Title:
SOLID SALT FORM OF OPIOID RECEPTOR ANTAGONIST CONJUGATE, CRYSTAL FORM, PREPARATION METHOD THEREFOR, COMPOSITION, AND USE
Document Type and Number:
WIPO Patent Application WO/2023/197934
Kind Code:
A1
Abstract:
The present invention relates to the technical field of pharmaceutical crystals, and relates to a solid salt form of an opioid receptor antagonist conjugate, a crystal form, a preparation method therefor, a composition, and a use. Specifically, the conjugate has a structure as shown in formula I, and can form a stable solid phosphate, wherein the molar ratio of phosphoric acid to the compound as shown in formula I is 1:1 to 3:1. The phosphate can be an amorphous substance, or a polymorph having a crystal form 1, 2, 3 or 4. Moreover, the preparation method is simple and feasible, and the present invention is suitable for preventing and treating intestinal dysfunction caused by opioids, such as constipation.
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Inventors:
HE MEI (CN)
Application Number:
PCT/CN2023/086632
Publication Date:
October 19, 2023
Filing Date:
April 06, 2023
Export Citation:
Assignee:
SHANGHAI HANMAI BIO PHARMA CO LTD (CN)
International Classes:
C07D519/00; A61K31/485; A61K47/60; A61P1/00; A61P1/10; A61P25/04; C07D489/08
Foreign References:
| CN107033154A | 2017-08-11 | |||
| CN103289075A | 2013-09-11 | |||
| CN102573918A | 2012-07-11 | |||
| US20160136153A1 | 2016-05-19 |
Other References:
DATABASE Registry 22 February 2022 (2022-02-22), ANONYMOUS: "Morphinan-3,14-diol, 6,6'-[3,6,9,12,15,18,21-heptaoxatricosane-1,23- diylbis(oxy)]bis[17-(cyclopropylmethyl)-4,5-epoxy-, (5α,6α)-(5'α,6'α)-, phosphate (1:2) (CA INDEX NAME)", XP093099209, retrieved from STNext Database accession no. 2760327-27-1
Attorney, Agent or Firm:
LINDA LIU & PARTNERS (CN)
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