Astrazeneca Ab

Michael Barry Gravestock

Neil James Hales

Sheila Irene Hauck

Fei Zhou

Folkert Reck

Daniel Robert Carcanague

Paul Robert Fleming

Michael John Betts

Neil James Hale

Stuart D Mills

Brian A Sherer

Gregory Steven Basarab

Michael Lingard Swain

Kenneth Gregory Hull

George Byron Mullen

Oluyinka Morenike Green

Pamela Hill

Haihong Ni

Marc Michel Girardot

Ian Richard Matthews

David Alan Griffin

Brian Dangel

Greg Basarab

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

Antibacterial piperdine derivatives

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

Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R, R, Rare for example selected from hydrogen, (1&#x2013;4C)alkyl, (1&#x2013;4C)alkoxy-carbonyl, (1&#x2013;4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.

Antibacterial oxalidinones

Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N&#x2014;HET is for example triazolyl substituted with R; Ris for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R, R, Rare for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.

Antibacterial 1,3-oxazolidin-2-one derivatives

Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof,   

Oxazolidinone derivatives with antibiotic activity

Heterocyclylaminomethyloxazolidinones as antibacterials

Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: Rand Rare independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, RCO&#x2014;, RSO&#x2014; or RCS&#x2014;; wherein Ris, for example, optionally substituted (1&#x2013;10C)alkyl or RC(O)O(1&#x2013;6C)alkyl wherein Ris optionally substituted (1&#x2013;10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described 

Substituted isoxazolines and their use as antibacterial agents

Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolyzable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R and R are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R CO&mdash;, R SO &mdash; or R CS&mdash;; wherein R is, for example, optionally substituted (1-10C)alkyl or R C(O)O(1-6C)alkyl wherein R is optionally substituted (1-10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

Growing community of inventors

Waltham, MA, United States of America

Michael Barry Gravestock