Actelion Pharmaceuticals Ltd

Idorsia Pharmaceuticals Ltd

Georg Rueedi

Christian N Hubschwerlen

Jean-Philippe Surivet

Cornelia Zumbrunn-Acklin

Cornelia Zumbrunn

Cornelia Zumbrunn Acklin

Daniel Ritz

Sylvaine Cren

Astrid Friedli

John-Philippe Surivet

Christian Hubschwerlen

Daniel Bur

Markus Gude

Jean-Luc Specklin

Philippe Panchaud

Stephanie Enderlin-Paput

Stefan Diethelm

Verena Kaegi-egger

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 antibacterial compounds of formula I wherein M is one of the groups M, Mand Mrepresented below and either Rrepresents H and Rrepresents a cleavable group as defined in the claims or Rrepresents H and Rrepresents a cleavable group as defined in the claims;and salts thereof.

Substituted 1,2-dihydro-3H pyrrolo[1,2-c]imidazol-3 one antibacterials

The invention relates to antibacterial compounds of formula I wherein R, R, R, R, R, R, R, U, U, U, U, V, V, V, V, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.

Antibacterial basic biaromatic derivatives with aminoalkoxy substitution

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 invention relates to antibacterial compounds of formula I wherein R, U, V and A are as defined in the description, to pharmaceutical compositions containing them and uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections.

Quinolone derivatives

The invention relates to antibacterial compounds of formula I and salts thereof and methods of treating bacterial infection using the compounds. 

Antibacterial biaromatic derivatives

The invention relates to antibacterial compounds of formula I wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRwherein Ris fluorine; Rrepresents alkoxy, halogen or cyano; Rrepresents H, CHOH, CHN, CHNH, alkylcarbonylaminomethyl or triazol-1-ylmethyl; Rrepresents H, or, when n is 1, Rmay also represent OH, NH, NHCORor triazol-1-yl; A represents CR; K represents O, NH, OCH, NHCO, NHCH, CHNH, CHCH, CH&#x2550;CH, CHOHCHOH or CHR; Rrepresents H or together with Rforms a bond, or also Rcan represent OH when K is not O, NH, OCHor NHCO; Rrepresents OH or together with Rforms a bond; Rrepresents alkyl; m is 0 or 1 and n is 0 or 1; and G is as defined in the description;and to salts of such compounds.

5-aminocyclylmethyl-oxazolidin-2-one derivatives

The invention relates to antibacterial compounds of formula I wherein wherein

Antibacterial oxadiazolone derivatives

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 wherein

2-oxo-oxazolidin-3,5-diyl antibiotic derivatives

The invention relates to antibacterial compounds of formula I wherein G and K are as defined in the description; and salts of such compounds.

3,7-disubstituted octahydro-2H-pyrido[4,3-E][1,3]oxazin-2-one antibiotics

The invention relates to antibacterial compounds of formula (I), wherein Ris H, halogen, (C-C)alkyl or (C-C)alkoxy; Ris H, halogen, (C-C)alkyl, (C-C)alkoxy or pyrrolidin-1-yl; Ris H, halogen, (C-C)alkyl, (C-C)alkoxy, vinyl or 2-methoxycarbonyvinyl or Rand Rtogether with the two carbon atoms which bear them form a phenyl ring; Ris H, halogen, (C-C)alkyl or (C-C)alkoxy; and Ris H, (C-C)alkyl or cyclopropyl, or Rand Rform together a &#x2014;CHCHCH&#x2014; group; A is the divalent group &#x2014;CH&#x2014;, &#x2014;CHCH&#x2014;, #&#x2014;CH(OH)CH&#x2014;*, #&#x2014;CHN(R)&#x2014;* and &#x2014;CHNHCH&#x2014;, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; Ris H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.

Quinazoline-2,4-dione derivatives

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.

The invention relates to antibacterial compounds of formula I wherein Ris alkoxy or halogen; U and V each independently are CH or N;is a bond or is absent; W is CH or N or, whenis absent, W is CHor NH, with the proviso that U, V and W are not all N; A is a bond or CH; Ris H or, provided A is CH, may also be OH; m and n each independently are 0 or 1; D is CHor a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C-C)alkoxy and halogen, or G is a group Gor G wherein Z, Zand Zmay each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH;and salts of such compounds.

Oxazolidinyl antibiotics

The invention relates to antibacterial compounds of formula I wherein wherein Q represents O or S, Z represents CH or N, Rrepresents halogen and Rrepresents alkyl;

Growing community of inventors

Allschwil, Switzerland

Georg Rueedi