PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR

The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- ]pyrazin-7(8H)-yl]-1-(2,4,5- trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non- insulin dependent diabetes mellitus, also...

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Hauptverfasser: CYPES STEPHEN HOWARD, CHEN ALEX MINHUA, WENSLOW ROBERT, FERLITA RUSSELL, LEE IVAN, VYDRA VICKY, HANSEN KARL
Format: Patent
Sprache:eng ; srp
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Zusammenfassung:The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- ]pyrazin-7(8H)-yl]-1-(2,4,5- trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non- insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The invention also relates to a crystalline monohydrate of the dihydrogenphosphate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of diabetes, obesity, and high blood pressure. Dihidrogenfosfatna so 4-okso-4-[3-(trifluorometil)-5,6-dihidro[1,2,4]triazolo[4,3-a]pirazin-7(8H)-il]-1-(2,4,5-trifluorofenil)butan-2-amina je snažan inhibitor dipeptidil peptidaze-IV i korisna je za prevenciju i/ili lečenje ne-insulin zavisnog dijabetes melitusa, koji je označen i kao dijabetes tipa 2. Pronalazak se takođe odnosi na kristalni monohidrat dihidrogenfosfatne soli, kao i na postupak za njegovo pripremanje, farmaceutske kompozicije koje sadrže ovaj novi oblik i postupke za njegovu primenu u lečenju dijabetesa, gojaznosti i visokog krvnog pritiska.