Pharmacia & Upjohn Company

Pfizer Corporation

The Upjohn Co.

Pharmacia Corporation

Pharmacia & Upjohn

Toni-Jo Poel

Richard Charles Thomas

Michael R Barbachyn

Jackson B Hester, Jr

Adam Renslo

Gary W Luehr

Eldon George Nidy

Upinder Singh

Douglas K Hutchinson

Mikhail Fedorovich Gordeev

Michael D Ennis

David John Anderson

Salvatore Charles Perricone

Donna Lee Romero

Paul A Aristoff

Robert Louis Hoffman

Paul D May

Paul D Johnson

Vara Prasad Venkata Nagendra Josyula

Lisa Marie Thomasco

Mikhail Fedor Gordeev

Joseph Patrick Martin, Jr

Salvatore Charges Perricone

Robert L Hoffman

Vara Prasad Venkata Negandra Josyula

The present invention provides antibacterial agents having the formulae I, II, and III described herein.

N-aryl-2-oxazolidinone-5-carboxamides and their derivatives

The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.

Indolone oxazolidinones and derivatives thereof

The present invention provides oxazolidinones having a benzannelated 6- or 7-membered heterocycle as antibacterial agents.

Oxazolidinones having a benzannulated 6-  or 7-membered heterocycle

N-Aryl-2-oxazolidinone-5-carboxamides and their derivatives

Oxazolidinone antibacterial agents having a thiocarbonyl funtionality

Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings

A process for preparing a compound of the formula I:

Phenyloxazolidinones having a C-C bond to 4-8 membered heterocyclic rings

The present invention provides compounds of Formula 1

Oxazolidinone antibacterial agents having a thiocarbonyl functionality

A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1 ; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -aryl, --COR.sub.1-1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1-1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h -aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h -aryl, or halo; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.

The present invention provides compounds of formula I and formula II useful as antimicrobial agents wherein R.sub.1 is methyl, ethyl, cyclopropyl, or dichloromethyl; R.sub.2 and R.sub.3 are independently hydrogen or fluoro; R.sub.4 is ethyl or dichloromethyl. The invention also relates to a novel assay for determining the inhibitory activity of oxazolidinones to human monoamine oxidase.

S-oxide and S,S-dioxide tetrahydrothiopyran phenyloxazolidinones

A process for preparing a compound of the formula I: ##STR1## or pharmaceutical acceptable salts thereof wherein X is --NR,--, --S(O).sub.g --, or --O--; R.sub.1 is --H, C.sub.1-6 alkyl optionally substituted with one or more --OH, --CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -aryl, --COR.sub.1-1, 13 COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1-1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h -aryl, or --(CO).sub.i -Het; R.sub.2 is --H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h -aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are --H or halo; R.sub.5 is --H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.

Phenyloxazolidinones having a c-c bond to 4-8 membered heterocyclic rings

A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.

Alkyl substituted piperadinyl and piperazinyl anti-AIDS compounds

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Wayland, MI, United States of America

Toni-Jo Poel