Crystalline forms, compositions containing same, and methods of their use
Inventors
Vaswani, Rishi G. • Gu, Chong-Hui
Assignees
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Publication Number
US-12606553-B2
Publication Date
2026-04-21
Expiration Date
Abstract
Disclosed are crystalline forms of the compound of formula (I): (I) Also disclosed are compositions containing the crystalline forms of the compound of formula (I) and methods of their use. The methods may be for treating cancer in a subject in need thereof, e.g., by administering to the subject an effective amount of the crystalline form disclosed herein or its composition.
Core Innovation
The disclosed subject matter relates to crystalline forms of a compound of formula (I). One crystalline form is characterized by a powder X-ray diffraction (PXRD) pattern having peaks at specified 2θ values, and further crystalline characterization is provided by differential scanning calorimetry (DSC) thermograms and thermal gravimetric analysis (TGA) observations.
The description further states that a second crystalline form is characterized by solvent inclusion, including solvent loss on melting, and differing hygroscopicity as measured by dynamic vapor sorption (DVS). The document links the crystalline forms to solid-form characterization outcomes obtained through solid-state screening and characterization using XRPD/DSC/TGA/DVS.
In addition, the document discloses pharmaceutical compositions and unit dosage forms comprising the crystalline forms for administration. The stated therapeutic use is to treat cancer and disorders by modulating a BAF chromatin remodeling complex, including inhibiting BRG1 and/or BRM, and therapeutic endpoints include tumor size, tumor growth, metastatic progression, and survival, together with apoptosis-related outcomes.
Claims Coverage
The partial document includes two independent claims. Across both independent claims, the core inventive coverage is the identification of specific crystalline forms of a compound of formula (I) by defined PXRD peak positions, optionally further characterized by additional thermal or formulation limitations in dependent claims.
Crystalline form with specified PXRD peaks at 14.4 and 17.4 2θ
A crystalline form of the compound of formula (I) is characterized by a powder x-ray diffraction pattern having peaks at 14.4±0.2° 2θ and 17.4±0.2° 2θ.
Crystalline form with specified PXRD peaks at 7.7, 9.4, and 17.0 2θ
A crystalline form of the compound of formula (I) is characterized by a powder x-ray diffraction pattern having peaks at 7.7±0.2° 2θ, 9.4±0.2° 2θ and 17.0±0.2° 2θ.
The independent claims define two different crystalline forms of a compound of formula (I) using PXRD peak positions, with further dependent claim refinements adding additional PXRD peak constraints, a DSC endothermic onset characterization, and inclusion in pharmaceutical composition and unit dosage form formats.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treating cancer and disorders by modulating a BAF chromatin remodeling complex, including inhibiting BRG1 and/or BRM, with therapeutic endpoints including tumor size, tumor growth, metastatic progression, and survival.
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