Title:
MODIFIED HYDROPHOBIC AUXILIARY MATERIAL, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/252713
Kind Code:
A1
Abstract:
The present invention relates to the preparation of a hydrophobic medicinal auxiliary material and a drug-loaded fat emulsion, and in particular to a hydrophobic auxiliary material with the structural formula as shown below, wherein R is a hydrophobic natural compound or hydrophobic synthetic compound with one to three hydroxyl groups (n=1-3), R1 is an alpha-amino protecting group, and R2 is an amino acid side chain; when m=0, R reacts with an amino acid derivative with a protecting group by means of esterification to form a hydrophobic auxiliary material carrying the amino acid derivative with a protecting group; or, when m＝1, R first introduces an amino acid linking arm of different chain lengths (l=1, 2, 4, 6) by means of an ester group, and then introduces an amino acid derivative with a protecting group to form a hydrophobic auxiliary material carrying an amino acid derivative polypeptide with a protecting group. The introduction of an amino acid derivative with an aromatic, alkoxycarbonyl or acyl amino protecting group on the hydrophobic auxiliary material is conducive to increasing the solubility of the drug in the hydrophobic auxiliary material and improving the stability of the drug-loaded fat emulsion.
Inventors:
GAO XIANG (CN)
Application Number:
PCT/CN2019/091964
Publication Date:
December 24, 2020
Filing Date:
June 19, 2019
Export Citation:
Assignee:
ZHEJIANG ZHIDA PHARMACEUTICAL CO LTD (CN)
International Classes:
C07C271/22; A61K9/107; A61K31/337; A61K47/18; A61K47/54; A61P35/00; C07C269/06; C07J9/00
Foreign References:
| CN108026138A | 2018-05-11 |
Other References:
WANG JUN, HU XIAO-LI ,WEN WEI-HE ,YANG LEI-LEI ,YANG JING ,ZHU YU-LIANG: "Synthesis of N Fmoc protection dipeptide of 11-deoxyglycyrrhetinic acid derivatives", CHEMICAL REAGENTS, vol. 34, no. 5, 15 May 2012 (2012-05-15), pages 473 - 475, XP055875366, ISSN: 0258-3283, DOI: 10.13822/j.cnki.hxsj.2012.05.023
WANG JUN, HU XIAO-LI ,WEN WEI-HE ,YANG LEI-LEI ,YANG JING ,ZHU YU-LIANG: "Synthesis of N Fmoc protection dipeptide of 11-deoxyglycyrrhetinic acid derivatives", CHEMICAL REAGENTS, vol. 34, no. 5, 15 May 2012 (2012-05-15), CN, pages 473 - 475, XP055875366, ISSN: 0258-3283, DOI: 10.13822/j.cnki.hxsj.2012.05.023
JINGHAN WANG, BEIJIA KUANG, XIAOQIAN GUO, JIANWEI LIU, YAHUI DING, JIANGNAN LI, SHENDE JIANG, YING LIU, FANG BAI, LUYUAN LI, QUAN : "Total Syntheses and Biological Activities of Vinylamycin Analogues", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 60, no. 3, 9 February 2017 (2017-02-09), pages 1189 - 1209, XP055766264, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.6b01745
WANG JUN, HU XIAO-LI ,WEN WEI-HE ,YANG LEI-LEI ,YANG JING ,ZHU YU-LIANG: "Synthesis of N Fmoc protection dipeptide of 11-deoxyglycyrrhetinic acid derivatives", CHEMICAL REAGENTS, vol. 34, no. 5, 15 May 2012 (2012-05-15), CN, pages 473 - 475, XP055875366, ISSN: 0258-3283, DOI: 10.13822/j.cnki.hxsj.2012.05.023
JINGHAN WANG, BEIJIA KUANG, XIAOQIAN GUO, JIANWEI LIU, YAHUI DING, JIANGNAN LI, SHENDE JIANG, YING LIU, FANG BAI, LUYUAN LI, QUAN : "Total Syntheses and Biological Activities of Vinylamycin Analogues", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 60, no. 3, 9 February 2017 (2017-02-09), pages 1189 - 1209, XP055766264, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.6b01745
Attorney, Agent or Firm:
BEIJING WEIZHENG PATENT AGENCY CO., LTD. (CN)
Download PDF:
Previous Patent: WIRELESS COMMUNICATION METHOD AND DEVICE
Next Patent: NOVEL ANTIOXIDANT FOR PRINTED CIRCUIT BOARD AND APPLICATION THEREOF
Next Patent: NOVEL ANTIOXIDANT FOR PRINTED CIRCUIT BOARD AND APPLICATION THEREOF