SYNTHESIS AND NEW SALINE FORMS OF (R)-5-((E)-2-(PYRROLIDIN-3-YLVINYL)PYRIMIDINE Russian patent published in 2014 - IPC C07D403/06 A61K31/506 A61P25/28 A61P25/24 A61P29/00 

Abstract RU 2533819 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new crystalline forms of acid addition salts of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, wherein the acid is specified in methanesulphonic, maleic, fumaric, citric, orotic, 10-camphor sulphonic acids and fencifose. The salts possess the agonist properties of neuronal nicotine receptor (NNR) and can be used for managing or preventing pain, an inflammation or a CNS disorder. Each of the crystalline salts is characterised by an X-ray powder diffraction diagram. The invention also involves an amorphous form of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine monocitrate and polymorphic forms of the above crystalline salts.

EFFECT: invention refers to a pharmaceutical composition containing an effective amount of the presented salts.

19 cl, 8 dwg, 33 ex

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RU 2 533 819 C2

Authors

Akireddi Srinivisa Rao

Bkhatti Balvinder Singkh

Katbertson Timoti Dzh.

Dall Gari Moris

Miller Krehjg Kharrison

Mitchener Ml., Dzhozef Pajk

Mun'Os Khulio A.

Otten Piter Al'Bert

Dates

2014-11-20Published

2009-11-30Filed