Heterobicyclic sulfonamide and sulfonic ester derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/04 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) C07D 209/08 (2006.01) C07D 209/12 (2006.01) C07D 209/30 (2006.01) C07D 209/34 (2006.01) C07D 209/42 (2006.01) C07D 231/56 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2146961

Novel heterobicyclic sulfonamide and sulfonic ester derivatives represented by the following general formula(I), which exhibit an antitumor activity and are lowly toxic, and processes for the preparation thereof. A sulfonamide derivative and a sulfonic ester derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: (see formula I) wherein A represents a monocyclic or bicyclic aromatic ring which may be substituted; B represents a six-membered unsaturated hydrocarbon ring or a six-membered unsaturated heterocycle containing one nitrogen atom, each of which may be substituted; C represents a five-membered heterocycle containing one or two nitrogen atoms which may be substituted; W represents a single bond or a group represented by formula -CH = CH-; X represents a group represented by formula -N(R1)- or oxygen; Y represents carbon or nitrogen; Z represents a group represented by formula -N(R2)- or nitrogen; and R1 and R2 may be the same or different from each other and each represent hydrogen or lower alkyl.

L'invention concerne des nouveaux dérivés bicycliques de sulfonamide hétérocyclique et d'esters sulfonique représentés par la formule générale (I) et présentant une activité antitumorale ainsi qu'une toxicité réduite. L'invention porte également sur des sels pharmacologiquement acceptables desdits dérivés ainsi que sur un procédé de production de ces derniers. Dans ladite formule le cycle A représente un groupe aromatique mono- ou bicyclique éventuellement substitué; le cycle B représente un cycle hydrocarbure insaturé à 6 éléments éventuellement substitué ou un groupe hétérocyclique insaturé à 6 éléments contenant un atome d'azote; le cycle C représente un groupe hétérocyclique à 5 éléments éventuellement substitué contenant un ou deux atomes de carbone; W représente une liaison simple ou -CH=CH-; X représente -NR<1>- ou oxygène; Y représente carbone ou azote; Z représente -NR<2>- ou azote; et R<1> et R<2> représentent chacun indépendamment hydrogène ou alkyle inférieur.

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