C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 285/08 (2006.01) A61K 31/41 (2006.01) A61K 31/495 (2006.01) C07D 213/83 (2006.01) C07D 241/26 (2006.01) C07D 241/28 (2006.01) C07D 285/135 (2006.01) C07D 295/155 (2006.01) C07D 417/04 (2006.01) C07D 417/12 (2006.01)
Patent
CA 2294581
This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; formula (1) is Ar2, Ar2CH2- or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
Cette invention concerne des composés de formule (I), des formes N-oxyde, les sels d'addition acide pharmaceutiquement acceptables et les formes stéréochimiquement isomères de ces derniers. Dans la formule, X représente CH ou N; R<1> représente hydrogène, alkyle C1-6, alkyloxy C1-6, alkylthio C1-6, amino, mono ou di(alkyle C1-6)amino, Ar<1>, Ar<1>NH-, cycloalkyl C3-6, hydroxyméthyle ou benzyloxyméthyle; R<2> représente hydrogène, alkyle C1-6, amino, aminocarbonyle, mono ou di(alkyle C1-6)amino, alkyloxycarbonyle C1-6, alkylcarbonylamino C1-6, hydroxy ou alkyloxy C1-6; R<3>, R<4> et R<5> sont indépendamment sélectionnés entre hydrogène, halo, alkyle C1-6, alkyloxy C1-6, trifluorométhyle, nitro, amino, cyano, azido, alkyloxy C1-6, alkyle C1-6, alkylthio C1-6, alkyloxycarbonyle C1-6 ou Het<1>; la formule (1) représente Ar<2>, Ar<2>CH2- ou Het<2>; Ar<1> et Ar<2> représente phényle facultativement substitué; Het<1> et Het<2> représentent des hétérocycles monocycliques facultativement substitués. On décrit ces composés ayant une activité inhibant l'angiogénèse, leur préparation, des compositions contenant ces composés ainsi que leur utilisation en tant que médicament.
Ceusters Marc Andre
Luyckx Marcel Gerebernus Maria
Stokbroekx Raymond Antoine
Tuman Robert W.
Van Der Aa Marcel Jozef Maria
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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