Preparing stable amorphous form of fezolinetant, used for treatment of moderate to severe vasomotor symptoms (hot flashes) due to menopause, by providing solution of fezolinetant in solvent/mixture of solvents, removing solvent from solution, and isolating stable amorphous form of fezolinetant
	BHAVSAR J; KUMAR N; CHATURVEDI V K; KUMAR A
	2023-08-31
专利权人	MANKIND PHARMA LTD (MANK-Non-standard)
申请日期	2023-08-31
专利号	IN202311058348-A
成果简介	NOVELTY - Preparing stable amorphous form of fezolinetant involves (a) providing a solution of fezolinetant in a solvent or mixture of solvents; (b) removing the solvent from the solution obtained in step (a); and (c) isolating a stable amorphous form of fezolinetant; or, (a) providing a solution of fezolinetant in one or more solvent; (b) adding suitable pharmaceutical acid to obtain pharmaceutical salt of fezolinetant; (c) adding suitable base to the solution of step (b); and (d) isolating the stable amorphous form of fezolinetant. USE - Method for preparing stable amorphous form of fezolinetant, that used for the treatment of moderate to severe vasomotor symptoms (hot flashes) due to menopause. No biological data is given. ADVANTAGE - The amorphous, crystalline form MK-1 and crystalline form MK-2 of fezolinetant are free from other polymorphic forms and having purity > 99.9%. DETAILED DESCRIPTION - INDEPENDENT CLAIMS are included for: 1. a method for the preparing of amorphous solid dispersion of fezolinetant and one or more pharmaceutical carriers which involves: (a) providing a solution or suspension of fezolinetant in combination with one or more pharmaceutical carriers in a solvent or mixture of solvents; (b) removing the solvent from the solution or suspension obtained in step (a) or combining the solution obtained in step (a), with an anti-solvent; and (c) isolating amorphous solid dispersion of fezolinetant together with one or more pharmaceutical carrier. 2. a method for the preparing of stable amorphous solid dispersion of fezolinetant and one or more pharmaceutical carriers which involves: (a) blending fezolinetant and at least one carrier/excipient; (b) heating the blend of step (a) to form a molten slurry; (c) extruding the slurry of step (b); and (d) milling the extrudates of step (c) to obtain amorphous solid dispersion of fezolinetant; 3. a crystalline form of fezolinetant of formula (I), where (i) crystalline form MK-1 of fezolinetant characterized by X ray powder diffraction spectrum (XRPD) comprising one or more peaks selected from 9.2, 9.9, 11.9, 16.6, 18.4, 19.6, 20.0, 22.3, 25.2, 27.3, 27.6 and 28.7±0.2° (at 26 angle), or as depicted in Figure 1; or (ii) crystalline form MK-2 of fezolinetant characterized by X ray powder diffraction spectrum (XRPD) comprising one or more peaks selected from 4.8, 8.7, 9.5, 12.0, 14.3, 15.3, 16.1, 16.4, 19.2, and 20.7 ±0.2° (at 26 angle), or as depicted in Figure 2;
IPC 分类号	A61K-031/4985 ; A61P-005/30 ; C07C-309/29 ; C07C-065/11 ; C07D-487/04
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/20599
专题	中国科学院新疆生态与地理研究所
作者单位	MANKIND PHARMA LTD (MANK-Non-standard)
推荐引用方式 GB/T 7714	BHAVSAR J,KUMAR N,CHATURVEDI V K,et al. Preparing stable amorphous form of fezolinetant, used for treatment of moderate to severe vasomotor symptoms (hot flashes) due to menopause, by providing solution of fezolinetant in solvent/mixture of solvents, removing solvent from solution, and isolating stable amorphous form of fezolinetant. IN202311058348-A[P]. 2023.

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