Abstract: The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
Type:
Grant
Filed:
June 28, 2004
Date of Patent:
September 9, 2008
Assignee:
Wyeth
Inventors:
Graham J. Durant, Michael Maillard, Jun Qing Guo
Abstract: This invention provides compounds of Formula I having the structure: wherein: B is alkyl of 1-4 carbons or alkoxy of 1-4 carbons; R1 is aryl or Het optionally substituted with R6; R2 and R3 are each independently, alkyl of 1-4 carbons, CF3, aryl or Het substituted with R6, or R2 and R3 are combined to form a cycloalkyl or heterocyclic ring optionally substituted with alkyl, benzyl, or acyl; R4, and R5 are each independently, hydrogen, halogen, alkyl of 1-4 carbons, CO2R7, SO2NHR7, CONHR7, CN, NO2 or CF3; R6 is hydrogen, halogen, NO2, alkyl of 1-4 carbons, alkoxy of 1-4 carbons, alkylcarbonyloxy of 2-7 carbon atoms, alkylcarbonyl of 2-7 carbon atoms, CF3, or COOH; and R7 is hydrogen, alkyl of 1-4 carbons, or alkylaryl where aryl group is substituted with R6; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
Abstract: The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.
Type:
Grant
Filed:
September 25, 2006
Date of Patent:
September 9, 2008
Assignee:
Wyeth
Inventors:
Michael Sotirios Malamas, James Joseph Erdei, William Floyd Fobare, Dominick Anthony Quagliato, Schuyler Adam Antane, Albert Jean Robichaud
Abstract: Compounds of formula II wherein each R1 and R2 is independently selected from H and —P(O)(R3)(R4), provided that at least one of R1 and R2 is —P(O)(R3)(R4); each R3 and R4 is independently selected from the group consisting of H, —OH, C1-C6 alkyl and C1-C6 alkoxy; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising a compound of formula II, and methods of administering such compounds and compositions.
Type:
Application
Filed:
February 20, 2008
Publication date:
September 4, 2008
Applicant:
WYETH
Inventors:
Mahdi B. FAWZI, Parimal R. DESAI, Tianmin ZHU
Abstract: A genetic deletion mutant live E. coli vaccine suitable for mass application to poultry, including chickens, is provided. Also provided is a safe and effective method to protect poultry against the ravages of Escherichia coli bacillosis infection and disease in which a live mutant aroA-gene deleted E. coli immunogen is administered to chickens, turkeys and the like via mass application routes such as coarse sprays and drinking water.
Type:
Application
Filed:
March 7, 2008
Publication date:
September 4, 2008
Applicant:
Wyeth
Inventors:
Henry H. FAN, Mahesh Kumar, Roberto Marcello La Ragione, Martin John Woodward
Abstract: Mutant cholera holotoxins comprising a cholera toxin subunit A having single amino acid substitutions in the amino acid positions 16 or 72 or a double amino acid substitution in the amino acid positions 16 and 68 or 68 and 72 have reduced toxicity compared to the wild-type cholera holotoxin. The mutant cholera holotoxins are useful as adjuvants in immunogenic compositions to enhance the immune response in a vertebrate host to a selected antigen from a pathogenic bacterium, virus, fungus, or parasite, a cancer cell, a tumor cell, an allergen, or a self-molecule.
Type:
Application
Filed:
October 22, 2007
Publication date:
September 4, 2008
Applicants:
Wyeth Holdings Corporation, The Regents of the University of Colorado, A Body Corporate Health Science Center
Inventors:
Bruce A. Green, Randall K. Holmes, Michael G. Jobling, Duzhang Zhu
Abstract: This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2— cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
Type:
Application
Filed:
April 7, 2008
Publication date:
September 4, 2008
Applicant:
Wyeth
Inventors:
Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, David Zenan Li, Lee D. Jennings, David LeRoy Crandall
Abstract: A drug and drug delivery system may be utilized in the treatment of vascular disease. A local delivery system is coated with rapamycin or other suitable drug, agent or compound and delivered intraluminally for the treatment and prevention of neointimal hyperplasia following percutaneous transluminal coronary angiography. The local delivery of the drugs or agents provides for increased effectiveness and lower systemic toxicity.
Abstract: The present invention relates to crystalline forms of 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-N-[(1S)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine salts; processes for the production thereof; pharmaceutical compositions thereof; and methods for inhibiting tumor growth therewith.
Type:
Grant
Filed:
May 19, 2006
Date of Patent:
September 2, 2008
Assignee:
Wyeth Holdings Corporation
Inventors:
Fang Fang Qi, Mannching Sherry Ku, Yanzhong Wu, David M. Blum
Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
Type:
Grant
Filed:
December 1, 2004
Date of Patent:
September 2, 2008
Assignee:
Wyeth
Inventors:
Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
Abstract: The invention relates to methods of treating a disease or condition, wherein expression or activity of soluble CLCA1 is up-regulated, by administering inhibitors of soluble CLCA1. The invention also relates to methods of isolating soluble CLCA1 from a bodily fluid.
Type:
Grant
Filed:
May 27, 2004
Date of Patent:
September 2, 2008
Assignee:
Wyeth
Inventors:
Andrew J. Long, Clive R. Wood, Michael Bowman, Samuel J. Goldman, Joseph P. Sypek
Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
October 12, 2004
Date of Patent:
September 2, 2008
Assignee:
Wyeth
Inventors:
Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
Abstract: The present invention provides processes and intermediates for the preparation of aminoethoxybenzyl alcohols of Formula I useful in the production of pharmaceutically useful compounds.
Type:
Application
Filed:
April 17, 2008
Publication date:
August 28, 2008
Applicant:
WYETH
Inventors:
Pietro ALLEGRINI, Giuseppe BARRECA, Giorgio SORIATO
Abstract: The invention relates to methods for producing storage stable virus compositions. In certain embodiments, the invention relates to one or more formulations and process steps which result in storage stable virus compositions, wherein the composition is storage stable as a lyophilized solid composition or a frozen liquid composition.
Type:
Application
Filed:
December 10, 2004
Publication date:
August 28, 2008
Applicant:
WYETH
Inventors:
Jee Loon Look, Vladimir G. Frolov, Nandini Konar
Abstract: Adatanserin is useful for treating neurodegenerative disorders, chronic pain, and other disorders associated with dysfunctional glutamate release. Methods of treating the same comprise administering a therapeutically effective amount of adatanserin or a pharmaceutical salt thereof, to a patient in need of said treatment.
Type:
Application
Filed:
February 26, 2008
Publication date:
August 28, 2008
Applicant:
Wyeth
Inventors:
Magid A. Abou-Gharbia, James E. Barrett, Wayne E. Childers, John A. Moyer
Abstract: Compounds of the formula: wherein: n is an integer from 1-3; X is N, CH, provided that when X is N, n is 2 or 3; R is alkyl of 1 to 3 carbon atoms; R1 is 2,4-diCl, 5-OMe; 2,4-diCl; 3,4,5-tri-OMe; 2-Cl, 5-OMe; 2-Me, 5-OMe; 2,4-di-Me; 2,4-diMe-5-OMe, 2,4-diCl, 5-OEt; R2 is alkyl of 1 to 2 carbon atoms, and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
November 3, 2004
Date of Patent:
August 26, 2008
Assignee:
Wyeth
Inventors:
Frank Boschelli, Kim T. Arndt, Jennifer M. Golas
Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.
Type:
Grant
Filed:
June 29, 2006
Date of Patent:
August 26, 2008
Assignee:
Wyeth
Inventors:
Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
Abstract: The invention provides isolated polypeptide and nucleic acid sequences derived from Staphylococcus epidermidis that are useful in diagnosis and therapy of pathological conditions; antibodies against the polypeptides; and methods for the production of the polypeptides. The invention also provides methods for the detection, prevention and treatment of pathological conditions resulting from bacterial infection.