发明名称 Fused pyrimidine derivatives for inhibition of tyrosine kinase activity
摘要 The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.
申请公布号 US8957065(B2) 申请公布日期 2015.02.17
申请号 US201113805183 申请日期 2011.06.20
申请人 Hanmi Science Co., Ltd 发明人 Cha Mi Young;Kang Seok Jong;Kim Mi Ra;Lee Ju Yeon;Jeon Ji Young;Jo Myoung Gi;Kwak Eun Joo;Lee Kwang Ok;Ha Tae Hee;Suh Kwee Hyun;Kim Maeng Sup
分类号 C07D495/04;A61K31/519;A61K31/55;A61K31/5355;A61P35/00;A61P29/00;A61P37/02;A61P37/06;A61P19/02;A61P17/06;A61P11/06;A61P9/00;A61P3/10;A61P13/12;A61P7/10;A61P25/28;A61P25/16;A61P25/02;C07D519/00;A61K31/675;C07D491/048;A61K31/5377;A61K31/541;A61K31/553;C07F9/6561;C07D491/04 主分类号 C07D495/04
代理机构 Sughrue Mion, PLLC 代理人 Sughrue Mion, PLLC
主权项 1. A compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein, W is S; X is O, NH, S, SO or SO2; Y is hydrogen atom, halogen atom, C1-6alkyl or C1-6alkoxy; A and B are each independently hydrogen atom, halogen atom, or di(C1-6alkyl)aminomethyl; Z is aryl or heteroaryl having one or more substituents selected from the group consisting of: hydrogen atom, halogen atom, hydroxy, nitro, cyano, C1-6alkyl, C1-6alkoxy, C1-6alkylcarbonyl, C1-6alkoxycarbonyl, di(C1-6alkyl)aminoC2-6alkoxycarbonyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, carbamoyl, C1-6alkylcarbamoyl, di(C1-6alkyl)carbamoyl, di(C1-6alkyl)aminoC2-6alkylcarbamoyl, sulfamoyl, C1-6alkylsulfamoyl, di(C1-6alkyl)sulfamoyl, di(C1-6alkyl)aminoC2-6alkylsulfamoyl, C1-6alkylsulfonyl, C1-6alkylsulfinyl, di(C1-6alkyl)phosphonyl, hydroxyC1-6alkyl, hydroxycarbonylC1-6alkyl, C1-6alkoxyC1-6alkyl, C1-6alkylsulfonylC1-6alkyl, C1-6alkylsulfinylC1-6alkyl, di(C1-6alkyl)phosphonylC1-6alkyl, hydroxyC2-6alkoxy, C1-6alkoxyC2-6alkoxy, aminoC1-6alkyl, C1-6alkylaminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoacetyl, aminoC2-6alkoxy, C1-6alkylaminoC2-6alkoxy, di(C1-6alkyl)aminoC2-6alkoxy, hydroxyC2-6alkylamino, C1-6alkoxyC2-6alkylamino, aminoC2-6alkylamino, C1-6alkylaminoC2-6alkylamino, di(C1-6alkyl)aminoC2-6alkylamino, heteroaryl, heterocycle, heterocyclic oxy, heterocyclic thio, heterocyclic sulfinyl, heterocyclic sulfonyl, heterocyclic sulfamoyl, heterocyclic C1-6alkyl, heterocyclic C1-6alkoxy, heterocyclic amino, heterocyclic C1-6alkylamino, heterocyclic aminoC1-6alkyl, heterocyclic carbonyl, heterocyclic C1-6alkylcarbonyl, heterocyclic carbonylC1-6alkyl, heterocyclic C1-6alkylthio, heterocyclic C1-6alkylsulfinyl, heterocyclic C1-6alkylsulfonyl, heterocyclic aminocarbonyl, heterocyclic C1-6alkylaminocarbonyl, heterocyclic aminocarbonylC1-6alkyl, heterocyclic carboxamido, and heterocyclic C1-6alkylcarboxamido; the aryl refers to a C6-12 cyclic or bicyclic aromatic ring; the heteroaryls each independently refer to a 5- to 12-membered cyclic or bicyclic aromatic hetero ring having one or more N, O or S; the heterocycles each independently refer to a saturated or partially unsaturated 3- to 12-membered cyclic or bicyclic hetero ring having one or more N, O, S, SO or SO2, in which a carbon atom forming the heterocycle optionally has one or more substituents selected from the group consisting of C1-6alkyl, hydroxy, hydroxyC1-6alkyl, hydroxycarbonyl, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminocarbonyl, heterocycle, heterocyclic C1-6alkyl, and heteroaryl, and in which, provided that the heterocycle optionally comprises a nitrogen atom, the nitrogen atom optionally has a substituent selected from the group consisting of hydrogen atom, C1-6alkyl, monohalogenoC1-6alkyl, dihalogenoC1-6alkyl, trihalogenoC1-6alkyl, C3-6cycloalkyl, hydroxyC2-6alkyl, C1-6alkoxyC2-6alkyl, C1-6alkylcarbonyl, hydroxyC1-6alkylcarbonyl, C1-6alkoxycarbonyl, carbamoyl, C1-6alkylcarbamoyl, di(C1-6alkyl)carbamoyl, sulfamoyl, C1-6alkylsulfamoyl, di(C1-6alkyl)sulfamoyl, C1-6alkylsulfonyl, aminoC2-6alkyl, C1-6alkylaminoC2-6alkyl, di(C1-6alkyl)aminoC2-6alkyl, di(C1-6alkyl)aminoC1-6alkylcarbonyl, heterocycle, heterocyclic oxy, heterocyclic thio, heterocyclic sulfinyl, heterocyclic sulfonyl, heterocyclic C1-6alkyl, heterocyclic carbonyl, heterocyclic C1-6alkylcarbonyl, heterocyclic C1-6alkylsulfinyl, and heterocyclic C1-6alkylsulfonyl (wherein, when the nitrogen atom forms tertiary amine, it is optionally of an N-oxide form); and optionally, the C1-6alkyl is partially unsaturated or has a C3-6cycloalkyl moiety, and a carbon atom in the heterocycle exists in a carbonyl form.
地址 Hwaseong-si KR