Inhibiting human integrin α5β1

Small molecule compounds targeting integrin α5β1 offer a promising oral therapy for pulmonary hypertension and heart failure, addressing the limitations of current treatments by providing effective inhibition of α5β1 integrin activity with improved safety and bioavailability.

WO2025064802A1 Publication Date: 2025-03-27MORPHIC THERAPEUTIC INC
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Patent Information

Application Number
PCT/US2024/047672
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-26
Filing Date
2024-09-20
Publication Date
2025-03-27

AI Technical Summary

Technical Problem

Current treatments for pulmonary hypertension, PAH, heart failure, and related diseases are limited by side effects, short drug half-life, and low bioavailability, necessitating the development of effective and safe oral α5β1 integrin inhibitors.

Method used

The development of small molecule compounds, such as those described in Formula (I), which specifically inhibit integrin α5β1, offering a potential oral therapy that can effectively target α5β1 integrin-mediated conditions without the need for frequent infusions.

Benefits of technology

These compounds demonstrate the ability to inhibit α5β1 integrin activity, providing a therapeutic benefit in treating diseases associated with increased expression or activity of integrin α5β1, such as pulmonary hypertension and heart failure, while minimizing adverse effects.

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Abstract

Disclosed are compounds of Formula (I) which may be used in the methods of treating or preventing a disease or condition responsive to inhibition of human α5β1 integrin by administering to a patient in need thereof a compound of Formula (I). Many diseases and conditions can be treated by administration of the compound of Formula (I).
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