[EN] COVALENT CDK2-BINDING COMPOUNDS FOR THERAPEUTIC PURPOSES<br/>[FR] COMPOSÉS DE LIAISON À CDK2 COVALENTS UTILISÉS À DES FINS THÉRAPEUTIQUES
申请人:UMBRA THERAPEUTICS INC
公开号:WO2022187693A1
公开(公告)日:2022-09-09
Heteroaryl sulfonyl compounds and compositions that have a CDK2 Recognition Moiety bound to an electrophile for the selective covalent modification of CDK2 to treat CDK2-mediated disorders are described.
In connection with the known antisecretory activity of the benzotriazepinone (1) and the pyridylurea (2), novel pyridotriazepinones (3 and 4) have been synthesized. They were prepared from aminopyridinecarboxylic acids via several steps, and their structures were confirmed by X-ray crystallographic analysis. Attempts to synthesize the positional isomer (24) resulted in formation of the pyridotriazine (25 or 26). Some of these compounds showed moderate antisecretory activity in rats.
根据已知的苯并三氮杂卓酮(1)和吡啶脲(2)的抗分泌活性,我们合成了新型吡啶三氮杂卓酮(3 和 4)。它们由氨基吡啶羧酸经过几个步骤制备而成,其结构已通过 X 射线晶体学分析得到证实。尝试合成位置异构体(24)的结果是形成了哒嗪(25 或 26)。其中一些化合物在大鼠体内显示出中等程度的抗分泌活性。