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Crystalline form of free base of imidazoisoindole derivatives and preparation method thereof

A technology of crystallization and crystal form, applied in the disease field with pathological characteristics of tryptophan metabolism pathway, can solve the problems of difficult filtration, fine crystallization, and the stability of crystal form needs to be improved.

Active Publication Date: 2021-10-08
JIANGSU HENGRUI MEDICINE CO LTD +2
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Generally speaking, amorphous pharmaceutical 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. These differences often lead to production Difficulty when zooming in
The stability of the existing crystal form needs to be improved

Method used

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  • Crystalline form of free base of imidazoisoindole derivatives and preparation method thereof
  • Crystalline form of free base of imidazoisoindole derivatives and preparation method thereof
  • Crystalline form of free base of imidazoisoindole derivatives and preparation method thereof

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Embodiment Construction

[0047] The starting material used in the preparation method of the crystal form of the present invention can be any form of the compound represented by formula (I), and the specific form includes but not limited to: amorphous form, any crystalline form, etc.

[0048] 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.

[0049] The "beating" in the present invention refers to the method of purifying substances with poor solubility in solvents but...

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Abstract

The invention relates to a crystal form of free base of imidazoisoindole derivatives and a preparation method thereof. Specifically, the present invention relates to A, B, C, D, E, F crystal forms of the compound shown in formula (I), and the chemical name is (S)-2-(4-(4-(4-(6- Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)piperidin-1-yl)phenyl)-1H-pyrazole-1-yl)ethanol. The present invention also relates to a preparation method for preparing A, B, C, D, E, F crystal forms, its application in pharmaceutical compositions and A, B, C, D, E, F crystal forms and pharmaceutical compositions in Preparation and treatment of diseases with pathological characteristics of IDO-mediated tryptophan metabolic pathway, the crystal forms A, B, C, D, E, and F of the compound of formula (I) obtained in the present invention have good stability, Moreover, the crystallization solvent used has low toxicity and low residue, and can be better used in clinical treatment.

Description

technical field [0001] The present invention relates to (S)-2-(4-(4-(4-(6-fluoro-5H-imidazo[5,1-a]isoindol-5-yl)piperidin-1-yl)benzene A, B, C, D, E, F crystal forms of -1H-pyrazol-1-yl) ethanol and their preparation methods, their application in pharmaceutical compositions, and the A, B, C, D, Use of E, F crystal forms and pharmaceutical compositions thereof in the preparation and treatment of diseases with pathological characteristics of IDO-mediated tryptophan metabolic pathway. Background technique [0002] Tumor biotherapy is a new treatment for tumor prevention and treatment using modern biotechnology and related products. Because of its safety, effectiveness, and low adverse reactions, it has become the fourth mode of tumor treatment after surgery, radiotherapy, and chemotherapy. It mobilizes The host's natural defense mechanism (such as the inhibition of IDO-mediated tumor immune escape mechanism) or the administration of naturally occurring highly targeted substanc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/454A61P35/00A61P35/02A61P35/04A61P25/28A61P25/24A61P37/06A61P25/22A61P25/00A61P31/18A61P27/12
CPCA61K31/454A61P25/00A61P25/22A61P25/24A61P25/28A61P27/12A61P31/18A61P35/00A61P35/02A61P35/04A61P37/06C07D487/04
Inventor 曹笑立尤凌峰肖昌琴杜振兴王立坤
Owner JIANGSU HENGRUI MEDICINE CO LTD
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