NOVEL SALT OF EMPAGLIFLOZIN DERIVATIVE, WHICH IS SGLT-2 INHIBITOR, AND HYDRATE OF SALT

• Main Authors: SUNG, Si-Young, SON, Byoung-Hwa, LIM, Hong-Gyu, JANG, Sun-Woo, OH, Yun-Seok, KIM, Ji-Hyeon, KIM, Jung-Soo, TERMSARASAB, Ubonvan
• Format: Patent
• Language: English; French; Korean
• Published: 31.03.2022
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SUGARS

The present invention relates to a novel salt of an empagliflozin derivative and a hydrate of the salt, which have a relatively higher fusion point, solubility and melting point than those of empagliflozin, which is a drug developed as an SGLT-2 inhibitor, and thus exhibit improved physical and chemical properties, which is very suitable for formulation. In addition, a salt of a compound of chemical formula 1 prepared according to the present invention and a hydrate of the salt exhibit excellent pharmacokinetic characteristics as compared to empagliflozin, and thus are effective as SGLT-2 inhibitors. La présente invention concerne un nouveau sel d'un dérivé d'empagliflozine et un hydrate de sel, qui ont un point de fusion, une solubilité et une température de fusion relativement plus élevés que ceux de l'empagliflozine, qui est un médicament développé en tant qu'inhibiteur de SGLT-2, et présente ainsi des propriétés physiques et chimiques améliorées, ce qui est très approprié pour la formulation. De plus, un sel d'un composé de formule chimique 1 préparé selon la présente invention et un hydrate du sel présentent d'excellentes caractéristiques pharmacocinétiques par rapport à l'empagliflozine, et sont donc efficaces en tant qu'inhibiteurs de SGLT-2. 본 발명은 엠파글리플로진 유도체의 신규염 및 염의 수화물에 관한 것으로서, SGLT-2 억제제로 개발된 약물인 엠파글리플로진보다 상대적으로 높은 융점, 용해도 및 녹는점을 가짐으로써 물리화학적 성상을 개선시켜 제제화에 매우 적합하다. 또한, 본 발명에 의해 제조된 화학식 1 화합물의 염 및 염의 수화물은 엠파글리플로진보다 우수한 약동력학(pharmacokinetics) 특성을 보여, SGLT-2 억제제로 유용하다.