Abstract: The present invention relates to a quinolone carboxylic acid derivative represented by the following the formula (I), ##STR1## wherein R.sub.1 is a lower alkyl group, R.sub.2 is a hydrogen atom or a lower alkyl group, R.sub.3 is a hydrogen atom or a halogen atom, R.sub.4 and R.sub.5 together form a five- or six-membered ring which may contain hetero atoms or may have substituents, provided that a compound wherein R.sub.1 is a methyl group, R.sub.2 and R.sub.3 are hydrogen atom and ##STR2## is a piperazinyl group is excluded; or a salt thereof; to an antimicrobial agent comprising the same as an effective component; and to an intermediate for producing same.
Abstract: Coffee products and other comestibles having an increased content of potassium are useful to enhance the gastric acid response of persons having abnormally low gastric acid secretion such as persons having gastric atrophy or atrophic gastritis. Preferred coffee beverages have an added potassium content of at least 1% by weight based on the dry weight of coffee solids in the beverage.
Abstract: A method for treating mammals suffering from rheumatoid arthritis and other tissue-destructive (chronic inflammatory or other) conditions associated with excess metalloproteinase activity comprising administering to the mammal an amount of a tetracycline that is effectively anti-metalloproteinase, but that is not effectively antimicrobial, and an amount of non-steroidal anti-inflammatory agent which, when combined with the effectively anti-metalloproteinase amount of tetracycline, results in a significant reduction of tissue destruction and/or bone loss.
Type:
Grant
Filed:
August 12, 1991
Date of Patent:
June 14, 1994
Assignee:
The Research Foundation of State University of New York
Inventors:
Lorne M. Golub, Nangavarum S. Ramamurthy, Thomas F. McNamara, Robert A. Greenwald
Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA receptor activation, e.g., a ganglioside such as GM.sub.1 or GT.sub.1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.
Type:
Grant
Filed:
April 6, 1993
Date of Patent:
June 14, 1994
Assignee:
Virginia Commonwealth University Medical College
Inventors:
David J. Mayer, Donald D. Price, Jianren Mao, John W. Lyle
Abstract: The invention relates to the use of substituted tetrahydrothiophenes, some of which are known, as medicaments, in particular as antimycotic agents, to new active substances and to processes for their preparation.
Type:
Grant
Filed:
October 8, 1992
Date of Patent:
June 14, 1994
Assignee:
Bayer Aktiengesellschaft
Inventors:
Joachim Mittendorf, Franz Kunisch, Manfred Plempel
Abstract: The invention concerns thiosulphinic acid derivatives, medicaments containing these compounds and their use in medicine. It has been found that thiosulphinic acid derivatives display outstanding inflammation-inhibiting properties. The compounds prove to be especially advantageous in the treatment of PAF-induced inflammatory processes of the bronchial area.
Abstract: The effective ingredient in the inventive inhibitive agent against activity of a .alpha.-amylase is tea, e.g., black tea, or a tea polyphenol as a constituent of tea including epigallocatechin gallate, epicatechin gallate, epigallocatechin, epicatechin, (+)catechin and the isomer thereof, free theaflavin, theaflavin monogallates A and B and theaflavin digallate.
Abstract: Reduction of urinary calcium excretion in humans or animals by the administration of GLA or DGLA as much or in salt or other pharmacologically acceptable form, optionally in association with EPA, DHA or other EFA in similar forms, is also useful in the treatment of nephrocalcinosis, renal stones and osteoporosis.
Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises substituted 1,2,4-triazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
Type:
Grant
Filed:
December 8, 1992
Date of Patent:
June 7, 1994
Assignees:
The Rockefeller University, Alteon Inc.
Inventors:
Peter C. Ulrich, Anthony Cerami, Dilip R. Wagle
Abstract: The oral absorption of antibiotics given of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of Laureth-12 together with a second component salts of capric acid and caprylic acids. The antibiotic containing two component enhancer system includes Miglyol-812 for optimum absorption.
Abstract: A biologically active preparation for human or veterinary use for the selective blockade of opioid binding sites of the brain responsible for respiratory depression containing in a biologically active quantity the codeinone derivative of general formula (I) or its saltR.sup.1 means amino--, hydroxyl--, --NH--phenyl or --NH--CO--NH.sub.2 groups,R.sup.2 means a hydrogen atom or a hydroxyl group.The invention also covers a process for selective blocking the opioid binding sites of the brain responsible for respiratory depression by administering to a patient in need of an analgetic a preparation containing a codeinone derivative of general formula (I) or its salt preferably three times per day in doses of 2,5-5 mg.
Type:
Grant
Filed:
October 2, 1992
Date of Patent:
May 31, 1994
Assignee:
Alkaloida Chemical Company Ltd.
Inventors:
Anna Borsodi, Zsuzsa Furst, Sandor Hosztafi, Schafferne E. Varga, BuzaBeata, Tamas Friedmann, Sandor Benyhe, Maria Szucs
Abstract: This invention relates to a method of lowering abnormally high serum cholesterol levels in the body without significantly reducing mevalonic metabolite synthesis and to novel pharmacological compositions containing as an active ingredient bisphosphonic acid and ester compounds containing a mono-, bi- or tricyclic ring linked with a bisphosphonate moiety through a basic amino alkylene group. This invention also provides novel bisphosphonate compounds and the processes for their preparation.
Type:
Grant
Filed:
May 1, 1992
Date of Patent:
May 31, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
John W. Ullrich, Raymond D. Youssefyeh, Daniel L. Cheney, Christopher J. Burns
Abstract: Methods for using substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzo[b] furanyl-, and benzo[b]thienylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes as agents for alleviating the symptoms of Parkinson's disease, dystonia, and other movement disorders are disclosed. Pharmaceutical compositions employing the compounds are also disclosed.
Type:
Grant
Filed:
September 8, 1992
Date of Patent:
May 31, 1994
Assignee:
Warner-Lambert Co.
Inventors:
Alexander McKnight, Geoffrey N. Wodruff
Abstract: Cholesterol lowering compounds and compositions are formed from the photochemical treatment of the Zaragozic Acids followed by esterification. These compounds and compositions are active squalene synthetase inhibitors useful in the treatment of hypercholesterolemia.
Type:
Grant
Filed:
November 24, 1992
Date of Patent:
May 31, 1994
Assignee:
Merck & Co., Inc.
Inventors:
John G. MacConnell, Byron H. Arison, George A. Doss, Richard L. Monaghan
Abstract: A method for the treatment of pertussis is disclosed which comprises administering a selective inhibitor of inducible nitric oxide synthase, preferably aminoguanidine, to a mammalian host susceptible to pertussis in a small but effective amount for inhibiting the toxic effects of TCT released by Bordetella pertussis.
Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
Abstract: Pharmaceutical compositions for the inhibition of bone resorption comprising a pharmaceutical carrier and a therapeutically effective amount of a benzopyran derivative represented by the general formula (I) ##STR1## wherein the broken-lined bond denotes an optional double bond, R.sub.1 denotes a hydrogen atom or a hydroxyl group, R.sub.2 denotes a cyano group, a phenylsulfonyl group or a halogen-substituted methoxyl group, and R.sub.3 denotes a group having the formula ##STR2## Since they inhibit bone resorption, they are useful for the treatment and prevention of diseases associated with bone metabolism.
Type:
Grant
Filed:
December 14, 1992
Date of Patent:
May 31, 1994
Assignee:
Hoechst Japan Limited
Inventors:
Mizuho Inazu, Ryoichi Satoh, Tsutomu Inoue, Hiroshi Kitagawa, Masakazu Katoh, Heinrich Englert, Denis Carniato, Hans-Jochen Lang
Abstract: Clear, stable, efficacious, aqueous microemulsions of a pyrethroid insecticide, optionally with another agriculturally active ingredient, are provided herein. The aqueous microemulsions are obtained by providing an inert matrix composition containing a defined mixture of nonionic surfactants, optionally including an anionic surfactant, mixing with a pyrethroid to form a microemulsion concentrate, and diluting with water. Preferably, the aqueous microemulsion includes an N-alkyl (C.sub.1 -C.sub.4) pyrrolidone therein as a cosolvent in the microemulsion system.