Patents Assigned to Syntex (U.S.A.) LLC
  • 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
  • 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
  • System and method for bridging a clinical remote data entry product to a back-end clinical data management system
    Patent number: 6556999
    Abstract: A back-end clinical definition is designed using a back-end clinical data management system (CDMS). The back-end clinical definition is automatically converted into a Remote Data Entry (front-end) study definition. The front-end study definition is transferred to a remote computer hosting a front-end RDE product where it is used to regulate the acquisition of clinical data. During the back-end clinical definition to front-end study definition conversion process, a conversion map is created. The conversion map allows for the automated conversion of clinical data acquired using the front-end RDE product to a format that can be read by the back-end CDMS. Clinical data is retrieved from remote computers hosting a front-end RDE product in an automated manner without manual back-end clinical definition/front-end study definition conflict resolution.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: April 29, 2003
    Assignee: Syntex (USA) LLC
    Inventors: Siegbert R. Kloos, Anja Bornhausen, John W. Egar, Richard Sayer, Peter J. O'Connor, Hugo De Schepper
  • 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
  • Sustained release ranolazine formulations
    Patent number: 6503911
    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: October 19, 2001
    Date of Patent: January 7, 2003
    Assignees: CV Therapeutics, Inc., Syntex USA, Inc.
    Inventors: Andrew A. Wolff, Fiona Baker, John Langridge
  • 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
  • 1,3-dihydroxy-20,20-cycloalkyl-vitamin D3analogs
    Patent number: 6492353
    Abstract: This invention relates to 1,3-dihydroxy-20,20-dialkyl-vitamin D3 analogs of Formula (I): compositions comprising the analogs, methods of preparing the analogs and methods of treatment of osteoporosis, secondary hyperparathyroidism, cancer and autoimmune diseases using such analogs.
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: December 10, 2002
    Assignees: Syntex LLC, Hoffmann-La Roche Inc.
    Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
  • 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
  • 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
  • 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
  • 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
  • Processes for preparing 3-arylsulfur hydroxamic acids
    Publication number: 20020133030
    Abstract: This invention provides processes for the preparation of a compound of Formula I:
    Type: Application
    Filed: May 8, 2002
    Publication date: September 19, 2002
    Applicant: Syntex USA, LLC
    Inventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
  • 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