NPY2 receptor agonists

JP2026026081A5Pending Publication Date: 2026-06-03BOEHRINGER INGELHEIM INT GMBH
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
BOEHRINGER INGELHEIM INT GMBH
Filing Date
2025-10-23
Publication Date
2026-06-03

AI Technical Summary

Technical Problem

There is a need for long-acting PYY analogues that selectively act on the NPY2 receptor with improved solubility, particularly at pH 7 and pH 6, to enhance formulation options and potential combination with other therapeutic agents for effective weight management.

Method used

PYY analogues are modified with specific amino acid sequences and attachment of half-life extending groups to the epsilon amino group of lysine or carboxylic acid groups of aspartic or glutamic acid, enhancing solubility and stability at pH 6 and pH 7, while maintaining receptor affinity.

Benefits of technology

The modified PYY analogues exhibit increased solubility and stability, allowing for improved formulation flexibility and potential combination therapies, with extended half-life for reduced administration frequency.

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Abstract

The present invention provides PYY analogs that are neuropeptide Y2 (NPY2) receptor agonists, their medical uses in the treatment and / or prevention of various diseases, conditions, or disorders, such as the treatment and / or prevention of excessive food intake, excess weight, obesity, metabolic disease, and other conditions or disorders associated with excess weight or obesity, such as diabetes and cardiovascular disease. The present invention relates to a PYY analog having an alanine at position 4, a lysine at position 7, a QRY at the C-terminus, and a half-life extending group. The analog is soluble at pH around 6 and 7. The present invention also relates to pharmaceutical compositions containing the PYY analog and pharmaceutical uses of the analog.
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