THIOPHENE [2, 3-D]PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF

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专利名称 THIOPHENE [2, 3-D]PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF 申请号 EP20120884787 专利类型 EP 公开(公告)号 EP2835372(B1) 公开(授权)日 2016.05.04 申请(专利权)人 中国科学院福建物质结构研究所 发明(设计)人 LU, CANZHONG;YONG, JIANPING 主分类号 C07D495/04 IPC主分类号 C07D495/04;A61K31/519;A61P35/00 专利有效期 THIOPHENE [2, 3-D]PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF 至THIOPHENE [2, 3-D]PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF 法律状态 说明书摘要 This invention provides thieno[2,3-d]pyrimidine derivatives containing isoxazole heterocycle represented by formula (I), or pharmaceutically acceptable salts thereof Wherein: R 1 and R 2 may be the same or different and is independently to each other selected from H, C 1-6 alkyl, C 1-6 alkoxy, halo-C 1-6 alkyl or halo-C 1-6 alkoxy, aryl group optionally substituted by R 7 or heteroaryl group optionally substituted by R 8 ; or R 1 and R 2 together with the carbon atoms to which they are attached, may form a 4- to 6-membered carbocyclic ring or heterocyclic ring; said carbocyclic ring or heterocyclic ring is optionally substituted by H, C 1-6 alkyl, halogen, nitro, or amino; said heterocyclic ring contains at least one heteroatom selected from N, O or S; Z is -NR 6 -, C(R 6 ) 2 , -S- or -O-, in which R 5 is H or C 1-6 alkyl, and R 6 is the same or different, selected from H, C 1-6 alkyl or hydroxyl substituted C 1-6 alkyl; R 3 is selected from H, halogen, C 1-6 alkyl, C 1-6 alkoxy, halo-C 1-6 alkyl or halo-C 1-6 alkoxy; n is an integer of 0-5; R 4 is selected from H, C 1-6 alkyl, C 1-6 alkoxy or halo-C 1-6 alkyl, aryl group optionally substituted by R 9 , or heteroarylgroup optionally substituted by R 10 ; R 7 , R 8 , R 9 or R 10 independently to each other, is selected from H, hydroxy, mercapto, cyano, amino, nitro, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, carboxy, halo-C 1-6 alkyl or halo-C 1-6 alkoxy. This invention also provides the preparation method and medicinal uses of the compounds of formula (I) and pharmaceutically acceptable salts thereof. and this class of compounds can be used as medicants or lead compounds for the treatment of diseases such as tumors, cancers.

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