Modulators of RXFP1 and methods of use thereof

Small molecule modulators of RXFP1, like compounds of Formula (A), (A*), and (I), address the short half-life issue of serelaxin by activating RXFP1, offering prolonged therapeutic benefits for cardiovascular and fibrotic diseases.

WO2026136248A1PCT designated stage Publication Date: 2026-06-25RUBIX THERAPEUTICS INC
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
RUBIX THERAPEUTICS INC
Filing Date
2025-12-15
Publication Date
2026-06-25

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Abstract

Provided herein are small molecule modulators of RXFP1, and methods of making and use thereof. These compounds are pharmacological mimetics of relaxin H2 signaling and are capable of activating RXFP1. This activation triggers intracellular signaling pathways that mediate physiological functions in many tissues, including the reproductive, cardiovascular, renal, hepatic, and connective tissues. As such, these compounds are useful in the treatment of a variety of indications, including heart failure and other RXFP1 related diseases in patients in need thereof.
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