FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to novel crystalline forms of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrol-2,5-dione acetate salt, their use for the treating the diseases mediated by T-lymphocytes or PKC, to a pharmaceutical compositions thereof, and a method for preparing them. The presented crystalline forms have: a strong diffraction peak at the angle of 2θ making 21.5° for the A form, or a strong diffraction peak at the angle of 2θ making 9.7° for the B form. The mentioned crystalline forms can be prepared by dissolving 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrol-2,5-dione in 2-propanol at higher temperature, and then cooling after salt formation for preparing the A form, or dissolving 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrol-2,5-dione in ethyl acetate at higher temperature and then cooling after salt formation for preparing the B form.
EFFECT: there are prepared novel crystalline form of the biologically active compound with the improved properties, which may be effectively used in medicine.
11 cl, 8 ex, 11 dwg
| Title |
Year |
Author |
Number |
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2008 |
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|
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2012 |
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|
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2014 |
- Le-Floik Aleksandr
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|
RU2680826C9 |
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2014 |
|
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2016 |
|
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2009 |
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- Novikov Fedor Nikolaevich
- Shtil' Aleksandr Al'Bertovich
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2006 |
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- Vu Rain
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- Brotsio Jerg
|
RU2483065C2 |
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2006 |
- Manli Pol U.
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|
RU2509767C1 |
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2013 |
- Barbudzhan Natale Alvaro
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|
RU2602071C2 |
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2010 |
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|
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