04-06-2015 дата публикации
Номер: US20150152069A1
Принадлежит:
Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers. 2. The N2 ,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2 ,4-diamine derivative or a pharmaceutically acceptable salt thereof ,{'sup': 1', '2', '6', '7', '8, 'wherein Rand Rare independently H, —ORor —NRR,'}{'sup': 6', '7', '8, 'where Ris methyl, ethyl, propyl, isopropyl, butyl, isobutyl or t-butyl unsubstituted or substituted with at least one selected from the group consisting of chloro, bromo, fluoro, iodine, and phenyl, Rand Rare independently H; methyl; ethyl; propyl; isopropyl; butyl; isobutyl; t-butyl; methylcarbonyl; ethylcarbonyl; propylcarbonyl; isopropylcarbonyl; butylcarbonyl; isobutylcarbonyl or phenyl;'}{'sup': 4', '5', '9', '10', '9', '10, 'sub': '2', 'Rand Rare independently H; methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, —C(═O)Ror —SO—Runsubstituted or substituted with hydroxyl, wherein Ris methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, methyloxy, ethyloxy, propyloxy, isopropyloxy, butyloxy, isobutyloxy, t-butyloxy, hydroxymethyl, hydroxyethyl, hydroxypropyl, hydroxyisopropyl, hydroxybutyl, hydroxyisobutyl, amino, methylamino, ethylamino, propylamino, isopropylamino, butylamino or isobutylamino, Ris methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, or amino; and'}{'sup': '3', 'Ris ...
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