Steven D Axt

US Patent:

6340756, Jan 22, 2002

Filed:

Feb 3, 2000

Appl. No.:

09/497319

Inventors:

Charles A. Dvorak - Palo Alto CA
Douglas L. Wren - Palo Alto CA
Lawrence E. Fisher - Mountain View CA
Steven D. Axt - San Jose CA
Eric R. Humphreys - San Bruno CA
Humberto B. Arzeno - Cupertino CA
Colin C. Beard - Palo Alto CA
Sam Linh Nguyen - Denver CO
Yeun-Kwei Han - Louisville CO
Christopher R. Roberts - Berthoud CO
Jan P. Lund - Boulder CO
Paul R. Fatheree - San Francisco CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

C07D47318

US Classification:

544276

US Patent:

20080139802, Jun 12, 2008

Filed:

Oct 10, 2007

Appl. No.:

11/973748

Inventors:

Steven D. Axt - Menlo Park CA, US
Qingwu Jin - San Jose CA, US
Suguna Rachakonda - Robbinsville NJ, US
Bruce Ross - Plainsboro NJ, US
Keshab Sarma - Sunnyvale CA, US
Justin Vitale - San Mateo CA, US
Jiang Zhu - Cupertino CA, US

International Classification:

C07H 19/06
C07H 13/04
C07D 307/20

US Classification:

536 285, 536115, 549478

Abstract:

The present process provides an improved method for converting 2′-deoxy-2′-fluoro-2′-methyl-D-ribonolactones derivatives to 3-fluoro-3-methyl-2-chlorofuran compounds which are useful for the synthesis of nucleosides and improved processes for the synthesis of the D-ribonolactone compounds.

US Patent:

20100056770, Mar 4, 2010

Filed:

Oct 5, 2007

Appl. No.:

12/444608

Inventors:

Steven D. Axt - Menlo Park CA, US
Keshab Sarma - Sunnyvale CA, US
Justin Vitale - San Mateo CA, US
Jiang Zhu - Cupertino CA, US
Bruce Ross - Plainsboro NJ, US
Suguna Rachakonda - Robbinsville NJ, US
Qingwu Jin - San Jose CA, US

International Classification:

C07H 19/067

US Classification:

536 285

Abstract:

The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydrox-ymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.

US Patent:

51985985, Mar 30, 1993

Filed:

Jul 19, 1991

Appl. No.:

7/732551

Inventors:

Karlheinz Hill - Erkrath, DE
Steven D. Axt - Cupertino CA
Kenneth J. Weese - Daly City CA

Assignee:

Henkel Kommanditgesellschaft auf Aktien - Duesseldorf-Holthausen

International Classification:

C07C 4311

US Classification:

568619

Abstract:

Alkadienyl ethers are prepared by the telomerization of conjugated dienes with polyols by continuous addition of the alkadiene to a reaction mixtue comprised of the polyol, secondary alcohol solvent, a portion of the alkadiene to be added, and low palladium catalyst concentration.

US Patent:

62185683, Apr 17, 2001

Filed:

Feb 3, 2000

Appl. No.:

9/497538

Inventors:

Charles A. Dvorak - Palo Alto CA
Douglas L. Wren - Palo Alto CA
Lawrence E. Fisher - Mountain View CA
Steven D. Axt - San Jose CA
Eric R. Humphreys - San Bruno CA
Humberto B. Arzeno - Cupertino CA
Colin C. Beard - Palo Alto CA
Sam Linh Nguyen - Denver CO
Yeun-Kwei Han - Louisville CO
Christopher R. Roberts - Berthoud CO
Jan P. Lund - Boulder CO
Paul R. Fatheree - San Francisco CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

C07C 67743
C07C 6702

US Classification:

560106

Abstract:

Process for preparing intermediates of formula (III) ##STR1## wherein Y. sup. 1 is acyloxy, wherein acyl is of the formula R--C(O)--, wherein R is alkyl of 1-6 carbon atoms, Y. sup. 2 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.

US Patent:

62150170, Apr 10, 2001

Filed:

Feb 3, 2000

Appl. No.:

9/497537

Inventors:

Charles A. Dvorak - Palo Alto CA
Douglas L. Wren - Palo Alto CA
Lawrence E. Fisher - Mountain View CA
Steven D. Axt - San Jose CA
Eric R. Humphreys - San Bruno CA
Humberto B. Arzeno - Cupertino CA
Colin C. Beard - Palo Alto CA
Sam Linh Nguyen - Denver CO
Yeun-Kwei Han - Louisville CO
Christopher R. Roberts - Berthoud CO
Jan P. Lund - Boulder CO
Paul R. Fatheree - San Francisco CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

C07C 67743
C07C 6702

US Classification:

560106

Abstract:

Intermediates of Formula (III) ##STR1## wherein Y. sup. 1 is acyloxy, wherein acyl is of the formula R--C(O)--, wherein R is alkyl of 1-6 carbon atoms, Y. sup. 2 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.

US Patent:

60404469, Mar 21, 2000

Filed:

Jul 31, 1998

Appl. No.:

9/127380

Inventors:

Charles A. Dvorak - Palo Alto CA
Douglas L. Wren - Palo Alto CA
Lawrence E. Fisher - Mountain View CA
Steven D. Axt - San Jose CA
Eric R. Humphreys - San Bruno CA
Humberto B. Arzeno - Cupertino CA
Colin C. Beard - Palo Alto CA
Sam Linh Nguyen - Denver CO
Yeun-Kwei Han - Louisville CO
Christopher R. Roberts - Berthoud CO
Jan P. Lund - Boulder CO
Paul R. Fatheree - San Francisco CA

Assignee:

Syntex (U.S.A.) Inc. - Palo Alto CA

International Classification:

C07D47318

US Classification:

544276

Abstract:

Process and novel intermediates for preparing the L-mono-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process and intermediates provide for reduced impurities in the mono-valine ester end-product and lower overall production costs. The process involves the condensation of a silylated guanine compound with a substituted glycerol derivative and esterification of this product with an L-valine derivative. These mono-valine products are of value as antiviral agents with improved absorption.