Abstract: The present invention is novel derivatives of pyrrolo[3,2-d]pyrimidines and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-cells in the presence of 2'-deoxyguanosine and, therefore, are for use in the treatment of autoimmune diseases, gout, psoriasis or rejection of transplantation.
Type:
Grant
Filed:
October 31, 1990
Date of Patent:
April 7, 1992
Assignee:
Warner-Lambert Company
Inventors:
Catherine R. Kostlan, Jagadish C. Sircar
Abstract: The present invention is novel derivatives of pyrrolo [3,2-d]pyrimidines and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-cells in the presence of 2'-deoxyguanosine and, therefore, are for use in the treatment of autoimmune diseases, gout, psoriasis or rejection of transplantation.
Type:
Grant
Filed:
October 31, 1990
Date of Patent:
March 31, 1992
Assignee:
Warner-Lambert Company
Inventors:
Catherine R. Kostlan, Jagadish C. Sircar
Abstract: Novel purine derivatives are described as agents for treating autoimmune diseases as well as a method of manufacture and pharmaceutical compositions as well as novel intermediates in the manufacture thereof.
Type:
Grant
Filed:
August 31, 1989
Date of Patent:
March 24, 1992
Assignee:
Warner-Lambert Company
Inventors:
Jagadish C. Sircar, Charles Schwender, Mark J. Suto
Abstract: The present invention is various 7-deazaguanines having activity as immunomodulators. Also included are pharmaceutical compositions and methods of use thereof.
Abstract: The novel 3,5-di-tertiary-butyl-4-hydroxyphenylthiazolyl, -oxazolyl, or -imidazolyl methanones and methanone oximes of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both.
Type:
Grant
Filed:
January 31, 1991
Date of Patent:
February 4, 1992
Assignee:
Warner-Lambert Company
Inventors:
Thomas Capiris, David T. Connor, Jagadish C. Sircar
Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migrains, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.
Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective ihibitors of cyclooxygenase and 5-lipoxygenase.
Type:
Grant
Filed:
October 16, 1990
Date of Patent:
December 24, 1991
Assignee:
Warner-Lambert Co.
Inventors:
Thomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
Abstract: The present invention is a novel process for preparing both known and novel nitroimidazoles having novel intermediates. The process advantageously reduces the number of process steps, provides increased yield with both greater safety and greater control of stereoisomerism in the products.
Abstract: The present invention is a stabilized enteric-coated pharmaceutical dosage form and processes for the preparation thereof. Dissolution stability after storage of the dosage form under high stress conditions is improved by an enteric-coated dosage form having an enteric coating wherein the coating is of the acrylic resin kind of from 14 mg/cm.sup.2 to 24 mg/cm.sup.2 or an enteric coating wherein the coating is of the acetate kind of from 14 mg/cm.sup.2 to 24 mg/cm.sup.2 and having a second coating of hydrophilic coating for example, hydroxypropyl cellulose, hydroxymethyl cellulose or hydroxypropylmethyl cellulose.
Type:
Grant
Filed:
July 14, 1989
Date of Patent:
November 26, 1991
Assignee:
Warner-Lambert Company
Inventors:
Mahdi B. Fawzi, Daniel A. Kubert, Kuchi S. Murthy
Abstract: The present invention is novel compounds which are 1,2,4-triazoles, derivatives of fenamates and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The nvention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like.
Type:
Grant
Filed:
April 3, 1990
Date of Patent:
November 19, 1991
Assignee:
Warner-Lambert Co.
Inventors:
Diane H. Boschelli, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar, Milton L. Hoefle
Abstract: The present invention is novel derivatives of pyrrolo[3,2-d]pyrimidines and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-cells in the presence of 2'-deoxyguanosine and, therefore, are for use in the treatment of autoimmune diseases, gout, psoriasis or rejection of transplantation.
Type:
Grant
Filed:
October 31, 1990
Date of Patent:
October 29, 1991
Assignee:
Warner-Lambert Company
Inventors:
Catherine R. Kostlan, Jagadish C. Sircar
Abstract: Preparation of 4-bromo-4'-demethylepipodophyllotoxin by reacting podophyllotoxin with hydrogen bromide at about -20.degree. C. New antitumor compounds of the formula: ##STR1## wherein R is A--(CH.sub.2).sub.n [A(CH.sub.2).sub.n ].sub.m (CHAH).sub.p --Q or ##STR2## each A, independently, is O, S, SO or SO.sub.2 ; n is an integer from 1 to 6, except when n and p, taken together, are zero, then n is 2 to 6; n is 0, 1, or 2; p is 0, 1, or 2; Q is H, alkyl from 1 to 6 carbon atoms which may be substituted with an NR.sub.1 R.sub.2 group wherein each R.sub.1 and R.sub.2, independently, is selected from the group of H, alkyl containing 1 to 6 carbon atoms which may be substituted with OH, alkanoyl containing 1 to 6 carbon atoms, or R.sub.1 and R.sub.2 are interconnected and together with the N to which they are connected form an N heterocyclic ring of 5 to 6 carbon atoms; R.sub.3 is hydrogen, and R.sub.
Abstract: Selected analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.
Abstract: Novel purine derivatives, particularly novel guanines and hypoxanthines, are described as agents for treating autoimmune diseases. Also novel methods of manufacture for the derivatives, pharmaceutical compositions thereof, and methods of use therefor are the invention.
Abstract: The present invention is novel 2-oxazolidinone analogs of nitroimidazoles; novel pharmaceutical compositions of selected analogs thereof and methods of use for the compositions as radiosensitizing or chemosensitizing agents in the treatment of hypoxic tumor cells.
Abstract: The present invention is novel aziridino derivatives of nitroimidazoles and pharmaceutical compositions of selected derivatives useful as radiosensitizing or chemosensitizing agents in the treatment of hypoxic tumor cells. Also, the present invention is a novel process for preparing both known and novel aziridino derivatives of nitroimidazoles having novel intermediates.
Abstract: The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
Type:
Grant
Filed:
April 11, 1990
Date of Patent:
May 21, 1991
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, Catherine R. Kostlan
Abstract: The present invention is various 7-deazaguanines having activity as immunomodulators. Also included are pharmaceutical compositions and methods of use thereof.
Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
Abstract: A method for treating bacterial or protozoal humans and animals by administering a 6-aryl pyrimidine compound or a salt thereof in association with a pharmaceutical carrier.