21-01-2021 дата публикации
Номер: US20210017154A1
Автор:
AO Wangwei,
CAO Kai,
Chen Shuo,
GE Xingfeng,
Li Yuan,
LIU Xushi,
LU Dandan,
LU Peng,
MA Xueqin,
Ni Jie,
SHEN Hangzhou,
Shi Wei,
Wang Hui,
WANG JIE,
WANG Xiaojin,
Wu Jie,
XU Hongjiang,
Zhang Huan,
Zhang Li,
ZHANG Yinsheng,
ZHAO Tianxiao
A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection. 2. The compound of Formula I claim 1 , a stereoisomer claim 1 , a tautomer claim 1 , a geometric isomer claim 1 , a solvate claim 1 , an active metabolite claim 1 , a hydrate claim 1 , a prodrug or a pharmaceutically acceptable salt thereof according to claim 1 , wherein:{'sup': 'a', 'sub': 1-3', '1-3', '2', '1-3', '6-10', '3-6, 'Ris selected from the group consisting of —C(O)Calkyl, Calkyl, —S(O)Calkyl, 5- to 6-membered heteroaryl, Caryl, Ccycloalkyl, and 3- to 6-membered heterocycloalkyl;'}{'sup': 'a', 'sub': 1-3', '1-3', '2', '1-3, 'alternatively, Ris selected from the group consisting of —C(O)Calkyl, Calkyl, and —S(O)Calkyl; and'}{'sup': 'a', 'sub': 3', '2', '3, 'alternatively, Ris selected from the group consisting of —C(O)CH, and —S(O)CH.'}3. The compound of Formula I claim 1 , a stereoisomer claim 1 , a tautomer claim 1 , a geometric isomer claim 1 , a solvate claim 1 , an active metabolite claim 1 , a hydrate claim 1 , a prodrug or a pharmaceutically acceptable salt thereof according to claim 1 , wherein:{'sup': b', 'c, 'sub': 1-3', '1-3', '2', '1-3', '6-10', '3-6, 'Rand Rare each independently selected from the group consisting of —C(O)Calkyl, Calkyl, —S(O)Calkyl, 5- to 6-membered heteroaryl, Caryl, Ccycloalkyl, and 3- to 6-membered heterocycloalkyl; and'}{'sup': b', 'c, 'sub': 1-3', '1-3', '2', '1-3, 'alternatively, Rand Rare each independently selected from the group ...
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