Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, and to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors.
Type:
Grant
Filed:
February 22, 1999
Date of Patent:
February 1, 2000
Assignee:
Warner-Lambert Company
Inventors:
David Thomas Connor, Stephen Joseph Johnson, Suzanne Ross Kesten, Steven Robert Miller, Paul Charles Unangst, Lawrence David Wise
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 include hydrogen, alkyl, substituted alkyl, halo, and arylalkyl; R.sub.3 is hydroxy, alkoxy, or hydroxyamino; X is O, S, or NOH; and R.sub.4 and R.sub.5 include hydrogen, alkyl, and aryl are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues.
Type:
Grant
Filed:
October 27, 1998
Date of Patent:
February 1, 2000
Assignee:
Warner-Lambert Company
Inventors:
Joseph Armand Picard, Drago Robert Sliskovic
Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
Type:
Grant
Filed:
July 26, 1999
Date of Patent:
January 25, 2000
Assignee:
Warner-Lambert Company
Inventors:
Helen Tsenwhei Lee, Mark Alan Massa, William Chester Patt, Bruce David Roth
Abstract: Amyloid aggregation in animals is inhibited by administering a naphthylazo compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, alkyl, substituted alkyl, or complete a heterocyclic ring, R.sup.3 is hydrogen or alkyl, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are substituent groups. The compounds are especially useful in preventing and treating Alzheimer's disease.
Type:
Grant
Filed:
May 3, 1999
Date of Patent:
January 25, 2000
Assignee:
Warner-Lambert Company
Inventors:
Sheryl Jeanne Hays, Harry LeVine, III, Jeffery David Scholten
Abstract: New 2-(arylalkenyl)azacycloalkane derivatives which are ligands for sigma receptors, of the formula (I) ##STR1## in which: Ar is aryl or heteroaryl, optionally mono- to trisubstituted,m has the value 1 or 2,n has the value 1 to 3,R is phenyl, or cycloalkyl containing 3 to 7 carbon atoms,their isomers and their addition salts.Medicinal drugs which are antipsychotic agents and are useful in gastroenterology.
Type:
Grant
Filed:
September 2, 1998
Date of Patent:
January 11, 2000
Assignee:
Warner-Lambert Company
Inventors:
Alain Pierre Calvet, Henry Jacobelli, Jean-Louis Junien, Pierre Riviere, Fran.cedilla.ois-Joseph Roman
Abstract: Combinations of a glitazone antidiabetic agent and a biguanide antidiabetic agent, and optionally a sulfonylurea antidiabetic agent, are useful for treating diabetes mellitus and improving glycemic control.
Abstract: This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, halo, CN, OR.sup.6, NR.sup.6 R.sup.7, --CO.sub.2 R.sup.6, CONR.sup.6 R.sup.7, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.6 R.sup.7, and R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5, when attached to adjacent ring atoms, can be --(CH.sub.2).sub.3 or 4 --;in which R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, and when taken together with the nitrogen to which they are attached, R.sup.6 and R.sup.7 can complete a cyclic ring having from 3 to 7 carbon atoms; ##STR2## in which R.sup.8, R.sup.8', R.sup.9, and R.sup.9' independently are hydrogen or C.sub.1 -C.sub.6 alkyl, n is 0, 1, or 2, and Z.sup..crclbar.
Type:
Grant
Filed:
March 20, 1998
Date of Patent:
December 14, 1999
Assignee:
Warner-Lambert Company
Inventors:
Joseph A. Cornicelli, Bradley D. Tait, Bharat K. Trivedi
Abstract: The present invention provides a method of imaging amyloid deposits and radiolabeled compounds useful in imaging amyloid deposits. The invention also provides a method of delivering a therapeutic agent to amyloid deposits, a method of inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of determining a compound's ability to inhibit aggregation of amyloid proteins.
Type:
Grant
Filed:
July 22, 1998
Date of Patent:
December 14, 1999
Assignee:
Warner-Lambert Company
Inventors:
Bradley W. Caprathe, John L. Gilmore, Sheryl J. Hays, Juan C. Jaen, Harry LeVine, III
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:
June 26, 1997
Date of Patent:
December 14, 1999
Assignee:
Warner-Lambert Company
Inventors:
Gary Louis Bolton, John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti, Terri Stoeber Purchase, Joseph Peter Sanchez, Bharat Kalidas Trivedi
Abstract: Amyloid aggregation in animals is inhibited by administering a 9-acridinone compound of formula I, defined herein. The compounds are especially useful in preventing and treating Alzheimer's disease.
Type:
Grant
Filed:
April 29, 1998
Date of Patent:
October 26, 1999
Assignee:
Warner-Lambert Company
Inventors:
Sheryl Jeanne Hays, Harry LeVine, III, Jeffery David Scholten
Abstract: Inhibitors of 15-lipoxygenase (15-LO) are useful to treat and prevent inflammation or atherosclerosis. Preferred inhibitors have a ratio of 5-LO to 15-LO inhibitory activity of at least about 10 or more. Typical 15-LO inhibitors have the formula ##STR1## wherein R.sup.13 is phenyl, 4-chlorophenyl, 4-fluorophenyl, 4-nitrophenyl, 2,5-dichlorophenyl, 2-furanyl, 2-thienyl, 3-pyridyl, or 4-pyridyl.
Type:
Grant
Filed:
April 20, 1999
Date of Patent:
October 26, 1999
Assignee:
Warner-Lambert Company
Inventors:
Joseph Anthony Cornicelli, Bradley Dean Tait, Bharat Kalidas Trivedi, Janak Khimchand Padia
Abstract: Combinations of a sulfonylurea antidiabetic agent and a glitazone antidiabetic agent are useful for treating diabetes mellitus and improving glycemic control.
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: Amyloid aggregation in animals is inhibited by administering a naphthylazo compound of formula (I), wherein R1 and R2 are hydrogen, alkyl, substituted alkyl, or complete a heterocyclic ring, R3 is hydrogen or alkyl, R4, R5, R6, and R7 are substitutent groups. The compounds are especially useful in preventing and treating Alzheimer's disease.
Type:
Grant
Filed:
April 29, 1998
Date of Patent:
September 21, 1999
Assignee:
Warner-Lambert Company
Inventors:
Sheryl Jeanne Hays, Harry LeVine, III, Jeffery David Scholten
Abstract: 6-Aryl naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.
Type:
Grant
Filed:
March 18, 1998
Date of Patent:
September 14, 1999
Assignee:
Warner-Lambert Company
Inventors:
Clifton John Blankley, Annette Marian Doherty, James Marino Hamby, Robert Lee Panek, Mel Conrad Schroeder, Howard Daniel Hollis Showalter, Cleo Connolly
Abstract: N-oxides of amino containing 6-aryl pyrido?2,3-d!-pyrimidine 7-imines, 7-ones, and 7-thiones have the formula ##STR1## where A and B are linkers, Ar is aryl, R.sub.2 is aklyl, X is O, S, or NH, or NAcyl, and R.sub.5 and R.sub.6 are alkyl. The compounds are inhibitors of protein tyrosine kinases and cyclin-dependent 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:
January 29, 1998
Date of Patent:
August 31, 1999
Assignee:
Warner-Lambert Company
Inventors:
Annette Marian Doherty, Hussein Osman Hallak, James Marino Hamby
Abstract: The present invention comprises a method of lowering plasma levels of Lp(a) in animals by administering an effective Lp(a)-reducing amount of a microsomal triglyceride transfer protein inhibitor of the structural formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is alkyl, alkenyl alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, cycloalkyl, or cycloalkylalkyl, each of which is independently optionally substituted through available carbon atoms with 1, 2, or 3 groups selected from halo, alkyl, alkenyl, alkoxy, aryloxy, aryl, arylalkyl, alkylmercapto, arylmercapto, cycloalkyl, cycloalkylalkyl, heteroaryl, and heteroarylalkyl. By lowering Lp(a) levels, the animals are protected against developing premature atherosclerosis and consequent cardiovascular and cerebrovascular diseases.
Type:
Grant
Filed:
October 5, 1998
Date of Patent:
July 27, 1999
Assignee:
Warner-Lambert Company
Inventors:
Helen Tsenwhei Lee, Randy Ranjee Ramharack