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A polymorphic form of a gnrh receptor antagonist and a preparation method thereof

A technology of crystal forms and compounds, applied in the field of polymorphic forms of GnRH receptor antagonists and their preparation, can solve the problems of easy agglomeration, fine crystallization, poor product stability, etc.

Active Publication Date: 2021-07-27
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally speaking, amorphous drug products have no regular crystal structure and often have other defects, such as poor product stability, fine crystallization, difficult filtration, easy agglomeration, poor fluidity, etc.

Method used

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  • A polymorphic form of a gnrh receptor antagonist and a preparation method thereof
  • A polymorphic form of a gnrh receptor antagonist and a preparation method thereof
  • A polymorphic form of a gnrh receptor antagonist and a preparation method thereof

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Embodiment Construction

[0036] In the specification and claims of the present application, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. However, for a better understanding of the present invention, definitions and explanations of some related terms are provided below. In addition, when the definitions and explanations of terms provided in this application are inconsistent with the meanings commonly understood by those skilled in the art, the definitions and explanations of terms provided in this application shall prevail.

[0037] The "beating" in the present invention refers to the method of purifying substances with poor solubility in solvents but good solubility of impurities in solvents. The beating purification can remove color, change crystal form or remove a small amount of impurities.

[0038] The "cyano group" in the present invention refers to groups such as -CN.

[0039] "C" described in the p...

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Abstract

The invention discloses a polymorphic form of a GnRH receptor antagonist and a preparation method thereof. Specifically, the present invention discloses 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazine-3- yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxyurea ( Polymorphic forms A, B, C, D of formula (I) compound) and preparation method thereof, its application in pharmaceutical composition and this polymorphic form and composition have GnRH receptor antagonist in the preparation treatment and / or prevention Use in related diseases.

Description

technical field [0001] The present invention relates to 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)- A, B of 4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxyurea , C, D crystal forms and their preparation methods, their application in pharmaceutical compositions, and the A, B, C, D crystal forms, and their pharmaceutical compositions in the preparation of treatment and / or prevention of diseases related to GnRH receptor antagonists Uses in medicine. Background technique [0002] Endometriosis is a common estrogen-dependent gynecological disease that often occurs during women's reproductive years, and its mechanism of action is still unclear. At present, endometriosis is mainly diagnosed by laparoscopy and treated by surgery, or controlled by taking contraceptives, GnRH receptor agonists or progestins to reduce estrogen levels in the body. [0003] Gonadotropin-releasing hormone (GnRH), also known as...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519C07D487/04A61P15/00A61P15/08
CPCA61K31/519A61P15/00A61P15/08C07D487/04
Inventor 张全良贾君磊边林高晓晖
Owner JIANGSU HENGRUI MEDICINE CO LTD
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