发明名称 Multikinase inhibitors for use in the treatment of cancer
摘要 The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I):;wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
申请公布号 US8937056(B2) 申请公布日期 2015.01.20
申请号 US201313794635 申请日期 2013.03.11
申请人 Eisai R&D Management Co., Ltd. 发明人 Agoulnik Sergei;Decosta Bruce;Du Hong;Jiang Yimin;Li Xiang-Yi;Nomoto Kenichi;Wang John (Yuan);Zhang Huiming
分类号 A01N57/00;A61K31/665;A01N43/02;A61K31/335;A01N43/76;A61K31/42;A61K31/415;A61K31/497;A61K31/535;A61K31/4178;A61K31/365;A61K31/422;A61K31/5377;A61K45/06;A61K31/496;A61K31/4025;A61K31/4523 主分类号 A01N57/00
代理机构 Lathrop & Gage LLP 代理人 Lathrop & Gage LLP ;Velema James H.
主权项 1. A method for treating a FLT3 mutated cancer in a subject, wherein the FLT3 mutated cancer carries a D835Y, Y842C, K663Q or V592A mutation, the method comprising: a) determining if the subject's cancer carries a D835Y, Y842C, K663Q or V592A mutation; and b) if the cancer is determined to carry a D835Y, Y842C, K663Q or V592A mutation, administering to the subject a composition comprising at least one compound of formula (I): wherein: R1 is HR2 is a moiety selected from the group consisting of H and trifluoromethylcarbonyl; or R1 and R2 are taken together with the core structure to form a heterocyclydiyl moiety of formula (a): R3 is a moiety selected from the group consisting of —ORa and —NRbRc;Ra is a C1-4 alkyl group optionally substituted with an imidazolyl;Rb is a moiety selected from the group consisting of a C1-4 alkyl group and a C1-4 alkoxy group, wherein Rb is substituted with 0, 1 or 2 groups each independently selected from the group consisting of —OCH3, —C(O)OH, —C(O)NR′R″, —NH(C1-3 alkyl), —NH(CH2CH2O)nCH3, wherein n is 2-4, piperazinyl, N-methylpiperazinyl, piperidinyl, N-methylpiperidinyl, N-morpholinyl, imidazolyl, pyrrolidinyl, —OPO3H2 and hydroxyl; wherein the —NH(C1-3 alkyl) group is substituted with 0, 1 or 2 hydroxyl moieties and wherein R′ and R″ are each independently selected from —H or —CH3; andRc is H, or Rb and Rv are taken together with the nitrogen to which they are attached to form a heterocyclyl moiety selected from the group consisting of formula (b) and formula (c): or a pharmaceutically acceptable salt or ester thereof; in an amount effective for treating the FLT3 mutated cancer.
地址 Tokyo JP