Abstract: The present invention relates to the use of nucleoside derivatives of formula I
wherein B signifies a 9-purinyl residue B1 of formula
or a 1-pyrimidyl residue B2 of formula
wherein the symbols are as defined in the specification,
and of pharmaceutically acceptable salts thereof; for the treatment of diseases mediated by the Hepatitis C Virus (HCV), for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
June 11, 2002
Date of Patent:
August 31, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
Type:
Grant
Filed:
October 1, 2001
Date of Patent:
August 17, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
Abstract: The present invention provides methods of preventing or treating West Nile virus as well as infections caused by other viruses of the Flaviviridae family in animals comprising administering to the animal a tehrapeutically effective amount of a compound of formula I either as alone or in combination with immunomodulators.
Abstract: This invention relates to certain cyclic amine derivatives of Formula (I)
that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
August 29, 2001
Date of Patent:
August 3, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Donald Roy Hirschfeld, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
Abstract: The present invention provides compounds of the formula:
a prodrug or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and Ar1 are those defined herein, and methods for preparation and uses thereof.
Type:
Grant
Filed:
December 10, 2002
Date of Patent:
June 22, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Humberto Bartolome Arzeno, Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
Abstract: A method for identifying compounds that can be useful for producing analgesia is disclosed. In particular, the method involves providing preparation of a cell, that expresses an alpha1B adrenergic receptor, combining a test compound with the cell preparation, measuring the effect of the test compound on the alpha1B receptor activity, and evaluating the compound thus identified for analgesic activity.
Type:
Grant
Filed:
March 8, 2000
Date of Patent:
May 11, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Anthony P. D. W. Ford, Timothy James Williams, Kathleen Ruth Gogas, Lupita O. Jacobson
Abstract: The present invention provides compounds of the Formula I and II:
wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
Type:
Grant
Filed:
February 11, 2002
Date of Patent:
February 24, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl
Abstract: The present invention provides an aminopyrrole compound of the formula:
a prodrug, individual isomer, a mixture of isomers or a pharmaceutically acceptable salt thereof, where R1, R2, Ar1 and Ar2 are those defined herein. The present invention also provides methods of using and preparing the aminopyrrole compounds of Formula I.
Type:
Grant
Filed:
August 29, 2002
Date of Patent:
February 24, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
David Michael Goldstein, David Mark Rotstein
Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I:
where:
R1 is a group represented by formula (A), (B) or (C);
and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.
Type:
Grant
Filed:
April 29, 2003
Date of Patent:
February 17, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I:
wherein:
R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl;
R4 is —COOH or tetrazolyl;
A, B, m, n, and r are as defined in the specification;
or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.
Type:
Grant
Filed:
March 14, 2001
Date of Patent:
February 17, 2004
Assignee:
Syntex (U.S.A) LLC
Inventors:
Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
Abstract: This invention relates to certain cyclic amine derivatives of Formula (I)
that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
September 26, 2001
Date of Patent:
January 27, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
Type:
Grant
Filed:
May 22, 2001
Date of Patent:
December 23, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
Abstract: Human aggrecanase and polypeptides related thereto, as well as nucleic acid compositions encoding the same, are provided. The subject polypeptides and nucleic acid compositions find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications. Also provided are methods of inhibiting aggrecanase activity in a host and methods of treating disease conditions associated with aggrecanase activity, e.g. rheumatoid arthritis, osteo-arthritis, infectious arthritis, gouty arthritis, psoriatic arthritis, spondolysis, sports injury, joint trauma, pulmonary disease, fibrosis, and the like.
Type:
Grant
Filed:
May 9, 2000
Date of Patent:
November 18, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
John David Allard, Renu Anand Ileller, Paul Klonowski, Harold Edgar VanWart
Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein X, Y, and Z are O, S, or NR4, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
Type:
Grant
Filed:
November 6, 2002
Date of Patent:
November 11, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
Abstract: Alkylamino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives are provided which are useful as inhibitors of p38, along with a process for their manufacture and pharmaceutical preparations containing them.
Type:
Grant
Filed:
October 20, 2000
Date of Patent:
November 4, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
James Patrick Dunn, David Michael Goldstein, William Harris, Ian Edward David Smith, Teresa Rosanne Welch
Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein R1, R2, R3 and R4 are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.
Abstract: The present invention relates to compounds of Formula (I)
that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Type:
Grant
Filed:
April 19, 2001
Date of Patent:
October 7, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
Abstract: This invention relates to compounds which are generally muscarinic receptor antagonists and which are represented by Formula I:
wherein p, R1, R2, R3 and A are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.
Type:
Grant
Filed:
December 2, 2002
Date of Patent:
September 30, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Christine E. Brotherton-Pleiss, Ann Marie Madera, Robert James Weikert