Development Center for Biotechnology

The Dupont Merck Pharmaceutical Company

Chia-Lin J Wang

Jaw-Yuh Chiu

Feng-Wen Yeng

John Matthew Fevig

Matthew M Abelman

Charles A Kettner

Joseph Cacciola

Shan-Yen Chou

Gregory James Pacofsky

Eugene Cruz Amparo

Shan-Shue Wang

Chin-Fen Lee

Hsiao-Hwa Lu

Hsiang-Ling Huang

Kae-Shyang Shih

Hsiao-Jen Chen

Paw-Hwa Yang

Su-Chen Yen

Ya-Chuan Lin

Pei-Ling Lee

Mei-Shey Lin

Lee-Tai Liu

Lie-Rong Chen

Ching-Wei Liu

Disclosed are novel 1,2,4-triazin-5-one biphenyl derivatives having structural formula (I) useful as non-peptide antagonists of angiotensin II receptor: ##STR1## where R.sub.1 represents alkyl, cycloalkyl, or substituted or unsubstituted aryl;

Angiotensin II receptor antagonistic 1,2,4-triazin-5-one derivatives

The invention relates to novel compounds of formula (I) ##STR1## wherein R.sub.1 represents hydrogen, hydroxy or alkoxy;

Antiatherosclerosis agents for lipid-lowering and antiperoxidative

The invention relates to compounds of formula (I) ##STR1## wherein R.sup.1 is an optional substituent any position of phenyl ring and is selected from halogen, --NO.sub.2, --NH.sub.2, --OH and --O--CR.sub.1-6 alkyl;

1,2,3,4-tetrahydroisoquinoline derivatives and pharmaceutical

A process for preparing fluconazole, including the steps of (1) acylating 1,3-difluorobenzene (DFB) to obtain 2-chloro-2',4'-difluoroacetophenone (CAP); (2) alkylating 4-amino-4H-1,2,4-triazole (4-AT) with CAP to obtain 2-(1H-1,2,4-triazol-1-yl)-2',4'-difluoroacetophenone (TAAP) salt; (3) deaminating TAAP salt to obtain TAAP; and (4) reacting TAAP with 1,2,4-triazole to obtain fluconazole.

Preparation of fluconazole and pharmaceutically acceptable salts thereof

A method for resolving racemic dimethyl-4,4'-dimethoxy-5,6,5',6'-di(methylenedioxy)biphenyl-2,2'-dicarbox ylate ('DDB'), in which a chiral .alpha.-alkyl benzyl alcohol is used as the resolving agent. More specifically, racemic DDB is first hydrolyzed to form dicarboxylic acid, which is then reacted with chiral .alpha.-alkyl benzyl alcohol to form two chiral isomers. The chiral isomers, after separation either by chromatography or by recrystalli-zation, are respectively hydrogenated and esterified to form chiral DDB isomers.

Method for resolving racemic compounds

The present invention relates to the discovery of new C-terminal boronic acid dipeptide inhibitors of trypsin-like enzymes such as thrombin and pharmaceutical compositions thereof.

Dipeptide boronic acid inhibitors of trypsin-like enzymes

Growing community of inventors

Taipei, Taiwan

Chia-Lin J Wang