Fused polycyclic heterocycle derivatives

Details Fused polycyclic heterocycle derivatives Fused polycyclic heterocycle derivatives

C - Chemistry, Metallurgy

07

D

C07D 487/06 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 471/06 (2006.01) C07D 471/16 (2006.01) C07D 487/16 (2006.01) C07D 491/16 (2006.01) C07D 495/16 (2006.01) C07D 498/06 (2006.01) C07D 513/06 (2006.01)

Patent

CA 2220509

Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same. A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof: (see formula I) wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula -e-f (wherein a represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl; provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded. Which has an excellent antitumor activity.

L'invention porte sur de nouveaux dérivés hétérocycliques polycycliques de formule générale (I) ou leurs sels pharmacocompatibles présentant une très bonne activité antitumorale, et sur leur procédé d'obtention. Dans la formule (I), le noyau A représente un noyau aromatique monocyclique facultativement substitué ou un noyau bicyclique fusionné dont l'un des cycles au moins est un cycle aromatique; le noyau B représente pyrrole, 4H-1,4-dioxane, 4H-1,4-thiazine ou 4(1H)-pyridone; le noyau C représente un anneau aromatique monocyclique ou bicyclique fusionné facultativement substitué; et Y représente -e-f (dans lequel e représente un alkylène inférieur, et f représente amidino, guanidino, ou amino facultativement substitué par hydroxy, ou un alkyle inférieur présentant éventuellement un groupe alkylaminé inférieur); à l'exclusion de la combinaison dans laquelle les noyaux A et C représentent chacun un noyau aromatique monocyclique facultativement substitué.

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