Smithkline Beecham Corporation

Beecham Group Plc

Novartis International Pharmaceutical, Ltd.

Replidyne, Inc.

Glaxo Group Limited

Pliva-Istrazivacki Institut

Richard Lewis Jarvest

Michael R Harnden

Andrew Keith Forrest

John Michael Berge

Graham R Geen

Robert John Sheppard

John Stephen Elder

Dieter Hamprecht

Catherine Simone Victoire Frydrych

Jian Qiu

Gorjana Lazarevski

Lee James Beeley

Joseph Guiles

Drazen Pavlovic

Sulejman Alihodzic

Theodore M Tarasow

David Jonathan McNair

Dieter Wolfgang Hamprecht

Pamela Brown

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.

14 and 15 membered ring compounds

The present invention relates to compounds 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.

Compounds

Compounds of formula (I): are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.

Compositions and methods for topical administration of 2-NH-heteroarylimidazoles

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

Pleuromutilin derivatives

Novel substituted thiophenes that are inhibitors of bacterial methionyl t-RNA synthetase (MRS) are disclosed. Also disclosed are method for their preparation and their use in therapy as anti-bacterial agents.

Substituted thiophenes with antibacterial activity

Compounds of formula (I):are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.

2-NH-heteroarylimidazoles with antibacterial activity

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

Antiviral guanine derivatives

The present invention provides a process for the synthesis of penciclovir and famciclovir by 9-substituting 2-amino-6-chloropurine (ACP) with an appropriate side chain precursor, followed by conversion of the 6-chloro moiety to a hydroxy moiety (i.e. to form a guanine) or hydrogen (to form a 2-aminopurine), respectively.

Process for the preparation of purine derivatives

Quinolones used as MRS inhibitors and bactericides

The present invention provides for the compound and synthesis of 9-(4-acetoxy-3-acetoxymethylbutyl)-2-amino-6-chloropurine, which compound is an intermediate involved in the synthesis of penciclovir and famciclovir.

The present invention provides a process for the synthesis of penciclovir and famciclovir by 9-substituting 2-amino-6-chloropurine (ACP) with an appropriate side chain precursor, followed by conversion of the 6-chloro moiety to a hydroxy moiety (i.e. to form a guanine) or hydrogen (to form a 2-aminopurine), respectively; and 2-acetoxymethyl-4-halo-butyl-1-yl acetates.

2-acetoxymethyl-4-halo-butyl-1-yl acetates

The present invention provides a process for the synthesis of penciclovir and famciclovir by 9-substituting the compound 2-amino-6-chloropurine (ACP) with 2-acetoxymethyl-4-(leaving group)-but-1-yl acetate, followed by displacement of the 6-chloro moiety with a hydroxy moiety (i.e. to form a guanine derivative) or with hydrogen (to form the 2-aminopurine derivative), respectively.

##STR1## A compound of formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein R.sup.0 represents a substituted or unsubstituted aryl group; R.sup.1 represents hydrogen or an alkyl group; R.sup.2 represents a moiety of formula (a) wherein R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R.sup.4 together with R.sup.5 represents (CH.sub.2).sub.n wherein n is 2, 3 or 4; T represents hydrogen, nitrile or a group --CO.R.sup.s wherein R.sup.s represents hydroxy, alkoxy or a group --NR.sup.t R.sup.u wherein R.sup.t and R.sup.u independently represent hydrogen, alkyl or R.sup.t and R.sup.u together with the nitrogen to which they are attached represent a saturated heterocyclic group; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine.

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Stevenage, United Kingdom

Richard Lewis Jarvest