Abstract: The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
Type:
Grant
Filed:
April 7, 2003
Date of Patent:
February 15, 2005
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Patricia Ann Basford, Peter Thomas Stephenson, Stefan Colin John Taylor, Anthony Wood
Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as inhibitors of phosphosdiesterase-7.
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
February 8, 2005
Assignee:
Pfizer Inc.
Inventors:
Fabrice Vergne, Patrick Bernardelli, Edwige Lorthiois, Pierre Ducrot
Abstract: NHE-1 inhibitor, methods of using the NHE-1 inhibitor and pharmaceutical compositions containing the NHE-1 inhibitor. The NHE-1 inhibitor is useful for the reduction of tissue damage resulting from tissue ischemia.
Type:
Grant
Filed:
April 17, 2001
Date of Patent:
February 8, 2005
Assignee:
Pfizer Inc.
Inventors:
Weichao G. Chen, Eric D. Cox, Angel Guzman-Perez
Abstract: The invention provides compounds of 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 to treat diseases or conditions in which ?7 is known to be involved.
Type:
Grant
Filed:
February 10, 2003
Date of Patent:
February 8, 2005
Assignee:
Pfizer Inc
Inventors:
Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.
Type:
Grant
Filed:
December 3, 2002
Date of Patent:
February 8, 2005
Assignee:
Pfizer Inc
Inventors:
Terence Vernon Silk, Julian Duncan Smith
Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
Type:
Grant
Filed:
August 22, 1997
Date of Patent:
February 1, 2005
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.
Type:
Grant
Filed:
October 17, 2002
Date of Patent:
February 1, 2005
Assignee:
Pfizer Inc
Inventors:
Daniel Patrick Walker, Eric Jon Jacobsen, David W. Piotrowski, Brad A. Acker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, Vincent E. Groppi, Jr.
Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
Type:
Grant
Filed:
October 28, 2003
Date of Patent:
February 1, 2005
Assignee:
Pfizer Inc.
Inventors:
Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
Abstract: This invention relates to certain indole-2-carboxamides of formula (I) and the pharmaceutically acceptable salts and prodrugs thereof, wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, C(O)NR8R9 or C(O)R12, useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds.
Type:
Grant
Filed:
June 17, 2003
Date of Patent:
January 25, 2005
Assignee:
Pfizer Inc.
Inventors:
Dennis J. Hoover, Bernard Hulin, William H. Martin, Judith L. Treadway
Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.
Type:
Grant
Filed:
April 16, 2003
Date of Patent:
January 25, 2005
Assignee:
Pfizer Inc.
Inventors:
Kristin Lundy DeMello, Brian S. Bronk, Rhonda Marie Crosson
Abstract: A system and method for statistically analyzing QT interval as a function of changes in the RR interval. The system and method utilize three statistical comparisons to fully characterize the QT response: (1) the comparison of curves to give an overall effect; (2) the incidence of points exceeding a baseline upper 95% single-point prediction bound to reflect the degree of heterogeneity of ventricular repolarization; and (3) the magnitude of these points to provide a quantitative assessment of treatment-induced changes in the QT-RR relationship. The system and method use the relationship between the QT interval and heart rate (RR interval) to reference a control baseline response. Data from mammals such as humans and dogs, and pharmacological maneuvers using both cardiac and non-cardiac therapeutic agents, may be used with this multi-parameter statistical system and method.
Type:
Grant
Filed:
September 21, 2001
Date of Patent:
January 25, 2005
Assignee:
Pfizer, Inc.
Inventors:
Michael J. DePasquale, Anthony A. Fossa, David L. Raunig
Abstract: A process for preparing a compound of the formula: wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of ?-adrenergic receptor agonists.
Abstract: The invention relates to succinate and malonate complexes of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide having the following formula I: More particular the present invention relates to monosuccinate, hemisuccinate, sesquisuccinate and di-malonate complexes of formula I. The invention also relates to pharmaceutical compositions containing the succinate and malonate complexes of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above complexes and to methods of preparing the above complexes.
Type:
Grant
Filed:
December 10, 2002
Date of Patent:
January 18, 2005
Assignee:
Pfizer Inc
Inventors:
John C. Kath, Daniel T. Richter, Zheng J. Li, Andrew V. Trask
Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
October 9, 2003
Date of Patent:
January 18, 2005
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon Mantell
Abstract: The present invention relates to compounds of formulas 1 and 2 wherein R1, R2, R4, R5, R6, R7, R8, R10 and Z are as defined herein. The present invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating hyperproliferative disorders, such as cancer, in a mammal by administering the above compounds.
Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.
Abstract: The present invention provides a device, preferably a collar or ear tag, capable of the controlled, sustained release of an effective amount of an active ingredient that can protect an animal against arthropod pests, comprising a reservoir containing a novel gel formulation comprising a fatty acid, an organic solvent which is a linear aliphatic ester, a silicone-based fluid, or a combination thereof, and an active ingredient that can protect the animal against one or more arthropod pests.