Idorsia Pharmaceuticals Ltd

Actelion Pharmaceuticals Ltd

Jean-Christophe Gauvin

Jean-Philippe Surivet

Azely Mirre

Jean-Luc Specklin

Gaelle Chapoux

Etienne Ochala

Christian N Hubschwerlen

Philippe Panchaud

Christine Schmitt

Gaëlle Chapoux

The invention relates to antibacterial compounds of formula I  

1,2-dihydro-3H-pyrrolo[1,2-C]imidazol-3-one derivatives and their use as antibacterial agents

The invention relates to antibacterial compounds of formula I wherein Ris H or halogen; Ris alkynyloxy or the group M; Ris H or halogen; M is one of the groups wherein A is a bond, CHCH, CH&#x2550;CH or C&#x2261;C and R, R, R, Rand Rare as defined in claimand salts thereof.

Antibacterial 2H-indazole derivatives

The invention relates to antibacterial compounds of formula I wherein Ris H or halogen; Ris the group M; Ris H or halogen; M is Mor M wherein A is a bond or C&#x2261;C; Ris H or halogen; Ris H, alkoxy or halogen; Ris H, alkoxy, hydroxyalkoxy, hydroxyalkyl, 1,2-dihydroxyethyl, dialkylamino, 1-hydroxymethyl-cycloprop-1-yl, 1-((dimethylglycyl)oxy)methyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, morpholin-4-ylalkyl or morpholin-4-ylalkoxy; and Ris a group as defined in claimand salts thereof.

Antibacterial quinazoline-4(3H)-one derivatives

The invention relates to antibacterial compounds of formula I wherein X is N or CH; Ris H or halogen; Ris alkynyloxy or the group M; Ris H or halogen; M is one of the groups Mand Mrepresented below wherein A is a bond, CHCH, CH&#x2550;CH or C&#x2261;C; Ris H or halogen; Ris H, alkoxy or halogen; Ris H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and Ris hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl, 1-(2-aminoacetyl)azetidin-3-yl, 1-glycylazetidin-3-yl, 1-(2-amino-2-methylpropanoyl)azetidin-3-yl, 3-(2-aminoacetamido)cyclopentyl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl or 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl; and salts thereof.

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Allschwil, Switzerland

Jean-Christophe Gauvin