Abstract: Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
Type:
Grant
Filed:
May 19, 1995
Date of Patent:
May 27, 1997
Assignee:
Warner-Lambert Company
Inventors:
John M. Domagala, John S. Kiely, Mel C. Schroeder
Abstract: 6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
Type:
Grant
Filed:
May 3, 1995
Date of Patent:
April 15, 1997
Assignee:
Warner-Lambert Company
Inventors:
Clifton J. Blankley, Diane H. Boschelli, Annette M. Doherty, James M. Hamby, Sylvester Klutchko, Robert L. Panek
Abstract: Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
April 15, 1997
Assignee:
Warner-Lambert Company
Inventors:
Gary L. Bolton, John M. Domagala, Edward F. Elslager, Rocco D. Gogliotti, Terri S. Purchase, Joseph P. Sanchez, Bharat K. Trivedi
Abstract: Benzothiophene, benzofuran and indolethiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.
Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.
Abstract: Novel inhibitors of protein farnesyltransferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer and restenosis.
Type:
Grant
Filed:
June 30, 1994
Date of Patent:
November 5, 1996
Assignee:
Warner-Lambert Company
Inventors:
Gary L. Bolton, John C. Hodges, Michael W. Wilson
Abstract: Prostate cancer is treated with 5-[(2-aminoethyl)amino]-2-[2-(diethylamino)ethyl]-2H-[1]benzothiopyrano-[4 ,3,2-cd]indazol-8-ol or a pharmaceutically acceptable salt thereof.
Abstract: Benzothiophene, benzofuran and indolethiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases; these compounds also inhibit the activation of human immunodeficiency virus (HIV).
Type:
Grant
Filed:
May 19, 1995
Date of Patent:
October 15, 1996
Assignee:
Warner-Lambert Company
Inventors:
Diane H. Boschelli, David T. Connor, James B. Kramer, Paul C. Unangst
Abstract: Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
Type:
Grant
Filed:
May 3, 1995
Date of Patent:
October 8, 1996
Assignee:
Warner-Lambert Company
Inventors:
John M. Domagala, John S. Kiely, Mel C. Schroeder
Abstract: 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran inhibits MEK and, as such, is effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
Abstract: Polyamines inhibit vascular smooth muscle proliferation and thus are useful in treating and preventing vascular proliferative disorders such as restenosis following balloon angioplasty.
Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
Type:
Grant
Filed:
December 19, 1994
Date of Patent:
April 23, 1996
Assignee:
Warner-Lambert Company
Inventors:
Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.
Abstract: The novel 3,5-ditertiarybutyl-4-hydroxy-phenylmethylene derivative of 2-substituted thiazolidinones, oxazolidinones, and imidazolidinones as antiinflammatory agents having inhibiting activity for 5-lipoxygenase, cyclooxygenase, or both.
Type:
Grant
Filed:
December 9, 1994
Date of Patent:
February 27, 1996
Assignee:
Warner-Lambert Company
Inventors:
Wiaczeslaw A. Cetenko, David T. Connor, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst
Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
Type:
Grant
Filed:
December 19, 1994
Date of Patent:
February 13, 1996
Assignee:
Warner-Lambert Company
Inventors:
Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
Abstract: Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases.
Type:
Grant
Filed:
December 12, 1994
Date of Patent:
February 6, 1996
Assignee:
Warner-Lambert Company
Inventors:
Diane H. Boschelli, David T. Connor, James B. Kramer, Paul C. Unangst
Abstract: 5-Aryltriazol-3-thiones are useful for inhibiting adhesion of Mac-1 and thereby providing cytoprotection for diseases mediated by Mac-1 adhesion.