Pharmacia & Upjohn Company

The Upjohn Co.

Pfizer Corporation

Pharmacia Corporation

Pharmacia & Upjohn

Richard Charles Thomas

Michael R Barbachyn

Toni-Jo Poel

Gary J Cleek

Donna Lee Romero

Douglas K Hutchinson

David R White

Adam Renslo

Gary W Luehr

David John Anderson

Donn G Wishka

Joel Morris

Upinder Singh

Stephen T Schlachter

Paul A Aristoff

Mikhail Fedorovich Gordeev

Michael D Ennis

Richard Allen Nugent

Michael J Murphy

Gordon L Bundy

Herman W Smith

Joseph Walter Strohbach

Robert C Gadwood

Ronald B Gammill

Steven J Brickner

Harvey I Skulnick

Robert Louis Hoffman

Suvit Thaisrivongs

John R Palmer

Fritz Reusser

Paul D May

Paul D Johnson

Steven Ronald Turner

Vara Prasad Venkata Nagendra Josyula

Lisa Marie Thomasco

Karen Rene Romines

Hiroyoshi Yamada

Mikhail Fedor Gordeev

Paul K Tomich

Gary Edward Zurenko

David R Graber

Edward L Fritzen, Jr

Michael John Bohanon

Robert L Hoffman

James J Vavra

Chih-Ping Yang

Vara Prasad Venkata Negandra Josyula

Lee S Banitt

Qingwei Zhang

Irene W Althaus

Gary L Cleek

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

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

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

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

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 ##STR1## or a pharmaceutical acceptable salt thereof wherein Q, X, Y and R.sub.1 are as defined in the claims which are antibacterial agents.

Isoxazoline derivatives useful as antimicrobials

The present invention provides novel substituted amionphenyl isoxazoline derivatives of formula I ##STR1## wherein R.sub.1 is H, alkyl, cycloalkyl, alkoxy, amino, or alkylamino; X and Y are the same and different and are H, F, or CH.sub.3 ; W is O, or S;

Substituted aminophenyl isoxazoline derivatives useful as antimicrobials

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

Alpha-substituted pyrimidine-thioalkyl and alkylether compounds as

The present invention provides compounds of formula 1 ##STR1## or pharmaceutical acceptable salts thereof wherein A and R.sub.1 are as defined in the claims which are antibacterial agents.

Pyrimidine-thioalkyl and alkylether compounds

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.

This invention provides novel oxazolidinone derivatives represented by chemical Formula (I), or pharmaceutically acceptable salts thereof: ##STR1## wherein X is NR.sub.1, CR.sub.2 R.sub.3, O, S, SO, or SO.sub.2 ; and Z is NR.sub.4, S, SO, SO.sub.2 or O. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.

Oxazolidinone antibacterial agent with tricyclic substituents

Bicyclic oxazine and thiazine oxazolidinone antibacterials

Growing community of inventors

Kalamazoo, MI, United States of America

Richard Charles Thomas