TRANS-AMANTADINE DERIVATIVE OR SALT THEREOF, AND PREPARATION METHOD THEREFOR, COMPOSITION THEREOF AND USE THEREOF

WIPO Patent Application WO/2022/193368

A1

The present invention belongs to the technical field of medicinal chemistry, and disclosed are a trans-amantadine derivative or a salt thereof, and a preparation method therefor, a composition thereof and the use thereof. Provided in the present invention is a trans-amantadine derivative having a structure as represented by formula I or a pharmaceutically acceptable salt thereof. The preparation method of the present invention comprises a two-step reaction: step 1, performing a condensation reaction by means of taking a compound as shown in formula III, a compound as shown in formula IV or a salt thereof as a starting raw material to prepare a compound as shown in formula II; and step 2, performing a reduction reaction on the compound of formula II and a reducing agent to obtain the trans-amantadine derivative as represented by formula I. The trans-amantadine derivative of the present invention has better drug efficacy in treating lung injury and coughing relative to ambroxol hydrochloride, and can be used for the preparation of a drug for treating lung injury and coughing, especially for the preparation of a drug for treating acute lung injury and refractory cough.

MOU XIA (CN)
DONG BO (CN)
ZHANG HAI (CN)
ZENG YANQUN (CN)
XU XIA (CN)
JINAG JIE (CN)

PCT/CN2021/084407

September 22, 2022

March 31, 2021

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CHENGDU SHIBEIKANG BIOMEDICAL TECH CO LTD (CN)

C07C211/52; A61K31/137; A61P11/10; C07C209/52; C07C213/02; C07C215/44; C07C249/02; C07C251/24

CN112279774A	2021-01-29
CN105693764A	2016-06-22
CN101544572A	2009-09-30
US3536713A	1970-10-27

CHENGDU JIUDING TIANYUAN INTELLECTUAL PROPERTY AGENCY LTD. (CN)

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