Anti-cancer compounds
AssigneeCyclacel Limited
InventorsShudong Wang, Peter M. Fischer
Life of this patent
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Abstract
The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
Claims28
A compound of general formula I:
- 8
- 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, halogen, 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 halogen, 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, halogen, amino, carbamoyl, sulfamyl, 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)mNR′R″, (CH2)nCO2(CH2)mOR′″ wherein n is 0, 1, 2 or3 and m is 1, 2 or 3;
- wherein R′, R″ and R′″ are each independently alkyl groups that may be the same or different;
- and pharmaceutically acceptable salts thereof.
The method of 19, wherein said compound is administered in combination with one or more other anticancer compounds.
The method of 20, wherein said compound is administered in combination with one or more other anticancer compounds.
The method of 21, wherein said compound is administered in combination with one or more other anticancer compounds.
The method of 22, wherein said compound is administered in combination with one or more other anticancer compounds.
Dependencies are inferred from the claim text.