Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Type:
Grant
Filed:
March 8, 1999
Date of Patent:
December 26, 2000
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
Abstract: The present invention provides compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of diseases whose treatment benefits from the inhibition of phosphodiesterase (PDE-IV) or Tumor Necrosis Factor (TNF) including asthma, allergic diseases, rheumatoid arthritis, osteoarthritis, septic shock. The compounds provided by this invention have formula (I) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein.
Type:
Grant
Filed:
February 7, 2000
Date of Patent:
December 19, 2000
Assignee:
Warner-Lambert Company
Inventors:
David Thomas Connor, Joseph Peter Menetski
Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.
Type:
Grant
Filed:
October 5, 1999
Date of Patent:
November 28, 2000
Assignee:
Warner-Lambert Company
Inventors:
Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
Abstract: This invention relates to the inhibition of protein tyrosine kinase (PTK) and cell cycle kinase mediated cellular proliferation. More specifically, this invention relates to naphthyridinones and their use in inhibiting cellular proliferation and PTK or cell cycle kinase enzymatic activity.
Type:
Grant
Filed:
January 26, 2000
Date of Patent:
November 21, 2000
Assignee:
Warner-Lambert Company
Inventors:
Mark Robert Barvian, William Alexander Denny, Ellen Myra Dobrusin, James Marino Hamby, Howard Daniel Hollis Showalter, Andrew Mark Thompson, Roy Thomas Winters, Zhipei Wu
Abstract: The present invention provides ras farnesyl transferase inhibiting compounds of Formula I ##STR1## 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:
January 20, 2000
Date of Patent:
November 7, 2000
Assignee:
Warner-Lambert Company
Inventors:
James Stanley Kaltenbronn, Daniele Marie Leonard, Joseph Thomas Repine
Abstract: The present invention provides compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase. The present invention also provides pharmaceutical compositions that contain a compound that inhibits the association of platelet-derived growth factor and phosphatidylinosital 3-kinase, and methods of treating cancer, restenosis, arthritis, dermatitis, atherosclerosis, vein graft intimal hyperplasia, neointimal hyperplasia of vascular smooth muscle and psoriasis using compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase.
Type:
Grant
Filed:
February 22, 1999
Date of Patent:
October 24, 2000
Assignee:
Warner-Lambert Company
Inventors:
Wayne Livingston Cody, Annette Marian Doherty, Scott R. Eaton, Robert Lee 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:
June 26, 1997
Date of Patent:
October 17, 2000
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: The present invention relates to compositions comprising a compound which inhibits the actions of angiotensin-converting enzyme and a compound which inhibits the actions of matrix metalloproteinase enzymes and the use of such compositions for treating ventricular dilation, heart failure and cardiovascular fibrotic pathologies.
Type:
Grant
Filed:
February 7, 2000
Date of Patent:
October 17, 2000
Assignee:
Warner-Lambert Company
Inventors:
Joseph Thomas Peterson, Jr., Milton Lethan Pressler
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:
August 2, 1999
Date of Patent:
October 17, 2000
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 is directed to a method for preventing visceral and gastrointestinal damage such as gastric ulcers by administering a gamma-aminobutyric acid (GABA) analog and for treating gastrointestinal diseases such as inflammatory bowel disorders (IBD), functional bowel disorders (FBD) including dyspepsia and other visceral pain.
Type:
Grant
Filed:
April 19, 1999
Date of Patent:
October 3, 2000
Assignee:
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 P. Watson
Abstract: This invention provides irreversible inhibitors of tyrosine kinases having for formula ##STR1## which compounds are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis.
Abstract: This invention relates to pyrrolo[1,2-a]pyrazine-1,4-diones of general formula: ##STR1## wherein B is carbonyl or methylene, R.sup.2, R.sup.4, R.sup.5, and R.sup.6 are hydrogen, alkyl, or substituted alkyl, A is a basic group, and Q is hydrogen or a keto heterocycle group.The compounds are inhibitors of serine proteases, typically thrombin, Factor Xa, and Factor VIIa, and are useful for treating and preventing thrombotic disorders.
Type:
Grant
Filed:
October 27, 1998
Date of Patent:
September 26, 2000
Assignee:
Warner-Lambert Company
Inventors:
Kent A. Berryman, Annette M. Doherty, Jeremy J. Edmunds, M. Arshad Siddiqui
Abstract: Process for the preparation of cericlamine which consists: i) in arylating methacrylic acid with the diazonium chloride of 3,4-dichloroaniline, to obtain (+/-)2-chloro-3-(3,4-dichlorophenyl)-2-methylpropionic acid, ii) in aminating the acid with dimethylamine, to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropionic acid, or an alkaline metal salt thereof, iii) in esterifying the amino-acid or its salt, then, iv) in reducing the ester by a metal or organometal hydride to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methyl-propan-1-ol.
Type:
Grant
Filed:
December 20, 1999
Date of Patent:
September 19, 2000
Assignee:
Warner-Lambert Company
Inventors:
Marc Nicolas, Blandine Laboue, Dominique Depernet
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## 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:
January 19, 1999
Date of Patent:
September 12, 2000
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Todd Robert Ryder, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilatation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
Type:
Grant
Filed:
July 26, 1999
Date of Patent:
September 12, 2000
Assignee:
Warner-Lambert Company
Inventors:
Joseph Armand Picard, Bruce David Roth, Drago Robert Sliskovic
Abstract: Compounds that are antagonists of dopamine D4 receptors, methods of treating psychosis and schizophrenia using the compounds, and pharmaceutically acceptable compositions that contain the dopamine D4 receptor antagonists are disclosed.
Type:
Grant
Filed:
January 29, 1998
Date of Patent:
July 11, 2000
Assignee:
Warner-Lambert Company
Inventors:
Thomas Richard Belliotti, David Juergen Wustrow
Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula I, II, or III. ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.
Type:
Grant
Filed:
April 9, 1999
Date of Patent:
July 4, 2000
Assignee:
Warner-Lambert Company
Inventors:
Hamish John Allen, Kenneth Dale Brady, William Glen Harter, Elizabeth Ann Lunney, Mark Stephen Plummer, Tomi Sawyer, Aurash Shahripour, Nigel Walker
Abstract: The invention provides substituted furanone antiarthritic and analgesic pharmaceutical agents defined by Formula I, ##STR1## wherein: R.sup.1 is selected from the group consisting of(a) S(O).sub.2 CH.sub.3,(b) S(O).sub.2 NH.sub.2,(c) S(O).sub.2 NHC(O)CF.sub.3,(d) S(O)(NH)CH.sub.3,(e) S(O)(NH)NH.sub.2,(f) S(O)(NH)NHC(O)CF.sub.3,(g) P(O)(CH.sub.3)OH, and(h) P(O)(CH.sub.3)NH.sub.2 ;R.sup.2 and R.sup.3 independently are selected from(1) hydrogen,(2) halo,(3) C.sub.1 -C.sub.6 alkyl,(4) C.sub.1 -C.sub.6 alkoxy, and(5) C.sub.1 -C.sub.6 alkylthio;n is an integer from 1 to 3;m is an integor from 1 to 3;or a pharmaceutically acceptable salt thereof.
Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations at risk for developing noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed. In one embodiment, the compounds of the invention are used to treat polycystic ovary syndrome in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus. In another embodiment, the compounds of the invention are used to treat gestational diabetes in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus.
Type:
Grant
Filed:
June 4, 1997
Date of Patent:
April 4, 2000
Assignee:
Warner-Lambert Company
Inventors:
Tammy Antonucci, Dean Lockwood, Rebecca Norris