Abstract: A polyketide synthase complex composed of polyketide synthase with 15 total modules, a non-ribosomal peptide synthetase with 1 module, and a cytochrome P450 hydroxylase is described. Also provided are novel Streptomyces species and methods of modified Streptomyces species. Further described are novel compounds, 36-ketomeridamycin, C9-deoxomeridamycin, and C9-deoxoprolylmeridamcyin and uses thereof.
Type:
Application
Filed:
July 25, 2008
Publication date:
April 23, 2009
Applicant:
Wyeth
Inventors:
Min He, John Hucul, Bradley Arnold Haltli, Melissa M. Wagenaar, Edmund Idris Graziani, Mia Summers, Kerry Kulowski, Kevin Pong, Xidong Feng
Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
Type:
Application
Filed:
December 9, 2008
Publication date:
April 23, 2009
Applicant:
Wyeth
Inventors:
Kevin Liu, Albert Jean Robichaud, Jennifer Rebecca Lo, Hassan Mahmoud Elokdah
Abstract: This disclosure provides antibodies and antigen-binding fragments that can act as agonists and/or antagonists of PD-1 (Programmed Death 1), thereby modulating immune responses in general, and those mediated by TcR and CD28, in particular. The disclosed compositions and methods may be used for example, in treating autoimmune diseases, inflammatory disorders, allergies, transplant rejection, cancer, and other immune system disorders.
Type:
Grant
Filed:
December 22, 2003
Date of Patent:
April 21, 2009
Assignees:
MedImmune Limited, Wyeth
Inventors:
Mary Collins, Clive R. Wood, Beatriz M. Carreno, Deborah Luxenberg, Jason Jussif, Laura L. Carter, Frances K. Bennett, Viia Valge-Archer, John Andrews, Caroline Russell
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:
June 21, 2006
Date of Patent:
April 21, 2009
Assignee:
Wyeth
Inventors:
Douglas C. Harnish, Marshall S. Scicchitano, Sotirios K. Karathanasis, Chu-Lai Hsiao
Abstract: There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.
Type:
Grant
Filed:
December 8, 2004
Date of Patent:
April 21, 2009
Assignee:
Wyeth
Inventors:
Yanzhong Wu, Arkadiy Rubezhov, Jean Schmid, Jay Thomas Afragola
Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
Type:
Grant
Filed:
February 23, 2005
Date of Patent:
April 21, 2009
Assignee:
Wyeth
Inventors:
Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Bruce C. Follows, Steven J. Kirincich, Michael J. Smith, Jun-Jun Wu, Kenneth W. Foreman, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam
Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, 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:
Application
Filed:
December 15, 2008
Publication date:
April 16, 2009
Applicant:
Wyeth
Inventors:
Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
Abstract: The present invention discloses methods for activating Caspase 9 in such a way that it can be used in assays to discover modulators of Caspase 9.
Abstract: Bioadhesive films for delivery of active agent to the mucosa are disclosed. Particularly, bioadhesive films for treating the vaginal mucosa are disclosed.
Abstract: The invention relates to thienopyrimidine and pyrazolopyrimidine compounds of the Formulas (Ia) and (IIa), or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein compositions comprising the compounds, and methods for making and using the compounds.
Type:
Application
Filed:
October 15, 2008
Publication date:
April 16, 2009
Applicant:
Wyeth
Inventors:
Arie Zask, Joshua Aaron Kaplan, Jeroen Cunera Verheijen, Kevin J. Curran, David James Richard, Semiramis Ayral-Kaloustian
Abstract: Methods of preparing and purifying 9-nitrominocycline and 9-aminominocycline and salts thereof used in the process of making tigecycline, are disclosed. In one embodiment, the invention is directed to a method of preparing the compound of formula 1 or a pharmaceutically acceptable salt thereof, comprising: (a) reacting nitric acid with the compound of formula 2, or a salt thereof, to produce a reaction mixture comprising an intermediate; and (b) further reacting the intermediate to form the compound of formula 1, wherein the intermediate is isolated from the reaction mixture, the method further comprising sparging with an inert gas prior to step (a).
Type:
Application
Filed:
October 15, 2008
Publication date:
April 16, 2009
Applicant:
Wyeth
Inventors:
Michel Bernatchez, Warren Chew, Sylvain Daigneault, Ernest Palus, Mahmoud Mirmehrabi, Luc Bouchard
Abstract: The present invention provides novel isolated BFLP0169 polynucleotides and polypeptides encoded by the BFLP0169 polynucleotides. Also provided are the antibodies that immunospecifically bind to a BFLP0169 polypeptide or any derivative (including fusion derivative), variant, mutant or fragment of the BFLP0169 polypeptide, polynucleotide or antibody. The invention additionally provides methods in which the BFLP0169 polypeptide, polynucleotide and antibody are utilized in the detection and treatment of a broad range of pathological states, as well as to other uses.
Type:
Application
Filed:
September 23, 2008
Publication date:
April 16, 2009
Applicants:
Wyeth, Genetics Institute, LLC
Inventors:
Margot O'Toole, William Martin Mounts, Negin Shojaee
Abstract: The present invention relates to a color method and multivariate model whose color measurements of reconstituted tigecycline for injection is predictive of appearance and oxidative degradation wherein said method is a means of detecting the presence of a degradant which forms when tigecycline is contacted with oxygen.
Type:
Application
Filed:
October 8, 2008
Publication date:
April 16, 2009
Applicant:
Wyeth
Inventors:
Jean Marie Akin, Peter John Larkin, Tianmin Zhu, Jan Szeliga
Abstract: The present invention is directed to a process for preparing compounds of formula (I): wherein A, R1-R3, X, s, t, u, m and Z are defined herein, comprising the step of reacting a reagent of formula (II): in the presence of Pd(O) metal with a compound of formula (III): or salts thereof. Another aspect of this invention is a method of preparing compounds of formula (VI).
Type:
Application
Filed:
January 23, 2007
Publication date:
April 16, 2009
Applicant:
WYETH
Inventors:
Yanong Daniel Wang, Dan Maarten Berger, Minu Dutia, Middleton Brawner Floyd
Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
Type:
Application
Filed:
December 17, 2008
Publication date:
April 16, 2009
Applicant:
Wyeth
Inventors:
Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
Abstract: The present invention provides a purified preparation containing a polynucleic acid encoding at least one polypeptide selected from the group consisting of proteins encoded by one or more open reading frames (ORF's) of an Iowa strain of porcine reproductive and respiratory syndrome virus (PRRSV), proteins at least 80% but less than 100% homologous with those encoded by one or more of ORF 2, ORF 3, ORF 4 and ORF 5 of an Iowa strain of PRRSV, proteins at least 97% but less than 100% homologous with proteins encoded by one or both of ORF 6 and ORF 7 of an Iowa strain of PRRSV, antigenic regions of such proteins which are at least 5 amino acids in length and which effectively stimulate immunological protection in a porcine host against a subsequent challenge with a PRRSV isolate, and combinations thereof, in which amino acids non-essential for antigenicity may be conservatively substituted.
Type:
Grant
Filed:
March 8, 2006
Date of Patent:
April 14, 2009
Assignees:
Iowa State University Research Foundation, Inc., Wyeth Holding Corporation
Inventors:
Prem S. Paul, Xiang-Jin Meng, Patrick Halbur, Igor Morozov, Melissa A. Lum
Abstract: Disclosed herein are nucleic acid and polypeptide sequences of a novel rat voltage-gated potassium channel, KCNQ5. Also disclosed herein are methods related to the use of the aforementioned potassium channel.
Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, 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:
March 28, 2005
Date of Patent:
April 14, 2009
Assignee:
Wyeth
Inventors:
Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.
Type:
Application
Filed:
December 10, 2008
Publication date:
April 9, 2009
Applicant:
Wyeth
Inventors:
Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, 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:
Application
Filed:
December 15, 2008
Publication date:
April 9, 2009
Applicant:
WYETH
Inventors:
Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye