Salts of 3-(4-amino-1-oxo-1,3-dihydro-iso-indol-2-yl)piperdine-2,6-dione and derivatives thereof, polymorph of the salts, preparation and application thereof

A technology of polymorphs and preparations, applied in 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione and its Salts of derivatives or polymorphs of salts and their preparation and application fields can solve problems such as easy hydrolysis, compound instability, and no compound reports yet

Active Publication Date: 2014-07-09
XIAJIANG HEMEI PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, compound (II) is unstable under alkaline conditions and is easily hydrolyzed
Thereby, do not see the report of the salt of relevant compound (II) so far

Method used

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  • Salts of 3-(4-amino-1-oxo-1,3-dihydro-iso-indol-2-yl)piperdine-2,6-dione and derivatives thereof, polymorph of the salts, preparation and application thereof
  • Salts of 3-(4-amino-1-oxo-1,3-dihydro-iso-indol-2-yl)piperdine-2,6-dione and derivatives thereof, polymorph of the salts, preparation and application thereof
  • Salts of 3-(4-amino-1-oxo-1,3-dihydro-iso-indol-2-yl)piperdine-2,6-dione and derivatives thereof, polymorph of the salts, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0190] Take the compound (518 mg) represented by (II, where Y represents H) and an equimolar organic acid and add it to ethanol, heat and stir, add a small amount of water, continue stirring for 30 minutes, then stir at room temperature, and continue stirring for 4 hours after the solid is precipitated , suction filtration, and the filter cake was vacuum-dried for 10 hours. The water solubility of the obtained salt (1:1) is shown in Table 1.

[0191] Table one: (II, wherein Y represents the solubility of the organic acid salt of H) in water

[0192] Example Organic Acid Solubility (mg / mL, 15°C)

Embodiment 1

[0193] Embodiment 1 benzenesulfonic acid 3.76

Embodiment 2

[0194] Embodiment 2 methanesulfonic acid 1.85

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PUM

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Abstract

3-(4-Amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione and its derivatives salts or polymorphs of salts and salts thereof Preparation and application The present invention discloses a pharmaceutically acceptable strong acid of 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione Salts and solvates thereof, their preparation and use in the preparation of medicaments for the treatment of those diseases or physiological abnormalities for which the curative effect can be achieved by inhibiting inflammatory factors or angiogenesis. The pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione provided by the present invention, Its water solubility is far greater than that of 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione free base, and the present invention also has Pharmaceutically acceptable strong acid salts of 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione and solvates thereof are disclosed of polymorphs.

Description

technical field [0001] The present invention relates to salts of 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione with various acids or solvents for these salts Compounds, polymorphs of salts or solvates of salts, methods for their preparation, and applications in the preparation of medicaments for treating those diseases whose curative effect can be achieved by inhibiting inflammatory factors or neovascularization. Background technique [0002] 3-(4-Amino-1-oxo-1,3-dihydroisoindol-2-yl)piperidine-2,6-dione (II, wherein Y represents H) has multiple pharmacological effects. Compound (II) can inhibit the release of inflammatory factors in the body, and can also inhibit the formation of new blood vessels, so it can be widely used in the treatment of various diseases, including but not limited to inflammation, autoimmune abnormalities, cancer and immune rejection syndrome (see US Patent 5635517, 6281230, Chinese Patent 200510013292.3). [0003] [0004] Tumor ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04A61K31/454A61P29/00A61P43/00A61P19/02A61P25/16A61P17/06A61P17/00A61P35/00A61P35/02
CPCC07D209/46C07D211/88C07D401/04A61P1/00A61P1/16A61P9/00A61P11/00A61P13/00A61P17/00A61P17/06A61P19/00A61P19/02A61P25/16A61P29/00A61P35/00A61P35/02A61P37/00A61P43/00
Inventor 张和胜马丽鹃李幸稳曾广怀
Owner XIAJIANG HEMEI PHARMA CO LTD
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