[EN] TRICYCLIC HETEROARYL-SUBSTITUTED QUINOLINE AND AZAQUINOLINE COMPOUNDS AS PAR4 INHIBITORS [FR] COMPOSÉS TRICYCLIQUES DE QUINOLÉINE ET D'AZAQUINOLINE À SUBSTITUTION HÉTÉROARYLE INHIBITEURS DE PAR4
我们报告了 (+)-1-de乙酰caesalmin C、(+)-δ-caesalpin、(+)-norcaesalpinin MC 和 (+)-norcaesalpinin P 的首次对映选择性全合成。合成策略的显着特征是外切-呋喃醌单缩酮的选择性分子内狄尔斯-阿尔德反应,随后对所得五环糠基缩酮进行化学选择性还原,提供关键中间体。后者可以通过实施立体选择性氧化来收集天然产物。在获得了卡桑呋喃二萜类化合物后,我们揭示了以前未知的生物活性:(+)-1-脱乙酰凯撒明 C 刺激棕色脂肪细胞的呼吸,这被认为在肥胖治疗中发挥着核心作用。
[EN] ORAL COMPLEMENT FACTOR D INHIBITORS<br/>[FR] INHIBITEURS ORAUX DU FACTEUR D DU COMPLÉMENT
申请人:BIOCRYST PHARM INC
公开号:WO2021072198A1
公开(公告)日:2021-04-15
Disclosed are compounds of formula (I), and pharmaceutically acceptable salts thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof:
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.