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Monofluoro beta-secretase inhibitors
专利权人:
Astrazeneca AB
发明人:
MINIDIS, Anna,RAHM, Fredrik,VIKLUND, Jenny
申请号:
ES12773365
公开号:
ES2566373T3
申请日:
2012.10.10
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound according to formula (I): ** Formula ** wherein: A is -O-, -CH2-, -CH2CH2-, -OCH2-, -CH2O-, or -CF2-; n is 0 or 1; R1 is H, C1-6 alkyl or C0-6 alkyl C3-6 alkyl; R2 is C0-6 alkylaryl, C0-6 alkylheteroaryl, C2-6 alkynyl, C1-6 alkyl, halogen, cyano, or OR8, wherein said C0-6 alkylaryl, C0-6 alkylheteroaryl, C2-6 alkynyl, or C1 alkyl -6 is optionally substituted with one to three R7; R3 is H; R4 is H; R5 and R6 is independently hydrogen, heterocyclyl, C3-6 cycloalkyl, aryl, heteroaryl or C1-6 alkyl, wherein said heterocyclyl, C3-6 cycloalkyl, aryl, heteroaryl or C1-6 alkyl is optionally substituted with one or two selected substituents independently of halogen, C1-6 alkyl, C1-6 haloalkyl, cyano, or OR8; since R5 and R6 are not hydrogen at the same time; or R5 and R6 together with the carbon to which they are attached, form a B ring, which is a 3-7 membered cycloalkyl or heterocyclyl monocyclic ring, or a 7-12 membered cyclic cycloalkyl or heterocyclyl ring; and wherein ring B is optionally substituted by one or more substituents independently selected from oxo, halogen, C1-6 alkyl, C1-6 haloalkyl, cyano, or OR8; and ring B is optionally fused with an aryl or heteroaryl to form a bi or polycyclic system; R7 is independently C1-6 alkyl, halogen, cyano, C0-6 alkylaryl, C0-6 alkylheteroaryl, C0-6 alkylC3-6cycloalkyl, C1-6 alkyl or C2-6 alkynyl, wherein said C1-6 alkyl, alkylaryl C0-6, C0-6 alkylheteroaryl, C0-6 alkylC3-6cycloalkyl, C1-6alkyl, or C2-6 alkynyl is optionally substituted with 1-3 substituents independently selected from halogen, cyano, C1-6 alkyl, C0- alkyl 6C3-6cycloalkyl, C1-6 haloalkyl, C1-6alkyl, and C1-6alhaloalkyl; R8 is independently hydrogen, C1-6 alkyl, C0-6 alkyl, C3-6cycloalkyl, C2-6 alkynyl, aryl or heteroaryl; wherein said C1-6 alkyl, aryl or heteroaryl is optionally substituted with one or more substituents independently selected from halogen, cyano, and C1-6 alkyl; and R9 is H, F, OH, CH3, Cl or OCH3; R9 is one or more substituents ind
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