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Title:
POLYMYXIN B COMPONENT OR SALT THEREOF, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/135732
Kind Code:
A1
Abstract:
Provided are a polymyxin B component or a salt thereof, and a preparation method therefor and the use thereof. The polymyxin B component comprises 1-position α,γ-diaminobutyric acid, 2-position threonine, 3-position α,γ-diaminobutyric acid, 4-position α,γ-diaminobutyric acid, 5-position α,γ-diaminobutyric acid, 6-position phenylalanine, 7-position leucine, 8-position α,γ-diaminobutyric acid, 9-position α,γ-diaminobutyric acid and 10-position threonine, which are sequentially connected, wherein the 10-position threonine is connected with the 4-position α,γ-diaminobutyric acid via an amide bond; and the 1-position α,γ-diaminobutyric acid is connected with 6-methyloctan-2 alkenoyl. The polymyxin B component or the salt thereof has a relatively strong antimicrobial activity and also has a potential application value.

Inventors:
ZHANG HANZHI (CN)
LIU HAO (CN)
HUANG ZHENHUI (CN)
SUN NING (CN)
LUO WENYAN (CN)
DING JINGUO (CN)
LIU XIAOFEN (CN)
BIAN XINGCHEN (CN)
Application Number:
PCT/CN2020/131148
Publication Date:
July 08, 2021
Filing Date:
November 24, 2020
Export Citation:
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Assignee:
SPH NO 1 BIOCHEMICAL & PHARMACEUTICAL CO LTD (CN)
International Classes:
C07K7/62; A61K38/12; A61P31/04; C07K1/16
Foreign References:
CN111072757A2020-04-28
CN109206486A2019-01-15
CN107367562A2017-11-21
CN108350034A2018-07-31
CN104086633A2014-10-08
CN110845579A2020-02-28
Other References:
ZHANG HAN-ZHI, QIN FENG, LIU HAO: "Identification of Unknown Impurities in Polymyxin B Sulfate by HPLC-MS / MS", CHINESE PHARMACEUTICAL JOURNAL, ZHONGGUO YAOXUEHUI ZHUBAN CHUBAN. ZHONGGUO-YAOXUE-ZAZHI BIANJI WEIYUANHUI, CN, vol. 53, no. 11, 1 January 2018 (2018-01-01), CN, pages 918 - 924, XP055827864, ISSN: 1001-2494, DOI: 10.11669 /cpj.2018.11.013
ZHANG HAN-ZHI, QIN FENG, LIU HAO: "Identification of Unknown Impurities in Polymyxin B Sulfate by HPLC-MS / MS", CHINESE PHARMACEUTICAL JOURNAL, ZHONGGUO YAOXUEHUI ZHUBAN CHUBAN. ZHONGGUO-YAOXUE-ZAZHI BIANJI WEIYUANHUI, CN, vol. 53, no. 11, 1 January 2018 (2018-01-01), CN, pages 918 - 924, XP055827864, ISSN: 1001-2494, DOI: 10.11669 /cpj.2018.11.013
TONY VELKOV, THOMPSON PHILIP E., NATION ROGER L., LI JIAN: "Structure−Activity Relationships of Polymyxin Antibiotics", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 53, no. 5, 11 March 2010 (2010-03-11), pages 1898 - 1916, XP055043339, ISSN: 00222623, DOI: 10.1021/jm900999h
ZHANG HANZHI: "Identification of Unknown Impurity in Polymyxin B Sulfate via HPLC-MS/MS and Photochemical Reaction", BRITISH JOURNAL OF DERMATOLOGY, OXFORD : WILEY-BLACKWELL, UK, 22 November 2017 (2017-11-22), UK, XP055827860, ISSN: 0007-0963
ZHANG HANZHI: "Identification of Unknown Impurity in Polymyxin B Sulfate via HPLC-MS/MS and Photochemical Reaction", BRITISH JOURNAL OF DERMATOLOGY, OXFORD : WILEY-BLACKWELL, UK, 22 November 2017 (2017-11-22), UK, XP055827860, ISSN: 0007-0963
SAKURA N; ITOH T; UCHIDA Y; OHKI K; OKIMURA K; CHIBA K; SATO Y; SAWANISHI H: "The contribution of the N-terminal structure of polymyxin B peptides to antimicrobial and lipopolysaccharide binding activity", BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN, CHEMICAL SOCIETY OF JAPAN,NIPPON KAGAKUKAI, JP, vol. 77, no. 10, 1 January 2004 (2004-01-01), JP, pages 1915 - 1924, XP009094340, ISSN: 0009-2673, DOI: 10.1246/bcsj.77.1915
Attorney, Agent or Firm:
WAYNE INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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