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Free alkali crystal form of phenylpropionamide derivative and preparation method of free alkali crystal form

A technology of crystal form and diffraction angle, which is applied in the preparation methods of peptides, chemical instruments and methods, and medical preparations containing active ingredients, etc., can solve the problems of poor fluidity, high hygroscopicity, and poor product stability.

Active Publication Date: 2019-03-05
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 alkali crystal form of phenylpropionamide derivative and preparation method of free alkali crystal form
  • Free alkali crystal form of phenylpropionamide derivative and preparation method of free alkali crystal form
  • Free alkali crystal form of phenylpropionamide derivative and preparation method of free alkali crystal form

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Embodiment Construction

[0018] 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.

[0019] 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 alkali crystal form of phenylpropionamide derivative and a preparation method of the free alkali crystal form. The invention particularly relates to a novel crystal form of phenylpropionamide derivative free alkali, i.e. a crystal form I of a compound shown in formula (I). The invention also relates to a preparation method of the crystal form I, a medicine composition, and an application of the medicine composition in preparing medicine for preventing and / or treating relevant KOR agonist-mediated diseases. The crystal form I of the compound shown in the formula(I) has good stability and can be better used for clinic treatment. (Shown in the description).

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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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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