| 摘要 |
A compound of formula (I), pharmaceutically acceptable salts or an in vivo hydrolysable ester thereof are described wherein: R1 is halo, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; p is 0-4; R2 is sulphamoyl or a group B-E-; q is 0-2; and wherein p + q = 1-5; R3 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl or C3-8cycloalkyl; wherein R3 may be optionally substituted on carbon; R4 is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl or heterocyclyl; wherein R4 may be optionally substituted wherein if said heterocyclyl contains an -NH-moiety that nitrogen may be optionally substituted; or R3 and R4 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted on carbon; wherein if said heterocyclic ring contains an-NH- moiety that nitrogen may be optionally substituted; B is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, phenyl, a heterocyclic group, phenylC1-6alkyl or (heterocyclic group)C1-6alkyl; wherein B may be optionally substituted on carbon; and wherein if said heterocyclic group contains an-NH-moiety that nitrogen may be optionally substituted; 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 and r is 1-2. Also disclosed is the preparation of the compound The compound can be used in a pharmaceutical composition for use in the production of a cell cycle inhibitory (anti-cell proliferation) effect and for use I the treatment of leukaemia, breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, pancreatic cancer, ovarian caner, liver caner, kidney cancer, skin cancer, cancer of the vulva, solid tumours, fibroproliferative and differentiative disorders, psoriasis, rheumatoid arthritis, Kaposi's sarcoma, haemangioma, acute and chronic nephropathies, atheroma, atherosclerosis, arterial restenosis, autoimmune disease, acute and chronic inflammation, bone disorders and ocular diseases with retinal vessel proliferation..
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