High potency glucocorticoid polymorphs, methods of making and uses thereof

CN122180697APending Publication Date: 2026-06-09ZHEJIANG PALOALTO PHARMA TECH CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHEJIANG PALOALTO PHARMA TECH CO LTD
Filing Date
2024-12-09
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing glucocorticoids have many side effects and insensitivity problems when treating inflammation and autoimmune diseases, especially when used at high doses, which lead to diabetes, osteoporosis, etc., and some patients are resistant to drugs, affecting the treatment effect.

Method used

A highly potent and highly selective glucocorticoid polymorph, including crystal forms K, A, C, E, F, I, L, were developed, and polymorphs with specific XRPD and DSC patterns were obtained by specific preparation methods such as suspension stirring and filtration in different solvents.

Benefits of technology

Reduces side effects during the treatment process, improves therapeutic effect, achieves the same therapeutic effect at low doses, and improves the bioavailability and stability of the drug.

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Abstract

This invention relates to a novel polymorph of (1R,2R,3aS,3bR,10aS,10bR,11S,12aS)-5,10b-difluoro-1-(((fluoromethyl)thio)carbonyl)-11-hydroxy-2,10a,12a-trimethyl-7-phenyl-1,2,3,3a,3b,7,10,10a,10b,11,12,12a-dodecylhydrocyclopenta[5,6]naphtho[1,2-F]indazole-1-ylfuran-2-carboxylic acid ester as shown in formula (I), its preparation method, and its uses. The polymorph of this invention exhibits significant efficacy, good stability, high yield, and high purity, which is helpful for the selection and design of drug delivery routes and the determination of pharmaceutical formulation process parameters, thereby improving the quality of drug production. (I)
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