Quinazoline derivatives and their use as pharmaceuticals

Details Quinazoline derivatives and their use as pharmaceuticals Quinazoline derivatives and their use as pharmaceuticals

C - Chemistry, Metallurgy

07

D

C07D 239/94 (2006.01) A61K 31/517 (2006.01) A61P 35/00 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 403/04 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 417/04 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2384291

The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O)2, NH or NR12 where R12 is hydrogen or C1-6 alkyl; R5 is selected from a group NHC(O)OR9, NHC(O)R9, NHS(O)2R9, C(O)R9, C(O)OR9, S(O)R9, S(O)OR9, S(O)2OR9, C(O)NR10 R11, S(O)NR10R11 S(O)ONR10R11, where R9, R10 or R11 are various specified organic groups; R6 is hydrogen, optionally substituted hydrocarbyl or optionally substituted heterocyclyl; R7 and R8 are various specified organic groups, and R1, R2, R3, R4 are independently selected from halogeno, cyano, nitro, C1-3alkylsulphanyl, -N(OH)R13-(wherein R7 is hydrogen, or C1-3alkyl), or R15X1-(wherein X1 represents a direct bond, -O-, -CH2-, -OCO-, carbonyl, -S-, -SO-, -SO2-, - NR16CO-, -CONR16-, -SO2NR16-, -NR17SO2- or -NR18-(wherein R16, R17 and R18 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl), and R9 is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy; in the preparation of a medicament for use in the inhibition of aurora 2 kinase.

L'invention concerne l'utilisation d'un composé de formule (I) ou bien d'un sel, ester, amide ou promédicament correspondant; dans cette formule X est O, ou S, S(O)¿2?, NH ou NR?12¿, sachant que R?12¿ est hydrogène ou alkyle C¿1-6?; R?5¿ peut être NHC(O)OR?9¿, NHC(O)R?9¿, NHS(O)¿2?R?9¿, C(O)R?9¿, C(O)OR?9¿, S(O)R?9¿, S(O)OR?9¿, S(O)¿2?OR?9¿, C(O)NR?10¿ R?11¿, S(O)NR?10¿R?11¿ S(O)ONR?10¿R?11¿, sachant que R?9¿, R?10¿ ou R?11¿ sont différents groupes organiques spécifiés; R?6¿ est hydrogène, hydrocarbyle éventuellement substitué ou hétérocyclyle éventuellement substitué; R?7¿ et R?8¿ sont différents groupes organiques spécifiés, et R?1¿, R?2¿, R?3¿, R?4¿ peuvent être indépendamment halogéno, cyano, nitro, alkylsulphanyle C¿1-3?, -N(OH)R?13¿-(sachant que R?7¿ est hydrogène, ou alkyle C¿1-3?), ou R?15¿X?1¿-(sachant que X?1¿ est une liaison directe, -O-, CH¿2?-, -OCO-, carbonyle, -S-, -SO-, -SO¿2?-, -NR?16¿CO-, -CONR?16¿, -SO¿2?NR?16¿-, -NR?17¿SO¿2?- ou -NR?18¿-(sachant que R?16¿, R?17¿ et R?18¿ sont chacun indépendamment hydrogène, alkyle C¿1-3? ou alcoxy C¿1-3? alkyle C¿2-3?), et que R?9¿ est hydrogène, hydrocarbyle éventuellement substitué, hétérocyclyle éventuellement substitué ou alkoxy éventuellement substitué. Ce type de composé entre dans la préparation d'un médicament utilisé pour inhiber l'aurora 2 kinase.

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