Abstract: The instant invention is directed to a process for enhancing the efficacy of alcohol-based skin antiseptics comprising adding at least one alcohol-soluble viscosifying agent to an alcohol-based disinfectant, thereby lowering its alcohol evaporation rate and markedly increasing the exposure time that disinfecting concentrations of alcohol are present on skin. The improved alcohol-based antiseptics thus obtained are also claimed.
Abstract: Novel avermectin derivatives are disclosed, wherein the 4"-hydroxy group is replaced by a substituted acylamino or benzoylamino group. These avermectin derivatives can be further derivatized at the 5- and 23-positions as ketoximes or O-substituted ketoximes. The 4"-substituted avermectin derivatives are prepared by the acylation of the known 4"-aminoavermectins with acylating reagents. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
Abstract: A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizi ne-2,4'-imidazolidin]-3'-yl)ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2 -yl)amino]ethyl]methanesulfonamide is described.
Type:
Grant
Filed:
March 16, 1989
Date of Patent:
July 17, 1990
Assignee:
Merck & Co., Inc.
Inventors:
Ann E. DeCamp, Ralph P. Volante, Anthony O. King, Ichiro Shinkai
Abstract: Disclosed are compounds having the formula: ##STR1## wherein: R.sub.1 is hydrogen, analkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group;R.sub.2 is an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group, an alkyl group having 1 to 6 carbon atoms which contains an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups having 1 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.These compounds increase the sensitivity of hypoxic cancer cells to radiation. Methods of preparing such compounds, protocols for administering them to human patients and animals, and pharmaceutical compositions containing them are also disclosed.
Abstract: Novel 5-carbamoylthieno[2,3-b]thiophene-2-sulfonamides and derivatives thereof are prepared in reactions of 5-methoxycarbonylthieno-[2,3-b]thiophene-2-sulfonamide with alkylamines, alkoxyalkylamines and hydroxyalkylamines. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
Abstract: A compound of the formula: ##STR1## wherein: n is an integer 2,3,4, or 5; R.sub.1 is hydrogen or an alkyl group; andR.sub.2 and R.sub.3 are defined as follows:R.sub.2 is hydrogen or an alkyl group;R.sub.3 is hydrogen or an alkyl group; orR.sub.2 and R.sub.3 together form a heterocyclic ring, e.g. piperidine, pyrrolidine.The compounds have high radiosensitizing activity, and act as agents toxic to hypoxic cells in the absence of radiation.
Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R.sup.1 is halogen, --SR.sup.4 wherein R.sup.4 is H or alkyl of 1 to 4 carbon atoms, --OCH.sub.3, --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, --NR.sup.4 R.sup.5 wherein R.sup.4 is as defined above and R.sup.5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R.sup.1 is --N(CH.sub.3).sub.3.sup.+ X.sup.-whereinX is halogen or --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms;R.sup.2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl;R.sup.3 is A or B whereinA is ##STR2## and B is ##STR3## wherein R.sup.6 and R.sup.7 are independently selected from H and ##STR4## wherein R.sup.8 and R.sup.9 are independently selected from pharmaceutically acceptable cations and H, or R.sup.6 and R.sup.
Type:
Grant
Filed:
February 29, 1988
Date of Patent:
January 30, 1990
Assignee:
Merck & Co., Inc.
Inventors:
Richard L. Tolman, Wallace Ashton, Malcolm Maccoss
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: 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: 1-Aryloxy-3-(substituted alkylamino)-2-propanols having the general information: ##STR1## and their pharmaceutically acceptable salts exhibit cardioselective .beta.-adrenergic blocking activity, and are useful as antihypertensive, cardioprotective, antiarrhythmic and, antianginal agents.
Abstract: A compound of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are defined as follows:R.sub.1 is hydrogen, an alkyl group, or an alkyl group having one or more hydroxy groups;R.sub.2 is an alkyl group having one or more hydroxy groups, or an alkyl group containing an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups same or different, or two alkyl groups which together form a cyclic amine, e.g. piperidine;R.sub.3 is hydrogen or an alkyl group; andR.sub.4 is hydrogen or an alkyl group.The compounds have high radiosensitizing activity and selectivity for hypoxic cells.
Abstract: (S)-9-(2,3-dihydroxy-1-propoxymethyl)guanine has potent antiherpetic activity which is superior to the corresponding racemic mixture or the (R)-enantiomer and also is much more potent than 9-(2-hydroxyethoxymethyl)guanine. Acyl derivatives (prodrugs) of the (S)-enantiomer, which are more effective than the corresponding (R)-enantiomer analogs or related racemic mixtures provide formulation advantages and even higher plasma half lives in animals or man than the (S)-isomer.
Type:
Grant
Filed:
February 8, 1988
Date of Patent:
November 14, 1989
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Laura F. Canning, Arthur K. Field, Richard L. Tolman
Abstract: A multilaminate transdermal drug delivery system containing only dissolved drug in the drug reservoir is described. The delivery system comprises a backing layer, a reservoir layer and a membrane layer, wherein the drug in the reservoir is completely dissolved and the control of delivery is effected by the joint action of reservoir and membrane.
Abstract: The compound 4"-deoxy-4"-N-methylamino avermectin Bla/Blb has been discovered to have unexpected properties when used as an agricultural insecticide. Specifically, the compound is considerably more active against insects, particularly lepidoptera, than closely related compounds, and the compound exhibits significantly lower levels of mammalian toxicity and aquatic animal toxicity. Thus the compound presents a much wider margin of safety towards the human appliers of the compound and to other mammals that come in contact with treated areas as well as wider margins of safety to aquatic animals to which any spray drift or run-off containing the compound may be directed.
Abstract: Certain fungistats when employed in combination have been found to exhibit synergistic antifungal properties and further exhibit fungicidal properties.
Abstract: Carboxyalkyl urea compounds and derivatives thereof are disclosed which are useful as angiotensin converting enzyme (ACE) inhibitors and as antihypertensives. These compounds and derivatives are represented by the general formula: ##STR1## An illustrative specie falling within this general formula is:N-(2-carboxy-4-phenylbutyl-N-isopropylaminocarbonyl-L-tryptophan.
Type:
Grant
Filed:
June 27, 1983
Date of Patent:
September 12, 1989
Assignee:
Merck & Co., Inc.
Inventors:
William J. Greenlee, David G. Hangauer, Jr., Arthur A. Patchett
Abstract: Novel antiestrogen compositions are disclosed as having anabolic activities. The compositions disclosed herein are useful for enhancing growth and feed conversion animals, particularly to poultry, usually in admixture with animal sustenance. Also, disclosed herein are methods of administering said compositions to animals.
Type:
Grant
Filed:
June 10, 1986
Date of Patent:
August 22, 1989
Assignee:
Merck & Co., Inc.
Inventors:
Gaylord E. McKissick, Roger M. Weppelman
Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.