Karl J Hansen

US Patent:

6384244, May 7, 2002

Filed:

May 11, 2001

Appl. No.:

09/853796

Inventors:

Ian Davies - Princeton NJ
Karl Hansen - Atlantic Highlands NJ
Paul N. Devine - Lincroft NJ
Louis Matty, Jr. - Hillsborough NJ
Yuan Cheng - Edison NJ
Philippe M. Rabbat - Baie dUrfe, CA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D31104

US Classification:

549399

Abstract:

cis-aminochromanols are obtained in high yield and with high selectivity over their trans counterparts by hydrogenating the corresponding oximes in the presence of a catalyst and an acid selected from HBr, HCl, and organic sulfonic acid. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.

US Patent:

6531617, Mar 11, 2003

Filed:

Oct 24, 2001

Appl. No.:

10/001369

Inventors:

Karl Hansen - Atlantic Highlands NJ
Paul Devine - Lincroft NJ
Philippe M. Rabbat - New York NY

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D31122

US Classification:

549400, 549401

Abstract:

Enantiomerically enriched hydroxychromanones are obtained by the AlCl -catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.

US Patent:

20080227786, Sep 18, 2008

Filed:

Jan 12, 2005

Appl. No.:

10/585603

Inventors:

Russell R. Ferlita - Westfield NJ, US
Karl Hansen - Atlantic Highlands NJ, US
Vicky K. Vydra - Fair Lawn NJ, US
Yaling Wang - Westfield NJ, US
Christopher M. Lindemann - Loveland CO, US

International Classification:

A61K 31/4985
C07D 487/02
A61P 3/10

US Classification:

514249, 544350

Abstract:

Novel crystalline salts of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-&agr; amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.