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Novel triphenyl compound salt

A technology of phenyl and benzoate salts, which is applied in the field of new triphenyl compound salts, can solve problems such as difficulties in the uniformity of pharmaceutical compositions, and achieve the effect of reducing hygroscopicity

Pending Publication Date: 2022-07-08
TAIHO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hygroscopic compounds are problematic due to their hygroscopic properties, which lead to changes in the quality of the compound depending on the amount of water present in the surrounding environment, making it difficult to accurately assess the biological efficacy of the compound and ensure the uniformity of pharmaceutical compositions including the compound

Method used

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  • Novel triphenyl compound salt
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Examples

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preparation example Construction

[0098] Oral solid dosage forms are prepared as follows. After the excipients and binders, disintegrants, lubricants, colorants, taste-masking agents or flavoring agents, etc. are optionally added to the benzoate of Compound A or the sorbate of Compound A, the The resulting mixture is formulated into tablets, coated tablets, granules, powders, capsules and the like by known methods.

[0099] Examples of excipients include lactose, sucrose, D-mannitol, glucose, starch, calcium carbonate, kaolin, microcrystalline cellulose, and silicic anhydride. Examples of binders include water, ethanol, 1-propanol, 2-propanol, simple syrup, liquid glucose, liquid alpha-starch, liquid gelatin, D-mannitol, carboxymethylcellulose, hydroxypropylcellulose , hydroxypropyl starch, methyl cellulose, ethyl cellulose, shellac, calcium phosphate, polyvinylpyrrolidone, etc. Examples of disintegrants include dry starch, sodium alginate, powdered agar, sodium bicarbonate, calcium carbonate, sodium lauryl ...

Embodiment 1

[0208] Product Example 1: 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl ]Phenyl]-2-Fluoro-benzonitrile (Compound A) Preparation

[0209] Compound A was prepared by the synthetic method of Example Compound 37 described in PCT Publication No. WO2017 / 090756.

Embodiment 2

[0210] Product Example 2: Synthesis of Benzoate Crystals of Compound A

[0211] 260 mg of benzoic acid was dissolved in 26 mL of methyl isobutyl ketone, and the mixture was added to 1000 mg of Compound A obtained according to the method of Product Example 1. The suspension was stirred at room temperature for about 16.5 hours, filtered, and the solid was collected and dried to give 845.2 mg of the purported crystals (yield: 67%).

[0212] The obtained crystals were subjected to powder X-ray diffraction, differential scanning calorimetry (DSC) measurement and moisture absorption / desorption tests.

[0213] figure 1 is the powder X-ray diffraction spectrum of the crystal of the benzoate of Compound A. figure 2 is the differential scanning calorimetry (DSC) curve of a crystal of Compound A's benzoate salt.

[0214] exist figure 1 , the crystal of the benzoate of Compound A has characteristic peaks at diffraction angles (2θ±0.2°) of 15.3°, 16.2°, 17.8°, 21.4° and 25.5° in the p...

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Abstract

The present invention provides a benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl) phenyl] phenyl]-2-fluoro-benzonitrile. The present invention also provides a method for preparing the same. Also provided is a sorbate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl) phenyl] phenyl]-2-fluoro-benzonitrile.

Description

technical field [0001] The present disclosure relates to 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]benzene yl]-2-fluoro-benzonitrile salt. Background technique [0002] Compound 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl] -2-Fluoro-benzonitrile (referred to herein as Compound A) is known to be a potent LSD1 inhibitor and is used as an antineoplastic agent or as an agent for the prevention and / or treatment of cancer (PL 1). [0003] It is expected that this LSD1 inhibitor will exhibit stability when used in pharmaceutical formulations. [0004] Furthermore, it would be desirable to develop such a tractable inhibitor of LSD1. It is well known that the hygroscopicity of a biologically active compound affects the handling of the compound during its incorporation into a potential pharmaceutical composition. Hygroscopic compounds are problematic due to their hygroscopicity, wh...

Claims

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Application Information

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IPC IPC(8): C07D207/14
CPCC07D207/14A61K31/40A61P35/00A61P35/02C07C63/08C07B2200/13A61K31/203A61K2300/00
Inventor 中村浩之
Owner TAIHO PHARMA CO LTD