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Publication Number
US-12698271-B2
Publication Date
2026-08-04
Expiration Date
Abstract
This Invention relates to a hemihydrate crystalline form of (S)-1′-(6-((2-amino-3-chloropyridin-4-yl)thio)-1,2,4-triazin-3-yl)-1,3-dihydrospiro[indene-2,4′-piperidin]-1-amine free base (Form 1). The invention also relates to pharmaceutical compositions comprising this crystalline form, and to methods of using the crystalline form and such compositions for the treatment of abnormal cell growth, such as cancer, in a mammal.
Core Innovation
The invention is a hemihydrate crystalline form of (S)-1′-(6-((2-amino-3-chloropyridin-4-yl)thio)-1,2,4-triazin-3-yl)-1,3-dihydrospiro[indene-2,4′-piperidin]-1-amine free base. The crystalline form is characterized by PXRD peaks at 2̸ values of 10.9, 14.0, 15.4, and 16.0±0.2°. Supporting characterization further includes solid-state NMR and FT-Raman spectroscopic signatures.
Comparative testing reports greater chemical stability for Form 1 than for the amorphous form. The supplied content describes pharmaceutical compositions comprising the crystalline form and its use in treatment of abnormal cell growth, including cancer. The background section is not included in the partial content, so the problem identified in that section is not explicitly described.
Claims Coverage
The provided relevant claims identify one independent claim, claim 1, comprising one inventive feature directed to the crystalline form and its PXRD characterization.
Hemihydrate crystalline form characterized by PXRD peaks
A hemihydrate crystalline form of the specified compound free base, characterized by a PXRD pattern comprising peaks at 2̸ values of 10.9, 14.0, 15.4, and 16.0±0.2°.
The independent claim centers on the specified hemihydrate crystalline form and its defining PXRD peaks. The dependent claims further describe spectroscopic signatures, limits on other physical forms, a pharmaceutical composition, cancer-treatment uses and cancer subtypes, and combination compounds.
Stated Advantages
Form 1 is reported to have greater chemical stability than the amorphous form in comparative testing.
Documented Applications
Pharmaceutical compositions comprising the hemihydrate crystalline form and at least one pharmaceutically acceptable excipient.
Treatment of abnormal cell growth, including cancer, such as ALK-positive non-small cell lung cancer, ROS1-positive non-small cell lung cancer, and B-type Raf proto-oncogene V600E mutation colorectal cancer.
Cancer-treatment use with an additional pharmaceutical compound selected from lorlatinib, binimetinib, cetuximab, or encorafenib.
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