IP Library Granted Patent US 11,136,339
Granted Patent B2
US 11,136,339 · App. 16/488,568 · Granted Oct 5, 2021

Dihydroartemisinin diploid derivative, pharmaceutical composition thereof, and application

Inventors: Xinsong Li (Nanjing, CN); Ma Si (Nanjing, CN); Longbing Ling (Nanjing, CN)
Assignee: SOUTHEAST UNIVERSITY
C07D519/00A61P17/06A61P19/02A61P33/06A61P35/00C07F9/65525
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Quick Facts
Patent No.
US 11,136,339
App. No.
16/488,568
Granted
Oct 5, 2021
Kind
B2
Abstract

Disclosed are a dihydroartemisinin dimer derivative, a pharmaceutical composition, and an application thereof. The derivative is an artemisinin dimer used for drugs treating or preventing malaria caused by plasmodium, drugs treating autoimmune diseases such as lupus erythematosus, and anti-tumour drugs, which is a pharmaceutical composition prepared from the dihydroartemisinin dimer derivative and a pharmaceutically acceptable carrier.

Claims (7)

1. A method for treating parasitosis, autoimmune disease, tumor, leukemia, toxoplasmosis or skin disease comprising a step of administrating a dihydroartemisinin dimer derivative to a subject in need of treatment;

wherein the dihydroartemisinin dimer derivative has a general formula (1) or a pharmaceutically acceptable salt thereof:

wherein X is selected from a group consisting of

CH 2 , CH 2 —CH 2 , CH 2 —CH 2 —CH 2 , CH 2 —CH 2 —CH 2 —CH 2 , CH 2 —S—S—CH 2 , CH 2 —CH 2 —S—S—CH 2 —CH 2 , CH 2 —O—CH 2 , O—CH 2 —CH 2 —O, O—CH 2 —CH 2 —CH 2 —O, O—CH 2 —CH 2 —CH 2 —CH 2 —O, O—CH 2 —CH 2 —O—CH 2 —CH 2 —O, O—CH 2 —CH 2 —O—CH 2 —CH 2 —O—CH 2 —CH 2 —O, O—CH 2 —CH 2 —SS—CH 2 —CH 2 —O—CO—CH 2 —CH 2 , O—CH 2 —CH 2 —CH 2 —CH 2 —O—CO—CH 2 —CH 2 , O—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —O—CO—CH 2 —CH 2 , O—CH 2 —CH 2 —CH 2 —O—CO—CH 2 —CH 2 , O—CH 2 —CH 2 —O—CO—CH 2 —CH 2 , NH—CH 2 —CH 2 —NH, NH—CH 2 —CH 2 —CH 2 —NH, NH—CH 2 —CH 2 —CH 2 —CH 2 —NH, NH—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —NH, NH—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —NH, O—CH 2 —CH 2 —S—S—CH 2 —CH 2 —O and NH—CH 2 —CH 2 —S—S—CH 2 —CH 2 —NH;

and Y is selected from a group consisting of

2. The method according to claim 1 , wherein the parasitosis is selected from a group consisting of malaria, schistosomiasis, toxoplasmosis, leishmaniasis, filariasis and ancylostomiasis.

3. The method according to claim 1 , wherein the autoimmune disease is selected from a group consisting of systemic lupus erythematosus, rheumatoid arthritis, systemic vasculitis, pemphigus, mixed connective tissue disease, autoimmune hemolytic anemia, thyroid autoimmune disease and ulcerative colitis.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 23, 2019
From: LI, XINSONG; SI, MA; LING, LONGBING
To: SOUTHEAST UNIVERSITY
Reel/Frame 050154/0989 →
Priority Claims (1)
CN 201710115410.4 · Feb 28, 2017 · national
Continuity (1)
Related Publication 20200040008A1 · Feb 6, 2020