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    Fermentation analogs of virginiamycin M.sub.1
    5.
    发明授权
    Fermentation analogs of virginiamycin M.sub.1 失效
    维吉尼亚霉素M1的发酵类似物

    公开(公告)号：US5006466A

    公开(公告)日：1991-04-09

    申请号：US426836

    申请日：1989-10-26

    申请人： Yiu-kuen T. Lam ,  Otto D. Hensens ,  Raymond S. Chang ,  Cheryl D. Schwartz ,  Deborah L. Zink

    发明人： Yiu-kuen T. Lam ,  Otto D. Hensens ,  Raymond S. Chang ,  Cheryl D. Schwartz ,  Deborah L. Zink

    IPC分类号： A61K38/00 ,  C07K5/078 ,  C12P17/18

    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。

    Therapeutic virginiamycin M.sub.1 analogs
    7.
    发明授权
    Therapeutic virginiamycin M.sub.1 analogs 失效
    治疗维吉尼亚霉素M1类似物

    公开(公告)号：US4859690A

    公开(公告)日：1989-08-22

    申请号：US934212

    申请日：1986-11-21

    申请人： Yiu-kuen T. Lam ,  Raymond S. Chang ,  Otto D. Hensens ,  Cheryl D. Schwartz ,  Deborah L. Zink

    发明人： Yiu-kuen T. Lam ,  Raymond S. Chang ,  Otto D. Hensens ,  Cheryl D. Schwartz ,  Deborah L. Zink

    IPC分类号： A61K38/00 ,  C07K5/078 ,  C12P17/18

    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。