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Free base crystal form of phenylpropanamide derivatives and preparation method thereof

A technology of crystal form and diffraction angle, which is applied in the preparation method of peptides, chemical instruments and methods, medical preparations containing active ingredients, etc., can solve problems such as poor fluidity, difficult filtration, and large hygroscopicity

Active Publication Date: 2021-07-02
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Generally speaking, amorphous pharmaceutical products often have other defects due to the lack of regular crystal structure, such as poor product stability, fine crystallization, difficult filtration, high hygroscopicity, easy caking, poor fluidity, etc. These defects often bring difficulties to practical mass production

Method used

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  • Free base crystal form of phenylpropanamide derivatives and preparation method thereof
  • Free base crystal form of phenylpropanamide derivatives and preparation method thereof
  • Free base crystal form of phenylpropanamide derivatives and preparation method thereof

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Embodiment Construction

[0019] 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.

[0020] The "C1-6 alkyl" in the present invention means a linear or branched alkyl group containing 1-6 carbon atoms. Specific examples include but are not limited to: methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, 2-methylbutyl, neopentyl, 1-ethylpropyl, n-hexyl, isohexyl, 3- Methylpentyl, 2-methylpentyl, 1-methylpentyl, 3,3-dimethyl...

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Abstract

The invention relates to a free base crystal form of phenylpropanamide derivatives and a preparation method thereof. Specifically, the present invention relates to a new crystal form of the free base of phenylpropanamide derivatives, that is, crystal form I of the compound represented by formula (I). The present invention also relates to the preparation method of the I crystal form, the pharmaceutical composition and its use in the preparation of medicines for preventing and / or treating related diseases mediated by KOR agonists. The crystal form I of the compound of formula (I) obtained in the present invention has good stability and can be better used in clinical treatment.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a chemical named (R)-N-((R)-6-amino-1-(4-(3-methylureido)piperidin-1-yl)-1-oxygen Hexan-2-yl)-2-((R)-2-((R)-2-amino-3-phenylpropanylamino)-3-phenylpropanylamino)-4-methylpentane The crystal form I of the amide compound, its preparation method, pharmaceutical composition and its use in the preparation of medicines for preventing and / or treating related diseases mediated by κ opioid receptor agonists. Background technique [0002] Opioid receptors are an important class of G protein-coupled receptors, and they are targets for the binding of endogenous opioid peptides and opioids. After activation, opioid receptors have a regulatory effect on the nervous system immunity and endocrine system. Opioids are Currently the strongest and commonly used central analgesic. Endogenous opioid peptides are opioid active substances naturally produced in mammals. The known endogenous opioid pepti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/107C07K1/02A61K38/07A61P29/00A61P17/04A61P7/10A61P3/12A61P1/00A61P11/14A61P27/06
CPCA61K38/00A61P1/00A61P3/12A61P7/10A61P11/14A61P17/04A61P27/06A61P29/00C07K5/1016
Inventor 张浩宇王林邵启云冯君贺峰
Owner JIANGSU HENGRUI MEDICINE CO LTD
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