Merck + Co., Inc.

Other

Merck Frosst Canada & Co.

Banyu Pharmaceutical Co. Ltd

Richard D Tillyer

David M Tschaen

Lisa F Frey

Ulf H Dolling

Cheng Yi Chen

Paul O'Shea

Feng Xu

Xin Wang

Paul N Devine

Edward J Grabowski

Lushi Tan

Edward J J Grabowski

Paul J Reider

Dalian Zhao

Richard Desmond

Sophie-Dorothee Clas

Richard M Heid, Jr

Chad Dalton

Yoshiaki Kato

Robert D Larsen

Ian W Davies

Zhiguo Jake Song

Robert A Reamer

Weirong Chen

Mangzu Zhao

Mandana Asgharnejad

Jose M Vega

Philippe Dagneau

Anthony On-Ping King

Stephane G Ouellet

Ben Marcune

Charles Boudreau

The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.

Dihydroxy open-acid and salts of HMG-CoA reductase inhibitors

Synthesis of ketosulfone esters

2-lithio-5-halopyridine is formed as a predominant component of a reaction mixture by reacting BuLi with 2,5-dihalopyridine in a non-coordinating solvent.

Process for making 2, 5-substituted pyridine

This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.

Asymmetric conjugate addition reaction

This invention encompasses a novel process for synthesizing compounds represented by formula A:

Synthesis of methylthiophenyl hydroxyketones

A rearrangement process for the preparation of a 6,5,5-tricyclic, a 6,6,5-tricyclic and 6,5,5,7-tetracyclic ring system is disclosed.

Rearrangement process and tricyclic and tetracyclic compounds

This invention encompasses a novel process for synthesizing the compound represented by formula I:

Synthesis of 4-&lsqb;(5-substituted phenyl)-3-substituted-1H-pyrazol-1-yl&rsqb;benzenesulfonamide

This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.

This invention encompasses a novel process for synthesizing the compound represented by formula I: ##STR1## These compounds are useful as non-steroidal anti-inflammatory agents.

Synthesis of 4-[5-substituted or unsubstituted

An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.

Efficient synthesis of A 1,4-dihydro-2H-3,1-benzoxazin-2-one

This invention relates to a cyclization process useful in the preparation of a key intermediate in the preparation of an endothelin antagonist of the general formula shown below: ##STR1##

Phosphate-mediated cyclization

Pyridine propanoic acid derivatives

An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.

Efficient enantioselective addition reaction using an organozinc reagent

This invention relates to a process for the preparation of a key intermediate using an chiral additive to effect an asymmetric conjugate addition.

Asymmetric conjugate addition reaction using a chiral additive

This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.

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Westfield, NJ, United States of America

Richard D Tillyer