Abstract: The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy.
Type:
Grant
Filed:
August 20, 2002
Date of Patent:
January 20, 2004
Assignee:
Pfizer Inc
Inventors:
Alan Craig Bentham, Alan John Pettman, Keith Stephen Ruddock
Abstract: Compounds of the formula (I):
wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
Type:
Grant
Filed:
October 6, 2000
Date of Patent:
January 13, 2004
Assignee:
Pfizer Inc
Inventors:
Mark Edward Bunnage, Keith Michael DeVries, Laurence James Harris, Philip Charles Levett, John Paul Mathias, Joanna Teresa Negri, Stephen Derek Albert Street, Albert Shaw Wood
Abstract: This invention relates to improved processes for preparing compounds of Formula II,
and compounds of Formula III,
wherein R1, R2, R3 and Prt are defined as set forth in the specification.
Type:
Grant
Filed:
October 30, 2002
Date of Patent:
January 6, 2004
Assignee:
Pfizer Inc.
Inventors:
Frank R. Busch, Charles K. Chiu, Clifford N. Meltz, Ronald J. Post, Peter R. Rose
Abstract: There is provided compounds of formula IA and of formula IB,
wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
Type:
Grant
Filed:
October 22, 1999
Date of Patent:
December 30, 2003
Assignee:
Pfizer Inc
Inventors:
Mark Edward Bunnage, John Paul Mathias, Stephen Derek Albert Street, Anthony Wood
Abstract: The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7Å crystal structure of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer.
Type:
Grant
Filed:
December 14, 1999
Date of Patent:
December 30, 2003
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Ping Chen, Mark Anderson, Ya-Li Deng, Smita Gaur, Chen Chen Kan, Chun Luo, Karen Lundgren, Stephen Margosiak, Binh Nguyen, Patrick O'Connor, James Register, Anna Tempczyk Russell, Jay Sarup
Abstract: Compounds of formula (I), pharmaceutical formulations thereof and the use of such compounds for treating endothelin mediated diseases or conditions are described herein.
The compounds of the present invention have affinity for endothelin receptors, are selective for ETA over ETB, and thus are useful in the treatment of conditions mediated by endothelin.
Type:
Grant
Filed:
September 12, 2001
Date of Patent:
December 30, 2003
Assignee:
Pfizer Inc.
Inventors:
Bernard Joseph Banks, Anthony Logan Chubb, Douglas James Critcher, James John Eshelby, Darren John Schulz
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 &bgr;-adrenergic receptor agonists.
Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.
Type:
Grant
Filed:
June 12, 2002
Date of Patent:
December 30, 2003
Assignee:
Pfizer Inc.
Inventors:
Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
Abstract: This invention relates to methods of treating traumatic brain injury (TBI) or hypoxic or ischemic stroke, comprising administering to a patient in need of such treatment an NR2B subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist in combination with either: (a) a neutrophil inhibitory factor (NIF); (b) a sodium channel antagonist; (c) a nitric oxide synthase (NOS) inhibitor; (d) a glycine site antagonist; (e) a potassium channel opener; (f) an AMPA/kainate receptor antagonist; (g) a calcium channel antagonist; (h) a GABA-A receptor modulator (e.g., a GABA-A receptor agonist); or (i) an antiinflammatory agent.
Type:
Grant
Filed:
September 6, 2001
Date of Patent:
December 23, 2003
Assignee:
Pfizer Inc
Inventors:
Bertrand L. Chenard, Frank S. Menniti, Mario D. Saltarelli
Abstract: Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by adding one or more water-miscible co-solvents. In a preferred embodiment, the one or more co-solvents is propylene glycol.
Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.
Type:
Grant
Filed:
June 12, 2002
Date of Patent:
December 23, 2003
Assignee:
Pfizer Inc
Inventors:
Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
Abstract: There is provided a process for the production a compound of general formula I:
wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises the reaction of a compound of formula II,
wherein Rx is a group substitutable by an aminopyrazole, with a compound of general formula III
Abstract: This invention relates to compounds of the formula 1
and to pharmaceutically acceptable salts and solvates thereof wherein X1, X2, R2, R15, R16 and R6 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.
Type:
Grant
Filed:
December 10, 1999
Date of Patent:
December 16, 2003
Assignee:
Pfizer Inc.
Inventors:
Wei-Guo Su, Takushi Kaneko, Yong-Jin Wu
Abstract: The present invention relates to novel benzotriazoles of the formula I
wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen;
R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;
R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;
s is an integer from 0-5;
to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Type:
Grant
Filed:
April 4, 2002
Date of Patent:
December 16, 2003
Assignee:
Pfizer Inc
Inventors:
Michael A. Letavic, Mark A. Dombroski, Kim F. McClure, Ellen R. Laird
Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I,
wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith.
Type:
Grant
Filed:
March 10, 2003
Date of Patent:
December 9, 2003
Assignee:
Pfizer Inc
Inventors:
Margaret Y. Chu-Moyer, Jerry A. Murry, Banavara L. Mylari, William J. Zembrowski
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, —NR2 R3 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:
March 12, 2002
Date of Patent:
December 9, 2003
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 methods of making quinoline amides of Formula I below, which are microsomal triglyceride transfer protein inhibitors and can be used as medicines.
The present invention also relates to compounds that are used to make quinoline amides of Formula I and methods of making these compounds.
Abstract: 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-one compounds which are selective inhibitors of cGMP PDE are useful in the treatment of erectile dysfunction (impotence) in male animals, including man.
Type:
Grant
Filed:
June 13, 2001
Date of Patent:
December 2, 2003
Assignee:
Pfizer Inc
Inventors:
Simon Fraser Campbell, Alexander Roderick MacKenzie, Anthony Wood
Abstract: This invention is directed to pharmaceutical compositions comprising &bgr;3 adrenergic agonists including (4-(2-(2-(6-aminopyridin-3-yl)-2(R)-hydroxyethylamino)ethoxy)phenyl)acetic acid and growth hormone or growth hormone secretagogues, prodrugs thereof or pharmaceutically acceptable salts of said compounds or said prodrugs. The invention is also directed to methods of using those compositions in the treatment of obesity, diabetes, hypertension and frailty in animals and particularly in humans.