Patents Assigned to Syntex (U.S.A.) Inc.
  • Patent number: 7074763
    Abstract: Aqueous formulations of nerve growth factor suitable for lyophilization and subsequent reconstitution in which nerve growth factor is admixed with sugars and buffer are provided.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: July 11, 2006
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Victoria M. Knepp
  • Patent number: 6844175
    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 find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: January 18, 2005
    Assignees: The Regents of the University of the California, Syntex (U.S.A.) INC
    Inventors: Annette Bistrup, Steven D. Rosen, Kirsten Tangemann, Stefan Hemmerich
  • 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
  • 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
  • Patent number: 6340756
    Abstract: wherein Z1 is hydrogen or an amino-protecting group selected from the group consisting of acyl of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms; trityl, optionally substituted with methoxy; and N-(9-fluorenylmethoxycarbonyl); Y1 is halo, aralkyloxy or acyloxy, wherein acyl is as defined above; and Y2 is aralkyloxy. These intermediates 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: January 22, 2002
    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
  • Patent number: 6338944
    Abstract: This invention relates to a human stromelysin-1 (i.e., HSL-1) promoter and uses therefor. In particular, the invention provides a purified DNA containing a functional HSL-1 promoter region that corresponds in structure to the native genomic form of this promoter, an expression vector containing a portion of the purified promoter DNA operatively linked to a heterologous DNA sequence encoding a detectable gene product, a host cell transformed with this factor, a pharmacologic screening assay for stromelysin-1 promoter modulating activity, and a method-of modulating TNF &agr; level and matrix metalloproteinase activities in inflamed tissues of a mammal.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: January 15, 2002
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Paula Ann Borden, Renu Anand Heller
  • 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
  • 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
  • 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
  • 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
  • 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
  • Patent number: 6166015
    Abstract: This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): ##STR1## 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: December 26, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Daniel Harry Rogers, John Saunders, John Patrick Williams
  • Patent number: 6150397
    Abstract: The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I): ##STR1## that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: November 21, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Mark Rotstein, Eric Brian Sjogren
  • Patent number: 6143744
    Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: November 7, 2000
    Assignees: Syntex (U.S.A.) Inc., 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
  • Patent number: 6140344
    Abstract: This invention relates to certain piperidine quaternary salts of Formula (I) ##STR1## that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: November 17, 1999
    Date of Patent: October 31, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Leyi Gong, Denis John Kertesz, David Berard Smith, Robert Stephen Wilhelm
  • Patent number: 6136844
    Abstract: Compounds selected from the group of compounds represented by formula I: ##STR1## where: R.sub.10 is represented by the formula (A), (B), or (C): ##STR2## R.sub.20 is represented by the formula (U), (V), or (W): ##STR3## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts;are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: October 24, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Denis J. Kertesz, Edvige Galeazzi Toscani, Deborah C. Reuter, Eric B. Sjogren
  • Patent number: 6127402
    Abstract: Compounds selected from the group of compounds represented by formula I: where:R.sub.10 is represented by the formula (A), (B), or (C): ##STR1## R.sub.20 is represented by the formula (U), (V), or (W): ##STR2## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts;are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: October 3, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Denis J. Kertesz, Edvige Galeazzi Toscani, Deborah C. Reuter, Eric B. Sjogren
  • Patent number: 6103901
    Abstract: Intermediates of Formula (III) ##STR1## wherein P.sup.1 is hydrogen or an amino-protecting group, R is lower alkyl, allyl or aralkyl, and Z is hydrogen, lower alkyl, aryl or aralkyl; and Formula (VI) ##STR2## wherein P.sup.1 is hydrogen or an amino-protecting group, P.sup.2 is an amino protecting group, and Z is hydrogen, lower alkyl, aryl or aralkyl, 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: July 23, 1998
    Date of Patent: August 15, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Humberto B. Arzeno, Eric R. Humphreys, Jim-Wah Wong, Christopher R. Roberts
  • Patent number: 6083953
    Abstract: The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
    Type: Grant
    Filed: March 4, 1997
    Date of Patent: July 4, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John Joseph Nestor, Scott William Womble, Hans Maag
  • Patent number: 6083973
    Abstract: This invention provides methods of of inhibiting mucin production in a mammal comprising administering to the mammal an RAR antagonist. Preferably, the RAR antagonist is an RAR.alpha. selective antagonist.In another aspect, this invention provides methods of inhibiting mucin gene expression in a human epithelial cell by contacting the cell with an RAR antagonist, preferably an RAR.alpha. selective antagonist.
    Type: Grant
    Filed: February 24, 1999
    Date of Patent: July 4, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Paula Nanette Belloni