申请人:Nishimura Shinichiro
公开号:US20080113924A1
公开(公告)日:2008-05-15
There are provided a novel compound having irreversible inhibitory activity against neuraminidase, a therapeutic agent and a detection agent for a disease involving neuraminidase. A compound represented by the following formula (I) and a salt thereof, a production method thereof, and an application method thereof,
wherein:
A
1
represents an aryl group optionally having a substituent group or a heteroaryl group optionally having a substituent group;
A
2
represents —CX
2
R
6
or —CHXR
6
wherein X represents —F, —Cl, —Br, or —I;
R
1
represents a hydrogen atom or an alkyl group optionally having a substituent group;
R
2
, R
3
, R
4
, and R
5
represent each independently —OC(═O)R
6
, —OR
6
, —N(R
6
)
2
, —N
3
, —NHC(═NH)NHR
6
, —NHCOR
6
, —OSO
3
R
6
, —OPO
3
(R
6
)
2
, F, Cl, Br, or I; and
R
6
represents each independently a hydrogen atom, an alkyl group optionally having a substituent group, an aryl group optionally having a substituent group, or an optionally substituted heteroaryl group.
提供了一种具有对神经氨酸酶具有不可逆抑制活性的新型化合物,一种治疗剂和一种用于涉及神经氨酸酶的疾病的检测剂。一种由以下式(I)表示的化合物及其盐,其生产方法和应用方法,其中:A1表示可选地具有取代基的芳基或可选地具有取代基的杂芳基;A2表示—CX2R6或—CHXR6,其中X表示—F、—Cl、—Br或—I;R1表示氢原子或可选地具有取代基的烷基;R2、R3、R4和R5分别独立地表示—OC(═O)R6、—OR6、—N(R6)2、—N3、—NHC(═NH)NHR6、—NHCOR6、—OSO3R6、—OPO3(R6)2、F、Cl、Br或I;和R6分别独立地表示氢原子、可选地具有取代基的烷基、可选地具有取代基的芳基或可选地取代的杂芳基。