Beecham Group Plc

Pfizer Corporation

Smithkline Beecham Corporation

Pzifer Inc.

George Burton

Stephen C Fell

John Hargreaves Bateson

John P Clayton

Brian Charles Gasson

Andrew W Taylor

Richard L Elliott

Desmond John Best

Kenneth D Hardy

Elzbieta Watson

Eric Hunt

Stephen Frederick Moss

Steven Coulton

Jeremy David Hinks

George R Fosker

Stephen Christopher Martin Fell

Neal Frederick Osborne

Graham Walker

Antoinette Naylor

Alfred John Eglington

A compound of formula (I):whereinRis hydrogen, optionally substituted (C)alkyl or optionally substituted aryl;Ris hydrogen, optionally substituted (C)alkyl or optionally substituted aryl; orRand Rtogether form an optionally substituted 5 or 6 membered heterocyclic ring with or without additional heteroatoms;Ris (C)alkyl which is unsubstituted or substituted by fluoro, a hydroxy group which is optionally protected by a removable hydroxy protecting group, or by an amino group which is optionally protected by a removable amino protecting group;Ris hydrogen or methyl; and&#x2014;CORis carboxy or a carboxylate anion or the group Ris a removable carboxy protecting group. This invention also relates to processes for its preparation, intermediates and pharmaceutical compositions comprising compounds of formula (I). Compounds of formula (I) which include pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof have a broad spectrum of anti-bacterial activity and show good stability towards DHP-1.

2-(pyrazol-3-yl)carbapenem derivatives

Process for the preparation of cephalosporin compounds and synthetic intermediates

Compounds of formula (I) or salts thereof: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a carboxy protecting group, pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4 represents hydrogen or up to four substituents; X is O, S, SO or SO.sub.2 ; Y is O, S, SO or SO.sub.2 ; n is 0 or 1; and m is 1 or 2. The compounds have antibacterial activity. Methods of synthesis of, and pharmaceutical formulations containing, compounds (I) are also described.

2-isocephem and oxacephem derivatives and use as antibacterial agents

A compound of formula (II) or a salt: ##STR1##

Cephaloporins and homologues

.beta.-Lactam antibiotics of formula (I) or a salt thereof, wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acy group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a readily removable carboxy protecting group; R.sup.4 represents up to four substituents; X is S, SO, SO.sub.2, O or CH.sub.2 ; m is 1 or 2; and n is 0, useful in the treatment of bacterial infec ##STR1##

Cephaloporins and homologues, preparations and pharmaceutical

3-substituted carbacephems

Alphalosporins and 1-carba-1-dethia cephalosporins

Cephalosporin compounds

2-isocephem and oxacephem derivatives, and use as antibacterial agents

Cephalosporin derivatives

.beta.-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido;

.beta.-Lactam antibiotics of the formula (Ia) or a pharmaceutically acceptable salt or pharmaceutically acceptable in vivo hydrolysable ester thereof are disclosed: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is a acyl group, in particular that of an antibacterially active cephalosporin; CO.sub.2 R.sup.6 is carboxy group or a carboxylate anion; R.sup.4 is a butenolide or butanolide ring, optionally substituted by one or two alkyl, dialkylamino, alkoxy, hydroxy or aryl groups, which may be the same or different, or, wherein two adjacent carbon atoms which are available for substitution define the common bond of an aromatic fused bicyclic system; X is S, SO, SO.sub.2, O or CH.sub.2 ; and the dashed line adjacent to R.sup.4 represents an optional double bond. Processes for the preparation of compounds together with intermediates for use therein are disclosed.

A compound having the partial structure (I) ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a group --COR.sup.5 or --CO--OR.sup.5 wherein R.sup.5 represents an optionally substituted hydrocarbon group; R.sup.3 is halogen and R.sup.4 is hydrogen, methoxy, hydroxymethyl or formamido. These compounds are suitably bicyclic .beta.-lactam antibiotics.

Antibacterial penicillins and cephalosporins

The preparation and use of 6,.alpha.-methoxy-6,.beta.-[2-(2-methylphenoxycarbonyl)-2-(thien-3-yl) acetamido] penicillanic acid of formula (II): ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.

Penicillin derivatives

Growing community of inventors

Wallington, United Kingdom

George Burton