CRYSTALLINE FORM OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE Russian patent published in 2013 - IPC C07D239/48 A61K31/505 A61P31/18 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel polymorph I 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile, i.e., polymorph I TMC278, which is characterised by X-ray powder diffraction peaks at positions two theta 9.0°±0.2°, 14.3°±0.2°, 17.1°±0.2° and 24.2°±0.2°. In particular, the invention relates to a pharmaceutical composition of micro- or nanoparticles for administration via intramuscular or hypodermic injection. The invention also relates to the method of producing the polymorph I TMC278. The method involves dissolving TMC278 in ketone, heating the solution to boiling point and cooling to temperature below 0°C.

EFFECT: polymorph has HIV inhibiting properties and can be used to treat HIV infection or prevent HIV infection in case of risk of HIV infection as an active ingredient of a pharmaceutical composition.

15 cl, 8 dwg, 6 ex