Title:
SALT OF EBASTINE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/087611
Kind Code:
A1
Abstract:
Disclosed in the present invention is a salt of ebastine, a preparation method therefor and an application thereof. The salt of the ebastine is a 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone salt, and the preparation method therefor comprises: dissolving 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone in a solvent, adding an acid or an acid solution at 20-90°C, stirring for reaction, and then performing purification by means of column chromatography, thin-layer chromatography, recrystallization or pulping to obtain the salt. The preparation method is simple and easy to implement, high in yield, good in purity and suitable for industrial production. The salt of ebastine has good histamine H1 receptor antagonistic biological activity and water solubility, facilitates the preparation of various liquid preparations, and embodies a high clinical medication value.
Inventors:
ZHONG LINRUI (CN)
NIU BEN (CN)
LI JIAHUI (CN)
HUANG KUN (CN)
NIU BEN (CN)
LI JIAHUI (CN)
HUANG KUN (CN)
Application Number:
PCT/CN2022/086801
Publication Date:
May 25, 2023
Filing Date:
April 14, 2022
Export Citation:
Assignee:
JIANGSU LIANHUAN PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D211/46; A61P11/00; A61P11/06; A61P17/00; A61P37/08
Domestic Patent References:
| WO2011121099A2 | 2011-10-06 |
Foreign References:
| CN114014796A | 2022-02-08 | |||
| US4550116A | 1985-10-29 | |||
| CN109593058A | 2019-04-09 |
Other References:
KAMEI JUNZO, MORITA KAYO, MIYATA SHIGEO, ONODERA KENJI: "Effects of second generation of histamine H1 antagonists, cetirizine and ebastine, on the antitussive and rewarding effects of dihydrocodeine in mice", PSYCHOPHARMACOLOGY, SPRINGER VERLAG, BERLIN., DE, vol. 166, no. 2, 1 March 2003 (2003-03-01), DE , pages 176 - 180, XP093066470, ISSN: 0033-3158, DOI: 10.1007/s00213-002-1359-9
DUREJA, H. ET AL.: "Topochemical models for the prediction of permeability through blood–brain barrier.", INTERNATIONAL JOURNAL OF PHARMACEUTICS., vol. 323, no. 2,, 26 May 2006 (2006-05-26), XP027972584, ISSN: 0378-5173
FUJII T, MATSUMOTO S, AMEJIMA H, HATOYAMA T, NAKAO M, KAGEMOTO A, TANAKA K, MIYAZAKI H: "Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats.", ARZNEIMITTEL-FORSCHUNG DRUG RESEARCH, ECD EDITTIO CANTOR VERLAG , AULENDORF, DE, vol. 44, no. 4, 31 December 1994 (1994-12-31), DE , pages 527 - 538, XP009545471, ISSN: 0004-4172
DUREJA, H. ET AL.: "Topochemical models for the prediction of permeability through blood–brain barrier.", INTERNATIONAL JOURNAL OF PHARMACEUTICS., vol. 323, no. 2,, 26 May 2006 (2006-05-26), XP027972584, ISSN: 0378-5173
FUJII T, MATSUMOTO S, AMEJIMA H, HATOYAMA T, NAKAO M, KAGEMOTO A, TANAKA K, MIYAZAKI H: "Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats.", ARZNEIMITTEL-FORSCHUNG DRUG RESEARCH, ECD EDITTIO CANTOR VERLAG , AULENDORF, DE, vol. 44, no. 4, 31 December 1994 (1994-12-31), DE , pages 527 - 538, XP009545471, ISSN: 0004-4172
Attorney, Agent or Firm:
NANJING ZHIZHUAN HUIYI INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)
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