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Novel crystal form of sacubitril tromethamine salt, and preparation method and applications thereof

A kind of technology of sacubitril, tributanetriol, which is used in the field of pharmaceutical compositions for preventing or treating chronic heart failure or hypertension, and the new crystal form of sacubitril , which can solve the problems of unstable crystal form and long preparation period of crystal form

Inactive Publication Date: 2017-06-16
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the process of preparing and measuring the physical and chemical properties of the crystalline form α of the tritamine salt of Shakubi, we found that the crystalline form has disadvantages such as long preparation period and relatively unstable crystal form.

Method used

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  • Novel crystal form of sacubitril tromethamine salt, and preparation method and applications thereof
  • Novel crystal form of sacubitril tromethamine salt, and preparation method and applications thereof
  • Novel crystal form of sacubitril tromethamine salt, and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1: Preparation of Shakubi Trimethamine Salt Form II

[0066] At 20-25° C., the sacubitridine salt crystalline form I was placed in an airtight container (relative humidity of about 94%) filled with a saturated aqueous solution of potassium nitrate for 24 hours. The obtained sample was dried under reduced pressure at 20-25° C. to obtain crystalline form II of sacubitridine trioxide.

[0067] Measured 1 H NMR result is: 1 H NMR (400MHz) δ: 1.046-1.064(d, 3H), 1.115-1.141(q, 3H), 1.382-1.417(m, 1H), 1.740-1.788(m, 1H), 2.229-2.296(m, 4H ),2.649-712(m,2H),3.339(s,6H),3.900-4.019(m,3H),7.248-7.269(d,2H),7.321-7.362(m,1H),7.433-7.471(m , 2H), 7.568-7.589 (m, 2H), 7.640-7.663 (m, 2H), 7.786-7.807 (m, 2H).

[0068] Measured 1 In the H NMR results, the signal peaks at the chemical shift of 1.046-1.064 (d, 3H) are assigned to the methyl H on the chiral position in Shakubi, and the signal peaks at 3.339 (s, 6H) are assigned to ammonia The three methylene Hs in butane...

Embodiment 2

[0073] Example 2: Preparation of Shakubi Trimethamine Salt Form II

[0074] At 35-40°C, place sacubitrexate crystalline form I in an airtight container filled with a saturated aqueous solution of potassium nitrate (relative humidity of about 90%), and place it for 12 hours to obtain sacubitrexate Butane trioxide salt form II.

Embodiment 3

[0075] Example 3: Preparation of Shakubi Trimethamine Salt Form II

[0076] At 0-5°C, place Sacubitrexate trioxide crystal form I in a closed container (relative humidity 99%) filled with a saturated aqueous solution of potassium sulfate, and place it for 12 hours to obtain Sacubitrexate Trialkoxide Form II.

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PUM

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Abstract

The present invention relates to a new crystal form of sacubi trimethamine salt, which has high purity, low hygroscopicity and good solubility, and is suitable for preparing various preparations; the present invention also relates to the preparation of the new crystal form The method, the pharmaceutical composition containing the new crystal form, and the use of the new crystal form in the preparation of drugs for preventing or treating chronic heart failure or hypertension.

Description

technical field [0001] The present invention relates to the fields of organic chemistry and pharmacy, in particular to a new crystal form of sacubitridine salt and a preparation method thereof, and a pharmaceutical composition comprising the new crystal form of sacubitridine salt , and the use of the new crystal form in the preparation of drugs for preventing or treating chronic heart failure or hypertension. Background technique [0002] Sacubitril, English common name: Sacubitril, also known as: AHU-377, chemical name: 4-{[(2S,4R)-1-([1,1'-biphenyl]-4-yl)- 5-ethoxy-4-methyl-5-oxopent-2-yl]amino}-4-oxobutanoic acid is a kind of enkephalinase inhibitor, the structure is shown in formula a: [0003] [0004] When sacubitril or its salt is administered in combination with angiotensin II AT1 receptor antagonists, such as valsartan, it can simultaneously inhibit neprilysin and angiotensin receptors, that is, it can simultaneously act on the kidney It acts on the neuroendocr...

Claims

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Application Information

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IPC IPC(8): C07C233/47C07C215/10C07C231/24C07C213/10A61K31/216A61K31/4178A61K31/41A61K31/4184A61P9/12A61P9/04
CPCC07C233/47C07B2200/13C07C213/10C07C215/10C07C231/24
Inventor 陈大峰高炳坤赵永龙何永耀秦莉娜雷有成罗杰向志祥
Owner SICHUAN HAISCO PHARMA CO LTD
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