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AssigneeMerck & Co., Inc.
InventorsYiu-kuen T. Lam, Raymond S. Chang, Otto D. Hensens, Cheryl D. Schwartz, Deborah L. Zink
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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.
A pharmaceutical composition useful for treating gastrointestinal disorders, central nervous system disorders and regulating appetite in mammals comprising a pharmaceutically effective amount of virginiamycin M.sub.1 and an acceptable pharmaceutical carrier.
A pharmaceutical composition useful for treating gastrointestinal disorders, central nervous system disorders and regulating appetite in mammals comprising a pharmaceutically effective amount of the compound of Formula I ##STR9## and an acceptable pharmaceutical carrier.
A pharmaceutical composition useful for treating gastrointestinal disorders, central nervous system disorders and regulating appetite in mammals comprising a pharmaceutically effective amount of the compound of Formula III ##STR10## and an acceptable pharmaceutical carrier.
A pharmaceutical composition useful for treating gastrointestinal disorders, central nervous system disorders and regulating appetite in mammals comprising a pharmaceutically effective amount of the compound of Formula IV ##STR11## and an acceptable pharmaceutical carrier.
A pharmaceutical composition useful for treating bacterial infections in mammals comprising a pharmaceutically effective amount of the compound of Formula I ##STR12##
A pharmaceutical composition useful for treating bacterial infections in mammals comprising a pharmaceutically effective amount of the compound of Formula III ##STR13##
A pharmaceutical composition useful for treating bacterial infections in mammals comprising a pharmaceutically effective amount of the compound of Formula IV ##STR14##
A pharmaceutical composition useful for treating bacterial infections in mammals comprising a pharmaceutically effective amount of the compounds of Formula I ##STR15##
A pharmaceutical composition useful for treating bacterial infections in mammals comprising a pharmaceutically effective amount of virginiamycin M.sub.1 and the compounds of Formula I ##STR16##
Dependencies are inferred from the claim text.