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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Применить Всего найдено 2. Отображено 2.
02-11-2017 дата публикации

COMPOUND AND APPLICATION THEREOF FOR TREATMENT OF CATARACTS

Номер: WO2017186135A1
Автор: RAO, Yu, YAN, Yong-Bin, YANG, Xinglin, CHEN, Xiang-Jun
Принадлежит:

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 ...

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Номер записи: 1
08-11-2018 дата публикации

COMPOUND AND APPLICATION THEREOF FOR TREATMENT OF CATARACT

Номер: WO2018201516A1
Автор: RAO, Yu, YAN, Yongbin, YANG, Xinglin, YANG, Zimo, CHEN, Xiangjun
Принадлежит:

A compound and an application thereof for treatment of cataract. The structural formula of the compound is as shown in formula I. The compound of formula I, a prodrug thereof, or a pharmaceutically acceptable salt thereof, can be used to prevent, alleviate, or reverse aggregation of lens proteins in cells. In lens cells, more than 90% of protein components are crystallins (CRYs), comprising the three families of α, β, and γ-CRY, and mutation of the lens proteins causes aggregation of proteins in the cells, leading to cataract diseases. α-CRY family mutants αA-Y118D and αB-R120G, an β-CRY family mutant βB2-V187E, and γ-CRY family mutants γC-G129C and γD-W43R were selected for a study model of cataract diseases to detect effects of the compound. Compared with existing micromolecules (such as C29, Science 350, 674), the micromolecule with a novel structure has better activity in inhibiting protein aggregation caused by intracellular lens protein mutation, improves absorbability of drugs by ...

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Номер записи: 2