专利详情

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.