Actelion Pharmaceuticals Ltd

Hoffmann-la Roche Inc.

Morphochem Aktiengesellschaft Fur Kombinatorische Chemie

Other

Idorsia Pharmaceuticals Ltd

Morphochem Ag

Morphochem Aktiengesellschaft Fü Kombinatorische Chemie

Morphochem Aktiengesellschaft Fül Kombinatorische Chemie

Morphochem Aktiengesellschaft Fur Kominatorische Chemi

Morphochem Aktiengesellschaft Fuer Kombinatorische Chemie

Christian N Hubschwerlen

Jean-Philippe Surivet

Georg Rueedi

Jean-Luc Specklin

Cornelia Zumbrunn-Acklin

Daniel Baeschlin

Cornelia Zumbrunn Acklin

Christine Schmitt

Klaus Gubernator

Cornelia Zumbrunn

Philippe Panchaud

Robert Charnas

Ingrid Heinze

Gerard Schmid

Werner Hofheinz

Andre Furlenmeier

Hans P Isenring

Michael W Cappi

Daniel Ritz

Jean Phillippe Surivet

Hans Locher

Hans G Richter

Philippe Pflieger

Daniel Bur

Markus Gude

Stefan Müller

John-Philippe Surivet

Markus Bohringer

Daniel K Baeschlin

Synese Jolidon

Paul Hebeisen

Ivan Kompis

Sylvaine Cren

Pierre-Charles Wyss

Philippe Guerry

Hugues Matile

Erwin Gotschi

Jacques Chollet

Azely Mirre

Jean-Christophe Gauvin

Gaelle Chapoux

Astrid Friedli

Etienne Ochala

Rueedi Georg

Annabelle Perez Frutos Honer

Timo Rager

Gaëlle Chapoux

Stephanie Enderlin-Paput

Jawad Alzeer

Robert George Ridley

Annabelle Perez Frutos Höner

J L Specklin

Jean Philippe Surivet

Daniel Kaspar Baeschlin

Stefan Mueller

The present invention relates to crystalline forms of cadazolid.

Crystalline forms of cadazolid

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 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.

[object Object]

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 present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria: 

Oxazolidinone-quinolone hybrid antibiotics

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 3-ureidoisoquinolin-8-yl derivatives of formula I 

3-ureidoisoquinolin-8-yl 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 present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.

Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections

Growing community of inventors

Durmenach, France

Christian N Hubschwerlen