Abstract: An apparatus comprised of a canister having a valved opening thereon and containing, under pressure, heparin and a low boiling point propellant is disclosed. The valved opening can be activated to release a metered dose of aerosolized heparin to a patient or preferably to an inhalation device which improves efficiency with respect to the amount of heparin reaching the lungs of the patient.
Abstract: The invention relates to a controlled release dosage form comprising three actives: acetaminophen, pseudoephedrine sulfate and dexbrompheniramine maleate.
Abstract: There is disclosed a multistep process for producing (-)-5-[(R)-1-hydroxy-2-((R)-1-methyl-3-phenyl-propyl)aminoethyl]salicylami de in high yields which does not require chromatography.The process is stereoselective for the desired products starting with the reaction of D-(+)-alpha-methylbenzylamine with benzylacetone followed by reduction of the resulting Schiff's base to form an amine as an R,R: R,S diastereomeric mixture, resolution of the mixture to obtain the R,R stereoisomer as a salt, conversion to a free base, reaction of the R,R free base with an O-protected alpha-bromo-3-carbamoyl-acetophenone to produce the corresponding R,R-ketobenzamide, reduction to produce a mixture of S,R,R;R,R,R hydroxybenzamide, removal of the protecting groups, resolution of the deprotected product and then conversion to the free R,R-amine.
Type:
Grant
Filed:
April 26, 1982
Date of Patent:
April 14, 1987
Assignee:
Schering Corporation
Inventors:
Elijah J. Gold, Esther Babad, Lydia Peer, Wei K. Chang
Abstract: A means of aiding in the prevention of Sudden Infant Death Syndrome (SIDS) is disclosed. The means comprises administering a pharmaceutically effective amount of the drug 6-methylene-6-desoxy-N-cylopryplymethyl-14-hydroxydihydronormorphone to an infant determined to be susceptible to SIDS. The drug is preferably administered bi-daily via the GI tract. The drug attaches to the nerve receptor sites responsible for the actuation of respiration thus blocking the attachment of endogenous endorphins which, if present in high levels, prevents such actuation resulting in apnea and SIDS. A suppository containing the drug for use in carrying out the method is also disclosed.
Abstract: Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
Type:
Grant
Filed:
November 12, 1985
Date of Patent:
October 7, 1986
Assignee:
Schering Corporation
Inventors:
Bernard R. Neustadt, David R. Andrews, Paul E. McNamara, Robert W. Watkins
Abstract: This invention relates to 2-(N-heterocycloaliphaticthio)penems wherein the nitrogen of the heterocyclic ring is connected to the alkyl group, and to their use as antibacterial agents.
Type:
Grant
Filed:
March 25, 1983
Date of Patent:
September 30, 1986
Assignee:
Schering Corporation
Inventors:
Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
Abstract: The invention relates to a controlled release dosage form comprising three actives: acetaminophen, psueudoephedrine sulfate and dexbrompheniramine maleate.
Abstract: Substituted 1,8-naphthyridinones are anti-allergic, anti-inflammatory and cytoprotective agents. Methods for their preparation and use are disclosed.
Abstract: Novel compounds with angiotensin-converting enzyme inhibitory activity are disclosed. Such compounds are useful in the treatment of cardiovascular disorders, especially hypertension and congestive heart failure, and are useful in the treatment of glaucoma.
Type:
Grant
Filed:
July 30, 1984
Date of Patent:
May 6, 1986
Assignee:
Schering Corporation
Inventors:
Elijah H. Gold, Bernard R. Neustadt, Elizabeth M. Smith
Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.
Type:
Grant
Filed:
September 17, 1984
Date of Patent:
April 22, 1986
Assignee:
Schering Corporation
Inventors:
Ronald J. Doll, Bernard R. Neustadt, Elizabeth M. Smith, Charles V. Magatti, Elijah H. Gold
Abstract: Improved processes for the production of 6-hydroxyethyl-2-substituted thio penem-3-carboxylates which eliminate the step of using a silver reagent are disclosed.
Type:
Grant
Filed:
November 7, 1983
Date of Patent:
April 22, 1986
Assignee:
Schering Corporation
Inventors:
Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
Abstract: There are disclosed benzothiadiazinyl and quinazolinyl substituted carboxylalkyl dipeptides, wherein the benzothiodiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group. Compounds of this invention are useful as antihypertensive agents, in the treatment of congestive heart failure and in the treatment of glaucoma. In addition, compounds of this invention have diuretic activity.
Type:
Grant
Filed:
November 25, 1983
Date of Patent:
December 17, 1985
Assignee:
Schering Corporation
Inventors:
Bernard R. Neustadt, David R. Andrews, Paul E. McNamara
Abstract: Antihypertensive compounds with angiotensin-converting enzyme inhibitory activity and diuretic activity are disclosed. Such compounds are useful in the treatment of cardiovascular disorders, especially hypertension and congestive heart failure, and are useful in the treatment of glaucoma.
Abstract: There is disclosed a high yielding process for cleaving penicillinates with acyl or aroyl nitrates to produce acyloxy or aroyloxy azetidinones which are intermediates in the multistep process for producing penems from penicillinates.
Abstract: Disclosed are 6-(1'-hydroxyethyl)-2-[(R)-amino acid alkyl]penem-3-carboxylic acids and salts thereof having an absolute stereochemisty of 5R,6S,8R. The compounds are useful and potent antibacterial agents and can be formulated into a variety of forms suitable for oral, parenteral or topical use.
Abstract: Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite.Also described are novel penems useful as antibacterials which are prepared by the described process.