Cocristales de N-{cis-3-[metil(7H-pirrolo[2,3-d]pirimidin-4-yl)amino]ciclobutil}propane-1-sulfonamida

ES3040374B2Undetermined Publication Date: 2026-07-09MOEHS IBERICA SL (100 00)

Patent Information

Authority / Receiving Office
ES · ES
Patent Type
Patents
Current Assignee / Owner
MOEHS IBERICA SL (100 00)
Filing Date
2024-04-30
Publication Date
2026-07-09

AI Technical Summary

Technical Problem

Existing formulations of N-{cis-3-[methyl (7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide, such as abrocitinib, suffer from inadequate hygroscopicity and solubility, which hinders further pharmaceutical development and drug formulation.

Method used

The formation of cocrystals with hydroxylated derivatives like 4-hydroxybenzoic and 3,4-dihydroxybenzoic acids improves the hygroscopicity and solubility of N-{cis-3-[methyl (7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide, leading to more stable and easily handled solid dosage forms.

Benefits of technology

The cocrystals exhibit reduced hygroscopicity and enhanced solubility, particularly at pH below 4.5, facilitating improved handling and dosing regimens, and maintaining stability under forced stability conditions.

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Abstract

N-{cis-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide cocrystals. The present invention relates to N-{cis-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide cocrystals, a process for obtaining said cocrystals, pharmaceutical compositions comprising said cocrystals, and their medical uses, in particular for the treatment or prevention of diseases known to be improved by inhibition of the Janus kinase 1 enzyme.
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