Keith R Mccarthy

US Patent:

20050080252, Apr 14, 2005

Filed:

Sep 13, 2004

Appl. No.:

10/939819

Inventors:

Andrew Briggs - Mountain View CA, US
Charles Dvorak - Palo Alto CA, US
Anthony Prince - , US
Keith McCarthy - Old Lyme CT, US

International Classification:

C07H019/056

US Classification:

536028700

Abstract:

Process and novel intermediates for preparing 2-aminocarboxylic acid esters of the 5-hydroxymethyl group of levovirin (1-(3S,4R-dihydroxy-5S-hydroxymethyl-tetrahydro-furan-2S-yl)-1H-[1,2,4]triazole-3-carboxylic acid amide; Id: R═R═R═H) and acid addition salts thereof. The present process provides the monoesters selectively in high purity with increased efficiency with reduced number of production steps. The process involves condensation of a cyclopentylidene levovirin compound with a N-urethane-N-carboxylic anhydride and subsequent deprotection to directly provide the hydrochloride salt of the product. The mono esters are useful for treatment of viral diseases and are absorbed more efficiently than the parent compound.

US Patent:

20050130915, Jun 16, 2005

Filed:

Sep 13, 2004

Appl. No.:

10/939648

Inventors:

Kondamraj Birudaraj - Belmont CA, US
Anthony Prince - Old Lyme CT, US
Keith McCarthy - Old Lyme CT, US

International Classification:

C07H019/056
A61K031/7056
A61K038/21

US Classification:

514043000, 536028700, 424085400

Abstract:

The present invention relates to the polymorphic crystalline hydrochloride salts of a nucleoside valinate ester according to formula Ib, methods of treating diseases mediated by Hepatitis C Virus and pharmaceutical composition containing Ib.

US Patent:

53429532, Aug 30, 1994

Filed:

Jan 31, 1991

Appl. No.:

7/648117

Inventors:

Gary F. Cooper - Portola Valley CA
Keith E. McCarthy - Palo Alto CA

Assignee:

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

International Classification:

C07D24104

US Classification:

548122

Abstract:

Compounds of the formula: ##STR1## wherein: A is oxo or dioxo; R. sup. 1, R. sup. 2 and R. sup. 3 are independently hydrogen or lower alkyl of one to six carbon atoms; R. sup. 4, R. sup. 5, R. sup. 6 and R. sup. 7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo; are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.

US Patent:

55169104, May 14, 1996

Filed:

May 19, 1994

Appl. No.:

8/245789

Inventors:

Gary F. Cooper - Portola Valley CA
Keith E. McCarthy - Palo Alto CA

Assignee:

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

International Classification:

C07D49504

US Classification:

546114

Abstract:

Compounds of the formula: ##STR1## wherein: A is oxo or dioxo; R. sup. 1, R. sup. 2 and R. sup. 3 are independently hydrogen or lower alkyl of one to six carbon atoms; R. sup. 4, R. sup. 5, R. sup. 6 and R. sup. 7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo; are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.