发明名称 Thiazole derivatives
摘要 The present invention relates to a compound represented by the formula (I) or (I′):;wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
申请公布号 US9090601(B2) 申请公布日期 2015.07.28
申请号 US201012657854 申请日期 2010.01.28
申请人 Millennium Pharmaceuticals, Inc. 发明人 Banno Hiroshi;Hirose Masaaki;Kurasawa Osamu
分类号 C07D417/14;C07D487/04;C07D513/04;C07D495/04;A61K9/20;C07D417/04;C07D471/04 主分类号 C07D417/14
代理机构 Choate, Hall & Stewart LLP 代理人 Choate, Hall & Stewart LLP ;Reid Andrea L.C.
主权项 1. A compound of formula Ia:or a pharmaceutically acceptable salt thereof, wherein R1 is (i) an optionally substituted group represented by (ii) a group represented by: whereinRa and Rc are each hydrogen atom, an alkyl group or a halogen atom,Rb is (i) a hydrogen atom, (ii) an optionally substituted hydrocarbon-carbonyl group, (iii) an optionally substituted heterocyclyl-carbonyl group, (iv) an optionally substituted carbamoyl group, (v) an optionally substituted alkoxycarbonyl group, (vi) an optionally substituted hydrocarbon-sulfonyl group, (vii) an optionally substituted heterocyclyl-sulfonyl group, (viii) an optionally substituted sulfamoyl group, (ix) an optionally substituted hydrocarbon group or (x) an optionally substituted heterocyclic group, andRd is (i) a hydrogen atom, (ii) an optionally substituted hydrocarbon group or (iii) an optionally substituted heterocyclic group; R2 is a halogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, wherein a) the optionally substituted group bonded via a carbon atom is selected from cyano, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted C1-8 alkyl-carbonyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted aryl group, an optionally substituted C6-18 aryl-C1-4 alkyl group, an optionally substituted C6-18 aryl-carbonyl group, an optionally substituted C6-18 aryl-C1-4 alkyl-carbonyl group, an optionally substituted heterocyclic group bonded via a carbon atom, an optionally substituted heterocyclyl-C1-4 alkyl group, an optionally substituted heterocyclyl-carbonyl group, an optionally substituted heterocyclyl-C1-4 alkyl-carbonyl group, and an optionally substituted carbamoyl group, b) the optionally substituted group bonded via a nitrogen atom is selected from i) amino;ii) mono- or di-substituted amino, wherein the amino is substituted by an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted C1-8 alkyl-carbonyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted aryl group, an optionally substituted C6-18 aryl-C1-4 alkyl group, an optionally substituted C6-18 aryl-carbonyl group, an optionally substituted C6-18 aryl-C1-4 alkyl-carbonyl group, an optionally substituted heterocyclic group bonded via a carbon atom, an optionally substituted heterocyclyl-C1-4 alkyl group, an optionally substituted heterocyclyl-carbonyl group, an optionally substituted heterocyclyl-C1-4 alkyl-carbonyl group, or an optionally substituted carbamoyl group, andiii) an optionally substituted heterocyclic group bonded via a nitrogen atom; c) the optionally substituted group bonded via an oxygen atom is selected from hydroxy optionally substituted by an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted C1-8 alkyl-carbonyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted aryl group, an optionally substituted C6-18 aryl-C1-4 alkyl group, an optionally substituted C6-18 aryl-carbonyl group, an optionally substituted C6-18 aryl-C1-4 alkyl-carbonyl group, an optionally substituted heterocyclic group bonded via a carbon atom, an optionally substituted heterocyclyl-C1-4 alkyl group, an optionally substituted heterocyclyl-carbonyl group, an optionally substituted heterocyclyl-C1-4 alkyl-carbonyl group, and an optionally substituted carbamoyl group , and d) the optionally substituted group bonded via a sulfur atom is selected from mercapto optionally substituted by: an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted C1-8 alkyl-carbonyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted aryl group, an optionally substituted C6-18 aryl-C1-4 alkyl group, an optionally substituted C6-18 aryl-carbonyl group, an optionally substituted C6-18 aryl-C1-4 alkyl-carbonyl group, an optionally substituted heterocyclic group bonded via a carbon atom, an optionally substituted heterocyclyl-C1-4 alkyl group, an optionally substituted heterocyclyl-carbonyl group, an optionally substituted heterocyclyl-C1-4 alkyl-carbonyl group, and an optionally substituted carbamoyl group; R3 is (1) an optionally substituted 5-membered aromatic heterocyclic group containing 2 to 4 nitrogen atoms besides carbon atom, which is bonded via a carbon atom, or (2) an optionally substituted 5-membered aromatic heterocyclic group containing 1 to 3 nitrogen atoms besides carbon atom and further containing one oxygen atom or sulfur atom, which is bonded via a carbon atom.
地址 Cambridge MA US