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    • 3. 发明公开
    • Virginiamycin analogs
    • Fermentationsanaloge von弗吉尼亚霉素M1。
    • EP0269322A1
    • 1988-06-01
    • EP87310022.6
    • 1987-11-12
    • Merck & Co., Inc.
    • Lam, Yiu-Kuen T.Chang, Raymond S.Hensens, Otto D.Schwartz, Cheryl D.Zink, Deborah L.Woodruff, H. Boyd
    • C12P17/18C12P17/16C12P1/06C07D498/18A61K31/395A61K31/41A23K1/17
    • C12R1/58A61K38/00
    • Virginiamycin M₁ having the Formula:
      and virginiamycin M₁ analogs having the Formulae I-IV:


      Virginiamycin M₁ 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 M₁ 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.
    • 具有式:的弗吉尼亚霉素M1和具有式I-IV的维吉尼亚霉素M1类似物: 维生素M1和类似物I-IV是缩胆囊素(CCK)和胃泌素的拮抗剂。 缩胆囊素拮抗剂可用作止痛剂,以及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胃泌素的受体,并且可用作治疗溃疡,肿瘤或其他胃肠道疾病的药剂。 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制备。