文献类型：专利

英文题名：Use of substituted 4-piperazin-1-yl-pyrimidin-2-ylamine compounds in broad spectrum anti-tumor medicine

作者：BAI Y;CHAI Y;LAN M;LI S;YANG C;YANG F;ZHAO H;YUAN H

机构：[1]UNIV EAST CHINA SCI & TECHNOLOGY

申请号：CN103181926-A

申请日：2013-01-04

公开日：2013-07-03

语种：英文

收录：DERWENT

摘要：NOVELTY - In broad spectrum anti-tumor medicine, substituted 4-piperazin-1-yl-pyrimidin-2-ylamine compounds, are used. USE - As anti-tumor medicine for preventing and treating cancer and related diseases (claimed) where tumors and cancers include colon, lung, cervical, breast, renal, head and neck, liver, gastric, ovarian, oral cavity, and esophagus cancers. ADVANTAGE - When screened from anti-tumor activity the compounds show good broad spectrum anti-tumor activity, and inhibit growth of tumor cells and kill cancer cells, especially show good curative effect for treatment of colon cancer. Further when compounds are tested by cell toxicity and cell immune activity assay, at highest concentration of 100 mol/L only slight toxicity is observed i.e. compounds show no toxicity at low concentration; and show enhanced immunity. DETAILED DESCRIPTION - In broad spectrum anti-tumor medicine, substituted 4-piperazin-1-yl-pyrimidin-2-ylamine compound of formula (I), is used. L'=1-4C lower alkyl, 1-4C lower alkoxy, 1-4C lower alkylamino, 1-4C lower alkenyl, 1-4C lower alkynyl, O, OR4, S, SR4, NH, or NR4; R4=1-4C lower alkyl, 1-4C lower alkoxy, or 1-4C lower monoalkyl amino; R1=5-9 membered aryl, 5-9 membered aromatic heterocyclyl, aromatic bicyclic heteroaryl (all substituted), or optionally substituted phenyl (where 5-9 membered aromatic heterocyclyl, and aromatic bicyclic heteroaryl contain 1-3 heteroatoms selected from O, S, and N; phenyl and aromatic bicyclic heteroaryl are substituted by halo, 1-6C straight chain or branched-chain hydrocarbyl, cyano, nitro, amino, hydroxyl, hydroxymethyl, trifluoromethyl, trifluoromethoxy, carboxyl, 1-4C alkoxy, sulfhydryl, or 1-4C acyl; and 5-9 membered aryl and 5-9 membered aromatic heterocyclyl are substituted by Ar) (preferably optionally substituted phenyl or substituted 5-9 membered aryl); Ar=benzyl, benzyloxy, benzyl amino, 5-9 aryl, or aromatic heterocyclyl (all substituted), or optionally substituted phenyl (where substituent is selected from 1-4 of halo, 1-6C straight-chain or branched-chain hydrocarbyl, cyano, nitro, amino, hydroxyl, hydroxymethyl, trifluoromethyl, trifluoromethoxy, carboxyl, 1-4C alkoxy, naphthyl, or 1-4C acyl); R2=aliphatic heterocyclyl, aliphatic ring, aryl, aromatic heterocyclyl, or 3-9 membered bicyclic heteroaryl (all substituted), H, 1-9C alkyl, 1-9C alkoxy, OH, NH2, NO2, SH, or NR5R6 (preferably H, 1-9C alkyl, or 1-9C alkoxy); R5 and R6=H, 1-9C alkyl, 1-9C alkoxy, or 3-9C mono alkylamino. An INDEPENDENT CLAIM is included for a pharmaceutical composition comprising: at least one compound (I), or its salt selected from sodium, potassium, hydrochloride, sulfate and calcium salt.