Actelion Pharmaceuticals Ltd

Idorsia Pharmaceuticals Ltd

Daniel Ritz

Georg Rueedi

Christian N Hubschwerlen

Jean-Philippe Surivet

Cornelia Zumbrunn-Acklin

Cornelia Zumbrunn

Christian Hubschwerlen

The invention relates to aryloxazolidinone compounds of formula I: wherein Y represents hydrogen or certain chemical groups. These compounds are useful antimicrobial agents effective against a variety of pathogens including inter alia Gram-negative aerobic and anaerobic bacteria.

Aryloxazolidinone antibiotic compounds

The invention relates to compounds of formula I whereinis a bond or is absent, V is CH, CRor N; Ris H or, ifis a bond, may also be alkoxy; Ris H or halogen; U is CH or N whenis a bond, or, ifis absent, U is CH, NH or NR; Ris H, alkylcarbonyl or &#x2014;CH&#x2014;R; Ris H, alkyl or hydroxyalkyl; Ris H or, if n is not 0 and Ris H, may also be OH; Ris H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; Ris hydroxyalkyl, carboxy, alkoxycarbonyl or &#x2014;(CH)&#x2014;NRR, q being 1, 2 or 3 and each of Rand Rindependently being H or alkyl or Rand Rforming with the N atom bearing them a ring; Ris alkyl or hydroxyalkyl; A is &#x2014;(CH)&#x2014;, &#x2014;CHCHCH(OH)&#x2014; or &#x2014;COCHCH(OH)&#x2014;; G is substituted phenyl or Gor G wherein Q is O or S and X is CH or N; and Y, Yand Ymay each be CH or N; and n is 0 when A is &#x2014;CHCHCH(OH)&#x2014; or &#x2014;COCHCH(OH)&#x2014;, and n is 0, 1 or 2 when A is &#x2014;(CH)&#x2014;, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts thereof.

Tricyclic oxazolidinone antibiotic compounds

The present invention relates to antibacterial compounds of formula (I) wherein '----' is a bond or is absent, V is CH, CRor N; Ris H or, if '----' is a bond, may also be alkoxy; Ris cyano, alkyl, or ethynyl; U is CH or N when &#x201c;----&#x201d; is a bond, or, if &#x201c;----&#x201d; is absent, U is CH, NH or NH; Ris H, alkylcarbonyl or CH&#x2014;R; Ris H, alkyl or hydroxyalkyl; Ris H or, if n is not 0 and Ris H, may also be OH; Ris H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; Ris hydroxyalkyl, carboxy, alkoxycarbonyl or &#x2014;(CH)&#x2014;NRR, q being 1, 2 or 3 and each of Rand Rindependently being H or alkyl or Rand Rforming with the N atom bearing them a ring; Ris alkyl or hydroxyalkyl; A is &#x2014;(CH)&#x2014;, &#x2014;CHCHCH(OH)&#x2014; or &#x2014;COCHCH(OH)&#x2014;; G is substituted phenyl or Gor G, wherein Q is O or S and X is CH or N; and Y, Yand Ymay each be CH or N; and n is 0 when A is &#x2014;CHCHCH(OH)&#x2014; or &#x2014;COCHCH(OH)&#x2014;, and n is 0, 1 or 2 when A is &#x2014;(CH)&#x2014;, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.

The invention relates to antibacterial compounds of formula I whereinis a bond or is absent, V is CH, CRor N; Ris H or, ifis a bond, may also be alkoxy; Ris notably H or halogen; U is CH or N whenis a bond, or, ifis absent, U is CH, NH or NR; Ris H, alkylcarbonyl or &#x2014;CH&#x2014;R; Ris H, alkyl or hydroxyalkyl; Ris H or, if n is not 0 and Ris H, may also be OH; Ris H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; Ris hydroxyalkyl, carboxy, alkoxycarbonyl or &#x2014;(CH)&#x2014;NRR, q being 1, 2 or 3 and each of Rand Rindependently being H or alkyl or Rand Rforming with the N atom bearing them a ring; Ris alkyl or hydroxyalkyl; A is &#x2014;(CH)&#x2014;, &#x2014;CHCHCH(OH)&#x2014; or &#x2014;COCHCH(OH)&#x2014;; G is substituted phenyl or Gor G wherein Q is O or S and X is CH or N; and Y, Yand Ymay each be CH or N; and n is 0 when A is &#x2014;CHCHCH(OH)&#x2014; or &#x2014;COCHCH(OH)&#x2014;, and n is 0, 1 or 2 when A is &#x2014;(CH)&#x2014;, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4;and to salts of such compounds.

Growing community of inventors

Allschwil, Switzerland

Daniel Ritz