INTESTINAL MCT1 CARRIER PROTEIN DESIGN-BASED PRODRUG AND PREPARATION METHOD THEREFOR

WIPO Patent Application WO/2019/228319

A1

The present invention belongs to the field of medical technology and relates to an intestinal MCT1 carrier protein design-based prodrug and a preparation method therefor, and in particular relates to a preparation method for a short-chain fatty acid analogue taking an intestinal mono-carboxylate transporter 1, MCT1 as a target point, comprising design and synthesis of a prodrug structure containing hydroxyl or amino antitumor drugs modified with acetic acid, lactic acid and pyroracemic acid analogues. A series of prodrugs provided by the present invention can improve the oral bioavailability of drugs and adjust the release speed of prodrugs. The related derivative shown in formula (I) or (II), and a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug structure thereof are as follows, wherein X, Y, n and Drug have the definitions given in the description and claims.

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SUN JIN (CN)
HE ZHONGGUI (CN)
WANG GANG (CN)

PCT/CN2019/088705

December 05, 2019

May 28, 2019

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UNIV SHENYANG PHARMACEUTICAL (CN)

A61K31/7068; C07H1/00; A61K47/54; A61P35/00; C07H19/073

WO1995018636A2	1995-07-13
WO2015066053A2	2015-05-07

CN108610384A	2018-10-02
JPS5635199B2	1981-08-15

SHENYANG JACK INTELLECTUAL PROPERTY AGENT LTD. (CN)

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