Patents Assigned to Wyeth
  • Publication number: 20060183917
    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
  • Publication number: 20060183790
    Abstract: The present invention provides an azolylacylquanidine 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: Application
    Filed: February 13, 2006
    Publication date: August 17, 2006
    Applicant: Wyeth
    Inventors: Derek Cole, Eric Manas, Lee Jennings, Frank Lovering, Joseph Stock, William Moore, John Ellingboe, Jeffrey Condon, Mohani Sukhdeo, Ping Zhou, JunJun Wu, Koi Morris
  • Publication number: 20060183792
    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.
    Type: Application
    Filed: February 13, 2006
    Publication date: August 17, 2006
    Applicant: Wyeth
    Inventors: William Fobare, William Solvibile
  • Publication number: 20060183766
    Abstract: A CCI-779 oral dosage form is provided in which, after oral administration to a subject, the CCI-779 has a whole blood peak concentration (Cmax) of 5.4±1.8 ng/mL and an area under the curve (AUC) of about 66±about 22 ng-hr/ml and the sirolimus has a Cmax of 18.7±9.6 ng/mL and an AUC of about 600±about 228 ng-hr/ml, for a 25 mg unit dose of CCI-779. Another CCI-779 oral dosage form is provided which, after oral administration thereof to a subject, the CCI-779 has a Cmax of 5.7±1.7 ng/mL and an AUC of about 60±about 20 ng-hr/ml and the sirolimus has a Cmax of 17.1±8.1 ng/mL and an AUC of about 548±about 187 ng-hr/ml in whole blood, for a 25 mg unit dose of CCI-779. Products containing these oral dosage forms, and methods of use thereof, are also described.
    Type: Application
    Filed: February 13, 2006
    Publication date: August 17, 2006
    Applicant: Wyeth
    Inventors: Joseph Boni, Muhammad Ashraf, Eric Benjamin
  • Publication number: 20060183943
    Abstract: The present invention provides terphenyl guanidine compounds 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: Application
    Filed: February 13, 2006
    Publication date: August 17, 2006
    Applicant: Wyeth
    Inventor: Baihua Hu
  • Publication number: 20060183734
    Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.
    Type: Application
    Filed: April 11, 2006
    Publication date: August 17, 2006
    Applicant: Wyeth
    Inventors: Amedeo Failli, Jay Shumsky, Thomas Caggiano, John Dusza, Kevin Memoli
  • Patent number: 7091234
    Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: August 15, 2006
    Assignee: Wyeth
    Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
  • Patent number: 7091349
    Abstract: A process for formation of N-aryl piperazines with chiral N?-1-[benzoyl(2-pyridyl)amino]-2-propane side-chains having the structure shown in formula below, and for making intermediate compounds therefor. In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N, N? disubstituted piperazines act on the central nervous system at 5HT receptors.
    Type: Grant
    Filed: February 18, 2004
    Date of Patent: August 15, 2006
    Assignee: Wyeth
    Inventors: Gregg Brian Feigelson, Joseph Zeldis, Ivo Ladislav Jirkovsky
  • Publication number: 20060178412
    Abstract: Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
    Type: Application
    Filed: March 15, 2006
    Publication date: August 10, 2006
    Applicant: Wyeth
    Inventor: Lee Jennings
  • Publication number: 20060178392
    Abstract: The present invention provides CCI-779 polymorph Form II. This invention also provides processes for preparing CCI-779 polymorph Form II and pharmaceutical compositions including CCI-779 polymorph Form II.
    Type: Application
    Filed: January 25, 2006
    Publication date: August 10, 2006
    Applicant: Wyeth
    Inventor: Subodh Deshmukh
  • Publication number: 20060173049
    Abstract: The present invention provides an amino-pyridine 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: Application
    Filed: January 31, 2006
    Publication date: August 3, 2006
    Applicant: Wyeth
    Inventors: Michael Malamas, William Fobare, William Solvibile, Frank Lovering, Jeffrey Condon, Albert Robichaud
  • Publication number: 20060171960
    Abstract: The present invention encompasses methods and compositions both for providing protection against disease in an animal and for inducing increased intake of an orally administered vaccine by an animal. The methods of the invention are directed to admixing a bacterial or viral antigen with a water soluble palatable flavorant, further admixing the antigen and flavorant mixture with a water soluble vehicle for oral administration of the vaccine to an animal in order to provide protection against disease associated with infection by the admixed antigen and to induce the increased intake of the vaccine with the flavorant. The present invention thus encompasses methods and compositions for the oral vaccination of healthy animals through drinking water or syrups as an aid in the prevention of disease.
    Type: Application
    Filed: December 29, 2005
    Publication date: August 3, 2006
    Applicant: Wyeth
    Inventors: Hsien-Jue Chu, Wumin Li
  • Patent number: 7084168
    Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: August 1, 2006
    Assignee: Wyeth
    Inventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H.W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 7084276
    Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, R4, R5, and R6 are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Grant
    Filed: May 13, 2004
    Date of Patent: August 1, 2006
    Assignee: Wyeth
    Inventors: An Thien Vu, Stephen Todd Cohn, Richard Eric Mewshaw
  • Publication number: 20060167059
    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: March 29, 2006
    Publication date: July 27, 2006
    Applicant: Wyeth
    Inventors: Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, David Zenan Li, Lee Jennings, David LeRoy Crandall
  • Patent number: 7081448
    Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1, R2, R3, R4, R5, R6, R7, and R8 are each, independently, acyl of 2–7 carbon atoms, haloacyl of 2–7 carbon atoms, nitroacyl of 2–7 carbon atoms, cyanoacyl of 2–7 carbon atoms, trifluoromethylacyl of 3–8 carbon atoms, benzoyl, or —SO3H; R9 is hydrogen, CN, NO2, halo, CF3, alkyl of 1–6 carbon atoms, or alkoxy of 1–6 carbon atoms; R10 is hydrogen, —NO2, —NHR11, —NHR13, —N(R13)2, —NCH3R13, —NHCO2alkyl, wherein the alkyl moiety contains 1–6 carbon atoms, alkylsulfonamide of 1 to 4 carbon atoms, Z is O or S; R11 is an ?-amino acid in which the ? carboxyl group forms an amide with the nitrogen of R10, wherein if said amino acid is glutamic acid or aspartic acid, the non-? carboxylic acid is an alkyl ester in which the alkyl moiety contains from 1–6 carbon atoms; R12 is hydrogen, CN, NO2, halo, CF3, alkyl of 1–6 carbon atoms, alkoxy of 1–6 carbon atoms, acyl of 2–7 carbon atoms, or benzoyl;
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: July 25, 2006
    Assignee: Wyeth
    Inventor: Scott C Mayer
  • Patent number: 7081457
    Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: July 25, 2006
    Assignees: Wyeth, Ligand Pharmaceuticals, Inc.
    Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
  • Publication number: 20060160892
    Abstract: This invention provides methods and pharmaceutical compositions for treating, inhibiting or preventing hyperactive gastric motility in a mammal utilizing agonists of KCNQ potassium channels, including KCNQ2, KCNQ3, KCNQ4 and KCNQ5 potassium channels, alone or in combination. The hyperactive gastric motility may be associated with maladies including, colitis, irritable bowel syndrome and Crohn's disease. Compounds useful in these methods include the 1,2,4-triamino-benzene derivatives described in U.S. Pat. No. 5,384,330 (Dieter et al.) and the substituted 3-phenyl oxindole compounds described in U.S. Pat. No. 5,565,483 (Hewawasam et al.). Among the preferred compounds of this invention is N-[2-amino-4-(4-fluorobenzylamino)-phenyl]carbamic acid ethyl ester, also referred to as retigabine.
    Type: Application
    Filed: March 20, 2006
    Publication date: July 20, 2006
    Applicant: Wyeth
    Inventor: Thomas Argentieri
  • Publication number: 20060160828
    Abstract: The present invention provides an amino-imidazolone compound of formula I Also provided are compositions and methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.
    Type: Application
    Filed: January 13, 2006
    Publication date: July 20, 2006
    Applicant: Wyeth
    Inventors: Michael Malamas, James Erdei, Iwan Gunawan, Pawel Nowak, Boyd Harrison
  • Publication number: 20060159655
    Abstract: Methods and compositions for modulating interleukin-21 (IL-21)/IL-21 receptor (MU-1) activity using agonists of IL-21 or IL-21 receptor (“IL-21R” or “MU-1”), are disclosed. IL-21/IL-21R agonists can be used by themselves or in combination with anti-inflammatory agents to treat, e.g., ameliorate, symptoms associated with immunological disorders of the nervous system, e.g., multiple sclerosis.
    Type: Application
    Filed: March 22, 2004
    Publication date: July 20, 2006
    Applicant: Wyeth
    Inventors: Mary Collins, Elaine Chin, Mayra Senices, Deborah Young