Patents Assigned to Syntex (U.S.A.)
  • 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
  • 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
  • Quinazoline derivatives as alpha-1 adrenergic antagonists
    Patent number: 6559153
    Abstract: This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I): wherein R′, R″, R1, R2, m, n, and A are as defined in the specification, or acceptable prodrug, salt or solvate 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: August 29, 2001
    Date of Patent: May 6, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Cyrus Kephra Becker, Chris Richard Melville, Jürg Roland Pfister, Xiaoming Zhang
  • 3-Desoxy-vitamin D3 analog esters
    Patent number: 6559138
    Abstract: The present invention provides 3-desoxy vitamin D3 analog esters of the formula: and methods for use and preparation of the same, wherein the dotted line, R1, R2, R3, R4 and L are those defined herein.
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: May 6, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventor: Milan Radoje Uskokovic
  • 2,4-substituted pyrrolidine derivatives-CCR-3 receptor antagonists
    Patent number: 6552028
    Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: April 22, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Denis John Kertesz, Michael Garret Roepel
  • Processes for preparing 3-arylsulfur hydroxamic acids
    Patent number: 6518460
    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: May 8, 2002
    Date of Patent: February 11, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
  • 7-oxo-pyridopyrimidines (II)
    Patent number: 6518276
    Abstract: The present invention provides compounds of the formula: wherein R1, R3, and Ar1 are those defined herein, and R2 is —CR′R″—Ra (where R′ and R″ are hydrogen, hydroxyalkyl or alkyl with at least one being alkyl or hydroxyalkyl and Ra is hydroxyalkyl), Rx—S—Ry— (where Rx is alkyl and Ry is alkylene), alkoxy-substituted alkyl, heterocyclylalkyl or C4-C5 cycloalkyl, wherein each of the hydroxy group present in R2 can be independently Ra—C(═O)—O, RaRbN—C(═O)—O, or Ra—S(O)2—O—, wherein Ra and Rb are independently hydrogen, alkyl, aryl, or aralkyl, and methods for preparation and uses thereof.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: February 11, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Humberto Bartolome Arzeno, Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
  • Use of purinergic receptor modulators and related reagents
    Patent number: 6515198
    Abstract: The invention provides a method of treatment for an animal having a disease state associated with a genitourinary disorder with a purinergic receptor modulator. Also provided, is a transgenic animal having a disrupted purinergic receptor gene. The invention further provides for a method of screening using the transgenic animal as a positive control.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: February 4, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Debra Ann Cockayne, Anthony P. D. W. Ford, Quan-Ming Zhu, Wilhelm G. Lachnit, Annika B. Malmberg
  • 7-oxo-pyridopyrimidines (I)
    Patent number: 6506749
    Abstract: The present invention provides compounds of the formula: wherein R2 is substituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl-alkyl, optionally substituted heterocyclyl, spiro-substituted cycloalkyl, aralkoxy, alkoxy, -alkylene-S(O)n-alkyl (wherein n is 1 or 2), or —SO2Ar2; and R1, R3, and Ar1 are those defined herein, and methods for preparation and uses thereof.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: January 14, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
  • Benzocycloalkylenylamine derivatives as muscarinic receptor antagonists
    Patent number: 6500822
    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: May 22, 2001
    Date of Patent: December 31, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler