Solid forms of APOL1 inhibitor and methods of using same
Inventors
GAGNON, Kevin James • Li, Jicong • Medek, Ales • MINCHOM, Jack Raphael • Shi, Yi • Shrestha, Muna • WITKOS, Faith
Assignees
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Publication Number
US-12577233-B2
Publication Date
2026-03-17
Expiration Date
Abstract
The disclosure provides novel solid state forms of Compound I selected from ethanol solvate Form A, ethanol solvate Form B, citric acid cocrystal Form A, and Form B, compositions comprising the same, and methods of making and using the same, including use in treating APOL1 mediated kidney disease. (I).
Core Innovation
The invention relates to solid forms of Compound I, including Ethanol solvate Form A, Ethanol solvate Form B, Citric acid cocrystal Form A, and Form B, alongside methods for their preparation. These solid forms are characterized using solid-state analytical techniques, including X-ray powder diffraction, solid-state NMR, thermogravimetric analysis, and differential scanning calorimetry. The disclosed subject matter further encompasses pharmaceutical compositions comprising these solid forms.
The solid forms are directed to APOL1 inhibition and the treatment of APOL1-mediated kidney diseases, including focal segmental glomerulosclerosis and non-diabetic kidney disease. Stated technical benefits for Form A include reduced agglomeration, improved dissolution, and improved processability during filtration and drying. Because the background section is omitted from the available content, the specific technical problem being solved is not explicitly described in patent.
Claims Coverage
The claims identify six inventive features across six independent claims, covering solid forms of Compound I and methods for their preparation.
Solid forms of Compound I
Claim 1 covers a solid form of Compound I selected from Ethanol solvate Form A, Ethanol solvate Form B, Citric acid cocrystal Form A, and Form B.
Preparation of Ethanol solvate Form A
Claim 24 covers a method of preparing Ethanol solvate Form A of Compound I.
Preparation of Ethanol solvate Form B
Claim 25 covers a method of preparing Ethanol solvate Form B of Compound I.
Preparation of Citric acid cocrystal Form A
Claim 26 covers a method of preparing Citric acid cocrystal Form A of Compound I from Compound I and citric acid.
Preparation of Form A
Claim 27 covers alternative methods of preparing Form A of Compound I, including methods involving crystallization and isolation.
Preparation of Form B
Claim 28 covers a method of preparing Form B of Compound I from Compound I Amorphous Form.
The independent claims cover four identified solid forms of Compound I and methods for preparing Ethanol solvate Form A, Ethanol solvate Form B, Citric acid cocrystal Form A, Form A, and Form B. Dependent claims further identify pharmaceutical compositions and therapeutic uses involving APOL1-mediated kidney disease and APOL1 inhibition.
Stated Advantages
Form A is stated to have reduced agglomeration.
Form A is stated to have improved dissolution.
Form A is stated to have improved processability, including filtration and drying.
Documented Applications
Pharmaceutical compositions comprising a solid form of Compound I and a pharmaceutically acceptable carrier.
Inhibition of APOL1 activity by contacting APOL1 with a solid form of Compound I.
Treatment of APOL1-mediated kidney disease, including ESKD, NDKD, FSGS, HIV-associated nephropathy, arterionephrosclerosis, lupus nephritis, microalbuminuria, and chronic kidney disease.
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