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Salt of fused heterocyclic derivative and crystal thereof

A technology of crystals and compounds, applied in the field of salts of fused heterocyclic derivatives and their crystals, can solve the problems of no reports, etc., and achieve the effects of easy handling, good storage stability and fluidity

Active Publication Date: 2012-10-24
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] This document only includes a general description of the salt as a pharmaceutically acceptable salt of compound (B), and does not report a specific salt

Method used

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  • Salt of fused heterocyclic derivative and crystal thereof
  • Salt of fused heterocyclic derivative and crystal thereof
  • Salt of fused heterocyclic derivative and crystal thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Compound (A)

[0040] The 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3 ,4-Tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid (3.07g) and 46% choline hydroxide aqueous solution (1.64g) are suspended in 1-propanol and water (about 1:1 volume ratio; 30mL) in the mixed solution, and the mixture was heated at 60°C and stirred for 15 minutes. To the mixture was added 1-propanol (30 mL) at 60°C, and the mixture was stirred at room temperature for 1 hour, and then stirred for another hour under ice cooling. After collecting the precipitate by filtration, it was washed twice with 1-propanol (1 mL). The obtained solid was dried under reduced pressure at 40° C. to obtain compound (A) (2.93 g). In addition, the compound was heated and stirred at 60° C. in a mixed solvent of 1-propanol and water (about 1:1 volume ratio; 30 mL), and 1-propanol (30 mL) was added to the solution obtained after hot filtration. The mixture was cooled to room temperat...

Embodiment 2

[0056] Compound (A)

[0057] The 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3 ,4-Tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid (4.07g), 46% choline hydroxide aqueous solution (2.18g), 2-propanol (200mL) and water (100mL) are mixed, And heated at 40°C for 15 minutes. After the insoluble matter was removed by filtration, the resulting solution was concentrated and 2-propanol (80 mL) and diisopropyl ether (80 mL) were added. Then, the mixture was stirred at room temperature for about 1 hour, and then stirred under ice cooling for about 4 hours. The precipitated solid was collected and dried under reduced pressure at 90° C. overnight (yield 3.59 g). Then a mixed solution of ethanol and water (about 1:1 volume ratio; 25 mL) was added to the obtained solid (3.56 g). The mixture was heated to 65°C, and after adding a mixed solution of ethanol and water (1:1 volume ratio; 10 mL) at the same temperature, it was subjected to hot filtration. Th...

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Abstract

The purpose of the present invention is to improve the solubility of a 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)- 4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d] pyrimidine-5-carboxylic acid. Disclosed is a choline salt represented by formula (A), which has excellent solubility and excellent storage stability.

Description

Technical field [0001] The present invention relates to a compound represented by the following formula (chemical name: 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2 ,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt; hereinafter referred to as "compound (A)"): [0002] [Chemical formula 1] [0003] [0004] The compound has antagonistic activity against gonadotropin-releasing hormone and can be used as a preventive or therapeutic agent for sex hormone-dependent diseases such as benign prostatic hypertrophy, uterine fibroids, endometriosis, Uterine fibroids, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, etc. Background technique [0005] Patent Document 1 discloses a compound represented by the following formula (hereinafter referred to as "compound (B)"), which has antagonistic activity against gonadotropin releasing hormone and can be used as a preventive or therapeutic agent for sex hormone-dependent dise...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/519A61P5/04A61P15/08A61P15/16A61P15/18A61P35/00
CPCC07D495/04A61K31/14A61K31/519A61P1/04A61P13/08A61P15/00A61P15/02A61P15/08A61P15/10A61P15/16A61P15/18A61P17/00A61P17/10A61P17/14A61P25/20A61P25/28A61P35/00A61P35/04A61P43/00A61P5/04A61P5/06A61P5/08A61P5/24C07C211/63A61K9/0053C07B2200/13
Inventor 城一道竹内秀树
Owner KISSEI PHARMA
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