Abstract: This invention relates to a suppository applicator adapted for administering medicament in a suppository form to a body cavity. More particularly, it relates to a one-piece injection molded article having a main body portion and a flexible chamber whereby the flexible chamber is inverted in use to expel the medicament from the applicator into a body cavity.
Abstract: Novel 2,2,4-trialkyl-1,2-dihydroquinazoline-3-oxides and their synthesis are described. These compounds possess cardiotonic activity, and are useful for the treatment of heart failure.
Type:
Grant
Filed:
November 6, 1991
Date of Patent:
July 5, 1994
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Donald W. Combs, Robert Falotico, Victor Bandurco
Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
Abstract: This invention relates to aminoethylthiophene derivatives and more particularly 2- and 3-aminoethylthiophene derivatives which are useful as antiarrhythmic agents, their methods of use as antiarrhythmic agents, and novel intermediate compounds useful for preparation of the aminoethylthiophene derivatives of the invention.
Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.
Type:
Grant
Filed:
July 18, 1991
Date of Patent:
April 5, 1994
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Charles Schwender, Keith Demarest, David Wustrow
Abstract: 1,5-Diphenyl-3-pyrazolylalkyl-N-hydroxydithiocarbamates of the general formula: ##STR1## are disclosed to have anti-inflammatory activity in mammals.
Abstract: This invention relates to thieno tetrahydropyridine and isoquinoline derivative compounds which are useful as antiarrhythmic agents, pharmaceutical compositions comprising such compounds, novel intermediates for their preparation and their methods of use. More particularly these thieno tetrahydropyridine and isoquinoline derivative compounds have been demonstrated to increase the effective refractory period (ERP) of isolated perfused cardiac tissue in vitro.
Abstract: A latex film product such as a prophylactic condom, a surgical glove, a medical examination glove, and the like, having improved chemical resistance, such product comprising a shaped film consisting essentially of a cured mixture of (a) a copolymer of acrylonitrile and butadiene or isoprene, and (b) a high styrene content styrene-butadiene copolymer.
Type:
Grant
Filed:
July 26, 1991
Date of Patent:
February 8, 1994
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Robert G. Miller, Oskar Tankovitz, Duncan A. Mackillop
Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
Type:
Grant
Filed:
December 21, 1990
Date of Patent:
February 8, 1994
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
Abstract: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.
Abstract: Biphenylyl tetrazoles for treating hypertension in mammals of the formula: ##STR1## where X is CH.sub.2, O, S, N--R.sup.4, NH, NCHO, NCOCH.sub.3 or NCO.sub.2 R.sup.4 ;R.sup.1 and R.sup.2 are the same or different and are C.sub.1-6 alkyl; andR.sup.4 is C.sub.1-6 alkyl;including methods and intermediates for the production of the same.
Abstract: A process for producing a compound of formula I: ##STR1## comprising reacting 5-(2-fluorophenyl)-1H-tetrazole with a Grignard reagent to produce the desired product is disclosed. Novel compounds produced by this process for use as intermediates in making certain angiotension II antagonists are also disclosed.
Abstract: Novel 6-substituted purinyl piperazine derivatives are described. The novel derivatives are useful as cardiotonic agents and antiarrhythmic agents.
Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
Abstract: This invention relates to novel N-biphenylyl lactam compounds having a substituted methylidene or methyl moiety adjacent to the lactam nitrogen, and pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.
Abstract: N-1 and C-5 heterocyclic pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.
Abstract: This invention relates to novel bis-biphenyl substituted 3-mercapto-1,2,4-tetrazoles and to pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infection or diabetic nephropathy.The invention also relates to pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.
Type:
Grant
Filed:
January 30, 1992
Date of Patent:
August 31, 1993
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Victor T. Bandurco, William V. Murray, Michael P. Wachter, Charles F. Schwender
Abstract: The invention relates to a process for the synthesis of compounds of the formula I ##STR1## wherein R.sub.1 -R.sub.5 are as defined herein. The process is a multistep process which comprises acylating a 2-benzoxazolinone with an alkanoic anhydride to form an acylated carbamate, hydrolyzing the carbamate, reacting the resultant aminophenol with haloalkanoyl halide to form a substituted benzoxazine, reacting the benzoxazine with an aldehyde, alkylating the resultant aminomethyl compound with an alkylating agent to form a quaternary ammonium salt, reacting the salt with an alkali metal cyanide to form a nitrile, hydrolyzing the nitrile and reacting the resultant carboxylic acid with hydrazine.The compounds are useful as cardiotonic and vasodilating agents and as inhibitors of phosphodiesterase fraction III and platelet aggregation. In addition, the compounds are active as smooth muscle relaxants and bronchodilators.