Eli Lilly and Company

James A Aikins

Eddie V Tao

Tony Yantao Zhang

John Robert Rizzo

John P Gardner

Billy G Jackson

Dennis Michael Zimmerman

J Jeffry Howbert

James R Beck

Timothy Alan Shepherd

Richard Waltz Harper

Larry C Blaszczak

Brent Jeffrey Rieder

Edward C R Smith

Barbara S Briggs

William David Miller

Gerald A Poore

Randal Scot Miller

Andrew Hendley Fray

Milton Zmijewski, Jr

Kevin P Lund

The present invention relates to a compound of formula (Ia) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.

Sulfonamide derivatives

The present invention provides certain cyclopentyl sulfonamide derivatives of formula (I): useful for potentiating glutamate receptor function in a mammal. It also relates to novel cyclopentyl sulfonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Cyclopentyl sulfonamide derivatives

This invention provides processes for preparing intermediates useful for the preparation of cryptophycin compounds.

Stereoselective process for producing intermediates of cryptophycins

A process for resolving amino protected racemic 3-amino-2-methylpropionic acid which comprises the steps of: (1) reacting said amino protected acid with a protected amino group with an enantiomer of a chiral amine to form diastereomeric salts; (2) recrystallizing the diastereomeric salts from ethyl acetate to separate the diastereomeric salts into crystal fractions; and (3) releasing the resolved acid from the diastereomeric salt by treating the diastereomeric salt with a basic solution is disclosed. A process for the preparation of the cryptophycin molecules is also disclosed.

Optical resolution of aminoisobobutyric acid

The present invention is directed to a new process for the synthesis of vinyl sulfoxides, in particular diarylvinyl sulfoxides

Process for the synthesis of vinyl sulfoxides

The present invention is directed to new diarylvinyl sulfoxides.

Diarylvinyl sulfoxides

7.beta.-Amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are provided via cyclization of cis-3-(substituted amino)-1-(2-substituted 2-oxoethyl)-4-substituted azetidinones. The 7.beta.-amino-3-hydroxy-1-carba (1-dethia)-3-cephem-4-carboxylic acid esters are useful chiral intermediates to .beta.-lactam antibiotics.

Azetidinone intermediates to carbacephalosporins and process

The present invention is directed to a process for the synthesis of 2-arylbenzo[b]thiophenes.

Process for the synthesis of benzo[b]thiophenes

This invention provides certain sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.

Anti-tumor method and compounds

The invention provides 1,3,4 substituted and bicyclic derivatives of 2-azetidinones and processes therefor. These compounds are valuable intermediates useful in the preparation of 1-carba(dethia)cephalosporin antibiotics.

1,3,4 substituted and bicyclic derivatives of 2-azetidinones and

7.beta.-Amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are provided via cyclization of cis-3-(substituted amino)-1-(2-substituted 2-oxoethyl)-4-substituted azetidinones. The 7.beta.-amino-3-hydroxy-1-carba(1-dethia)-3-cephem-4-carboxylic acid esters are useful chiral intermediates to .beta.-lactam antibiotics.

Disclosed is a process using hydrolysis and hydrogenation for converting enamino .beta.-lactams to their saturated alkyl ester acid salts, key intermediates to 1-carbacephalosporins. Also disclosed are intermediates resulting from the process.

Intermediates to 1-carbacephalosporins and process for preparation

The present invention provides a process for selectively alkylating pyrazoles comprising reacting a 3(5)-cyano-1H-pyrazole-4-carboxylic acid ester with a C.sub.4 -C.sub.8 alkene, or a C.sub.5 -C.sub.6 cycloalkene substituted at the 1-position with a C.sub.1 -C.sub.4 alkyl group, and a strong acid in a solvent which contains a strong electron withdrawing group. Also provided are new 3(5)-cyano-1H-pyrazole-4-carboxylic acid ester useful as starting materials in the process of the invention.

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Indianapolis, IN, United States of America

James A Aikins