Patents Assigned to Syntex (U.S.A.)
  • Sulfonamide hydroxamates
    Patent number: 6492394
    Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: December 10, 2002
    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
  • Human peripheral nerve, tetrodotoxin-resistant sodium channel &agr;-subunit polypeptide
    Patent number: 6479259
    Abstract: The present invention relates to a voltage-gated sodium channel present in peripheral nerve tissue that is tetrodotoxin-resistant. One aspect of the present invention is purified and isolated DNA encoding this sodium channel. Another aspect of the present invention is the recombinant protein expressed by this DNA, expression vectors comprising the DNA sequence, and host cells transformed with these expression vectors. Another aspect of this invention is the use of this voltage-gated, tetrodotoxin-resistant sodium channel as a therapeutic target for compounds to treat disorders of the peripheral nervous system.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: November 12, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Ronald Herman, Stephen Gregory Delgado, Linda Marie Fish, Lakshmi Sangameswaran, Douglas Kenneth Rabert
  • 3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3&bgr;
    Patent number: 6479490
    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
  • p38 MAP kinase inhibitors
    Patent number: 6479507
    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: November 12, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
  • Antiinflammation agents
    Publication number: 20020161004
    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
  • 2-(substituted-phenyl)amino-imidazoline derivatives
    Patent number: 6472536
    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
  • Heteroalkylamino-substituted bicyclic nitrogen heterocycles
    Patent number: 6451804
    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
  • Pyrazole derivatives P38 MAP kinase inhibitors
    Patent number: 6444696
    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
  • Benzofuran and benzothiophene derivatives as anti-inflammatory agents
    Patent number: 6433005
    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
  • Peptidic procollagen C-proteinase inhibitors
    Patent number: 6426402
    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
  • Processes for preparing 3-arylsulfur hydroxamic acids
    Patent number: 6420573
    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: November 9, 2001
    Date of Patent: July 16, 2002
    Assignee: Syntex (U.S.A.) LLP
    Inventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
  • Substituted-phenyl ketone derivatives as IP antagonists
    Patent number: 6417186
    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.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: July 9, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventor: Alam Jahangir
  • Methods, compositions and modes of delivery for the treatment of emphysema using 13-cis-retinoic acid
    Publication number: 20020049252
    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.
    Type: Application
    Filed: September 26, 2001
    Publication date: April 25, 2002
    Applicant: Syntex (U.S.A) LLC
    Inventor: Paula N. Belloni
  • Substituted 2-(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones
    Patent number: 6376500
    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.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: April 23, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Robin Douglas Clark, Counde O'Yang
  • Sulfamide-metalloprotease inhibitors
    Patent number: 6376506
    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
  • Pyrazole derivatives-p38 map kinase inhibitors
    Patent number: 6376527
    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
  • Processes for preparing 3-arylsulfur hydroxamic acids
    Publication number: 20020038037
    Abstract: This invention provides processes for the preparation of a compound of Formula I:
    Type: Application
    Filed: November 9, 2001
    Publication date: March 28, 2002
    Applicant: Syntex (U.S.A.) Inc.
    Inventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
  • Oxazolone derivatives and uses thereof
    Patent number: 6355641
    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
  • Processes for preparing 3-Arylsulfur hydroxamic acids
    Patent number: 6342639
    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
  • Piperidine quaternary salts- CCR- 3 receptor antagonists
    Patent number: 6342509
    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