| 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 NR1R2); or phenyl substituted by phenyl, optionally substituted by 1-3 of halo, alkyl, OH, alkoxy, alkylthio or NR'1R'2; R1, R2H or alkyl; or NR1R24-7 membered heterocycle containing 1 or 2 heteroatoms, the members of the ring being selected from CR3R4, O, S and NR5; R3, R4H, OH, alkyl, OH, alkoxy, NH2 or mono- or dialkylamino; R5, R'1, R'2H or alkyl; B' : -(CH2)n-CO-, -NH-CO-(CH2)n- or -(CH2)p-; n : 0-2; p : 0 or 1; W : H or alkyl; X : -(CH2)q- or -(CH2)r-CO-(CH2)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 IC50 100 MicroM or less for inhibition of purified recombinant cdc25-C phosphatase.
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