您的位置: 首页 > 农业专利 > 详情页

5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
专利权人:
JANSSEN PHARMACEUTICA NV
发明人:
TRESADERN, GARY, JOHN,GIJSEN, HENRICUS, JACOBUS, MARIA,ROMBOUTS, FREDERIK, JAN, RITA,MACDONALD, GREGOR, JAMES,MARTINEZ LAMENCA, CAROLINA,TRABANCO-SUAREZ, ANDRES, AVELINO,VAN GOOL, MICHIEL, LUC, MARIA
申请号:
NZ60342711
公开号:
NZ603427A
申请日:
2011.06.08
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Abstract - 603427 Disclosed are 5-(3-(aryl / heteroaryl)-phenyl)-5,6-dihydro-2H-1,4-oxazin-3-amine derivatives as represented by the general Formula (I) or a tautomer or a stereoisomeric form thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen, fluoro, cyano, alkyl, mono- and polyhalo-alkyl, and cycloalkyl R4 is fluoro or trifluoromethyl or R1 and R2, or R3 and R4 taken together with the carbon atom to which they are attached may form a cycloalkanediyl ring R5 is selected from the group consisting of hydrogen, alkyl, cyclopropyl, mono- and polyhalo-alkyl, homoaryl and heteroaryl X1, X2, X3, X4 are independently C(R6) or N, provided that no more than two thereof represent N each R6 is selected from the group consisting of hydrogen, halo, alkyl, mono- and polyhalo-alkyl, cyano, alkyloxy, mono- and polyhalo-alkyloxy L is a bond or -N(R7)CO-, wherein R7 is hydrogen or alkyl Ar is homoaryl or heteroaryl homoaryl is phenyl or phenyl substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkyloxy, mono and polyhalo-alkyl, mono- and polyhalo-alkyloxy heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, tetrazolyl, thiazolyl, isothiazolyl, thiadiazolyl, oxazolyl, isoxazolyl and oxadiazolyl, each optionally substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkynyl, alkyloxy, mono- and polyhalo-alkyl, mono- and polyhalo-alkyloxy, and alkyloxy-alkyloxy or an addition salt or a solvate thereof. Also disclosed are compounds such as 5-biphenyl-3-yl-5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine trifluoroacetate salt, 5-(3,5-dichlorobiphenyl-3-yl)-5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine, 5-methyl-5-(3-pyrimidin-5-ylphenyl)-5,6-dihydro-2H-1,4-oxazin-3-amine trifluoroacetate salt, 5-[3-(5-methoxypyridin-3-yl)phenyl]-5-methyl-5,6-dihydro-
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