| 摘要 |
The use of aryl-substituted secondary or tertiary amines (I) is claimed in the production of medicaments for inhibiting cdc25 phosphatases, especially cdc25-C phosphatases. The use of aryl-substituted amines of formula A-B'-N(W)-X-Y (I) or their salts is claimed in the production of medicaments for inhibiting cdc25 phosphatases, especially cdc25-C phosphatases. A : carbocyclic aryl (optionally substituted by 1-3 of halo, alkyl, OH, alkoxy, alkylthio or NR 1R 2); or phenyl substituted by phenyl, optionally substituted by 1-3 of halo, alkyl, OH, alkoxy, alkylthio or NR' 1R' 2; R 1, R 2H or alkyl; or NR 1R 24-7 membered heterocycle containing 1 or 2 heteroatoms, the members of the ring being selected from CR 3R 4, O, S and NR 5; R 3, R 4H, OH, alkyl, OH, alkoxy, NH 2or mono- or dialkylamino; R 5, R' 1, R' 2H or alkyl; B' : -(CH 2) n-CO-, -NH-CO-(CH 2) n- or -(CH 2) p-; n : 0-2; p : 0 or 1; W : H or alkyl; X : -(CH 2) q- or -(CH 2) r-CO-(CH 2) r-; q : 0-4; r : 0-6; and Y : nitrophenyl, aminophenyl, mono- or dialkylaminophenyl or ((amino-(2-thienyl)-methylidene)-amino)-phenyl of formula (a). [Image] An independent claim is also included for medicaments or pharmaceutical compositions containing compounds (I') or their salts, where (I') are as for (I) except that Y is other than group (a). ACTIVITY : Antialopecia; cytostatic; protozoacide; virucide; neuroprotective; antipsoriatic; vasotropic; antibacterial; fungicide. MECHANISM OF ACTION : cdc25 Phosphatase inhibitor; inhibitor of spontaneous or induced apoptosis in normal cells; meiosis and 'fecundation' inhibitor; oocyte maturation inhibitor. (Ia) had IC 50100 MicroM or less for inhibition of purified recombinant cdc25-C phosphatase. |
