专利号:US-2024390383-A1 优先权日:2021-09-28 标题 :Dioxazines and their use in treatment of gba-related diseases 发明人:NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH 权利人:ZEVRA DENMARK AS 摘要:The present invention relates to dioxazines, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.
专利号:WO-2024159287-A1 优先权日:2023-01-30 标 题:Nav1.7- and/or nav1.8-inhibiting hydroxamates, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits 发明人:BARREIRO GABRIELA; SANT’ANA DANILO PEREIRA DE; MONTEIRO JÚLIA LAMMOGLIA; GAMBA LUIS EDUARDO REINA; LIMA LÃ?DIA MOREIRA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA 权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO – UFRJ 摘要:The invention relates to Nav1.7- and/or Nav1.8-inhibiting hydroxamates. More specifically, the present invention relates to hydroxamates that comprise formula (I): (I), in which the substituents R1 to R10, as well as the derivatives thereof, R11 to R20, are selected independently of the groups defined in the description, as well as to the processes for the preparation thereof, compositions comprising at least one of said compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits. The present invention pertains to the fields of medicinal chemistry and organic synthesis, as well as to the treatment of pain-related disorders.
参考文献:10.1021/bi1012518 摘要:French JB, Cen Y, Vrablik TL, Xu P, Allen E, Hanna-Rose W, Sauve AA. Characterization of nicotinamidases: steady state kinetic parameters, classwide inhibition by nicotinaldehydes, and catalytic mechanism. Biochemistry. 2010 Dec 14;49(49):10421–39.