Abstract: The present invention is novel 9-substituted-8-hydroxy or -8-halo-9 deazaguanines 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.
Abstract: The novel 3,5-di-tertiary-butyl 4-hydroxyphenylimidazolyl methanones and methanone oximes of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both.
Type:
Grant
Filed:
October 17, 1991
Date of Patent:
August 10, 1993
Assignee:
Warner-Lambert Company
Inventors:
Thomas Capiris, David T. Connor, Jagadish C. Sircar
Abstract: The novel 3,5-di-tertiary-butyl-4-hydroxyphenyloxazolyl methanones and methanone oximes of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both.
Type:
Grant
Filed:
October 17, 1991
Date of Patent:
August 10, 1993
Assignee:
Warner-Lambert Company
Inventors:
Thomas Capiris, David T. Connor, Jagadish C. Sircar
Abstract: The present invention is a method of use for the prevention or reduction of the effects of stroke in a subject susceptible to or at risk of stroke with ketamine. The method also includes combination of ketamine and a benzodiazepine in the use.
Abstract: 7-Substituted quinolones and naphthyridones are described as antibacterial agents as well as a process for their manufacture, compositions therefor, wherein the 7-substituent is a pyrrolidine ring substituted at the 3-position by a substituted aromatic hydrocarbon or a heteroaromatic group.
Abstract: The present invention is novel compounds, which are derivatives of 4'-hydroxyphenylacetic acid having antiinflammatory activity for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, and having analgesic activity. Particularly, the analgesia may be useful for the treatment of dental pain and headache, especially vascular headache, such as migraine, cluster and mixed vascular syndromes, as well as nonvascular tension headache.
Abstract: The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are described as having 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. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
Type:
Grant
Filed:
November 16, 1992
Date of Patent:
June 15, 1993
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, David T. Connor, Catherine R. Kostlan
Abstract: The present invention is for EGF receptor truncates which retain the activity of ligand binding for the EGF receptor. The specific truncates include LD.sub.1 D.sub.2 D.sub.3.Apa L encompassing amino acids Met.sub.-24 to Val.sub.505 of the EGF receptor; for LD.sub.2 D.sub.3 D.sub.4 which melds the EGF receptor leader peptide (amino acids Met.sub.-24 to Ala.sub.-1), 9 amino acids of the mature amino terminus of the receptor (Leu.sub.1 to Gly.sub.9) and receptor sequences Ser.sub.150 to Gly.sub.625 ; for LD.sub.3 D.sub.4 which is the leader peptide (Met.sub.-24 to Ala.sub.-1), Leu.sub.1 to Gln.sub.8 of the mature amino terminus and the receptor sequence Asp.sub.297 to Gly.sub.625.
Abstract: Novel 5, 6, or 7 membered oxaza heterocycles substituted at the 4-carbon by a 5-hydroxypyrimidinylmethylene group inhibitors of 5-lipoxygenase and/or cyclooxygenase and are thus useful in treating inflammatory diseases are described as well as pharmaceutical compositions, methods of manufacture of the compounds, and compositions and methods of treating the noted diseases.
Type:
Grant
Filed:
June 1, 1992
Date of Patent:
June 1, 1993
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Catherine R. Kostlan, Gary P. Shrum, Paul C. Unangst
Abstract: The present invention provides pharmaceutically useful compounds which are aminosulfonyl urea compounds which are ACAT inhibitors rendering them useful in controlling blood cholesterol levels, pharmaceutical compositions and methods of using the ACAT inhibitors and closely related compounds which are also aminosulfonyl urea compounds.
Abstract: The present invention is a novel compound which is a thiadiazole or oxadiazole analog of a fenamic acid having a substituted hydroxamate side chain and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use thereof. The invention compounds are now found to have activity as inhibitors of one or both of cyclooxygenase and 5-lipoxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like. Thus, the present invention is also a pharmaceutical composition or method of use thereof.
Type:
Grant
Filed:
December 17, 1991
Date of Patent:
May 18, 1993
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, David T. Connor, Catherine R. Kostlan
Abstract: Heterocyclic methyl derivatives of biphenyl oxadiazoles and thiadiazoles are described, as well as methods for the preparation of said derivatives and pharmaceutical compositions of the same, which are useful as antagonists of the angiotensin II enzyme and thus useful in treating hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.
Abstract: The present invention is for selected novel compounds, as well as, pharmaceutical compositions and methods of use for known and the selected novel compounds both of the formula ##STR1## having activity useful for treating allergies and inflammation.
Type:
Grant
Filed:
May 13, 1991
Date of Patent:
May 4, 1993
Assignee:
Warner-Lambert Company
Inventors:
Wiaczeslaw A. Cetenko, David T. Connor, Roderick J. Sorenson, Paul C. Unangst, Stephen S. Stabler
Abstract: The present invention is 3,5-substituted, isoxazoles, pyrazoles, isothiazoles, and analogs thereof having 5-lipoxygenase or cyclooxygenase inhibiting activity or as a sunscreen.
Type:
Grant
Filed:
August 16, 1989
Date of Patent:
May 4, 1993
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, Donald E. Nies
Abstract: 3-Alkyloxy-, aryloxy-, or arylalkyloxy-benzo[b]thiophene-2-carboxamides are described as agents which block leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these compounds are novel and methods of preparation are also described.
Type:
Grant
Filed:
February 24, 1992
Date of Patent:
May 4, 1993
Assignee:
Warner-Lambert Company
Inventors:
Diane H. Boschelli, David T. Connor, Clifford D. Wright
Abstract: Continuous administration of compositions containing a fixed quantity of synthetic estrogen in combination with a synthetic progestogenic agent are useful to relieve menopausal symptoms, to prevent osteoporosis and for other hormone-replacement treatments. Also described is an improved manufacturing process for such compositions especially for low tablet dosage forms.
Type:
Grant
Filed:
October 22, 1991
Date of Patent:
May 4, 1993
Assignee:
Warner-Lambert Company
Inventors:
Roger M. Boissonneault, Henry A. Miller, Jr.
Abstract: Novel compounds of the formula ##STR1## wherein R is hydrogen, a straight or branched alkyl group having from 1 to 8 carbon atoms or benzyl; wherein each of R.sub.1 and R.sub.2 is hydrogen, an aralkyl group, a straight or branched hydrocarbon group having from 1 to 20 carbon atoms and may be saturated or unsaturated, an alkyl group of from 1 to 6 carbon atoms wherein the terminal carbon is substituted, the group --(CH.sub.2).sub.p)--Q wherein p is zero to three and Q is a 5- or 6-membered monocyclic or fused bicyclic heterocycle, phenyl or NR.sub.1 R.sub.2 taken together form a monocyclic heterocyclic ring, and R.sub.3 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, --(CH.sub.2).sub.p --Q wherein p and Q are as defined above, an aralkyl group or a straight or branched hydrocarbon group having from 1 to 20 carbon atoms and being straight or branched.
Abstract: The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are described as having 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. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
Type:
Grant
Filed:
February 24, 1992
Date of Patent:
March 23, 1993
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, David T. Connor, Catherine R. Kostlan
Abstract: A method of treatment of central nervous system disorders with compounds having the formula ##STR1## and isomers thereof wherein R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 and as defined in the specification; as well as pharmaceutical compositions thereof.
Abstract: The compounds of the present invention have the formula ##STR1## wherein each of X and Y is oxygen or sulfur, R is hydrogen or lower alkyl, and each of R.sub.1 and R.sub.2 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, aralkyl, a hydrocarbon chain, a hetero group, or a heteroalkyl group, and the compounds are useful in treating atherosclerosis.
Type:
Grant
Filed:
April 9, 1991
Date of Patent:
February 23, 1993
Assignee:
Warner-Lambert Company
Inventors:
Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic