Crystalline hydrate of a JAK inhibitor compound
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Publication Number
US-11702415-B2
Publication Date
2023-07-18
Expiration Date
Abstract
Provided herein is a crystalline hydrate of the compound of formula 1:Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.
Core Innovation
The disclosure relates to Form I, a crystalline hydrate (monohydrate) of the JAK inhibitor compound of formula 1. The crystalline hydrate is characterized by a powder X-ray diffraction pattern comprising diffraction peaks at 2̈ values of 5.680.20, 10.430.20, 10.940.20, and 13.080.20. Characterization further includes a differential scanning calorimetry melt endotherm peak at 212.43C, single-crystal X-ray analysis, and thermogravimetric analysis demonstrating about 3.4% weight loss consistent with monohydrate dehydration.
The disclosed form displays reversible moisture sorption, moderate hygroscopicity, and stability under accelerated conditions, including 25C/60% RH and 40C/75% RH. The disclosure additionally describes pharmaceutical compositions, including inhaled formulations, for treating respiratory diseases and lung transplant rejection. Because background and summary sections are absent from the provided partial content, the underlying problem being solved is not explicitly described in the patent.
Claims Coverage
The claims define one independent claim directed to one inventive feature encompassing a crystalline hydrate of the compound of formula 1.
Crystalline hydrate characterized by powder X-ray diffraction peaks
A crystalline hydrate of the compound of formula 1, characterized by a powder X-ray diffraction pattern comprising diffraction peaks at 2̈ values of 5.680.20, 10.430.20, 10.940.20, and 13.080.20.
The independent claim covers the crystalline hydrate defined by the specified powder X-ray diffraction peaks.
Stated Advantages
The crystalline form is reported to show stability under accelerated conditions.
Documented Applications
Pharmaceutical compositions, including inhaled formulations, and proposed treatment of respiratory diseases, including asthma, chronic obstructive pulmonary disease, cystic fibrosis, and pneumonitis, as well as lung transplant rejection.
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