Abstract: A process for the preparation of 2-[alkyl(aryl)]sulfonylbenzene sulfonyl chlorides of the following formula is provided:
in which R is alkyl or aryl substituted at the ortho or meta positions with alkyl, aryl, NHAc or alkoxy, comprising the steps of:
a) reacting 2-chloronitrobenzene, 2-fluoronitrobenzene or 2-bromonitrobenzene with a compound of the following formula:
RSO2−M+
wherein R is defined above; and M is sodium, potassium, lithium, ammonium or quaternary ammonium, in a polar aprotic solvent at a temperature of about 50 to 190° C.;
b) reacting the material prepared in step (a) with hydrogen at a pressure of about 20 to about 60 psi in a polar aprotic solvent at a temperature of about 20 to about 60° C.
Type:
Grant
Filed:
October 31, 2002
Date of Patent:
November 4, 2003
Assignee:
Wyeth
Inventors:
Lalitha Krishnan, Bogdan K. Wilk, Jennifer P. Varriano
Abstract: A safe and effective process for the oxidation of a primary or secondary alcohol to the corresponding aldehyde or ketone via the reaction of said alcohol with an anhydride solution of a 1,1,1-tri(C2-C4 alkanoyloxy-1,1 -dihydro-1,2-benziodoxol-3(1H)-one, and a composition useful in this process.
Type:
Application
Filed:
April 3, 2003
Publication date:
October 30, 2003
Applicant:
Wyeth
Inventors:
Ugo Chiacchio, Antonio Rescifina, Giuseppe Miraglia, Mariangela Magnano, Paola Di Raimondo
Abstract: The present invention provides a coating system for solid pharmaceutical dosage units, such as tablets. The coating system comprising (a) a subcoat; (b) an optional colorcoat; and (c) a polish coat. In a preferred embodiment, the present invention provides (a) a subcoat comprising (i) hydroxypropyl methylcellulose (HPMC) and (ii) a polysaccharide; (b) a colorcoat comprising (i) a colorant and (ii) a polysaccharide which may be the same as or different from the polysaccharide of the subcoat; and (c) a polish coat comprising (i) a polyethylene glycol and, optionally, (ii) a wax. Also disclosed is a method for providing gloss to a coated pharmaceutical solid dosage unit by coating a pharmaceutical core with the aforementioned polish coat.
Abstract: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: 1
Type:
Application
Filed:
October 3, 2002
Publication date:
October 30, 2003
Applicant:
Wyeth
Inventors:
James Harrison Pickar, Barry Samuel Komm
Abstract: The present invention provides enantiomers of N-Desmethyl venlafaxine, as well as their use in pharmaceutical compositions and medically useful treatments, particularly including central nervous system uses.
Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
Abstract: This invention provides compounds of formula 1, having the structure
which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.
Type:
Grant
Filed:
December 29, 2000
Date of Patent:
October 28, 2003
Assignee:
Wyeth
Inventors:
Dan M. Berger, Minu D. Dutia, Frenel F. DeMorin, Diane H. Boschelli, Dennis W. Powell, Hwei-Ru Tsou, Allan Wissner, Nan Zhang, Fei Ye, Biqi Wu
Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
Type:
Grant
Filed:
October 3, 2002
Date of Patent:
October 28, 2003
Assignee:
Wyeth
Inventors:
Michael Gerard Kelly, Lynne Padilla Greenblatt, Gan Zhang, Yvette L. Palmer, Steven Edward Lenicek
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1
Type:
Application
Filed:
December 4, 2002
Publication date:
October 23, 2003
Applicant:
Wyeth
Inventors:
Michael S. Malamas, Robert E. McDevitt, Iwan Gunawan, Eric S. Manas, Michael D. Collini, Heather A. Harris, James C. Keith, Leo M. Albert, C. Richard Lyttle
Abstract: The invention pertains to adjuvant and vaccine compositions of monophosphoryl lipid A, sugar and optionally an amine based surfactant, which when frozen and thawed or lyophilized and reconstituted reform a colloidal suspension having a light transmission of greater than or equal to 88% as measured spectrophotometrically.
Type:
Grant
Filed:
August 30, 2001
Date of Patent:
October 21, 2003
Assignee:
Wyeth Holdings Corporation
Inventors:
Vincent James LaPosta, John Hayward Eldridge
Abstract: Compounds of the formula
in which R, R′, R7-R11, X, n1 and n3 are as defined herein. These compounds are useful as intermediates for preparing pharmaceutical compounds having pharmacological activity as chemical inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes.
Type:
Grant
Filed:
November 22, 2002
Date of Patent:
October 21, 2003
Assignee:
Wyeth
Inventors:
John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
Abstract: This invention comprises methods of inducing or maintaining sphincter continence, or inhibiting or alleviating incontinence, in a mammal comprising administration of 2-(4-Hydroxy phenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl-1H-indol-5-ol
Type:
Grant
Filed:
March 1, 2002
Date of Patent:
October 21, 2003
Assignee:
Wyeth
Inventors:
Simon Nicholas Jenkins, Timothy Michael Argentieri
Abstract: The present invention includes compounds of formula I
wherein A, X, n, Ar1, and Ar2 are defined as set forth herein. These compounds may be used to treat depression. The invention also includes formulations containing these compounds, and methods for making and using compounds of this invention.
Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.
Type:
Application
Filed:
April 1, 2003
Publication date:
October 9, 2003
Applicant:
Wyeth
Inventors:
Gary S. Grubb, James H. Pickar, Ginger D. Constantine, Michael S. Dey
Abstract: The present invention relates, at least in part, to polypeptides which include Bcl-xL binding domains, novel Bcl-xL binding domains of Pablo polypeptides, nucleic acid molecules encoding such polypeptides, and uses thereof. For example, such polypeptides and nucleic acid molecules are useful in modulating apoptosis, particularly in neural cells, as well as in the treatment or prevention of disorders that can benefit from modulation of cell death.
Type:
Application
Filed:
April 4, 2002
Publication date:
October 9, 2003
Applicant:
Wyeth
Inventors:
Robert Mark, Kathleen H. Young, Andrew T. Wood
Abstract: Methods are provided for using IL-12 to treat Kaposi's sarcoma (KS), particularly AIDS-associated KS.
Type:
Application
Filed:
December 2, 2002
Publication date:
October 9, 2003
Applicant:
Wyeth and National Institutes of Health
Inventors:
Robert Yarchoan, James M. Pluda, Kathleen Wyvill, Jill Lietzau, Gene M. Shearer, Ellen Feigal, Giovanna Tosato, Richard Little, Matthew L. Sherman
Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.
Type:
Application
Filed:
April 1, 2003
Publication date:
October 9, 2003
Applicant:
Wyeth
Inventors:
Gary S. Grubb, James H. Pickar, Ginger D. Constantine, Michael S. Dey