Abstract: Novel inhibitors of protein farnesyltransferase enzymes 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, restenosis, atherosclerosis, psoriasis and endometriosis.
Type:
Grant
Filed:
June 2, 1999
Date of Patent:
August 28, 2001
Assignee:
Warner-Lambert Company
Inventors:
Annette M. Doherty, James S. Kaltenbronn, Daniele M. Leonard, Dennis J. McNamara
Abstract:
The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).
Type:
Grant
Filed:
April 5, 2000
Date of Patent:
July 31, 2001
Assignee:
Warner-Lambert Company
Inventors:
David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson
Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1
The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
Type:
Grant
Filed:
December 8, 1999
Date of Patent:
July 24, 2001
Assignee:
Warner-Lambert Company
Inventors:
Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
Abstract: The present invention provides compounds of Formula I
The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
Type:
Grant
Filed:
April 28, 2000
Date of Patent:
July 24, 2001
Assignee:
Warner-Lambert Company
Inventors:
Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
Abstract: The present invention provides compounds having the structure represented by formula (I). Also provided is a method of treating cancer, restenosis, atherosclerosis, or psoriasis or preventing restenosis, and a pharmaceutical composition comprising a compound of formula (I).
Type:
Grant
Filed:
June 28, 1999
Date of Patent:
July 24, 2001
Assignee:
Warner-Lambert Company
Inventors:
Annette Marian Doherty, Daniele Marie Leonard, Dennis Joseph McNamara, Kevon Ray Shuler
Abstract:
The instant invention provides aqueous soluble prodrugs of formula (I) or a pharmaceutically acceptable salt thereof wherein R is —CH2OZ, —C(═O)OCH2OZ or Z, wherein Z is formula (a), —P(═O)(OH)2 or —C(═O)Q: n is an integer of from 0 to 3; m is an integer of from 0 to 1, of certain tachykinin antagonists (NK1 antagonists) useful in the treatment of emesis.
Type:
Grant
Filed:
August 3, 2000
Date of Patent:
July 10, 2001
Assignee:
Warner-Lambert Company
Inventors:
Michael Huai Gu Chen, Om Prakash Goel, Fred M. Hershenson, Zhijian Zhu, Oilun Helen Chan
Abstract: The present invention provides a method for treating or preventing septic shock. Specifically, the present invention provides a method of treating or preventing septic shock by administering to a patient a MEK inhibitor.
Type:
Grant
Filed:
August 2, 1999
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert Company
Inventors:
Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1
The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
Type:
Grant
Filed:
August 7, 2000
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert Company
Inventors:
Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.
Type:
Grant
Filed:
June 14, 1999
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
Abstract: The present invention provides human and murine genomic and complementary DNA and the proteins that are encoded by the DNA, which is called “Protein Targeting to Glycogen”. Also provided is a method of increasing the amount of glycogen in a cell.
Type:
Grant
Filed:
February 25, 1999
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert Company
Inventors:
Matthew Jemail Brady, John Andrew Printen, Alan Robert Saltiel
Abstract: The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of formula (I).
Type:
Grant
Filed:
September 29, 1999
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
Abstract: GABA analogs are useful to prevent and treat gastrointestinal damage and ethanol withdrawal syndrome. Preferred treatments employ gabapentin or pregabalin.
Type:
Grant
Filed:
May 9, 2000
Date of Patent:
June 5, 2001
Assignees:
University of Oklahoma, Warner-Lambert Company
Inventors:
Lionel Bueno, Maria Chovet, Laurent Diop, Antonio Guglietta, Hilary J. Little, Michael Francis Rafferty, Jiayuan Ren, Charles Price Taylor, Jr., William Patrick Watson
Abstract:
The present invention presents compounds that inhibit phosphodiesterase 4 having Formula (I). The present invention also provides methods of using the compounds of Formula (I) to prevent or treat asthma, atopic dermatitis, rheumatoid arthritis, inflammatory bowel disorders, pulmonary hypertension, liver injury, bone loss, septic shock, or multiple sclerosis, and to pharmaceutical compositions that contain the compounds of Formula (I).
Type:
Grant
Filed:
November 10, 1999
Date of Patent:
May 29, 2001
Assignee:
Warner-Lambert Company
Inventors:
Yves Pascal, Catherine Burnouf, Bernard Gaudilliere, Henry Jacobelli, Alain Calvet, Adrian Payne, Svein Dahl
Abstract: The present invention provides a method of inhibiting connective tissue degradation that comprises administering to a patient having a condition in which connective tissue is degraded a therapeutically effective amount of a compound having the formula
where R1, R2, R3, and R4 are independently hydrogen, hydroxy, halo, amino, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, CF3, CN, S(O)n—,
R6 and R7 are independently hydrogen, C1-C6 alkyl, or acyl;
n is 0 to 2;
R8 is hydrogen or C1-C6 alkyl;
W is S or O;
Z is C1-C6 alkyl, C1-C6 alkoxy, or NR9R10;
R9 and R10 are independently hydrogen or C1-C6 alkyl; and
R5 is
where Y is hydroxy, thiol, amino, or NHCN;
X is sulfur or oxygen; and Q is sulfur, oxygen, NH, or NCN, and the pharmaceutically acceptable salts and prodrugs thereof.
Type:
Grant
Filed:
August 6, 1998
Date of Patent:
April 3, 2001
Assignee:
Warner-Lambert Company
Inventors:
Vijaykumar Baragi, Diane Harris Boschelli, David Thomas Connor, Richard Raymond Renkiewicz, Howard Glenn Welgus
Abstract: The present invention relates to a composition for the delivery of a pharmaceutical agent to a patient that comprises polyethylene glycol, an aqueous solution containing polyvinylpyrrolidone, and a pharmaceutical agent. The invention also relates to methods of making a composition for the delivery of a pharmaceutical agent.
Type:
Grant
Filed:
October 21, 1998
Date of Patent:
March 27, 2001
Assignee:
Warner-Lambert Company
Inventors:
Howard Yoshihisa Ando, Steven Edward Rose
Abstract: A compound of the formula
wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.
Type:
Grant
Filed:
April 11, 1995
Date of Patent:
March 6, 2001
Assignee:
Northwestern University
Inventors:
Richard B. Silverman, Ryszard Andruszkiewicz
Abstract: This invention provides 6-amino-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one oximes and hydrazones which are useful in treating Parkinson's disease.
Type:
Grant
Filed:
September 27, 1999
Date of Patent:
February 13, 2001
Assignee:
Warner-Lambert Company
Inventors:
Stephen Joseph Johnson, Leonard Theodore Meltzer, Lawrence David Wise
Abstract: The present invention provides compounds that block calcium channels and have the Formula I:
and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein
R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl,
A is —C(O)— or —CH2—;
R3 is H or —CH3;
R4 is C1-C4 alkyl or piperidin-1-ylethyl;
R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2.
The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.
Type:
Grant
Filed:
November 4, 1998
Date of Patent:
January 23, 2001
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, Lawrence D. Wise, David J. Wustrow