Long-acting prodrugs of rasagiline, preparing methods and uses thereof

    公开(公告)号:US11369583B2

    公开(公告)日:2022-06-28

    申请号:US16641802

    申请日:2018-08-27

    摘要: Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from each of R1 and R2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH2)n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH2)m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(═O)NH—, —NHC(═O)—; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane aliphatic group, —R3a—C(═O)O—R3b, —R3a—OC(═O)—R3b, —R3a—C(═O)NH—R3b, —R3a—NHC(═O)—R3b, —R3a—S(═O)1-2O—R3b and —R3a—OS(═O)1-2—R3b.

    Cyclohexene compounds and use thereof

    公开(公告)号:US10919856B2

    公开(公告)日:2021-02-16

    申请号:US16331797

    申请日:2017-09-05

    摘要: A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.

    CYCLOHEXENE COMPOUNDS AND USE THEREOF
    8.
    发明申请

    公开(公告)号:US20190241520A1

    公开(公告)日:2019-08-08

    申请号:US16331797

    申请日:2017-09-05

    IPC分类号: C07D211/42 C07D211/32

    摘要: A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.