Janssen Pharmaceutica Nv

Christophe Denis Adelinet

Marc Gaston Venet

Dominique Mabire

Imré Christian Csoka

Patrick René Angibaud

Eddy Jean Edgard Freyne

Isabelle Noëlle Constance Pilatte

Pierre-Henri Storck

Virginie Sophie Poncelet

Andrew Pate Owens

Laurence Anne Mevellec

Christophe Meyer

Bruno Roux

Jorge Eduardo Vialard

Laurence Françoise Bernadette Marconnet-Decrane

Jacqueline Anne Macritchie

Xavier Marc Bourdrez

James Edward Stewart Duffy

Elisabeth Thérèse Jeanne Pasquier

Elisabeth Thèrése Jeanne Pasquier

Imr&eacute; Christian Csoka

Isabelle Noelle Constance Pilatte

Laurence Francoise Bernadette Marconnet-Decrane

The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R, R, R, R, R, R, R, n, m and X have defined meanings.

Quinolinone derivatives as PARP and tank inhibitors

Quinolinone derivatives as PARP and TANK inhibitors

The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR; Rrepresents hydrogen, hydroxy, Calkyl or aryl; Rrepresents hydrogen; optionally substituted Calkyl; Ccycloalkyl; Calkenyl; aryl; Het; Rrepresents hydrogen, optionally substituted Calkyl, aryl, Het; Rrepresents hydrogen; hydroxy; mercapto; Calkyloxy; Calkylthio; aryloxy; arylthio; Het-oxy; Het-thio; optionally substituted Calkyl; optionally substituted Calkenyl; optionally substituted Calkynyl; optionally substituted Ccycloalkyl; optionally substituted Ccycloalkenyl; aryl; Het; or -Alk-NRR(i) or &#x2014;NRR(ii) wherein Alk represents Calkanediyl; and Rrepresents hydrogen, Calkyl, aryl, Het, (aryl or Het)Calkyl, (aryl or Het)carbonyl or (aryl or Het)Calkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Hetrepresents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

Retinoic acid mimetic anilides

The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR; Rrepresents hydrogen, hydroxy, Calkyl or aryl; Rrepresents hydrogen; optionally substituted Calkyl; Ccycloalkyl; Calkenyl; aryl; Het; or Rand Rtaken together may form a bivalent radical of formula &#x2014;(CH)&#x2014; wherein n is 2, 3, 4, 5 or 6; Rrepresents hydrogen, optionally substituted Calkyl, aryl, Het; Rrepresents hydrogen; hydroxy; mercapto; Calkyloxy; Calkylthio; aryloxy; arylthio; Het-oxy; Het-thio; optionally substituted Calkyl; optionally substituted Calkenyl; optionally substituted Calkynyl; optionally substituted Ccycloalkyl; optionally substituted Ccycloalkenyl; aryl; Het; or -Alk-NRR(i) or &#x2014;NRR(ii) wherein Alk represents Calkanediyl; and Rrepresents hydrogen, Calkyl, aryl, Het, (aryl or Het)Calkyl, (aryl or Het)carbonyl or (aryl or Het)Calkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Hetrepresents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

The present invention is concerned with compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR; Rrepresents hydrogen, hydroxy, Calkyl or aryl; Rrepresents hydrogen; optionally substituted Calkyl; Ccycloalkyl; Calkenyl; aryl; Het; or Rand Rtaken together may form a bivalent radical of formula &#x2014;(CH)&#x2014; wherein n is 2, 3, 4, 5 or 6; Rrepresents hydrogen, optionally substituted Calkyl, aryl, Het; Rrepresents hydrogen; hydroxy; mercapto; Calkyloxy; Calkylthio; aryloxy; arylthio; Het-oxy; Het-thio; optionally substituted Calkyl; optionally substituted Calkenyl; optionally substituted Calkynyl; optionally substituted Ccycloalkyl; optionally substituted Ccycloalkenyl; aryl; Het; or -Alk&#x2014;NRR(i) or &#x2014;NRR(ii) wherein Alk represents Calkanediyl; and Rrepresents hydrogen, Calkyl, aryl, Het, (aryl or Het)Calkyl, (aryl or Het)carbonyl or (aryl or Het)Calkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Hetrepresents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

The present invention is concerned with compounds of formula

Retinoic acid mimetic anlides

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Iville, France

Christophe Denis Adelinet