Derivatives of ([1,2,4]triazolo[5,1-a]isoquinoline-5-carbonyl)glycinate as PHD inhibitor compounds, compositions, and methods of use

Novel small molecule PHD inhibitors stabilize HIF to treat and prevent diseases by inhibiting PHD proteins, addressing hypoxia-induced tissue damage and inflammation, effectively managing conditions such as ischemic heart disease, lung inflammation, and chronic kidney disease.

AU2024407543A1Pending Publication Date: 2026-07-09AKEBIA THERAPEUTICS INC
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Patent Information

Authority / Receiving Office
AU · AU
Patent Type
Applications
Current Assignee / Owner
AKEBIA THERAPEUTICS INC
Filing Date
2024-12-18
Publication Date
2026-07-09

AI Technical Summary

Technical Problem

Current treatments for conditions such as ischemic heart disease, lung inflammation, pulmonary fibrosis, and chronic kidney disease are inadequate in addressing the underlying mechanism of hypoxia-induced tissue damage and inflammation, as they do not effectively inhibit the activity of prolyl hydroxylase domain-containing proteins (PHDs), which regulate HIF stability and contribute to these pathologies.

Method used

Development of novel small molecule PHD inhibitors, represented by compounds of Formula (I) and their pharmaceutically acceptable salts, which can selectively target and inhibit PHD proteins, thereby stabilizing HIF and reducing tissue inflammation and promoting repair.

Benefits of technology

The PHD inhibitors effectively treat and prevent a range of diseases by stabilizing HIF, reducing inflammation, and promoting tissue repair, offering therapeutic benefits for conditions like ischemic heart disease, lung inflammation, pulmonary fibrosis, and chronic kidney disease.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (I), and sub-formulas thereof: Formula (I) or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment or prevention of diseases including heart (e.g. ischemic heart disease, congestive heart failure, and valvular heart disease), lung (e.g., lung inflammation, pneumonia, acute lung injury, pulmonary hypertension, pulmonary fibrosis, and chronic obstructive pulmonary disease), respiratory (e.g.,respiratory infection, acute respiratory distress syndrome), liver (e.g. acute liver failure and liver fibrosis and cirrhosis), and kidney (e.g. acute kidney injury and chronic kidney disease) disease, inflammatory bowel disease (IBD), ischemic reperfusion injury (e.g., stroke), retinopathy of prematurity (ROP), bronchopulmonary dysplasia (BPD), and white matter injury (WMI).
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