发明名称 PYRIMIDO[4,5-D]PYRIMIDINYL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
摘要 A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.;
申请公布号 US2014296216(A1) 申请公布日期 2014.10.02
申请号 US201114125304 申请日期 2011.12.21
申请人 Ding Ke;Chang Shaohua;Xu Shilin;Zhang Lianwen;Tu Zhengchao;Ding Jian;Geng Meiyu;Chen Yi 发明人 Ding Ke;Chang Shaohua;Xu Shilin;Zhang Lianwen;Tu Zhengchao;Ding Jian;Geng Meiyu;Chen Yi
分类号 C07D487/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I) or (II): or a pharmaceutically acceptable salt, isomer or prodrug thereof,wherein, Y is CH or N; R1 is selected from: 1) H; 2) C1-C5 alkyl; 3) C3-C6 cycloalkyl; 4) C1-C5 fluoroalkyl; 5) (CH2)nX, n is an integer of 0-6, X is —OH, —NH2, C1-C6 heteroalkyl, or C3-C7 heterocycloalkyl; 6)wherein each of A1, A2, A3, A4, A5 is independently selected from: a. H; b. halo; c. —CN; d. —NO2; e. —OH; f. —NH2; g. C1-C6 alkyl; h. C3-C6 cycloalkyl; i. C1-C6 fluoroalkyl; j. C1-C6 heteroalkyl; k. C1-C7 heterocycloalkyl; l. ester, amide, sulfone, sulfoxide, urea formed from the above alkyl;wherein, the heteroatom in the above C1-C6 heteroalkyl or C1-C7 heterocycloalkyl is O, N or S; R2 is selected from: 1) H; 2) C1-C5 alkyl; 3) C3-C6 cycloalkyl; 4) C1-C5 fluoroalkyl; 5) aryl; 6) heterocycloalkyl;wherein, the heteroatom in the above heterocycloalkyl is O, N or S; R3 is selected from: 1) H; 2) halo; 3) —NH2, —OH, —CN, —NO2; 4) C1-C5 alkyl; 5) C3-C6 cycloalkyl; 6) aryl; 7)wherein W is selected from —CH2, —CH2CH2, O, S, —NH, —NR; R is C1-C5 alkyl or aryl; R4 is selected from: 1) H; 2) halo; 3) C1-C5 alkyl; 4) C3-C6 cycloalkyl; 5) aryl;wherein, the above C3-C6 cycloalkyl and aryl each can be independently substituted by 0, 1, 2 or 3 substituents selected from R5;wherein R5 is selected from: 1) H; 2) halo; 3) C1-C3 alkyl; 4) C3-C6 cycloalkyl; 5) C1-C3 alkoxy; 6) C1-C3 fluoroalkyl; 7) heterocycloalkyl; 8) C0-C3 alkylene heterocyclic; 9) phenyl;wherein, the heteroatom in the above heterocycloalkyl or C0-C3 alkylene heterocyclic is O, N or S.
地址 Guangdong CN