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: This invention relates to novel (Z,Z), (Z,E) and (E,Z) olefin isomers of substituted benzylidene cycloketones and their pharmaceutically acceptable salts. The compounds of the invention are potent factor Xa inhibitors thereby acting as anticoagulants useful in a number of thrombotic disease states. Pharmaceutical compositions are proposed for the compounds.
Type:
Grant
Filed:
July 5, 1994
Date of Patent:
May 27, 1997
Assignee:
Berlex Laboratories, Inc.
Inventors:
Jerry L. Dallas, William J. Guilford, Sunil K. Koovakkat, Michael M. Morrissey, Kenneth J. Shaw
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: This invention relates to derivatives of polyanhydroaspartic acid which are non-systemic water soluble polymers and which are intended to be lipid lowering agents. The pharmaceutical compositions/formulations incorporating these compounds are also discussed.
Abstract: Novel and known compounds are described which inhibit endothelin converting enzyme (ECE), thereby preventing the conversion of Big Endothelin (BET) to Endothelin (ET). Pharmaceutical usefulness and preparations are described.
Type:
Grant
Filed:
December 5, 1991
Date of Patent:
April 2, 1996
Assignee:
Berlex Laboratories, Inc.
Inventors:
Ron H. Bihovsky, Paul W. Erhardt, John W. Lampe, Raju Mohan, Kenneth J. Shaw
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: 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: An arrangement for retaining blister pack tablets comprises a container with at least a front cover and a rear cover with a blister pack sandwiched therebetween and visible through a window in the front cover. The blister pack includes indicia thereon indicating the order in which the tablets should be taken and the container includes a pointer identifying the first tablet in the array of tablets to be consumed. Preferably, the container includes a daily calendar in the form of a loop or cylinder which is moveable with respect to the container so that a desired starting day can be selected by the user or prescriber. Preferably, the loop or cylinder is lockable in its selected position. In accordance with two embodiments of the invention, front and rear lids are pivoted to the front and rear covers, respectively, to conceal the blister pack until it is necessary to take a tablet.
Abstract: A circular tissue recording chamber has a cavity therein for retaining tissue or cell samples immersed in a liquid bath. The temperature of the bath is maintained at a selected level by a transparent heater positioned beneath the bath, wherein the heater is comprised of a grid of fine wires supported on a transparent mylar substrate. Liquid is introduced into the bath through a serpentine passageway also in proximity with the heater, whereby the temperature of the liquid is raised to that of the bath as it traverses the passageway. The recording chamber has a thickness of approximately 1 cm so as to be readily usable with a high magnification microscope.
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: 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.