申请人:ELA PHARMA LTD
公开号:US10968185B2
公开(公告)日:2021-04-06
Inhibitor compounds and agents of Cathepsin C, CELA1, CELA3A and/or structurally related molecules thereto, compositions comprising same and uses thereof in the inhibition and/or prevention of cell and/or tissue necrosis are described. The compounds include thiazoles of Formula II,
where G1 is an optionally substituted pyrrolidine, an optionally substituted pyridine, an optionally substituted aryl, an optionally substituted piperidine, an optionally substituted piperazine, an optionally substituted imidazolidine, or an optionally substituted pyrazolidine. G3 is
or G3 is an optionally substituted alkyl, an optionally substituted aryl or an optionally cyloalkyl. G2 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted cyloalkyl or an optionally substituted heterocycle. Various applications for the described compounds, and combination therapies are described as well.
本发明描述了 Cathepsin C、CELA1、CELA3A 和/或其结构相关分子的抑制剂化合物和制剂、包含这些化合物和制剂的组合物及其在抑制和/或预防细胞和/或组织坏死中的用途。这些化合物包括式 II 的噻唑类化合物、
其中 G1 是任选取代的吡咯烷、任选取代的吡啶、任选取代的芳基、任选取代的哌啶、任选取代的哌嗪、任选取代的咪唑烷或任选取代的吡唑烷。G3 是
或 G3 是任选取代的烷基、任选取代的芳基或任选取代的环烷基。G2 是任选取代的烷基、任选取代的芳基、任选取代的环烷基或任选取代的杂环。还介绍了所述化合物的各种应用以及组合疗法。