Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Schering Corporation

Jinchu Liu

Joseph E Lynch

Norihiro Ikemoto

Russell R Ferlita

William Brian Morgan

Robert M Wenslow, Jr

Yuri Y Bereznitski

John L Leazer, Jr

Jungjun Yin

Frederick T Mattrey

Novel crystalline salts of 3-[4-(3-ethanesulfonyl-propyl)-bicyclo[2.2.2]oct-1-yl]-4-methyl-5-(2-trifluoromethyl-phenyl)-4H-1,2,4-triazole are potent inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. 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, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.

Crystalline forms of an inhibitor of 11-&#x3b2;-hydroxysteroid dehydrogenase type 1

A process for preparing &ggr;-hydroxy-4-&lsqb;&lsqb;2-oxazolyl&rsqb;alkyl&rsqb;-&agr;-&lsqb;(cyclo)alkyl- or aryl- or heteroaryl-substituted methyl&rsqb;-2-&lsqb;&lsqb;(un)substituted alkyl&rsqb;aminocarbonyl&rsqb;-1-piperazinepentanamides is disclosed. The piperazinepentanamides are useful as HIV protease inhibitors. A process for making a 4-&lsqb;&lsqb;2-oxazolyl&rsqb;alkyl&rsqb;-2-&lsqb;&lsqb;(un)substituted alkyl&rsqb;aminocarbonyl&rsqb;piperazine by treating a ketoamide precursor with fuming sulfuric acid in the presence of polyphosphoric acid is also disclosed. In addition, a process for enhancing the optical purity of 4-&lsqb;&lsqb;2-oxazolyl&rsqb;alkyl&rsqb;-2-&lsqb;&lsqb;(un)substituted alkyl&rsqb;aminocarbonyl&rsqb;-piperazines via the formation 2-naphthalenesulfonic acid crystal salts thereof is disclosed, as well as a method for purifying 2-naphthalenesulfonic acid.

Process for preparing piperazinepentaneamide HIV protease inhibitors

The invention relates to a process for preparing a substituted (6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidine compound of the formula (+)-I ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 alkyl, amino, --OCH.sub.3, --OCF.sub.3 and CF.sub.3, and the dotted line represents an optional double bond; comprising:

Enzymatic kinetic resolution of an intermediate useful for preparing

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Edison, NJ, United States of America

Jinchu Liu