发明名称 PYRAZINECARBOXAMIDE COMPOUND
摘要 [Problem];A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided.;[Means for Solution];The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention. The pyrazinecarboxamide compound of the present invention has an inhibitory action on an EGFR T790M mutation kinase, and can be used as an agent for preventing and/or treating EGFR T790M mutation positive cancer, in another embodiment, EGFR T790M mutation positive lung cancer, in a still other embodiment, EGFR T790M mutation positive non-small cell lung cancer, in further still another embodiment, EGFR T790M mutation protein positive cancer, in further still another embodiment, EGFR T790M mutation protein positive lung cancer, in further still another embodiment, EGFR tyrosine kinase inhibitor-resistant cancer, in further still another embodiment, EGFR tyrosine kinase inhibitor-resistant lung cancer, and in further still another embodiment, EGFR tyrosine kinase inhibitor-resistant non-small cell lung cancer, or the like.
申请公布号 US2014323463(A1) 申请公布日期 2014.10.30
申请号 US201313990006 申请日期 2013.01.15
申请人 ASTELLAS PHARMA INC. 发明人 Matsuya Takahiro;Kondoh Yutaka;Shimada Itsuro;Kikuchi Shigetoshi;Iida Maiko;Onda Kenichi;Fukudome Hiroki;Takemoto Yukihiro;Shindou Nobuaki;Sakagami Hideki;Hamaguchi Hisao
分类号 C07D241/24;C07D401/12;C07D471/10;C07D403/12;C07D491/113;C07D413/12;C07D241/28;C07D401/14 主分类号 C07D241/24
代理机构 代理人
主权项 1. A compound of the formula (I) or a salt thereof: (wherein R1 represents lower alkyl which may be substituted, —O-lower alkyl which may be substituted, —NH2, —NH-lower alkyl which may be substituted, —N(lower alkyl which may be substituted)2, -L4-cycloalkyl which may be substituted, -L4-aryl which may be substituted, -L4-aromatic heterocyclic group which may be substituted, or -L4-non-aromatic heterocyclic group which may be substituted, Ring A represents arene which may be substituted or aromatic heterocycle which may be substituted, L1 represents —O— or —NH—, R2 represents H, halogen, —OH, —NR5R6, —CONH2, —CN, -L4-cycloalkyl which may be substituted, -L4-aryl which may be substituted, -L4-aromatic heterocyclic group which may be substituted, -L4-non-aromatic heterocyclic group which may be substituted, lower alkyl which may be substituted, lower alkenyl which may be substituted, or lower alkynyl which may be substituted, L2 represents —O—, —S(O)p—, —NH—, —N(CH3)—, —NHCH2—, —NHCH2CH2—, —OCH2—, or a bond, Y represents Ring X or a bond, Ring X represents cycloalkane which may be substituted, arene which may be substituted, an aromatic heterocycle which may be substituted, or a non-aromatic heterocycle which may be substituted, L3 represents —O—, —NH—, —N(lower alkyl which may be substituted)-, —N(cycloalkyl which may be substituted), -lower alkylene which may be substituted-, -lower alkylene which may be substituted-NH—, —NH-lower alkylene which may be substituted-, -lower alkylene which may be substituted-N(lower alkyl which may be substituted)-, —N(lower alkyl which may be substituted)-lower alkylene which may be substituted-, or a bond, M represents —C(O)— or —S(O)2—, R3 represents H or lower alkyl which may be substituted, R4 represents lower alkyl which may be substituted with one or more substituents selected from the group consisting of —OH, halogen, —NH2, —NH-(lower alkyl which may be substituted), —N(lower alkyl which may be substituted)2, and a non-aromatic heterocyclic group which may be substituted, or H, R5 and R6 are the same as or different from each other, and represent H or lower alkyl which may be substituted, L4's are the same as or different from each other, and represent lower alkylene which may be substituted-, —NH—, —O—, —O-lower alkylene which may be substituted-, -lower alkylene which may be substituted-O—, or a bond, and p represents 0, 1, or 2.)
地址 Tokyo JP