C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 235/06 (2006.01) A61K 31/4184 (2006.01) A61P 25/00 (2006.01) C07D 235/14 (2006.01) C07D 401/08 (2006.01) C07D 403/08 (2006.01)
Patent
CA 2371174
The invention relates to a compound of formula (I) or (II), wherein A represents a saturated or mono-unsaturated carbocycle containing 3 to 8 carbon atoms which can also have a condensed benzol ring, whereby the rings can also be substituted with one or two different or identical radicals; R1 represents hydrogen, chlorine, fluorine, bromine, iodine, branched and unbranched C1-C6-alkyl, OH, nitro, CF3, CN, NR11R12, NH-CO-R13, O-C1-C4 alkyl; and R2 represents hydrogen, branched and unbranched C1-C6 alkyl, C1-C4 alkyl-phenyl. The invention also relates to the tautomeric forms, possible enantiomeric and diastereomeric forms, possible cis-trans isomers on the rings in A and their prodrugs. The substituted benzimidazoles of general formulas (I) and (II) are inhibitors of poly(ADP-ribose) polymerase (PARP), or poly(ADP-ribose) synthase (PARS), as it is also known and can be used for the treatment or prophylaxis of diseases which are associated with the increased enzyme activity of this enzyme.
L'invention concerne des composés correspondant aux formules (I) ou (II), dans lesquelles: A représente un carbocycle saturé ou insaturé, comportant 3 à 8 atomes de carbone, qui peut porter encore un cycle benzène condensé, les noyaux pouvant également être substitués par un ou deux restes différents ou identiques; R<1> représente hydrogène, chlore, fluor, brome, iode, alkyle C1-C6 ramifié ou non ramifié, OH, nitro, CF3, CN, NR<11>R<12>, NH-CO-R<13>, O-alkyle C1-C4; et R<2> représente hydrogène, alkyle C1-C6 ramifié ou non ramifié, alkyle C1-C4-phényle. L'invention concerne également les formes tautomères, les éventuelles formes énantiomères et diastéréomères, les éventuels isomères cis-trans, situés au niveau des noyaux de A, de ces composés, et leurs promédicaments. Les benzymidazoles substitués correspondant aux formules générales (I) et (II), constituent des inhibiteurs de la poly(ADP-ribose)polymérase (PARP), appelés aussi poly(ADP-ribose)synthase (PARS), et peuvent donc être utilisés pour le traitement et la prophylaxie de maladies qui sont associées à une activité élevée de cette enzyme.
Grandel Roland
Hoger Thomas
Kock Michael
Lubisch Wilfried
Muller Reinhold
Abbott Gmbh & Co. Kg
Basf Aktiengesellschaft
Robic
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