申请人:Juntendo Educational Foundation
公开号:EP4104835A1
公开(公告)日:2022-12-21
Providing a RyR2 activity inhibitor having an excellent RyR2 activity inhibitory effect.
A type 2 ryanodine receptor activity inhibitor comprising a compound represented by the following formula (α1) or a salt thereof, or a solvate of the compound or a salt thereof,
wherein
ring Q1 and ring Q2 each independently represent a condensed ring of a monocyclic heterocycle or monocyclic carbocyclic ring and a benzene ring, or a benzene ring,
R1 and R2 each independently represent a substituted or unsubstituted hydrocarbon group having 1 to 8 carbon atoms, a substituted or unsubstituted alkoxy group having 1 to 8 carbon atoms, a substituted or unsubstituted alkoxycarbonyl group having 2 to 8 carbon atoms, a substituted or unsubstituted alkanoyl group having 2 to 8 carbon atoms, a substituted or unsubstituted alkanoyloxy group having 2 to 8 carbon atoms, a hydroxy group, a cyano group or a halogen atom,
R3 represents a hydrogen atom or a substituted or unsubstituted hydrocarbon group having 1 to 8 carbon atoms,
R4 represents a divalent hydrocarbon group having 1 to 8 carbon atoms,
X represents an oxygen atom or a sulfur atom,
Y represents a methine group or a nitrogen atom, and
n and m each independently represent an integer of 0 to 5;
with the proviso that, if n is an integer of 2 to 5, n number of R1 may be the same or different and two R1 may join together to form a ring; and if m is an integer of 2 to 5, m number of R2 may be the same or different and two R2 may join together to form a ring.
提供一种具有优异RyR2活性抑制效果的RyR2活性抑制剂。
一种 2 型雷诺丁受体活性抑制剂,包含下式(α1)代表的化合物或其盐,或该化合物或其盐的溶液、
其中
环 Q1 和环 Q2 各自独立地代表单环杂环或单环碳环与苯环的缩合环或苯环、
R1 和 R2 各自独立地代表具有 1 至 8 个碳原子的取代或未取代的烃基、具有 1 至 8 个碳原子的取代或未取代的烷氧基、具有 2 至 8 个碳原子的取代或未取代的烷氧羰基、具有 2 至 8 个碳原子的取代或未取代的烷酰基、具有 2 至 8 个碳原子的取代或未取代的烷酰氧基、羟基、氰基或卤素原子、
R3 代表氢原子或具有 1 至 8 个碳原子的取代或未取代的烃基、
R4 代表具有 1 至 8 个碳原子的二价烃基、
X 代表氧原子或硫原子、
Y 代表甲基或氮原子,以及
n 和 m 各自独立地代表 0 至 5 的整数;
但条件是,如果 n 是 2 至 5 的整数,R1 的 n 数可以相同或不同,两个 R1 可以连接在一起形成一个环;如果 m 是 2 至 5 的整数,R2 的 m 数可以相同或不同,两个 R2 可以连接在一起形成一个环。