Abstract: This invention relates to human chondrocyte activity (growth)/differentiation/production of extracellular matrix) and to the effect of Sox9 transcription factor and Col2 enhancer as a measure for such activity. It also relates to a chimeric cell and assay utilizing such cell useful in predicting the effect of sample compounds on chondrocyte activity as measured by Sox9 and Col2 expression/activity.
Abstract: The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.
Abstract: The invention relates to novel erythromycin derivatives, particularly ones with novel C-13 R13 substitutents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are useful as antibacterial agents and antiprotozoa agents and for other applications (e.g., anticancer, atherosclerosis, gastric motility reduction, etc.) in mammals, including man, as well as in fish and. The invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial protozoa infections by administering such compounds. The invention also relates to methods of preparing such compounds and to intermediates useful in such preparation.
Abstract: The present invention is directed to a polymorph of the citrate salt of 4-(3,4-dichlorophenyl)-2-[2-(4-methylpiperazin-1-yl)-benzylidene]-thiomorpholin-3-one:
and pharmaceutical compositions thereof.
Abstract: The invention relates to processes for preparing compounds of formula 1
wherein R3 is as defined herein, and to pharmaceutically acceptable salts thereof, as well as intermediates useful in such processes. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing compounds prepared by the processes of the invention and to methods of treating bacterial protozoa infections by administering such compounds.
Type:
Grant
Filed:
April 25, 2002
Date of Patent:
November 30, 2004
Assignee:
Pfizer Inc.
Inventors:
Constantine Sklavounos, John L. Tucker, Lulin Wei, Kerry P. Mahon, Philip Hammen, Joanna T. Negri, Richard S. Lehner
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:
Grant
Filed:
July 30, 2001
Date of Patent:
November 30, 2004
Assignee:
Pfizer Inc.
Inventors:
Desmond John Best, George Burton, Brian Charles Gasson, Neal Frederick Osborne, Graham Walker
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:
May 28, 2002
Date of Patent:
November 30, 2004
Assignee:
Pfizer Inc
Inventors:
Phoebe Chiang, William A. Novomisle, Willard M. Welch, Jr.
Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the modulation of the cannabinoid receptors in animals are described herein.
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:
Application
Filed:
March 12, 2004
Publication date:
November 25, 2004
Applicant:
Pfizer Inc
Inventors:
Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
Abstract: The present invention provides substituted 2-aminopyridines of formula I, wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders.
Type:
Application
Filed:
January 16, 2004
Publication date:
November 25, 2004
Applicant:
Pfizer Inc
Inventors:
Cathlin Marie Biwersi, Dennis Joseph McNamara, Joseph Thomas Repine, Peter Laurence Toogood, Scott Norman Vanderwel, Joseph Scott Warmus
Abstract: The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.
Abstract: Methods for treating or preventing bacterial or protozoal infections in mammals by administering a single dose of an antibiotic composition comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are disclosed. Methods for increasing acute or chronic injection-site toleration in mammals by administering a single dose of antibiotic compositions comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are also disclosed. A combination comprising: an antibiotic composition comprising a mixture of azalide isomers, a pharmaceutically acceptable carrier, and instructions for use in a single-dose administration is also disclosed.
Type:
Application
Filed:
December 23, 2003
Publication date:
November 25, 2004
Applicant:
Pfizer Inc
Inventors:
Peter Connor Canning, Wayne Alan Boettner