Abstract: Experiments have been performed which test the stability of thymoxamine in aqueous solution at room temperature and above. It was determined that dimethyl-beta-cyclodextrin slows the hydrolysis degradation of thymoxamine while other beta-cyclodextrin analogs either accelerate the hydrolysis degradation or have no effect on the rate of hydrolysis degradation. Cytological experiments have been performed which show that chemical formulations containing thymoxamine and up to 5% by weight dimethyl-beta-cyclodextrin have the same toxicity as chemical formulations with thymoxamine alone.
Abstract: The invention relates to novel compounds, 2,9-dihydro(6 or 7)-3-oxo-2,3,4,5-tetrahydropyridazinyl)pyrazolo[4,3-b]benzoxazines. The claimed compounds are inhibitors of phosphodiesterase fraction III and have potent positive inotropic activity. These compounds are useful as cardiotonics or platelet aggregation inhibitors.This invention also pertains to compositions comprising an effective amount of the compounds, to methods for preparing the claimed compounds and to methods for treating a mammal with the compounds.
Abstract: The synthesis of novel ethanesulfonamide compounds is described. The novel ethanesulfonamide compounds have antisecretory activity and are used in the treatment of peptic ulcer disease. The intermediates used to prepare the ethanesulfonamides are useful in the treatment of osteoporosis and other bone wasting diseases.
Abstract: Novel substituted imidazole and pyridine derivatives and their synthesis are disclosed. The derivatives inhibit the enzyme, H.sup.+ /K.sup.+ ATPase, and are therefore useful for the treatment of gastrointestinal diseases.
Type:
Grant
Filed:
March 26, 1990
Date of Patent:
April 21, 1992
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Zoltan G. Hajos, Jeffery B. Press, Jerry R. Roberts
Abstract: The synthesis of benzoxazinyl- and benzothiazinylpyridazinone compounds is described. The novel compounds are cardiotonic agents and inhibitors of phosphodiesterase. In addition, the compounds are useful as smooth muscle relaxants and bronchodilators.
Abstract: The present invention relates to substituted hydroxyureas. These compounds inhibit the enzyme 5-lipoxygenase. In addition, certain of the compounds also inhibit the enzyme-cyclooxygenase. The compounds are useful for treating asthma, allergies, arthritis, posoriasis, ischemia, dermatitis, inflammation and/or broncho-constriction and/or inflammatory diseases of the eye.
Abstract: Natural rubber latex compounds are modified by the addition of a high styrene content styrene-butadiene copolymer. The films prepared from these modified NR latex compositions exhibit improved tear strength and a good balance of other properties.
Type:
Grant
Filed:
July 25, 1990
Date of Patent:
August 13, 1991
Assignee:
Ortho Pharmaceutical Ltd.
Inventors:
Robert G. Miller, Duncan A. MacKillop, Oskar T. Tankovitz
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:
November 5, 1990
Date of Patent:
July 9, 1991
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
Abstract: Novel 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides and their synthesis are described. These novel compounds are cardiotonic agents and bronchodilating agents, and as such are useful for the treatment of heart failure and asthma.
Type:
Grant
Filed:
August 8, 1990
Date of Patent:
July 9, 1991
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Donald W. Combs, Robert Falotico, David M. Ritchie
Abstract: 6-Substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.
Type:
Grant
Filed:
April 14, 1989
Date of Patent:
June 4, 1991
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Zoltan G. Hajos, Ramesh M. Kanojia, Jeffery B. Press
Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for reversing the effects of glucocorticoid-induced skin atrophy.
Type:
Grant
Filed:
August 31, 1989
Date of Patent:
May 28, 1991
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Albert M. Kligman, James A. Mezick, Robert J. Capetola
Abstract: Lowering of intraocular pressure, e.g. in the treatment of glaucoma is carried out by administering a phosphodiesterase inhibitor to a patient. Particular ophthalmic pharmaceutical compositions are disclosed for topical application to the eye.
Abstract: 4-Substituted pyrazolo[3,4-d]pyrimidine derivatives and a method of synthesis for the derivatives are described. The 4-substituted pyrazolopyrimidine derivatives are useful as cardiotonic agents and antiarrhythmic agents.
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:
September 23, 1988
Date of Patent:
February 12, 1991
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
Abstract: Lowering of intraocular pressure, e.g. in the treatment of glaucoma is carried out by administering a phosphodiesterase inhibitor to a patient. Particular ophthalmic pharmaceutical compositions are disclosed for topical application to the eye.
Abstract: Novel 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides and their synthesis are described. These novel compounds are cardiotonic agents and bronchodilating agents, and as such are useful for the treatment of heart failure and asthma.
Type:
Grant
Filed:
February 14, 1990
Date of Patent:
October 16, 1990
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Donald W. Combs, Robert Falotico, David M. Ritchie
Abstract: The synthesis of ring-fused thienopyrimidinedione derivatives is described. The novel ring-fused thienopyrimidinedione derivatives are generally vasodilating agents and antihypertensive agents and as such are useful as cardiovascular agents.