PROCESS FOR PREPARING [(3-HYDROXYPYRIDINE-2-CARBONYL)AMINO]ALKANOIC ACIDS, ESTERS AND AMIDES
申请人:Akebia Therapeutics, Inc.
公开号:US20210122715A1
公开(公告)日:2021-04-29
Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and [3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
本发明涉及制备[(3-羟基吡啶-2-羧基)氨基]-烷基酸,其衍生物,包括5-芳基取代和5-杂环芳基取代的[(3-羟基吡啶-2-羧基)氨基]乙酸。此外,本发明还公开了制备[(3-羟基吡啶-2-羧基)氨基]乙酸前药的方法,例如[(3-羟基吡啶-2-羧基)氨基]乙酸酯和[3-羟基吡啶-2-羧基)氨基]乙酸酰胺。所公开的化合物可用作脯氨酸羟化酶抑制剂或用于治疗需要脯氨酸羟化酶抑制的疾病的药物。