| 摘要 |
A compound of formula (I) or a pharmaceutically acceptable salt or an in, vivo hydrolysable ester thereof is described wherein: R1 is halo, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; p is 0-4; wherein the values of R1 may be the same or different; R2 is sulphamoyl or a group B-E-; wherein B is selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, phenyl, a heterocyclic group, phenylC1-6alkyl or (heterocyclic group)C1-6alkyl; wherein said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, phenyl, heterocyclic group, phenylC1-6alkyl or (heterocyclic group)C1-6alkyl are optionally substituted on carbon by one or more D; and wherein if said heterocyclic group contains an -NH- moiety that nitrogen may be optionally substituted by a group selected from G; E is -C(O)-, -N(Ra)C(O)-, -C(O)N(Ra)-, -S(O)r-, -SO2N(Ra)- or -N(Ra)SO2-; wherein Ra is hydrogen or C1-6alkyl optionally substituted by one or more D and r is 1-2; D is independently selected from halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, amino, carboxy, carbamoyl, mercapto, sulphamoyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C1-6alkanoyl, C1-6alkanoyloxy, N-(C1-6alkyl)amino, N,N-(C1-6alkyl)2amino, C1-6alkanoylamino, N-(C1-6alkyl)carbamoyl, N,N-(C1-6alkyl)2carbamoyl, C1-6alkylS(O)a wherein a is 0 to 2, C1-6alkoxycarbonyl, N-(C1-6alkyl)sulphamoyl and N,N-(C1-6alkyl)2sulphamoyl; G is selected from C1-4alkyl, C1-4alkanoyl, C1-4alkylsulphonyl, C1-4alkoxycarbonyl, carbamoyl, N-(C1-4alkyl)carbamoyl, N,N-(C1-4alkyl)carbamoyl, benzyl, benzyloxycarbonyl, benzoyl and phenylsulphonyl; and q is 0-2; wherein the values of R2 maybe the same or different; and wherein p+q is 1-5; with the proviso that that compound is not 2-(2,4-dimethylanilino)-4-amino-5-cyanopyrimidine; 4-amino-5-cyano-2-[2-(2-hydroxyethoxycarbonyl)anilino]pyrimidine, or 4-amino-5-cyano-2-[2-(methoxycarbonyl)anilino]pyrimidine. Also described is the process for preparing a compound of formula (I). The compound of formula (I) can be used in the manufacture of a medicament for use in the production of a cell cycle inhibitory (anti-cell-proliferation) effect, and in the treatment of cancers (solid tumors and leukaemias) fibroproliferative and differentiative disorders, psoriasis, rheumatoid arthritis, Kaposi's sarcoma, haemangioma, acute and chronic nephropathies, atheroma, atherosclerosis, arterial restenosis, autoimmune diseases, acute and chronic inflammation, bone diseases and ocular diseases with retinal vessel proliferation.
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