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    • 8. 发明申请
    • Neuramindase Inhibitor
    • 神经酰胺糖苷酶抑制剂
    • US20080113924A1
    • 2008-05-15
    • US11721581
    • 2005-12-16
    • Shinichiro NishimuraHiroshi HinouHirosato KondoKazuhiko Fujiwara
    • Shinichiro NishimuraHiroshi HinouHirosato KondoKazuhiko Fujiwara
    • A61K31/7048A61K31/366A61K31/35C07D311/02
    • C07H15/203C07H15/26C07H17/075C12Q1/04C12Q1/34G01N2333/924G01N2800/26
    • 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: A1 represents an aryl group optionally having a substituent group or a heteroaryl group optionally having a substituent group; A2 represents —CX2R6 or —CHXR6 wherein X represents —F, —Cl, —Br, or —I; R1 represents a hydrogen atom or an alkyl group optionally having a substituent group; R2, R3, R4, and R5 represent each independently —OC(═O)R6, —OR6, —N(R6)2, —N3, —NHC(═NH)NHR6, —NHCOR6, —OSO3R6, —OPO3(R6)2, F, Cl, Br, or I; and R6 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.
    • 提供了对神经氨酸酶具有不可逆抑制活性的新型化合物,治疗剂和涉及神经氨酸酶的疾病检测剂。 由下式(I)表示的化合物及其盐,其制备方法及其施加方法,其中:A 1表示任选具有取代基的芳基或杂芳基 任选具有取代基; 其中X代表-F,-Cl, - , - , - Br或-I; R 1表示氢原子或任选具有取代基的烷基; R 2,R 3,R 4和R 5各自独立地表示-OC(-O)R 6, - 6, - (R 6)2 - , - N 3 - ,-NHC(-NH)NHR 6,-NHCOR 6,-OSO 3,< 6< 6> -OPO 3(R 6)2,F,Cl,Br或I; 和R 6各自独立地表示氢原子,任选具有取代基的烷基,任选具有取代基的芳基或任选取代的杂芳基。