Substituting carbamate macrocyclic compounds and related therapeutic methods

Substituted macrocyclic compounds with specific structural features address the limitations of existing orexin-2 receptor agonists, enhancing therapeutic efficacy for narcolepsy and related disorders by improving brain permeability and safety.

JP7833486B2Active Publication Date: 2026-03-19ALKERMES INC
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2022-05-25
Publication Date
2026-03-19

AI Technical Summary

Technical Problem

Existing compounds with orexin-2 receptor agonist activity are unsatisfactory in terms of activity, pharmacokinetics, permeability to the brain/central nervous system, or safety, necessitating the development of improved compounds for treating conditions such as narcolepsy and other disorders.

Method used

Development of substituted macrocyclic compounds with specific structural features, including various alkyl, alkenyl, cycloalkyl, and heterocyclyl groups, which act as orexin-2 receptor agonists, potentially improving therapeutic efficacy.

Benefits of technology

The substituted macrocyclic compounds enhance orexin-2 receptor modulation, offering improved therapeutic potential for conditions like narcolepsy and other disorders by enhancing brain permeability and safety profiles.

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Abstract

The present invention provides Compound (I) useful for treating narcolepsy or cataplexy in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
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Citation Information

Patent Citations

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  • Medium- or large-cyclic benzyl-substituted heterocyclic derivatives and their use as orexin-2 receptor agonists

    JP2023540350A

  • Substituted piperidino compounds and related methods of treatment

    JP2023554282A