C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/14 (2006.01) A61K 31/506 (2006.01) A61P 35/00 (2006.01) C07D 409/04 (2006.01) C07D 417/04 (2006.01)
Patent
CA 2401748
The present invention relates to 2-substituted 4-heteroaryl- pyrimidines,(Fig.I), wherein: X1 is CH and X2 is S; or one of X1 and X2 is S, and the other of X1 and X2 is N; Z is NH, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH=CH; R1, R2 and R3 are independently H, alkyl, aryl, aralkyl, heterocycle, halogeno, NO2, CN, OH, alkoxy, aryloxy, NH2, NH-R', N-(R')(R''), NH-COR', NH- aryl, N-(aryl)2, COOH, COO-R', COO-aryl, CONH2, CONH-R', CON-(R')(R''),CONH- aryl, CON-(aryl)2, SO3H, SO2NH2, CF3, CO-R', or CO-aryl, wherein alkyl, aryl, aralkyl, heterocycle and NH-aryl groups may be further substituted with one or more groups selected from halogeno, NO2, CN, OH, O-methyl, NH2, COOH, CONH2 and CF3; at least one of the groups R1 and R2 being other than H when either X1 or X2 is S; R4, R5, R6, R7 and R8 are independently from each other H, substituted or unsubstituted lower alkyl, halogeno, NO2, CN, OH, substituted or unsubstituted alkoxy, NH2, NH-R', alkyl-aryl, alkyl-heteroaryl, NH(C=NH)NH2, N(R')3+, N(R')(R''), COOH, COO-R', CONH2, CONH-R', CON-(R')(R''), SO3H, SO2NH2, CF3 or (CH2)nO(CH2)m NR'R'', (CH2)nCO2(CH2)mOR''' wherein n is 0,1,2 or 3 and m is 1, 2 or 3; their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependant kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
La présente invention concerne des 4-hétéroaryle-pyrimidines substituées en 2 selon la formule (I) où: X?1¿ représente CH et X?2¿ représente S; ou bien X?1¿ ou X?2 ¿ représente S, l'autre représentant alors N; Z représente NH, NHCO, NHSO¿2?, NHCH¿2?, CH¿2?, CH¿2?CH¿2? or CH=CH; R?1¿ ; R?2¿ et R?3¿ représentent indépendamment H, alkyle, aryle, aralkyle, hétérocycle, halogène, NO¿2?, CN, OH, alcoxy, aryloxy, NH¿2?, NH-R', N-(R')(R''), NH-COR'', NH-aryle, N-(aryl)¿2?, COOH, COO-R', COO-aryle, CONH2, CONH-R', CON-(R')(R''),CONH-aryle, CON-(aryle)¿2?, SO¿3?H, SO¿2?NH¿2?, CF¿3?, CO-R' ou CO-aryle, sachant que les groupes alkyle, aryle, aralkyle, hétérocycle et NH-aryle peuvent être aussi substitués par au moins un groupe sélectionné parmi halogène, NO¿2?, CN, OH, O-méthyle, NH¿2,?COOH, CONH¿2? et CF¿3?; au moins un des groupes R?1¿ et R?2¿ représentant autre chose que H si X?1¿ ou X?2¿ représente S; R?4¿, R?5¿, R?6¿, R?7¿ et R?8¿ représentant indépendamment H, alkyle bas substitué ou non substitué, halogène, NO¿2?, CN, OH, alcoxy substitué ou non substitué, NH¿2?, NH-R', alkyle-aryle, alkyle-hétéroaryle, NH(C=NH)NH¿2?, N(R') ¿3??+¿, N(R')(R''), COOH, COO-R', CONH¿2?, CONH-R', CON-(R')(R''), SO¿3?H, SO¿2?NH¿2?, CF¿3? ou (CH¿2?)¿n?O(CH¿2?)¿m? NR'R'', (CH¿2?)¿n?CO¿2?(CH¿2?)¿m?OR''', sachant que n vaut 0, 1,2 ou 3 et m vaut 1, 2 ou 3. L'invention concerne également leur préparation, les compositions pharmaceutiques les contenant et leur utilisation comme inhibiteurs des kinases cycline-dépendantes (CDK) et donc leur utilisation dans le traitement de troubles proliférants tels que le cancer, la leucémie, le psoriasis et équivalent.
Fischer Peter Martin
Wang Shudong
Cyclacel Limited
Gowling Lafleur Henderson Llp
LandOfFree
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