Beecham Group Plc

Smithkline Beecham Corporation

Glaxo Group Limited

Glaxosmithkline LLC

Glaxosmithkline Istrazivacki Center Zagreb D.o.o

Eric Hunt

Steven Dabbs

Colin Henry Frydrych

Jeremy David Hinks

Steven Coulton

Francis Dominic Sanderson

Gary Woodnutt

Valerie Joan Berry

Thomas T Howarth

Steven Howard

Andrew Kenneth Takle

Gerald Brooks

George Burton

Stephen Frederick Moss

Andrew Keith Forrest

Antoinette Naylor

Drazen Pavlovic

Sulejman Alihodzic

Edward G Brain

Vlado Stimac

Stephen Christopher Martin Fell

Steven Aitken

Alfred John Eglington

Andrew K Forrest

Samra Kapic

Ivana Palej

Stephen Dabbs

The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.

Pleuromutilin derivatives as antimicrobials

The present invention relates to 14- or 15-membered macrolides substituted at the 4&#x2033; position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.

Ether linked macrolides useful for the treatment of microbial infections

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

2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which Ris a 5- or 6-membered optionally substituted heteroaryl group; and Ris vinyl or ethyl, are useful in the treatment of bacterial infections

2-Hydroxy-mutilin carbamate derivatives for antibacterial use

Pleuromutilin compounds of the formula:are of use in anti-bacterial therapy.

Heterocyclic mutilin esters and their use as antibacterials

Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R,is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use

Disclosed are a carbapenem compound represented by formula (I) and processes to its preparation.

Disclosed are 1-, 6- and 2-substituted-1-carba-2-penem-3-carboxylic acids, a process for their preparation, pharmaceutical compositions comprising said compounds and a method of using them to treat bacterial infections.

9-(N'-substituted hydrazone) derivatives of certain erythromycin compounds are novel, antibacterially active compounds which can be prepared by treatment of the corresponding 9-imine derivative with an N'-substituted hydrazine.

9-(N'-substituted hydrazone) derivatives of erythromycins

Antibacterially active 11,12-carbonate derivatives of erythromycin 9-(optionally substituted)oxime and 9-imino compounds and their pharmaceutically acceptable ester or acid addition salt thereof: ##STR1## wherein R.sup.1 denotes an oxime group, a substituted oxime group, or an imino group;

Erythromycin a 11,12-carbonate 9-oxime derivatives

An antibacterially active 9,11-O-methylene derivative of 9-dihydroerythromycin wherein the methylene group is optionally substituted by one or two hydrocarbon groups. In particular, compounds of formula I and their pharmaceutically acceptable esters and acid addition salts: ##STR1## wherein: R.sup.1 and R.sup.2 are each H, optionally substituted hydrocarbon, or optionally substituted 5 or 6-membered O or S heterocyclyl, or

9,11-O-methylene derivatives of 9-dihydroerythromycin

Compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, CO.sub.2 R.sub.2 is a carboxyl group, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable esterified carboxyl group, are useful for their .beta.-lactamase inhibitory activity and to synergize the antibacterial activity of penicillins and cephalosporin.

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Harlow, United Kingdom

Eric Hunt