Title:
ANTIFUNGAL WATER-SOLUBLE PRODRUG AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2021/129723
Kind Code:
A1
Abstract:
The present invention provides an antifungal water-soluble prodrug and a preparation method therefor. The structural formula of the antifungal water-soluble prodrug is represented by formula (I): in formula (I), when n is 0, R1 is methyl, and R2 is H; when n is an integer of 1-4, R1 is H, -CH3 or -C2H5, and R2 is H or NH2. In embodiments of the present invention, compounds 1-6 have good solubility; the solubility at pH of 5-6 can satisfy the requirements for preparing an injection; a solution prepared by the compounds 1-6 at pH of 5-6 is more stable at 2-8°C than at a room temperature. The prepared solution can be partially converted to hydroxy itraconazole in plasma by means of enzyme incubation. It is indicated that the compounds 1-6 can become prodrugs of the compound as represented by formula (1); and the solution prepared by the compounds 1-6 has no irritation or hemolysis, and is applicable to be prepared to the injection.
Inventors:
LIU WEI (CN)
LIU GUOQIANG (CN)
WANG YANDONG (CN)
LIU GUOQIANG (CN)
WANG YANDONG (CN)
Application Number:
PCT/CN2020/138944
Publication Date:
July 01, 2021
Filing Date:
December 24, 2020
Export Citation:
Assignee:
SHANGHAI YINGNUOFUCHENG BIOTECHNOLOGY CO LTD (CN)
International Classes:
C07D405/14; A61K31/496; A61P31/10
Foreign References:
| CN111138421A | 2020-05-12 | |||
| CN1236366A | 1999-11-24 | |||
| CN102369198A | 2012-03-07 |
Attorney, Agent or Firm:
JEEKAI & PARTNERS (CN)
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