CRYSTALLINE FORMS OF 6-(1H-IMIDAZOL-1-YL)-2-PHENYLQUINAZOLINE AND ITS SALTS Russian patent published in 2015 - IPC C07D403/04 A61K31/517 A61P29/00 A61P25/24 

Abstract RU 2557547 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel crystalline forms of 6-(1H-imidazol-1-yl)-2-phenylquinazoline of formula (I) in form of salt, selected from hydrochloride, (L)-tartrate and maleate. Compounds possess strong analgising action and can be applied in therapy in treatment of pain in case of such diseases as rheumatoid arthritis, osteoarthritis, pathologies of inflammatory diseases, gastrointestinal tract diseases, etc. Each crystalline form of salt is characterised by spectrum of X-ray powder diffraction (XRPD). Crystalline form of hydrochloride is also characterised by melting point with decomposition at approximately 240°C. Crystalline form of (L)-tartrate and crystalline form of maleate are also characterised by DSC thermograms and FTIR spectra. Crystalline form of maleate is additionally characterised by triclinic system with parameters of crystalline cell a = 8.9412 (5) E, b = 9.8081 (5) E, c = 10.5922 (6) E, α: 90.517° (4), β = 101.969° (5), γ = 99.132° (4), V = 896.34 (8) E3, space group P-1.

EFFECT: salts possess improved solubility, bioavailability and stability.

3 cl, 66 dwg, 19 tbl, 65 ex

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Authors

Dzhordani Antonio

Mandelli Stefano

Porta Francheska

Girri Matteo

Rovati Luchio Klaudio

Dates

2015-07-27Published

2010-06-04Filed