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Title:
COMPOUND AND APPLICATION THEREOF FOR TREATMENT OF CATARACTS
Document Type and Number:
WIPO Patent Application WO/2017/186135
Kind Code:
A1
Abstract:
Disclosed in the present invention are a compound and an application thereof for the treatment of cataracts. The structural formula of the compound is shown in formula I. The compound shown in formula I, a prodrug thereof, or a pharmaceutically acceptable salt thereof can be used for preventing, relieving, or reversing the accumulation of crystallin in cells; 90% of the protein component in crystallin cells is crystallin (CRY), comprising the three families of α-, β-, and γ-CRY, and mutation of the crystallin can trigger protein accumulation in the cell, leading to cataract disease; the present invention selected the α-CRY family mutants αA-Y118D and αB-R120G, the β-CRY family mutant βB2-V187E, and the γ-CRY family mutants γC-G129C and γD-W43R as research models of cataract disease to examine the effect of the compound of the present invention. Compared to existing small molecules (such as C29, Science, 350, 674), the small molecules of a novel structure provided in the present invention have better activity in inhibiting protein accumulation caused by intracellular crystallin mutation, improve absorption of the drugs by the body, and do not have toxic side-effects on normal crystallin cells.

Inventors:
RAO, Yu (Renhuan Building, Tsinghua UniversityHaidian District, Beijing 4, 100084, CN)
YAN, Yong-Bin (School of Life Sciences, Tsinghua UniversityHaidian District, Beijing 4, 100084, CN)
YANG, Xinglin (Renhuan Building, Tsinghua UniversityHaidian District, Beijing 4, 100084, CN)
CHEN, Xiang-Jun (School of Life Sciences, Tsinghua UniversityHaidian District, Beijing 4, 100084, CN)
Application Number:
CN2017/082111
Publication Date:
November 02, 2017
Filing Date:
April 27, 2017
Export Citation:
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Assignee:
TSINGHUA UNIVERSITY (Patent Office Box Tsinghua University, 4 Extension Box 82, Beijing 100084, 100084, CN)
International Classes:
C07J9/00; A61K31/575; A61K31/58; A61K31/585; A61P27/12; C07J17/00; C07J41/00; C07J71/00; C07J73/00
Domestic Patent References:
WO2014117710A12014-08-07
WO2008130449A22008-10-30
Other References:
ZHONG, HAN-TING: "Triterpenes in bark of broussonetia papyrifera", TIANRAN CHANWU YANJIU YU KAIFA, vol. 24, 31 December 2012 (2012-12-31), pages 2
SHAN, WEI-GUANG ET AL.: "Tirucallane-Type Triterpenoids from Celastrus stylosus", HELVETICA CHIMICA ACTA, vol. 97, no. 11, 31 December 2014 (2014-12-31), pages 1526 - 1530, XP055554409
JING, LIN: "Tirucallane-type triterpenoids from the fruit of Ficus", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 63, no. 3, 31 December 2015 (2015-12-31), pages 237 - 243, XP055554425, DOI: 10.1248/cpb.c14-00779
LIDA, TAKASHI: "Biomimetic oxidation of unactivated carbons in steroids by a model of cytochrome P-450, oxorutheniumporphyrinate complex, Lipids", LIPIDS, vol. 39, no. 9, 31 December 2004 (2004-12-31), pages 873 - 880, XP055554429
LIN, KAI-WEI: "Triterpenoids and an alkamide from Ganoderma tsugae", FITOTERAPIA, vol. 108, 18 November 2015 (2015-11-18), pages 73 - 80, XP029367050, DOI: 10.1016/j.fitote.2015.11.003
Attorney, Agent or Firm:
JEEKAI & PARTNERS (Floor 15A, Building No.59 Guang'an Road, Fengtai District, Beijing 5, 100055, CN)
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