Abstract: This invention relates to novel tricyclic pteridinones, their aza analogs and their pharmaceutically acceptable salts. Further encompassed by the invention is a novel process for the production of the tricyclic pteridinones and their aza analogs. The compounds of the invention exhibit cardiovascular properties, particularly mixed vasodilation and selective venous and arterial dilation. Pharmaceutical compositions are proposed for the compounds.
Abstract: A topical bioadhesive ointment composition comprising an aqueous mineral oil emulsion which is readily spread able and film-forming, and, upon application to moist skin or a mucosal surface, forms a stable, coherent layer thereon which resists removal therefrom by water or a body fluid associated with the mucosal surface to which the ointment composition is applied is disclosed. Also disclosed are pharmaceutical compositions containing the ointment compositions and a pharmaceutically active agent, e.g. , TGF.alpha.; and methods of using and methods of preparing the compositions.
Type:
Grant
Filed:
June 3, 1994
Date of Patent:
November 26, 1996
Assignee:
Berlex Laboratories Inc.
Inventors:
Thabiso M'Timkulu, Ze'ev Shaked, Richard Hsu
Abstract: This invention relates to novel potassium channel activators and their acid addition salts. The compounds of the invention as potassium channel activators/openers have therapeutic value in a number of physiological areas such as hypertension, cardiac ischemia, cerebral ischemia, broncho constriction and neurodegenerative diseases. Pharmaceutical compositions are proposed for the compounds which are of the following formulae: ##STR1## wherein: R is H or OH;- - - the dotted line at position 3,4 represents the presence or absence of a double bond. ##STR2## the pharmaceutically acceptable acid addition salts thereof, with the provisos that:a) R is H when 3,4 is a double bond; andb) R is OH when 3,4 is a single bond.
Abstract: A medicinal composition comprising an Epidermal Growth Factor-like protein derived from yeast, and a carrier which is pharmaceutically acceptable and suitable for the type of administration and treatment for which the composition is to be used. The yeast-derived protein Has a molecular weight of about 4770 daltons and a murine Epidermal Growth Factor (mEGF) activity equivalent to at least 100 nanograms of mEGF by Elisa Assay Titration. The medicinal composition may be applied topically for purposes such as the treatment of external body wounds, or in ophthalmic surgery such as in cataract or corneal surgery, by incorporating a carrier therein which is pharmaceutically acceptable for the particular topical use. The composition may be administered orally for treatment of such ailments as peptic ulcers by incorporating therein a carrier which is pharmaceutically acceptable for oral administration in oral dosage form.
Abstract: This invention relates to novel 5-pyrimidineamine derivatives. The compounds of the invention exhibit cardiovascular properties, particularly mixed vasodilative, selective venous and arterial dilation. Pharmaceutical compositions are proposed for the compounds.
Abstract: This invention relates to novel 2-substituted-1(4)-aryl piperazines and to a process for their preparation. The compounds of this invention have been found to have cardiovascular, primarily antiarrhythmic effects.
Abstract: A water-soluble yeast protein of about molecular weight 4770 daltons is isolated having murine Epidermal Growth Factor (mEFG) activity per milligram at least equivalent to 1000 nanograms of mEGF by Elisa Assay Titration. The protein is naturally present in yeast and is free of water-insoluble yeast components. The proten is insoluble in trichloroacetic acid, chloroform, absolute methanol, 95% ethanol, acetone, hexanes, petroleum ether, and 50% methanol--25% ether. The protein is soluble in acidic solutions containing 50% methanol, ethanol or acetone. The protein stimulates the growth and respiration of A431 cells in a culture without serum supplements.
Abstract: Novel imidazolybenzoyl substituted heterocycles and their use as cardiovascular agents most especially as Class III antiarrhythmic agents is described. Pharmaceutical formulations containing such compounds are also discussed.
Type:
Grant
Filed:
June 20, 1990
Date of Patent:
February 23, 1993
Assignee:
Schering AG
Inventors:
Yuo-Ling Chou, Paul W. Erhardt, Alfred A. Hagedorn, III, John W. Lampe, Lumma, Jr., William C., Thomas K. Morgan, Jay R. Wiggins
Abstract: This invention relates to novel substituted imidazo-[1,5-a]pyridines, most especially novel 8-phenylimidazo-[1,5-a]pyridines. It also relates to novel intermediates and to a novel process for the preparation of certain of these compounds. The compounds of the invention have been found to have significant cardiotonic, antiarrhythmic, hypotensive, CNS stimulant, and other pharmacological effects.
Abstract: This invention relates to novel substituted imidazo[1,5-a]pyridines, most especially novel 8-phenylimidazo[1,5-a]pyridines. It also relates to novel intermediates and to a novel process for the preparation of certain of these compounds. The compounds of the invention have been found to have significant cardiotonic, antiarrhythmic, hypotensive, CNS stimulant, and other pharmacological effects.
Abstract: This invention relates to novel imidazoquinoxalinones and their aza analogs and to a process for their preparation. The compounds of this invention have been found to have inodilatory, vasodilatory, venodilatory and other pharmacologic effects.
Abstract: This invention relates to novel imidazoquinoxalinones and their aza analogs and to a process for their preparation. The compounds of this invention have been found to have inodilatory, vasodilatory, venodilatory and other pharmacologic effects.
Abstract: This invention relates to novel 2-substituted-1(4)-aryl piperazines and to a process for their preparation. The compounds of this invention have been found to have cardiovascular, primarily antiarrhythmic effects and are of the following general formula I ##STR1## wherein R is hydrogen, lower alkyl or benzyl; and R.sub.1 and R.sub.2 are the same or independently hydrogen, lower alkyl, lower alkoxy or halogen;Z is ##STR2## --NR.sub.3 --CH.sub.2 --, --OCH.sub.2 --, --NR.sub.3 --, --O-- or --NR.sub.3 SO.sub.2 -- andQ is (C.sub.1 -C.sub.4) alkyl--SO.sub.2 --NR.sub.4 -- or ##STR3## R.sub.3 is hydrogen, lower alkyl, allyl or loweralkoxyloweralkyl; and included in the descriptors of the compounds of Formula I is the proviso that when R.sub.4 is methyl then ##STR4## must be in the 2 position of Formula I.
Type:
Grant
Filed:
September 15, 1989
Date of Patent:
September 24, 1991
Assignee:
Schering AG
Inventors:
William C. Lumma, Jr., Thomas K. Morgan, Jr., Gary B. Phillips
Abstract: Novel derivatized alkanolamines of the following structural formula ##STR1## are described as useful cardiovascular agents. Most especially described is their usefulness as cardiovascular agents exhibiting an antiarrhythmic effect. Said antiarrhythmic effect is of a combination Class II/Class III variety. Pharmaceutical formulations containing such compounds are also described.
Type:
Grant
Filed:
July 13, 1988
Date of Patent:
September 24, 1991
Assignee:
Schering AG
Inventors:
Randall E. Lis, William C. Lumma, Jr., Thomas K. Morgan, Jr., Klaus Nickisch, Ronald A. Wohl
Abstract: This invention relates to novel substituted imidazo-[1,5-a]pyridines, most especially novel 8-phenylimidazo-[1,5-a]pyridines. It also relates to novel intermediates and to a novel process for the preparation of certain of these compounds. The compounds of the invention have been found to have significant cardiotonic, antiarrhythmic, hypotensive, CNS stimulant, and other pharmacological effects.
Abstract: This invention relates to novel 3,4,5,6-tetrahydro-2H-1,7,4-benzodioxazonines and their pharmaceutically acceptable salts. The compounds of the invention are cardiovascular agents and especially Class III antiarrhythmic agents.
Type:
Grant
Filed:
September 15, 1989
Date of Patent:
October 30, 1990
Assignee:
Berlex Laboratories, Inc.
Inventors:
William C. Lumma, Jr., Gary B. Phillips
Abstract: This invention relates to novel pyrrolo[1,2-c]imidazolones and their pharmaceutically acceptable salts. The compounds of the invention are PDE inhibitors with primarily cardiovascular effects especially cardiotonic effects.
Abstract: N-(aminoalkyl)-substituted(N or C alkyl)-aryl-4-(methylsylfonylamino)benzamides of the formula ##STR1## wherein R is C.sub.1 -C.sub.4 straight chain alkyl, one of R.sub.1, R.sub.2 and R.sub.3 is a phenyl or naphthyl group and the others are hydrogen, --NR.sub.4 R.sub.5 is a secondary or teritary amino group, X and X.sub.1 are hydrogen or alkyl and n is 0 or 1, are useful as antiarrhythmic agents in the treatment of cardiac arrhythmias especially as combination Class I/Class III agents.
Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.
Type:
Grant
Filed:
March 8, 1988
Date of Patent:
March 6, 1990
Assignee:
Schering A.G.
Inventors:
Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
Abstract: This invention relates to a process for the preparation of substituted sulfonamidobenzamides which compounds are known antiarrhythmic agents and to the novel N-acylaziridine employed therein.