Eli Lilly and Company

Richard C Hoying

James E Ray

Lowell D Hatfield

Jack W Fisher

John Gordon Allen

Karin Briner

Natalia Pokrovskaia

Maria Angeles Martinez-Grau

Julie M Miyashiro

Charles J Barnett

Andrew Caerwyn Williams

Christopher Stanley Galka

Roger Ryan Rothhaar

Michael Philip Mazanetz

Matthew Robert Reinhard

Richard Edmund Rathmell

Manuel Javier Cases-Thomas

Selma Sapmaz

Anne Marie Camp

Thomas M Eckrich

Thomas L Emmick

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HTreceptor agonists for the treatment of 5-HTassociated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where Ris &#x2014;C&#x2261;C&#x2014;R, &#x2014;CH&#x2550;CRR, or &#x2014;(C-C)alkyl-Aroptionally substituted on the alkyl moiety with 1 to 6 fluoro substituents and other substituents are as defined in the specification. 

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The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HT2C receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: R6 D R?N&#x2014;R&#x2033;R* where R6 is &#x2014;(CrC3)alkyl-S&#x2014;(C0-C3)alkyl-R10, &#x2014;(C1-C3)alkyl-NR11R12, &#x2014;(CrC3)alkyl-O&#x2014;R13. and other substituents are as defined in the specification. 

The present invention is directed to azetidinone compounds of the following formula: ##STR1## which are useful as intermediates to carbacephalosporins: ##STR2## These carbacephalosporins are useful as antibacterials.

Chiral intermediates for the preparation of carbacephems

This invention is directed to carbacephems and methods for their preparation: ##STR1## In the foregoing formulae, R.sup.3 represents phenyl, C.sub.1 -C.sub.4 alkylphenyl, halophenyl, C.sub.1 -C.sub.4 alkoxyphenyl, naphthyl, thienyl, furyl, benzothienyl, or benzofuryl.

Intermediates for the preparation of carbacephems

A chiral process for preparing compounds of the formula: ##STR1## from a compound of the formula: ##STR2## in which the compound formula (IV) is reacted with trimethylsilyl iodide to remove the chiral auxiliary at the 7-position and the carboxy protecting group. The process allows for the retention of the amino and carboxy protecting groups throughout the preparation of Compound IV. Also disclosed are novel intermediates.

Methods and compounds for the preparation of carbacephems

The crystalline bis(DMF), dihydrate mono(DMF) and mono(DMF) forms of 7.beta.-[2'-(R)-2'-phenyl-2'-aminoacetamido[-3-chloro-3-(1-carbadethiaceph em)-4-carboxylic acid (LY163892) are useful intermediates to the monohydrate form of LY163892.

DMF solvates of a .beta.-lactam antibiotic

Preparation of substituted 2-aminopyrazines by reaction of an .alpha.-chloro or .alpha.-bromo oxime with an aminoacetonitrile in the presence of an acid-uptake agent, followed by separation of the intermediate novel hydroxyimino-substituted aminoacetonitrile, and cyclization thereof with acid.

Preparation of substituted 2-aminopyrazines

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Indianapolis, IN, United States of America

Richard C Hoying