British Biotech Pharmaceuticals Limited

De Novo Pharmaceuticals Limited

Vernalis (oxford) Limited

British Biotech

Raymond Paul Beckett

Mark Whittaker

Andrew Miller

Zoe Marie Spavold

Fionna Mitchell Martin

Michael George Hunter

John Martin Clements

Michael John Crimmin

Lisa Marie Pratt

Steven Launchbury

Richard Simon Todd

Stephen John Davies

Jonathan P Dickens

Barry Porter

Paul Gane

Kenneth Keavey

Andrew Paul Ayscough

Christopher David Floyd

Helen Katherine Smith

Daniel Christopher Brookings

Martin John Clements

Jac Wijkmans

Lydia Saroglou

Mark Hampton Davis

Henriette Willems

Alison Jane Thompson

Compounds of formula (I) or a pharmaceutically or veterinarily acceptable salts thereof wherein Rrepresents hydrogen, C-Calkyl or C-Calkyl substituted by one or more halogen atoms; Rrepresents a group R-(ALK)-, and A represents (i) a group of formula (IA): wherein the compounds inhibit the activity of bacterial PDF enzyme.

Antibacterial agents

Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(&#x2550;O) or of formula C(&#x2550;O)NH(OH); Rrepresents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(&#x2550;O), a hydroxy or amino group; Rrepresents a radical of formula R&#x2014;(X)-(ALK)- wherein Rrepresents hydrogen, or an optionally substituted c-Calkyl, C-Calkenyl, C-Calkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C-Calkylene, C-C6 ?alkenylene, or C-Calkynylene radical, and may be interrupted by one or more non-adjacent NH&#x2014;, &#x2014;O&#x2014; or S&#x2014; linkages, X represents NH&#x2014;, &#x2014;O&#x2014; or S&#x2014;, and m and n are independently 0 or 1; Rrepresents hydrogen, C-Calkyl, or benzyl; and Ris as defined in the specification.

Antimicrobial agents

Compounds of formula (I) are antibacterial agents: wherein: Z is &#x2014;N(OH)CH(&#x2550;O) or &#x2014;C(&#x2550;O)NH(OH); Rrepresents hydrogen, methyl or trifluoromethyl or, except when Z is a radical of formula &#x2014;N(OH)CH(&#x2550;O), a hydroxy, halo or amino group; R, Rand Rindependently represents hydrogen or a group R&#x2014;(D)&#x2014;(ALK)&#x2014; wherein R, D, n, m and ALK are as defined in the claims; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom to which Rand Rare attached and the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen 

Bacterial enzyme inhibitors

A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme: wherein A represents a group of formula (IA) or (IB) and wherein Ris hydrogen, Ris n-butyl, benzyl or cyclopentylmethyl, Ris hydrogen, Ris tert-butyl, iso-butyl, benzyl or methyl, Ris hydrogen or methyl and Ris methyl.

Selected compounds of formula (I) are antibacterial agents: formula (I) wherein Rrepresents a substituted or unsubstituted C-Calkyl, cycloalkyl (C-Calkyl)- or aryl (C-Calkyl)-group, and A represents a group of formula (IA), or (IB) wherein Rrepresents the side chain of a natural or non-natural alpha amino acid, and Rand Rare each independently hydrogen or C-Calkyl, heterocyclic or aryl (C-Calkyl)-, Rand Rwhen taken together with the nitrogen atom to which they are attached from an optionally substituted saturated heterocyclic ring of 3 to 8 atoms which ring is optionally fused to a carbocyclic or second heterocyclic ring

Antibacterial hydroxamic acid derivatives

Compounds of formula (I) are antibacterial agents wherein: R and R , taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R and R are as defined in the specification.

Compounds of formula (I) are in the preparation of antibacterial agents, wherein: R represents hydrogen, C -C alkyl or C -C alkyl substituted by one or more halogen atoms; R represents a group R (X) &mdash;(ALK)&mdash; wherein R represents hydrogen, a C -C alkyl, C -C alkenyl, C -C alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C -C )alkyl, (C -C )alkoyy, hydroxy, mercapto, (C -C )alkylthio, amino, halo, trifluoromethyl, cyano, nitro, &mdash;COOH, &mdash;CONH , &mdash;COOR , &mdash;NHCOR , &mdash;CONHR , &mdash;NHR , &mdash;NR R , or &mdash;CONR R wherein R and R are independently a (C -C )alkyl group, and ALK represents a straight or branched divalent C -C alkylene, C -C alkenylene, or C -C alkynylene radical, which may be interrupted by one or more non-adjacent &mdash;NH&mdash;, &mdash;O&mdash; or &mdash;S&mdash; linkages, X represents &mdash;NH&mdash;, &mdash;O&mdash; or &mdash;S&mdash;, and n is 0 or 1, R represents hydrogen or C -C alkyl, R represents the characterising group or a natural or non-natural &agr; amino acid in which any functional groups may be protected; and R represents an ester or thioester group.

N-formyl hydroxylamine derivatives as antibacterial agents

Compounds of formula (I) are antibacterials wherein: R represents hydrogen, or C -C alkyl or C -C alkyl substituted by one or more halogen atoms; R represents a group R &mdash;(X) &mdash;(ALK) &mdash; wherein R represents hydrogen, or a C -C alkyl, C -C alkenyl, C -C alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C -C )alkyl, (C -C )alkoxy, hydroxy, mercapto, (C -C )alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, &mdash;COOH, &mdash;CONH , &mdash;COOR , &mdash;NHCOR , &mdash;CONHR , &mdash;NHR , &mdash;NR R , or &mdash;CONR R wherein R and R are independently a (C -C )alkyl group, and ALK represents a straight or branched divalent C -C alkylene, C -C alkenylene, or C -C alkynylene radical, and may be interrupted by one or more non-adjacent &mdash;NH&mdash;, &mdash;O&mdash; or &mdash;S&mdash; linkages, X represents &mdash;NH&mdash;, &mdash;O&mdash; or &mdash;S&mdash;, and m and n are independently 0 or 1; and A represents a group as defined in the specification.

Hydroxamic acid derivatives as antibacterials

Metalloproteinase inhibitors

The present invention relates to therapeutically active hydroxamic acid, N-formyl-N-hydroxyamino and carboxylic acid derivatives, their preparation, and pharmaceutical compositions containing them. These compounds are useful in the inhibition of metalloproteases, such as stromelysin, gelatinase, matrilysin, and collagenase. These compounds are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.

Growing community of inventors

Oxford, United Kingdom

Raymond Paul Beckett