Echinocandin analogues and preparation method therefor

Patent metadata

Field	Value
Publication number	US-12466856-B2
Application number	US-202017756721-A
Country	US
Kind code	B2
Filing date	Dec 4, 2020
Priority date	Dec 6, 2019
Publication date	Nov 11, 2025
Grant date	Nov 11, 2025

Abstract

The present invention relates to an echinocandin analogue and a preparation method therefor. The compound can be used for preventing or treating fungal infection, or for preventing, stabilizing or inhibiting fungal growth or killing fungi. An exemplary compound is represented by formula I, wherein the definitions of R 1 , R 2 , R 3 and G groups are as described in the description.

First claim

The invention claimed is:

1 . A compound of formula I or a pharmaceutically acceptable salt or isomer thereof,

wherein R 1 is selected from the group consisting of:

R 2 is selected from the group consisting of hydrogen, R B1 R B2 N—, CH 2 CH 2 NR B1 R B2 , CH 2 C(O)NR B1 R B2 , C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, aryl, heteroaryl, cyclohydrocarbyl, heterocyclyl and PEG, wherein said PEG is polyethylene glycol;
R 3 is selected from the group consisting of H, OSO 3 H and CH 2 NR B1 R B2 ;
G is a C 10-36 lipophilic unit, or

R B1 and R B2 are independently selected from the group consisting of H, —C(O)R J and C 1-10 alkyl; and
R J is independently selected from the group consisting of hydrogen, deuterium, C 1-10 alkyl, cyclohydrocarbyl and cyclohydrocarbylene.

2 . The compound or the pharmaceutically acceptable salt or isomer thereof according to claim 1 , wherein the pharmaceutically acceptable salt is selected from the group consisting of an acetate salt, a trifluoroacetate salt and a formate salt.

3 . A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt or isomer thereof according to claim 1 , and a pharmaceutically acceptable excipient.

4 . The compound of formula I or the pharmaceutically acceptable salt or isomer thereof according to claim 1 , wherein the compound of formula I is:

5 . The compound or the pharmaceutically acceptable salt or isomer thereof according to claim 4 , wherein the pharmaceutically acceptable salt is selected from the group consisting of an acetate salt, a trifluoroacetate salt and a formate salt.

6 . A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt or isomer thereof according to claim 4 , and a pharmaceutically acceptable excipient.

Assignees

• Shanghai Senhui Medicine Co Ltd
• Shanghai Shengdi Pharmaceutical Co Ltd
• Jiangsu Hengrui Medicine Co

Inventors

• Huang Jian
• Zhu Lingjian
• Jiang Wei
• Cao Weicou

Classifications

• A61P31/10

  Antimycotics · CPC title

• A61K38/12

  Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)} · CPC title

• A61K38/00

  Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title

• C07K7/56 Primary

  the cyclisation not occurring through 2,4-diamino-butanoic acid · CPC title