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Crystal forms and amorphous solid of relugolix compound and preparation method of crystal forms and amorphous solid

A technology of relugoli and compounds, applied in the field of drugs with gonadotropin-releasing hormone (GnRH) antagonistic activity, which can solve the problems of lack of solid form characterization and research reports

Inactive Publication Date: 2021-02-23
SUZHOU PENGXU PHARM TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Other patents (such as CN100360538C) and literature reports (such as Journal of Medicinal Chemistry, 2011, 54, 4998-5012) also disclosed the synthesis process of Relugoli, but there was no characterization and research report on the relevant solid form

Method used

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  • Crystal forms and amorphous solid of relugolix compound and preparation method of crystal forms and amorphous solid
  • Crystal forms and amorphous solid of relugolix compound and preparation method of crystal forms and amorphous solid
  • Crystal forms and amorphous solid of relugolix compound and preparation method of crystal forms and amorphous solid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Preparation of Relugoli Form M:

[0091] Add relugoli to diethyl carbonate, heat to about 100 °C to dissolve, the concentration is about 10 mg / mL, magnetically stir and cool down to about 25 °C, filter to remove crystal form F, and place the filtrate in the open for 17 h in the laboratory , a solid was precipitated, and the test XRPD showed that it was Form M.

Embodiment 2

[0093] Preparation of Relugoli Form M:

[0094] Relugoli was slurried in isopropanol at room temperature for 15 days to obtain Form P:

[0095] Prepare 10 mg / mL of relugoli suspension in isopropanol, stir at 25 °C for 15 days, filter to collect the filter cake, XRPD test shows that it is crystal form P, and the filtrate is placed in the laboratory for 23 h, and a solid is precipitated , test XRPD showed Form M.

Embodiment 3

[0097] Preparation of Relugoli Form M:

[0098] Prepare 10 mg / mL dimethylamine suspension of relugoli, stir at 25 °C for 15 days, filter to collect the filter cake, measure the XRPD of the wet filter cake, place the wet filter cake in the laboratory for 23 h, precipitate a solid, and test the XRPD Shown as Form M.

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PUM

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Abstract

The invention discloses crystal forms and an amorphous form of a gonadotropin releasing hormone (GnRH) receptor antagonist drug relugolix and a preparation method of the crystal forms and the amorphous form, and relates to the field of chemical medicines. The crystal forms and the amorphous form provided by the invention have good stability, and have great significance for the purification processof active pharmaceutical ingredients and the preparation process of drugs.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, and relates to a crystal form, an amorphous form and a preparation method of relugoli, a drug with gonadotropin-releasing hormone (GnRH) antagonistic activity. Background technique [0002] Relugolix is ​​a small-molecule gonadotropin-releasing hormone (GnRH) receptor antagonist developed by Takeda Pharmaceutical Co., Ltd., Japan, which can rapidly reduce female estrogen and progesterone. In January 2019, Relugoli was approved for marketing in Japan and was approved for the treatment and symptom relief of uterine fibroids. A new drug application is expected to be submitted to the FDA in the third quarter of 2019. [0003] Relugoli compound has the structure of formula (I) and its chemical name is 1-(4-(1-(2,6-difluorophenyl)-5-((dimethylamino)methyl)-3- (6-methoxypyridazin-3-yl)-2,4-dioxy-1,2,3,4-tetrahydrothien[2,3-d]pyrimidin-6-yl)phenyl)- 3-Methoxyurea. [0004] [0005] The pate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/519
CPCC07B2200/13C07D495/04A61K31/519A61P15/00A61P35/00
Inventor 李丕旭王鹏陈嗣平
Owner SUZHOU PENGXU PHARM TECH CO LTD
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