Sepracor, Inc.

Seprachem, Inc.

Spectra Science Corporation

Richard F Rossi

Donald L Heefner

Gregory D Cuny

Charles M Zepp

James R Hauske

Michael Z Hoemann

Chris Hugh Senanayake

Stephen Alan Wald

Anita Melikian-Badalian

Gnanasambandam Kumaravel

Qun Kevin Fang

Roger P Bakale

Paul T Grover

Roger L Xie

Nabil M Lawandy

Patrick Koch

The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.

Antimicrobial agents uses and compositions related thereto

Di- and tetra-hydroquinoline-indole antimicrobial agents, uses and compositions related thereto

Quinoline-indole antimicrobial agents, uses and compositions related thereto

A method of treating fungal infections with a mixture of isomers of 2R,4S-hydroxyitraconazole and their sulfate and phosphate derivatives is disclosed. Pharmaceutical compositions containing these compounds are also disclosed.

2R,4S-hydroxyitraconazole isomers

The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacteria microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.

Quinoline-indole antimicrobial agents, uses and compositions related

Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.

Asymmetric grignard synthesis with cyclic 1,2 aminoalcohols

An aqueous system for the production of metal chalcogenide nanocrystalline salts such as zinc selenide, from a hydrolyzable chalcogen carbonyl compound, such as selenourea, by simple hydrolysis thereof under alkaline conditions in the presence of water soluble metal hydroxide, such as zinc hydroxide in the form of the zincate ion, i.e., Zn(OH).sub.4.sup.-2. Selenourea contains selenium in the correct oxidation state, is inexpensive, commercially-available and readily hydrolyzable under aqueous basic conditions in the presence of the zincate ion to form zinc selenide. The zinc selenide is insoluble in the alkaline aqueous vehicle and precipitates over time in the form of nanocrystallites or quantum dots of the zinc selenide.

Synthesis of metal chalcogenide quantum

Described herein is a process for resolving a racemic (C&gt;3) alkyl (R, S) chroman-2-carboxylate compound useful as intermediates in the synthesis of optically pure pharmaceutical compounds is disclosed. The process utilizes a microbial enzyme derived from Serratia marcescens to catalyze the enantioselective hydrolysis of the (C&gt;3) alkyl (S)-chroman-2-carboxylate enantiomer of the racemic mixture to its corresponding carboxylic acid at a faster rate than the R-enantiomer. An enantiomerically pure S-configured carboxylic acid is thereby formed which can undergo acidic esterification to provide an optically pure (C&gt;3) alkyl (S)-chroman-2-carboxylate intermediate for subsequent pharmaceutical synthesis. The nonhydrolyzed (C&gt;3) alkyl (R)-chroman-2-carboxylate enantiomer can also be isolated to provide an optically pure pharmaceutical precursor.

Optical resolution of alkyl chroman-2-carboxylates

A process for resolving racemic alkyl 1,4-benzodioxan-2-carboxylates useful as intermediates in the synthesis of optically pure pharmaceutical compounds such as (S)-doxazosin is disclosed. The process utilizes a microbial enzyme derived from Serratia marcescens to catalyze the enantioselective hydrolysis of the alkyl (S)-1,4-benzodioxan-2-carboxylate enantiomer of the racemic mixture to its corresponding carboxylic acid at a faster rate than the R-enantiomer. An enantiomerically pure S-configured carboxylic acid is thereby formed for subsequent pharmaceutical synthesis. The nonhydrolyzed alkyl (R)-1,4-benzodioxan-2-carboxylate enantiomer can also be isolated and racemized, and the enzymatic hydrolysis reaction repeated.

Optical resolution of alkyl 1,4-benzodioxan-2-carboxylates using

A process for enantioselectively converting an aldehyde, a bisulfite adduct of an aldehyde or a glycidate to a chiral carboxylic acid is disclosed. The process utilizes a microorganism or an enzyme preparation from a microorganism and is particularly useful for producing NSAIDs of the profen class from readily available precursors. Preferred microorganisms are Gram-negative rod bacteria.

Growing community of inventors

Norton, MA, United States of America

Richard F Rossi