Patents Assigned to Syntex (U.S.A.) LLC
  • Heterocyclylalkylamines as muscarinic receptor antagonists
    Patent number: 6667301
    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
  • Piperidine CCR-3 receptor antagonists
    Publication number: 20030229121
    Abstract: The invention provides compounds of Formula (I): 1
    Type: Application
    Filed: November 29, 2002
    Publication date: December 11, 2003
    Applicant: Syntex (U.S.A.) LLC
    Inventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
  • Human aggrecanase and nucleic acid compositions encoding the same
    Patent number: 6649377
    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
  • Benzocycloalkylenylamine derivatives as muscarinic receptor antagonists
    Patent number: 6645958
    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
  • Alkylamino-substituted bicyclic nitrogen heterocycles
    Patent number: 6642241
    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
  • Amino-tetralin derivatives as muscarinic receptor antagonists
    Patent number: 6635658
    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.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: October 21, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Ann Marie Madera, Robert James Weikert
  • p38 map kinase inhibitors
    Patent number: 6630485
    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
  • 4-piperidinyl alkyl amine derivatives as muscarinic receptor antagonists
    Patent number: 6627644
    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
  • Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3 betta
    Publication number: 20030176484
    Abstract: This invention relates to the use of inhibitors of glycogen synthase kinase-3&bgr; to increase bone formation.
    Type: Application
    Filed: January 9, 2003
    Publication date: September 18, 2003
    Applicant: Syntex (U.S.A.) LLC
    Inventors: Patricia Ann Day-Lollini, Leyi Gong
  • Sustained release ranolazine formulations
    Patent number: 6617328
    Abstract: A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below pH 4.5 and soluble in aqueous media above pH 4.5. The formulation is suitable for twice daily administration of ranolazine and is useful for controlling the rate of dissolution of ranolazine, and to maintain human plasma ranolazine levels at between 550 and 7500 ng base/mL.
    Type: Grant
    Filed: September 27, 2002
    Date of Patent: September 9, 2003
    Assignees: CV Therapeutics, Inc, Syntex (USA), LLC
    Inventors: Andrew A. Wolff, Fiona Baker, John Langridge
  • Heterocyclic retinoid compounds
    Publication number: 20030158178
    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.
    Type: Application
    Filed: October 30, 2002
    Publication date: August 21, 2003
    Applicant: Syntex (U.S.A.) LLC
    Inventors: Michael Klaus, Jean-Marc Lapierre
  • Alkyl urea retinoid agonists
    Publication number: 20030158226
    Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
    Type: Application
    Filed: September 17, 2002
    Publication date: August 21, 2003
    Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLC
    Inventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
  • 7-oxo-pyridopyrimidines (I)
    Publication number: 20030153586
    Abstract: The present invention provides compounds of the formula: 1
    Type: Application
    Filed: August 29, 2002
    Publication date: August 14, 2003
    Applicant: Syntex (U.S.A) LLC
    Inventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
  • Aminopyrimidine and aminopyridine anti-inflammation agents
    Publication number: 20030144303
    Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.
    Type: Application
    Filed: November 6, 2002
    Publication date: July 31, 2003
    Applicant: Syntex (U.S.A.) LLC
    Inventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
  • 1-oxa-3,9-diaza-spiro[5,5]undecan-2-ones
    Patent number: 6599900
    Abstract: The invention relates to compounds of the general formula wherein (R1)n is independently from from each other halogen, lower alkyl or lower alkoxy; R2 is hydrogen, lower alkyl, lower halogen-alkyl, —(CH2)m—OH, —(CH2)m—NR2, —(CH2)mO-lower alkyl, —(CH2)m—C(O)—NR2, or is —(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, —(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl; R is hydrogen or lower alkyl and may be the same or different in case of R2; n is 0, 1, or 2; m is 0, 1, 2, 3 or 4; and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: July 29, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Hai-Ying Cai, Michael Patrick Dillon, Guido Galley, Annick Goergler, Sabine Kolczewski, Dawn Muszynski Barsy
  • 2-(substituted-phenyl)amino-imidazoline derivatives
    Patent number: 6596876
    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 and their use as therapeutic agents.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: July 22, 2003
    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
  • Aminopyrrole compounds
    Publication number: 20030130319
    Abstract: The present invention provides an aminopyrrole compound of the formula: 1
    Type: Application
    Filed: August 29, 2002
    Publication date: July 10, 2003
    Applicant: Syntex (U.S.A.) LLC
    Inventors: David Michael Goldstein, David Mark Rotstein
  • T-type calcium channel variants; compositions thereof; and uses
    Patent number: 6589787
    Abstract: The invention provides TCCV-1 or TCCV-2 from human, reagents related thereto including polynucleotides encoding TCCV-1 or TCCV-2, purified polypeptides, and specific antibodies. Methods of making and using these reagents, in particular, methods for screening compounds which modulate TCCV-1 or TCCV-2 activity are provided. Also provided are methods of diagnosis and kits.
    Type: Grant
    Filed: August 23, 2001
    Date of Patent: July 8, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Paul Shartzer Dietrich, Joseph Gerrard McGivern
  • Substituted urea retinoid agonists
    Publication number: 20030125383
    Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
    Type: Application
    Filed: September 17, 2002
    Publication date: July 3, 2003
    Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLC
    Inventors: Michael Klaus, Jean-Marc Lapierre
  • Matrix metalloprotease inhibitors
    Patent number: 6579890
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: June 17, 2003
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Stephen Horne, Teng J. Liak