Patents Assigned to Syntex (U.S.A.)
  • Preparation of ketorolac
    Patent number: 6323344
    Abstract: 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula where R1 is alkyl and R2 is optionally substituted phenyl; and the method for their preparation and their conversion to ketorolac and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: January 1, 2001
    Date of Patent: November 27, 2001
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter J. Harrington, Hiralal N. Khatri, George C. Schloemer
  • 2-arylethyl-(piperidin-4-ylmethyl)amine derivatives
    Patent number: 6319920
    Abstract: This invention relates to muscarinic receptor antagonist compounds selected from the group of compounds represented by Formula I: wherein the substituents are as defined in the specification; and their pharmaceutically acceptable salts, individual isomers or a racemic or non-racemic mixture; pharmaceutical compositions containing them; and methods for their use as therapeutic agents.
    Type: Grant
    Filed: February 1, 1999
    Date of Patent: November 20, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Joan Marie Caroon, Robin Douglas Clark, Michael Patrick Dillon, Ralph New Harris, III, Sharathchandra Surendra Hegde, Clara Jeou Jen Lin, Hans Maag, David Bruce Repke
  • P38 MAP kinase inhibitors
    Patent number: 6316464
    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: October 16, 1998
    Date of Patent: November 13, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
  • Pyrazole derivatives P-38 MAP kinase inhibitors
    Patent number: 6316466
    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: September 22, 1999
    Date of Patent: November 13, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
  • T-type calcium channel variants; compositions thereof; and uses
    Patent number: 6309858
    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: September 23, 1999
    Date of Patent: October 30, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Paul Shartzer Dietrich, Joseph Gerard McGivern
  • Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use
    Patent number: 6306892
    Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R 5, X, Y, and are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: October 23, 2001
    Assignees: Agouron Pharmaceuticals, Inc., Syntex Inc.
    Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
  • Treatment of emphysema using RARy selective retinoid agonists
    Patent number: 6300350
    Abstract: This invention provides methods of treating emphysema and other diseases associated with alveolar damage by treatment with an RAR&ggr; selective agonist. In another aspect, this invention provides methods of promoting tropoelastin gene expression and alveolar matrix repair by contacting the pulmonary intestitial fibroblast with an RAR agonist, preferably an RAR&ggr; selective agonist.
    Type: Grant
    Filed: October 18, 2000
    Date of Patent: October 9, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Paula Nanette Belloni, Michael Klaus
  • Pharmaceutical formulations of nerve growth factor
    Patent number: 6277828
    Abstract: Stable, aqueous pharmaceutical formulations of human nerve growth factor (NGF) in aqueous isotonic solutions, buffered to maintain the pH from about 4.5 to about 6.0, and optionally containing a carrier such as human serum albumin are provided. Also provided are aqueous NGF formulations suitable for lyophilization and subsequent reconstitution in which rhNGF is admixed with sugars, optionally HSA, and buffer. The formulations are useful for the treatment of Alzheimer's disease and other neuronal disorders.
    Type: Grant
    Filed: August 20, 1993
    Date of Patent: August 21, 2001
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Victoria M. Knepp, Deborah M. Lidgate, Richard Maskiewicz, Leo Gu
  • Glycosly sulfortransferase-3
    Patent number: 6265192
    Abstract: A novel human glycosylsulfotransferase expressed in high endothelial cells (GST-3) 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 selectin mediated binding events and methods of treating disease conditions associated therewith.
    Type: Grant
    Filed: March 20, 1998
    Date of Patent: July 24, 2001
    Assignees: The Regents of the University of California, Syntex, Inc.,
    Inventors: Annette Bistrup, Steven D. Rosen, Stefan Hemmerich
  • Phenoxymethyl piperidine derivatives for the treatment of neuropathic pain
    Patent number: 6262078
    Abstract: Compounds selected from the group of compounds represented by Formula I: as an individual isomer or as a racemic or non-racemic mixture of isomers, and their pharmaceutically acceptable salts and N-oxides thereof; are sodium channel blockers, and thus exhibit useful pharmacological properties, including utility for the treatment of neuropathic pain conditions.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: July 17, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: David Garrett Loughhead, Xiao-Fa Lin, Robert James Weikert, Lee Allen Flippin
  • Substituted 2(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones
    Patent number: 6258819
    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: July 27, 2000
    Date of Patent: July 10, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Robin Douglas Clark, Counde O'Yang
  • Process for the preparation of enteric coated pharmaceutical dosage forms
    Patent number: 6224911
    Abstract: This invention is directed to a process for the preparation of enteric coated pharmaceutical dosage forms. This invention is further directed to the aqueous enteric coating dispersions suitable for use in the process and the enteric coated pharmaceutical dosage forms prepared by the process.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: May 1, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Zakauddin T. Chowhan, Patrick H. Vo
  • Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative
    Patent number: 6218568
    Abstract: Process for preparing intermediates of formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: April 17, 2001
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Charles A. Dvorak, Douglas L. Wren, Lawrence E. Fisher, Steven D. Axt, Eric R. Humphreys, Humberto B. Arzeno, Colin C. Beard, Sam Linh Nguyen, Yeun-Kwei Han, Christopher R. Roberts, Jan P. Lund, Paul R. Fatheree
  • Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative
    Patent number: 6215017
    Abstract: Intermediates of Formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: April 10, 2001
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Charles A. Dvorak, Douglas L. Wren, Lawrence E. Fisher, Steven D. Axt, Eric R. Humphreys, Humberto B. Arzeno, Colin C. Beard, Sam Linh Nguyen, Yeun-Kwei Han, Christopher R. Roberts, Jan P. Lund, Paul R. Fatheree
  • Preparation of ketorolac
    Patent number: 6197976
    Abstract: 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula where R1 is alkyl and R2 is optionally substituted phenyl, and the method for their preparation and their conversion to ketorolac and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: March 6, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Peter J. Harrington, Hiralal N. Khatri, George C. Schloemer
  • Nucleic acids encoding truncated forms of inhibitory kappa B protein
    Patent number: 6194175
    Abstract: Truncated forms of inhibitory kappa B protein (I&kgr;B-&agr;), nucleic acids encoding the truncates, expression and delivery vectors, and therapeutic and prophylatic uses thereof are provided.
    Type: Grant
    Filed: July 8, 1999
    Date of Patent: February 27, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Paula Nanette Belloni, Gary Allen Peltz
  • Cloned peripheral nerve, tetrodotoxin-resistant sodium channel &agr;-subunit
    Patent number: 6184349
    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: April 15, 1997
    Date of Patent: February 6, 2001
    Assignee: Syntex (USA) Inc.
    Inventors: Ronald Herman, Stephen Gregory Delgado, Linda Marie Fish, Lakshmi Sangameswaran, Douglas Kenneth Rabert
  • 2-(substituted-phenyl)amino-imidazoline derivatives
    Patent number: 6184242
    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: August 20, 1998
    Date of Patent: February 6, 2001
    Assignee: Syntex USA (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
  • Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses
    Patent number: 6174915
    Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R5, X, Y, and  are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: January 16, 2001
    Assignees: Agouron Pharmaceuticals, Inc., Syntex (U.S.A.) Inc.
    Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
  • Dihydrobenzodioxine carboxamide and ketone derivatives
    Patent number: 6172062
    Abstract: This invention relates to certain 5-HT4 receptor modulators, particularly 5-HT4 receptor antagonists, represented by Formula I: wherein Z is formula (A) or (B): wherein R1, R2, R3, R4, and R5 and the other substituents are as defined in the specification; or 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: September 2, 1999
    Date of Patent: January 9, 2001
    Assignee: Syntex (USA) LLC
    Inventors: Robin Douglas Clark, Alam Jahangir