您的位置: 首页 > 农业专利 > 详情页

Macrocyclic quinazoline derivatives as antiproliferative
专利权人:
詹森药业有限公司;JANSSEN PHARMACEUTICAL N.V.;詹森藥業有限公司
发明人:
E.J.E.弗雷纳,E.J.E.弗雷納,T.P.S.佩雷拉,P.J.J.A.布伊恩斯特斯,M.威廉斯,G.S.M.迪尔斯,G.S.M.迪爾斯,W.C.J.埃穆布雷希茨,P.滕 霍尔特,P.滕 霍爾特,F.J.R.罗姆布茨,F.J.R.羅姆布茨,C.舒尔茨法德姆雷希特,C.舒爾茨法德姆雷希特,E.J.E.弗雷纳,E.J.E.弗雷納,T.P.S.佩雷拉,P.J.J.A.布伊恩斯特斯,M.威廉斯,G.S.M.迪尔斯,G.S.M.迪爾斯,W.C.J.埃穆布雷希茨,P.滕 霍尔特,P.滕 霍爾特,F.J.R.罗姆布茨,F.J.R.羅姆布茨,C.舒尔茨法德姆雷希特,C.舒爾茨法德姆雷希特
申请号:
MOJ002151
公开号:
MOJ002151B
申请日:
2016.05.04
申请国别(地区):
MO
年份:
2016
代理人:
摘要:
The present invention relates to formula (I) compound and its N- oxide forms, pharmaceutically acceptable addition salt and its stereoisomeric forms in any ratio, wherein Z represents O, CH2, NH or S; Especially, Z represents NH; 9 alkyl of Y representatives-C3-,9 alkenyls of-C3-,9 alkynyls of-C3-,Optionally by amino,It is mono- or two(4 alkyl of C1)The substituted 7 alkyl-CO-NH of C3 of 4 alkoxycarbonyl amino of amino or C1-,Optionally by amino,It is mono- or two(4 alkyl of C1)7 alkenyl-the CO-NH of C3 that 4 alkoxycarbonyl amino of amino or C1-optionally replaces,5 alkyl of C1-5 alkyl of oxygroup-C1-,5 alkyl NR13 of-C1,5 alkyl of-C1-,5 alkyl-NR14-CO-C1 of C1,5 alkyl-,5 alkyl-CONR15-C1 of-C1,5 alkyl,6 alkyl-CO-NH- of-C1,6 alkyl-NH-CO- of-C1,3 alkyl-NH-CS-Het20- of C1,3 alkyl-NH-CO-Het20 of-C1,2 alkyl-CO-Het21-CO- of-C1,3 alkyl of-Het22-CH2-CO-NH-C1-,6 alkyl of-CO-NH-C1-,6 alkyl of-NH-CO-C1-,7 alkyl of-CO-C1-,7 alkyl-CO- of-C1,6 alkyl-CO-C1 of-C1,6 alkyl-,2 alkyl-NH-CO-CR16R17-NH- of-C1,2 alkyl-CO-NH-CR18R19-CO- of-C1,2 alkyl-CO-NR20-C1 of-C1,3 alkyl-CO-,3 alkyl-NH- of 2 alkyl-NR21-CH2-CO-NH-C1 of-C1,3 alkyl-or-NR22-CO-C1; X1 represents 2 alkyl of connecting key, O or-O-C1-, 2 alkyl of CO ,-CO-C1-, 2 alkyl of NR11 ,-NR11-C1-,-CH2- ,-O-N=CH- or 2 alkyl of C1-; X2 represents connecting key, O, 2 alkyl of-O-C1-, 2 alkyl of CO ,-CO-C1-, 2 alkyl of NR12 ,-NR12-C1-,-CH2- ,-O-N=CH- or 2 alkyl of C1-. In the enzyme test of receptor tyrosine kinase EGFR, it was demonstrated that the compounds of this invention has growth in vitro inhibitory action anti-tumor activity.本發明涉及式(I)化合物及其N-氧化物形式、藥學上可接受的加成鹽及其立體異構形式,其中,Z代表O、CH2、NH或S;尤其是,Z代表NH;Y代表-C3 9烷基-、-C3 9烯基-、-C3 9炔基-、任選被氨基、單-或二(C1 4烷基)氨基或C1 4烷氧基羰基氨基-取代的C3 7烷基-CO-NH、任選被氨基、單-或二(C1 4烷基)氨基或C1 4烷氧基羰基氨基-任選取代的C3 7烯基-CO-NH、C1 5烷基-氧基-C1 5烷基-、-C1 5烷基NR13、-C1 5烷基-、C1 5烷基-NR14-CO-C1 5烷基-、-C1 5烷基-CONR15-C1 5烷基、-C1 6烷基-CO-NH-、-C1 6烷基-NH-CO-、C1 3烷基-NH-CS-Het20-、-C1 3烷基-NH-CO-Het20、-C1 2烷基-CO-Het21-CO-、-Het22-CH2-CO-NH-C1 3烷基-、-CO-NH-C1 6烷基-、-N
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充