Abstract: Dipeptide mimics which contain phosphorus and their pharmaceutical use and preparation are disclosed. The compounds have dehydropeptidase (DHP) enzyme inhibitor activity.
Type:
Grant
Filed:
August 17, 1989
Date of Patent:
October 9, 1990
Assignee:
Merck & Co., Inc.
Inventors:
William H. Parsons, William R. Schoen, ARthur A. Patchett
Abstract: The 4-acryloxyazetidin-2-ones, which are intermediates in the production of carbapenems and penems, are produced from 4-furanylazetidin-2-ones by electrochemical methods.
Type:
Grant
Filed:
June 21, 1989
Date of Patent:
August 28, 1990
Assignee:
Merck & Co., Inc.
Inventors:
Joseph E. Lynch, Ralph P. Volante, William L. Laswell, Ichiro Shinkai
Abstract: 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, II and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No.
Abstract: Disclosed are steroidal derivatives of glycolipids, in which steroids are bridged, via a medium length hydrocarbon chain, to 1-thio-D-mannopyranoses or 1-thio-L-fucopyranoses that protect an immunocompromised host, particularly resulting from an AIDS-related virus, against opportunistic infection.
Type:
Grant
Filed:
June 18, 1987
Date of Patent:
July 17, 1990
Assignee:
Merck & Co., Inc.
Inventors:
Philippe L. Durette, Mitree M. Ponpipom, William K. Hagmann
Abstract: Mercaptan substituted silicon compounds are produced by the reaction of amine with carboxyl. UV curable silicon compositions are produced from such compounds.
Abstract: Compounds having the formula: ##STR1## wherein R.sup.1 is --NH(C.dbd.O)OR.sup.5, --NH(C.dbd.NH)NH.sub.2 or --NH(C.dbd.N--NO.sub.2)HN.sub.2 ; R.sup.2 is hydrogen, C.sub.1-8 alkyl or C.sub.6-8 aryl; n is 2 to 6; and R.sup.5 is hydrogen,C.sub.1-8 alkyl, C.sub.6-8 aryl, or C.sub.7-8 alkaryl; are disclosed in addition to methods to employ such compounds to induce migration of endothelial cells into denuded areas of vessel lining and to treat malignant hypercalcemia.
Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDs-related (HIV) virus.
Abstract: The 4-acyloxyazetidin-2-ones, which are intermediates in the production of carbapenems and penems, are produced from 4-furanylazetidin-2-ones by a sequential oxidation-reduction-oxidation reaction scheme.
Type:
Grant
Filed:
June 21, 1989
Date of Patent:
May 8, 1990
Assignee:
Merck & Co., Inc.
Inventors:
Joseph E. Lynch, William L. Laswell, Ralph P. Volante, Ichiro Shinkai
Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDS-related (HIV) virus.
Abstract: Sodium fluorosilanolate catalyst is disclosed which has improved effectiveness as a catalyst to produce fluorosilicone polymer and which at the same time improves fluorosilicone polymer purity.
Abstract: Immunologically intact protein or peptide immunogens are recovered from vaccines consisting of immunogen-aluminum hydroxide (alum) complexes. Recovery consists of dissolution of the complexes with an alkali metal salt of a carboxylic acid at a basic pH, reduction of the pH to physiological levels, removal of excess dissolvent and isolation of the protein or peptide immunogen.
Abstract: 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.
Type:
Grant
Filed:
March 25, 1988
Date of Patent:
January 16, 1990
Assignee:
Merck & Co., Inc.
Inventors:
Yiu-kuen T. Lam, Raymond S. Chang, Otto D. Hensens, Cheryl D. Schwartz, Deborah L. Zink
Abstract: An emulsion where water is a continuous phase and having a discontinuous oil phase comprising:(a) silicone hydrides containing units of the formula:R.sub.a H.sub.b SiO.sub.(4-a-b)/2where a may be 0, 1, or 2; b may be 1 or 2; a+b may be 1, 2, or 3; R is a substituted or unsubstituted hydrocarbon radical of 1 to 12 carbon atoms; and(b) hydroxy substituted silicone containing units of the formula:R.sub.c (OH).sub.d SiO.sub.(4-c-d)/2wherein c is 1, 2, or 3; d is 1 or 2; c+d may be 2, 3, or 4; and R is a substituted or unsubstituted hydrocarbon radical of from 1 to 12 carbon atoms.
Abstract: Disclosed are specific dipeptidyl 2-amino-1,2-dideoxy-D-glucoses which, either alone, or in combintion with an anti-AIDS drug, e.g. azidothymidine, protect an immunocompromised human host, resulting from an AIDS-related virus, against opportunistic, bacterial, fungal and viral infections, as well as help to suppress the AIDS-related virus itself.
Abstract: Disclosed are specific dipeptidyl 4-0, 6-0-acyl-2-amino-2-deoxy-D-glucose derivatives which, either alone, or in combination with an anti-AIDS drug, e.g. azidothymidine, protect against opportunistic bacterial, fungal and viral infection in a human host immunocompromised by an AIDS-related virus, as well as help to suppress the AIDS-related virus itself.
Abstract: Disclosed are specific dipeptidyl saccharide derivatives which alone, or in combination with an anti-AIDS drug, e.g. azidothymidine, provide protection against opportunistic infection in human individuals whose resistance to infection has been specifically suppressed by an AIDS-related (HIV) virus, as well as help to suppress the AIDS-related infection itself.
Abstract: Disclosed are specific dipeptidyl 5-0, 6-0-Acyl-2-amino-2-deoxy-D-glucofuranoses, which, either alone, or in combination with an anti-AIDS drug, e.g. azidothymidine, provide protection in human individuals whose resistance to infection has been specifically suppressed by an AIDS-related (HIV) virus, as well as help to suppress the AIDS-related infection itself.