Abstract: The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
Abstract: The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.
Type:
Grant
Filed:
December 23, 2002
Date of Patent:
August 2, 2005
Assignee:
Pfizer Inc.
Inventors:
James A. Sikorski, Richard C. Durley, Melvin L. Rueppel, Deborah A. Mischke, Barry L. Parnas
Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
Type:
Grant
Filed:
February 21, 2003
Date of Patent:
August 2, 2005
Assignee:
Pfizer Inc.
Inventors:
Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
Abstract: The invention provides a compound of formula I: wherein R1, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection, atherosclerosis or restenosis using such compounds or salts.
Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.
Type:
Grant
Filed:
October 10, 2003
Date of Patent:
August 2, 2005
Assignees:
Pfizer Inc., Pfizer Products Inc.
Inventors:
Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
Abstract: There is provided a process for the preparation of a compound according to Formula (II): which includes the step of cyclising a compound of Formula (III): wherein R1, R2, R3, R4, X and m have meanings which are given in the description.
Type:
Application
Filed:
November 22, 2004
Publication date:
July 28, 2005
Applicant:
Pfizer, Inc.
Inventors:
Desmond Best, George Burton, Brian Gasson, Neal Osborne, Graham Walker
Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.
Type:
Grant
Filed:
June 19, 2001
Date of Patent:
July 26, 2005
Assignee:
Pfizer Inc
Inventors:
Simon John Mantell, Sandra Marina Monaghan, Peter Thomas Stephenson
Abstract: The present invention relates to compounds of the formula Orosco wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.
Abstract: The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.
Type:
Grant
Filed:
August 13, 2003
Date of Patent:
July 26, 2005
Assignee:
Pfizer Inc.
Inventors:
Bertrand L Chenard, Willard M Welch, Anthony R. Reinhold
Abstract: The present invention provides processes useful in the preparation of certain ?3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.
Type:
Grant
Filed:
October 9, 2003
Date of Patent:
July 19, 2005
Assignee:
Pfizer Inc,
Inventors:
Robert J. Chambers, Robert W. Dugger, Ming Kang, Yong Tao, John W. Wong
Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
Abstract: The invention provides compounds of Formula I: Azabicyclo-N(R1)—C(?X)—W??Formula I These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.
Type:
Grant
Filed:
November 6, 2002
Date of Patent:
July 19, 2005
Assignee:
Pfizer Inc
Inventors:
David W. Piotrowski, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, Alice L. Bodnar, Vincent E. Groppi, Jr., Daniel Patrick Walker, Brad A. Acker
Abstract: Compounds according to formula (I) wherein n is 1-4, R1 is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7 and R8 are each independently selected from hydrogen and optionally substituted C1-6 alkyl are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.
Type:
Grant
Filed:
March 31, 2004
Date of Patent:
July 19, 2005
Assignee:
Pfizer, Inc.
Inventors:
Charlotte Moira Norfor Allerton, Mark Edward Bunnage, John Steele
Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
Abstract: The present invention is directed to a method of producing attenuated forms of bovine viral diarrhea (BVD) virus by mutating the Npro protease gene. The invention includes the attenuated viruses made by this method, antibodies generated using these viruses, and vaccines that can be used for immunizing cattle.
Abstract: The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of a matrix metalloproteinase inhibitor and an antineoplastic agent.
Type:
Grant
Filed:
September 20, 2004
Date of Patent:
July 12, 2005
Assignee:
Pfizer Inc
Inventors:
John P. McKearn, Gary Gordon, James J. Cunningham, Stephen T. Gately, Alane T. Koki, Jaime L. Masferrer
Abstract: The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position.
Abstract: This invention relates to novel nucleic acid sequences encoding three novel human phosphodiesterase (hPDE IV) isozymes. It also relates to polypeptides encoded by such sequences. This invention also relates to an assay method for detecting the presence of such novel isozymes in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozymes.
Abstract: The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine and (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine.
Type:
Grant
Filed:
October 9, 2003
Date of Patent:
June 28, 2005
Assignees:
Pfizer Inc., DSM Pharmaceuticals, Inc.
Inventors:
Robert Seemayer, Thomas C. Nugent, Jack Liang