Piperazinedione compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 241/18 (2006.01) A61K 31/4965 (2006.01) A61K 31/497 (2006.01) C07D 401/06 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2408649

The use of a compound for treatment of a tumor, comprising administering to a subject in need thereof an effective amount of a compound having the following formula: (see above formula) wherein A is C(R a R b); Z is R3O-(Ar)-B, in which B is C(R c); Ar is pyridyl linked to B at position 2; and R3 is H, alkyl substituted with aryl, or aryl; in which aryl is unsubstituted or substituted with one or more substitutents selected from the group consisting of halogen, hydroxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, C1~C6 alkyl, C1~C6 alkenyl, C1~C6 alkoxy, and aryl; each of R1 and R2, independently, is H, or C(O)R d; and one of R a and R b is thienyl, furyl, pyridinyl, indolyl, 2-oxo-indolyl, aryl, alkyl, or alkyl substituted with aryl, and each of the other of R a and R b, and R c, and R d, independently, is H, alkyl, or aryl; in which alkyl and aryl are unsubstituted or substituted with one or more substitutents selected from the group consisting of halogen, hydroxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, C1~C6 alkyl, C2~C6 alkenyl, C1~C6 alkoxy, and aryl.

L'invention concerne les composés de pipérazinedione de la formule (I) dans laquelle ---- et ---- représentent indépendamment une simple liaison ou une double liaison; A est H ou CH(R?a¿R?b¿) lorsque ---- est une simple liaison, ou C(R?a¿R?b¿) lorsque ---- est une double liaison; Z est R¿3?O-(Ar)-B avec B étant CH(R?c¿) lorsque ---- est une simple liaison, ou C(R?c¿) lorsque ---- est une double liaison; Ar est hétéroaryle; R¿3? est H, alkyle, aryle, hétéroaryle, C(O)R?d¿, C(O)OR?d¿, C(O)NR?d¿R?e¿, ou SO¿2?R?d¿, R¿1? et R¿2? sont indépendamment H C(O)R?d¿, C(O)OR?d¿, C(O)NR?d¿R?e¿, ou SO¿2?R?d¿; et R?a¿, R?b¿, R?c¿, R?d¿, et R?e¿ sont indépendamment H, alkyle, aryle, hétéroaryle, cyclyle, or hétérocyclyle. Eventuellement, R?a¿ et R?b¿ pris ensemble sont cyclyle ou hétérocyclyle; et également éventuellement, R¿1? et R?a¿ ou R¿1? et R?b¿ pris ensemble sont cyclyle ou hétérocyclyle.

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