Abstract: The present invention relates to processes for the preparation of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzoxazol-5-ol. The processes include the vinylation of a substituted benzoxazole compound having an appropriate substitutable moiety.
Abstract: Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
May 7, 2002
Date of Patent:
September 5, 2006
Assignees:
Elan Pharmaceuticals, Inc., Wyeth
Inventors:
Darren B. Dressen, Anthony Kreft, Dennis Kubrak, Charles William Mann, Michael A. Pleiss, Gary Paul Stack, Eugene D. Thorsett
Abstract: This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.
Type:
Grant
Filed:
November 22, 2002
Date of Patent:
September 5, 2006
Assignee:
Wyeth
Inventors:
John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
Abstract: Novel proteins which bind human ?-amyloid peptide, polynucleotides which encode these proteins, and methods for producing these proteins are provided. Diagnostic, therapeutic, and screening methods employing the polynucleotides and polypeptides of the present invention are also provided. Transgenic animals and knockout animals are also provided.
Type:
Grant
Filed:
July 16, 2004
Date of Patent:
September 5, 2006
Assignee:
Wyeth
Inventors:
Bradley A. Ozenberger, Jonathan A. Bard, Eileen M. Kajkowski, Jack S. Jacobsen, Stephen G. Walker, Heidi Sofia, David Howland
Abstract: Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these 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.
Abstract: The addition of buffer to a harvest stream during diafiltration can cause increased turbidity and have other undesirable effects including limiting product recovery. Methods and compositions related to the use of a non-ionic surfactant are provided for improving diafiltration.
Abstract: This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I): where R1 is H, alkyl or phenylalkyl; R2 is H, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together as Z are —CH2CH2—, —CH2(CR6)(R7)CH2— or —CH2C(R8)(R9)—C(R10)(R11)CH2—, where R6, R8 and R10 are, independently, H, alkyl or hydroxyl and R7, R9 and R11 are, independently, H or alkyl; A is alkylene or alkenylene; X is CO2R3, P(O)(OR4)(OR5), 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl in which R3, R4 and R5 are, independently, H or alkyl, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions for treating pain containing a pain treating effective amount of the compound of formula (I).
Type:
Grant
Filed:
October 9, 2002
Date of Patent:
August 29, 2006
Assignee:
Wyeth
Inventors:
Michael Richard Brandt, Margaret Maria Zaleska, John Allen Moyer
Abstract: This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1–6 carbon atoms; R? is hydrogen, alkyl of 1–6 carbon atoms, acyl of 2–7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1–6 carbon atoms, alkoxy of 1–6 carbon atoms, halogen, trifluoroalkyl, or trifluoroalkoxy of 1–6 carbon atoms; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1–6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least two of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.
Type:
Grant
Filed:
December 1, 2003
Date of Patent:
August 29, 2006
Assignee:
Wyeth
Inventors:
Annmarie Louise Sabb, Gregory Scott Welmaker, James Albert Nelson
Abstract: Pharmaceutical compositions and methods of use in regulation of mammalian bone forming activities of SFRPs (secreted frizzled-related proteins) are disclosed. SFRPs are secreted receptors for Wnts that are important polypeptide growth factors that are known to regulate fundamental biological processes like tissue polarity, embryonic development and tumorigenesis. A SFRP was isolated in human osteoblast cells and identified as SFRP-1 (also known as SARP-2) and shown to be regulated by osteogenic agents in the HOB cells in a differentiation selective manner modulating the life of osteoblasts/preosteocytes.
Abstract: The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.
Abstract: The present invention is directed to novel methods for diagnosis and prognosis of Systemic lupus erythematosus by identifying differentially expressed genes. Moreover, the present invention is also directed to methods that can be used to screen test compounds and therapies for the ability to inhibit systemic lupus erythematosus. Additionally, methods and molecule targets (genes and their products) for therapeutic intervention in systemic lupus erythematosus are described.
Abstract: The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.
Abstract: The present invention provides a safe and effective vaccine composition which comprises: an effective immunizing amount of an inactivated Ehrlichia canis bacterin; a pharmacologically acceptable carrier; and an immunogenically stimulating amount of an adjuvant system consisting essentially of an antibody response inducing agent and a cell-mediated immunity response inducing agent. The present invention also provides a method for the prevention or amelioration of canine ehrlichiosis in dogs.
Type:
Application
Filed:
April 20, 2006
Publication date:
August 24, 2006
Applicant:
Wyeth
Inventors:
Liangbiao Hu, Thomas Hess, Yu-Wei Chiang, Hsien-Jue Chu
Abstract: The present invention generally relates to the fields of molecular biology, clinical bacteriology and protein folding. More particularly, the invention relates to methods for recombinantly expressing a soluble mature Streptococcus pyogenesexotoxin B (SpeB) polypeptide in a host cell.
Type:
Application
Filed:
July 7, 2004
Publication date:
August 24, 2006
Applicant:
Wyeth Holdings corporation
Inventors:
Laurie Winter, Yury Matsuka, Elzabeth Anderson, Stephen Olmsted
Abstract: The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.
Abstract: A multi-composition stick product, such as a lip balm, sun screen, deodorant, or glue stick. The multi-composition stick product including a stick composition molded in the container so as to contact the walls thereof and be advanceable or ejected therefrom. The stick composition includes a first composition and a second composition. The first and second compositions differ in at least one component, such as a medicament, colorant, fragrance, flavorant, sunscreen, preservative, conditioner, moisturizer, emollient, or surfactant. Furthermore the first and second compositions are arranged in a predetermined non-random pattern that is reproducible. Also described is the method and apparatus for manufacturing the multi-composition stick product.
Type:
Application
Filed:
May 5, 2006
Publication date:
August 24, 2006
Applicant:
Wyeth
Inventors:
Jee Look, Paul Cooper, Khawla Abu-Izza, Joyce Wilson, Krishna Raman, Vincent Li
Abstract: The present invention relates to Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists.
Type:
Application
Filed:
February 24, 2006
Publication date:
August 24, 2006
Applicant:
WYETH
Inventors:
Abdolsamad Tadayon, Jacqueline Lunetta, Kiomars Karami, Zheng Wang
Abstract: The present invention relates to an assay system and method for testing compounds for their ability to regulate the hepatic lipase (HL) promoter. In particular, the invention relates to the identification of estrogen receptor ligands having this activity. Compounds that inhibit HL promoter activity are useful as leads, or on their own, to develop therapeutics in the prevention of heart disease.
Type:
Grant
Filed:
August 8, 2001
Date of Patent:
August 22, 2006
Assignee:
Wyeth
Inventors:
Douglas C. Harnish, Marshall S. Scicchitano, Sotirios K. Karathanasis, Chu-Lai Hsiao
Abstract: The present invention provides a substituted thienyl or furyl acylguanidine compound of formula I The present invention also provides methods for the inhibition of ?-secretase (BACE) and for the treatment of ?-amyloid deposits and neurofibrillary tangles.
Abstract: The present invention provides processes for the preparation of substituted naphthylindole derivatives that can be used as inhibitors of plasminogen activator inhibitor-1(PAI-1). In certain embodiments of the invention, the processes involve reactions that include one or more of an Oppenauer oxidation, a Fischer indole synthesis, a methyl ether cleavage, or coupling a substituted methyltetrazole with a substituted naphthol.
Type:
Application
Filed:
January 25, 2006
Publication date:
August 17, 2006
Applicant:
Wyeth
Inventors:
Vladimir Dragan, John Potoski, Wayne McMahon, Jean Helom, Xinxu Shi