Abstract: This invention relates to inhibitors of glycogen synthase kinase-3&bgr;, methods of treating diseases characterized by an excess of Th2 cytokines, and to 3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives of Formula (I):
that are inhibitors of glycogen synthase kinase -3&bgr;, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
July 27, 2001
Date of Patent:
November 12, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Andrew Grupe, Gary Allen Peltz
Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.
Type:
Application
Filed:
October 23, 2001
Publication date:
October 31, 2002
Applicant:
Syntex (U.S.A.) LLC
Inventors:
Michelle F. Browner, David L. Clark, Timothy D. Cushing, Xiaolin Hao, Ronald C. Hawley, Xiao He, Juan C. Jaen, Sharada S. Labadie, Marie-Louise Smith, Francisco X. Talamas, Nigel P.C. Walker, Marc Labelle
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:
September 19, 2000
Date of Patent:
October 29, 2002
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: The invention provides compounds represented by the formula:
wherein R1, R2, R3, R4, and n are as defined in the Summary of the Invention; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts 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:
October 20, 2000
Date of Patent:
September 17, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
James Patrick Dunn, Lawrence Emerson Fisher, David Michael Goldstein, William Harris, Christopher Huw Hill, Ian Edward David Smith, Teresa Rosanne Welch
Abstract: The present invention relates to certain pyrazole derivatives 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:
July 19, 2001
Date of Patent:
September 3, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I:
wherein A is a —CH2—, —C(O)—, —O—, —S—, —S(O)—, or —S(O)2— and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
Type:
Grant
Filed:
December 3, 2001
Date of Patent:
August 13, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Kevin L. McLaren, David Bernard Smith, Jahari Laurant Tracy
Abstract: This invention relates to compounds of Formula (I)
wherein R1-R7, A, Z and n are as described in the Summary of the Invention that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for their preparation.
Type:
Grant
Filed:
December 10, 1999
Date of Patent:
July 30, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Sharon Marie Dankwardt, Harold Edgar Van Wart, Keith Adrian Murray Walker
Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I:
wherein A, R1 and R2 are as defined in the specification; and 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.
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.
Abstract: This invention relates to sulfamides of formula (I)
that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
April 23, 2002
Assignees:
Syntex (U.S.A.) LLC, Agouron Pharmaceuticals, Inc.
Inventors:
Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
Abstract: This invention relates to compounds which are generally alpha1A/B-receptor antagonists and which are represented by Formula I:
wherein the substituents are as defined in the specification; or pharmaceutically acceptable salts, hydrates, or N-oxides thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and a process for their preparation.
Abstract: The present invention relates to certain pyrazole derivatives 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:
May 5, 1999
Date of Patent:
April 23, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
Abstract: This invention relates to compounds which are generally alpha1B-receptor antagonists, and which are represented by Formula (I):
wherein X, Y, and R1 are as defined in the specification, or individual isomers or racemic or non-racemic mixtures of isomers, or 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:
March 8, 2000
Date of Patent:
March 12, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
David Llewellyn Coffen, Michael Patrick Dillon, Anthony P. D. W. Ford, Zhe Li, Timothy James Williams
Abstract: This invention provides processes for the preparation of a compound of Formula I:
Y—C(═O—C(R1)(R2)—CH2—S(O)nR3
wherein:
Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl;
R1 is hydrogen or lower alkyl;
R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group;
R3 is aryl; and
n is 0, 1 or 2.
The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
Type:
Grant
Filed:
June 17, 1999
Date of Patent:
January 29, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
Abstract: This invention relates to certain piperidine quatemrwy salts 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:
November 18, 1999
Date of Patent:
January 29, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Donald Roy Hirschfeld, Denis John Kertesz, David Berard Smith
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 certain cyclic amine derivatives of Formula (I)
that are CCR-3 receptor antagonist, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
November 20, 1998
Date of Patent:
January 15, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
Abstract: DNA encoding for a voltage-gated, TTX-sensitive sodium channel is isolated. Also disclosed are polypeptide products of recombinant expression of these DNA sequences, expression vectors comprising the DNA sequences, and host cells transformed with these expression vectors. Other aspects of this invention are peptides whose sequences are based on the amino acid sequences deduced from these DNA sequences, antibodies specific for such proteins and peptides, procedures for detection and quantitation of such proteins, and nucleic acids related thereto. Another aspect of this invention is the use of this voltage-gated, tetrodotoxin-sensitive sodium channel as a therapeutic target for compounds.
Type:
Grant
Filed:
October 21, 1999
Date of Patent:
January 1, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Stephen Gregory Delgado, Paul Shartzer Dietrich, Linda Marie Fish, Ronald Charles Herman, Lakshmi Sangameswaran
Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor agonists, and which are represented by Formula I:
wherein R1, R2, R3, R4, R5, A, and B are as defined in the specification, and 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:
December 7, 1999
Date of Patent:
January 1, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Daniel Lee Severance
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 14, 1998
Date of Patent:
November 27, 2001
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm