Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II:
wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.
Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.
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:
August 1, 2003
Date of Patent:
November 16, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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 current invention is directed to methods of treating or preventing emphysema, pharmaceutical compositions suitable for the treatment or prevention of emphysema and methods for delivering formulations into the lung of a mammal suffering from emphysema.
More generally, the invention encompasses the use of 13-cis-retinoic acid to treat or prevent certain chronic obstructive airway disorders, particularly chronic obstructive pulmonary disease including chronic bronchitis, emphysema and asthma in mammals, especially humans that smoke or smoked cigarettes. In another aspect, the present invention encompasses the use of pharmaceutical compositions of 13-cis-retinoic acid to treat emphysema. Moreover, the current invention encompasses the use of electrohydrodynamic aerosol devices, aerosol devices and nebulizers to deliver formulations of 13-cis-retinoic acid into the lung of a mammal suffering from emphysema. The invention also encompasses the systemic use as well as the local use of 13-cis-retinoic acid.
Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I:
wherein R3 is SO2—Ar, Ar is aryl or heteroaryl; and R1, R2, R4 and R5 are as defined herein; 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 methods of preparation thereof.
Type:
Grant
Filed:
June 14, 2002
Date of Patent:
September 14, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Andrew John Briggs, Robin Douglas Clark, Ralph New Harris, III, David Bruce Repke, Douglas Leslie Wren
Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
October 9, 2002
Date of Patent:
September 7, 2004
Assignee:
Syntex (U.S.A.) LLC.
Inventors:
Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I:
wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; 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 methods of preparation thereof.
Type:
Grant
Filed:
June 6, 2002
Date of Patent:
September 7, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Colin Charles Beard, Robin Douglas Clark, Lawrence Emerson Fisher, Ralph New Harris, III, David Bruce Repke, David George Putman
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 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: 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: 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 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 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