SALTS OF OMECAMTIV MECARBIL AND PROCESS FOR PREPARING SALTS

• Main Authors: CHARLES BERNARD, KARTHIK NAGAPUDI, JACQUELINE WOO, NEIL FRED LANGILLE, CUI SHENG, MUCI ALEX, SHAWN WALKER, ALAN MARTIN ALLGEIER, STEVEN MENNEN, KARL BENNETT HANSEN, BRADLEY PAUL MORGAN, HENRY MORRISON
• Format: Patent
• Language: English; Japanese
• Published: 18.04.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide novel salts and polymorphic crystalline forms of omecamtiv mecarbil useful as therapeutic agents for heart failure.SOLUTION: There is provided a dihydrochloride salt of omecamtiv mecarbil having the structure in the figure. Preferably, the salt exhibits an X-ray powder diffraction pattern comprising peaks at about 6.6, 14.9, 20.1, 21.4, and 26.8±0.2° 2θ using Cu Kα radiation, and has crystalline forms having an endothermic transition at about 230°C to about 240°C as measured by differential scanning calorimetry.SELECTED DRAWING: None 【課題】心不全の治療薬として有用なオメカムチブメカルビルの新規な塩及び多形結晶形状の提供。【解決手段】下記構造を有するオメカムチブメカルビルのジヒドロクロリド塩。前記塩は、ＣｕＫα照射により、約６．６、１４．９、２０．１、２１．４及び２６．８±０．２°２θでのピークを含むＸ線粉末回折パターンを示し、示差走査熱量測定によって測定される場合、約２３０℃〜約２４０℃での吸熱転移を有する結晶形態であることが好ましい。【選択図】なし