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.
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
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.
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
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.
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
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
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
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
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
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
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
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
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
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
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
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
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
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.