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Publication Number
US-10927142-B2
Publication Date
2021-02-23
Expiration Date
Abstract
SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.
Core Innovation
A citrate salt of compound 1, identified as SCY-078, is provided with at least one specified citrate crystal form selected from Type A, Type B, Type E, Type F, Type M, Type N, Type O, Type Q, Type R, and Type S. Each crystal form is defined by an XRPD pattern comprising specific peaks at defined d-spacings and/or degrees 2 theta values.
The citrate salts and crystal forms are characterized using XRPD, DSC, TGA, and DVS, together with chemical purity by HPLC. The document also reports moisture uptake, hygroscopicity, stability under controlled humidity and temperature, thermal and moisture-related behavior, and retention after scale-up for selected citrate salts and types.
Solubility behavior is described using kinetic and equilibrium solubility measurements across multiple media and pH conditions, including dextrose buffer, phosphate buffer, SGF, FaSSIF, and FeSSIF. The disclosed characterization, conversion and interconversion among SCY-078 citrate crystalline forms, and performance properties are used to support citrate salt selection for injectable use.
Claims Coverage
The claim coverage centers on a citrate salt of compound 1 defined by multiple specified citrate crystal forms, with each form defined by an XRPD peak pattern. The coverage then narrows to essentially Type A, adds kinetic solubility constraints for Type A, and further restricts into injectable pharmaceutical compositions for intravenous use in humans and invasive fungal infection contexts.
Citrate salt of compound 1 comprising specified XRPD crystal-form types
A citrate salt of compound 1 comprising at least one of Type A, Type B, Type E, Type F, Type M, Type N, Type O, Type Q, Type R, and Type S citrate crystal forms, wherein each type is defined by an XRPD pattern comprising specified peaks at d-spacings and/or degrees 2 theta.
Citrate salt essentially made up of Type A citrate crystal form
The citrate salt of compound 1 is essentially made up of the Type A citrate crystal form.
Type A kinetic solubility thresholds in multiple media
A Type A citrate crystal form having an XRPD pattern as specified, with kinetic solubility constraints reported across multiple media including dextrose buffer pH 5.5, phosphate buffer pH 6.0, phosphate buffer pH 7.5, SGF media, FaSSIF media, and FeSSIF media.
Injectable pharmaceutical composition by dissolving in a pharmaceutically acceptable carrier
A pharmaceutical composition prepared by dissolving the citrate salt of claim 1 in a pharmaceutically acceptable carrier.
Intravenous injection pharmaceutical composition for human use
A pharmaceutical composition suitable for intravenous injection into a human.
Use for invasive candidiasis and/or invasive aspergillosis fungal infections
The method is applied to cases of invasive candidiasis and/or invasive aspergillosis fungal infections.
Overall, the claim set centers on a citrate salt of compound 1 defined by XRPD-characterized citrate crystal forms, with dependent limitations restricting composition to essentially Type A and imposing kinetic solubility thresholds. Further dependent claims narrow into an injectable pharmaceutical composition made by dissolving the citrate salt in a pharmaceutically acceptable carrier, specify intravenous administration into a human, and specify invasive candidiasis and/or invasive aspergillosis as the fungal indication.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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