Astrazeneca Ab

Zeneca Limited

Imperial Chemical Industries Limited

Neil James Hales

Michael Barry Gravestock

Philip N Edwards

Fei Zhou

Folkert Reck

Daniel Robert Carcanague

Michael S Large

Sheila Irene Hauck

Paul Robert Fleming

Alex Christian Comely

Sue Elizabeth Gibson

Robert Hugh Bradbury

Stuart D Mills

Michael Lingard Swain

Kenneth Gregory Hull

Alfred Arthur Rabow

David Timms

George Byron Mullen

Oluyinka Morenike Green

Derek W Young

Haihong Ni

Mark A Peplow

Alexander Louis Breeze

Marc Michel Girardot

The invention concerns bicyclic compounds of Formula I wherein the integers X, X, X, Ring A, R, Rand m are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of androgen-receptor associated conditions.

Bicyclic derivatives for use in the treatment of androgen receptor associated conditions-155

Compounds of Formula (1) and their pharmaceutically acceptable salts are described: Formula (1) Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. 

Pyrrol derivatives with antibacterial activity

A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: Wherein C is selected from (D) and (E), Ra, Ra, and Ra are independently selected from for example H, CF, Me and Et; Rb and R6b are independently selected from for example H, F, CF, Me and Et; Rb is for example optionally substituted diazolyl, triazolyl or tetrazolyl; Ris for example an optionally substituted 5- or 6-membered heterocyclic ring system. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described. 

Oxazolidinones as antibacterial agents

Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein &#x2014;N-HET is, for example, (Ic) or (If) wherein R1 is (1-4C)alkyl; wherein Rand Rare independently hydrogen or fluoro; wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

3-cyclyl-5-(nitrogen-containing 5-membered ring)methyl-oxazolidinone derivatives and their use as antibacterial agents

Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in (I) wherein C is for example wherein A and B are independently selected from Ra to Rb are independently selected from hydrogen and fluorine;Ra and Rb are independently selected from, for example, hydroxy, &#x2014;NHC(&#x2550;W)R, wherein W is O or S; Ris, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

Oxazolidinone and/or isoxazoline as antibacterial agents

Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein &#x2014;N-HET is, for example, (Ic) or (If) wherein R1 is, for example, halogen or a (1&#x2013;4C)alkyl group which is substituted by one substituent selected from, for example, hydroxy, (1&#x2013;4C)alkoxy, amino, cyano or azido; Q is selected from, for example, Q1 wherein Rand Rare independently hydrogen or fluoro;T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

Chemical compounds

Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, (I) R1a is NH(C&#x2550;W)Ror (a); W is O or S; Rand Rare for example H or F; Ris for example hydrogen, or halogen; Ris selected from hydrogen, (2&#x2013;6C)alkyl (optionally substituted); Rand Rare independently selected from hydrogen, and (1&#x2013;4C)alkyl (optionally substituted); wherein Ris either a hydroxymethyl substituent on C-4' of the isoxazoline ring; or Ris a hydroxymethyl substituent on C-5&#x2032; of the isoxazoline ring and the stereochemistry at C-5&#x2032; of the isoxazoline ring and at C-5 of the oxazolidinone ring is selected, such that the compound of formula (I) is a single diastereomer; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described 

Hydroxymethyl substituted dihydroisoxazole derivatives useful as antibiotic agents

The invention relates to new traceless linkers which use transition metal complexes to link a &pgr;-orbital containing substrate for subsequent synthesis by, for example, combinatorial chemistry or multiple parallel synthesis (MPS) to a support.

Transition metal complexes as linkers

The invention relates to the use of an immobilized transition metal carbonyl complex as a catalyst in the Pauson-Khand reaction and to processes using such as catalyst.

Catalyst for Pauson-Khand reaction

The present invention provides a phenanthroline derivative of formula (I)

Phenanthroline derivatives

The present invention provides a phenanthroline derivative of formula (I) ##STR1## wherein, for example, R.sup.1 is hydrogen, carboxy, cyano, nitro, (1-4C)alkyl, (1-6C)alkoxycarbonyl, (1-4C)alkylamino, (2-4C)alkanoyl, (1-4C)alkoxy-(2-4C)alkoxy-(2-4C)alkoxycarbonyl or N-�amino-(2-8C)alkyl!carbamoyl;

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Macclesfield, United Kingdom

Neil James Hales