Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5, R6, and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).
Abstract: A process for preparing a 2-(pyridin-4-ylamino)-pyrido[2,3-d]pyrimidine of Formula II comprising reacting a 4-aminopyridine of the formula with an alkali metal amide or hydride and a 2-alkylsulfanyl-pyrido[2,3-d]pyrimidine of Formula I wherein R1, R2, R? and R?, and aryl are as defined in the specification.
Type:
Grant
Filed:
July 12, 2001
Date of Patent:
May 31, 2005
Assignee:
Warner-Lamber Company
Inventors:
Howard Isaac Tjiong, Roy Thomas Winters
Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
May 31, 2005
Assignee:
Pharmacia Corporation
Inventors:
Jennifer Ann Van Camp, James W. Malecha, Julie M. Miyashiro, Gary A. DeCrescenzo, Joe T. Collins, Monica J. Kalman
Abstract: A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet.
Type:
Grant
Filed:
December 20, 2000
Date of Patent:
May 31, 2005
Assignee:
Pfizer Inc
Inventors:
William J. Curatolo, Kenneth C. Waterman, Avinash G. Thombre, Michael B. Fergione, Michael C. Roy, Leah A. Appel, Danni Supplee, Dwayne T. Friesen, Mark B. Chidlaw, Ronald A. Beyerinck
Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds as adenosine A2a receptor agonists.
Abstract: Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.
Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recit
Type:
Grant
Filed:
November 20, 2002
Date of Patent:
May 17, 2005
Assignee:
Pfizer Inc
Inventors:
Anthony Marfat, Michael William McKechney
Abstract: Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein
Type:
Grant
Filed:
June 5, 2002
Date of Patent:
May 17, 2005
Assignee:
Pfizer Inc.
Inventors:
Phoebe Chiang, William A. Novomisle, Willard M. Welch, Jr., Angel Guzman-Perez, Paul A. DaSilva-Jardine, Ravi S. Garigipati, Kevin K. Liu
Abstract: The present invention relates to compounds of Formula I, wherein R1, R2, R3, R4, and n are as defined, and to pharmaceutically acceptable salts of said compounds. Compounds of Formula I have activity in agonizing 5HT7 receptors and are useful in treating, for example, disorders that can be treated by modulating circadian rhythms.
Abstract: A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.
Type:
Grant
Filed:
May 20, 2003
Date of Patent:
May 10, 2005
Assignee:
Pfizer, Inc.
Inventors:
Todd A. Blumenkopf, Mark E. Flanagan, Matthew F. Brown, Paul S. Changelian
Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
Type:
Grant
Filed:
January 23, 2003
Date of Patent:
May 10, 2005
Assignee:
Warner-Lambert Company
Inventors:
Gordon William Rewcastle, Julie Ann Spicer, Stephen Douglas Barrett, Michael David Kaufman, Jared Bruce John Milbank, Haile Tecle
Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
Type:
Grant
Filed:
June 18, 2001
Date of Patent:
May 10, 2005
Assignee:
Pfizer Inc
Inventors:
John Charles Kath, Joel Morris, Samit Kumar Bhattacharya
Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
Type:
Grant
Filed:
February 15, 2003
Date of Patent:
May 10, 2005
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Maria Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
Abstract: The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
May 10, 2005
Assignee:
Pfizer Inc
Inventors:
David E. Bogle, Peter R. Rose, Glenn R. Williams
Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.
Abstract: A pharmaceutical composition for treating a disorder that is treated by modulation of serotonergic neurotransmission comprising administering (7S,9aS)-cis-2-Benzo[d]isoxazol-3-yl-7-(3-pyrrolidin-1-ylmethyl-phenoxymethyl)-octahydro-pyrido-[1,2-a]pyrazine and sertraline is disclosed.
Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.
Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant ?7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant ?7 nicotinic receptor agonist.
Type:
Grant
Filed:
April 27, 2004
Date of Patent:
April 19, 2005
Assignee:
Pfizer Inc.
Inventors:
Brian Thomas O'Neill, Jotham Wadsworth Coe, Christopher J. O'Donnell
Abstract: The invention concerns a method for chemoselective oxidation of an organic compound comprising several potentially oxidizable groups whereof at least one is a nitrogen group. Said method is characterised in that it consists in using at least a protic solvent, which is a good donor of hydrogen bonds, enabling to limit N-oxidation.
Abstract: A screen has been designed to genetically engineer microbial pathogens so that expression of specific genes can be regulated in vitro and during host infection to facilitate the identification of bacterial genes essential for maintaining an infection. Specifically, gene regulatory elements which respond to the presence or absence of tetracycline are used to regulate the expression of endogenous bacterial genes. Because tetracycline is not normally present in animals, a tetracycline-regulated microbial gene can be controlled in vivo by adding or removing tetracycline from the infected animals' diet.