| 摘要 |
<p>Purine derivatives (I) are used to produce medicaments for selectively inhibiting kinase activity. Purine derivatives (I) with the following formula are used to produce medicaments for selectively inhibiting kinase activity: [Image] R1>H, NHAr, OAr, SCH2Ar, SAr, Ar, CH=CH-Ar, CH2Ar, amino, 1-4C alkoxy or halo; Ar : optionally halo-substituted phenyl; R2>H or 1-4C alkyl; X : N or NR3>; Y : N, CR5> or NR6>; X : NR3> and Y = N or CR5> when there is a double bond between Y and CR4>; X : N and Y = NR6> when there is a double bond between X and CR4>; R3>H, 1-4C alkyl, CH2Ar or Ar; R4>H, halo, phenyl (optionally mono- or disubstituted with SOnA) or CC(CH2)mOH; A : 1-4C alkyl; n : 0-2; m : 1-3; R5>H; R6>H, Ar or CH2Ar. An independent claim is also included for a pharmaceutical composition comprising at least one compound (I) in which R1> is SCH2Ar or SAr. ACTIVITY : Cytostatic; Neuroprotective; Antidiabetic; Cerebroprotective; Antiinflammatory; Antirheumatic; Antiarthritic; Antiasthmatic; Antipsoriatic; Vasotropic; Cardiant; Ophthalmological. MECHANISM OF ACTION : Kinase inhibitor. N-Phenyl-9H-purin-6-ylamine gave the following kinase inhibition values (%) at a concentration of 30 mu M: c-RAF (19), GSK3beta (13), JNK3 (11), Lck (39), MAPK1 (22), MAPK2 (33), MEK1 (19), PKA (32), PKB (14), ROCK-II (48), SAPK2a (32).</p> |
