请号：US934231
申请日：1986-11-21
IPC分类号： A61K31/41 , A61K38/00 , A61K38/55 , A61P1/00 , A61P25/00 , C07D498/04 , C07K5/078 , C12P17/18 , C12R1/58 , C07D498/16 , A61K31/42 , C12P17/14
CPC分类号： C12R1/58 , C07K5/06139 , C12P17/188 , A61K38/00
摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III, and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.
摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 维生素霉素M1和式I，III和IV的类似物通过对链霉菌链霉菌ATCC No.55327的受控好氧发酵产生，而式II的类似物通过化学合成产生。
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公开(公告)号：US5240910A
公开(公告)日：1993-08-31
申请号：US870065
申请日：1992-04-17
摘要： Novel cyclic depsipeptides derived from a culture of Microbispora are antagonists of the receptor for endothelin, a potent vasoconstrictor, and are thus useful in treating cardiovascular disorders. Endothelin has other physiological effects, and the endothelin receptor antagonists of the present invention thus also have other therapeutic uses. The compounds are cyclical depsipeptides of N-(pyrrol-2-carboxy) - L-phe, D-allo-Thr, D-Phe, D-Ala, D- or L-dihydroxyphenyl-Gly, and D-dihydroxyphenyl-Gly.
摘要翻译： 衍生自微生物双孢子培养物的新型环状缩酚酸肽是内皮素受体的拮抗剂，其是有效的血管收缩剂，因此可用于治疗心血管疾病。 内皮素具有其他生理作用，因此本发明的内皮素受体拮抗剂也具有其它治疗用途。 化合物是N-（吡咯-2-羧基）-L-phe，D-allo-Thr，D-Phe，D-Ala，D或L-二羟基苯基-Gly和D-二羟基苯基-Gly的循环衰减肽。
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公开(公告)号：US4981980A
公开(公告)日：1991-01-01
申请号：US407162
申请日：1989-09-14
申请人： Robert A. Giocobbe , Leeyuan Huang , Yu L. Kong , Yiu-Kuen T. Lam , Sagrario M. Del Val , Carol F. Wichmann , Deborah L. Zink
发明人： Robert A. Giocobbe , Leeyuan Huang , Yu L. Kong , Yiu-Kuen T. Lam , Sagrario M. Del Val , Carol F. Wichmann , Deborah L. Zink
IPC分类号： C07D307/94 , C12P17/04
CPC分类号： C07D307/94 , C12P17/04
摘要： Fermentation of a nutrient medium by a Hypomycetes fungus of the genus Memnoniella or Stachybotrys yields a product with a major component of structural formula I: ##STR1## which is an inositol monophosphate phosphatase inhibitor and thereby useful in the treatment of manic depression.
摘要翻译： 通过Memnoniella或Stachybotrys属的假单胞菌真菌发酵营养培养基产生具有结构式I的主要成分的产物：作为肌醇单磷酸酯磷酸酶抑制剂的作用（I），从而可用于治疗躁狂抑郁症。
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公开(公告)号：US5089530A
公开(公告)日：1992-02-18
申请号：US562353
申请日：1990-08-03
IPC分类号： A61K31/12 , A01N35/04 , A61K35/66 , A61P33/00 , A61P33/10 , C07C49/84 , C12P7/24 , C12P7/26 , C12P15/00 , C12R1/645
摘要： The fermentation of a fungal organism identified as Chrysosporium meridarium produces a novel binaphthalene compound which is a highly potent antiparasitic, insecticidal, and anthelminthic agent.
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公开(公告)号：US5019593A
公开(公告)日：1991-05-28
申请号：US079192
申请日：1987-07-29
IPC分类号： A01N37/44 , A01N37/46 , A01N47/44 , A61K31/195 , C07C67/00 , C07C229/30 , C07C231/00 , C07C231/12 , C07C233/47 , C07C239/00 , C07C279/14 , C12P13/00 , C12P13/02 , C12P13/04 , C12R1/66
CPC分类号： A01N37/44 , A01N47/44 , C07C279/14 , C12P13/04
摘要： A mixture of derivatives of 2-amino-3,4,5,14-tetrahydroxy-6-eicosenoic acid has been isolated from a culture medium after cultivation of microorganisms belonging to the genus Aspergillus. The compounds are useful as antifungal agents.
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