Crystals
Inventors
Mcguirk, Paul Robert • Zamboni, Robert • BEVILL, Melanie • Parent, Stephan
Assignees
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Publication Number
US-11117909-B2
Publication Date
2021-09-14
Expiration Date
Abstract
Provided are crystals of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, compositions comprising the same, and methods of making and using such crystals.
Core Innovation
The invention relates to crystalline solid forms of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, including hydrate and non-solvate non-hydrate crystalline forms defined by XRPD pattern identity. The disclosure focuses on improved solid-state physical forms that are characterized by specific crystalline features rather than on the molecular identity alone.
The disclosed forms are characterized by XRPD fingerprints measured using an incident beam of Cu Kα radiation at a wavelength of 1.54059 Å. The hydrate forms are defined by at least five selected 2-theta values or, alternatively, at least five selected d-spacing values, with additional characterization by figure references and a quantitative hydration constraint.
The disclosure also provides non-solvate non-hydrate crystalline forms defined by XRPD patterns comprising specified 2-theta and/or d-spacing values under Cu Kα radiation at a wavelength of 1.54059 Å. Certain crystalline forms are further characterized by XRPD pattern conformity to referenced figures, supporting differentiation among crystalline forms and enabling defined solid-state material identification.
Claims Coverage
The consolidated claim coverage includes four distinct solid-state categories. The inventive features are centered on XRPD-based identity using listed 2-theta and/or d-spacing values measured with Cu Kα radiation at wavelength 1.54059 Å.
Cu Kα XRPD-defined hydrate by selected 2-theta values
A hydrate of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate wherein the hydrate exhibits an XRPD pattern comprising at least five 2-theta values selected from specified peak lists, wherein the XRPD is measured using an incident beam of Cu Kα radiation of wavelength 1.54059 Å.
Cu Kα XRPD-defined hydrate by selected 2-theta values or d-spacing values
A hydrate of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate wherein the hydrate exhibits at least one of an XRPD pattern comprising at least five 2-theta values selected from specified peak lists, wherein the XRPD is measured using an incident beam of Cu Kα radiation, or an XRPD pattern comprising at least five d-spacing values selected from specified peak lists.
Cu Kα XRPD-defined non-solvate non-hydrate crystalline form by selected 2-theta values
A non-solvate non-hydrate crystalline form of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate wherein the non-solvate non-hydrate crystalline form exhibits an XRPD pattern comprising at least five 2-theta values selected from specified peak lists, wherein the XRPD is measured using an incident beam of Cu Kα radiation of wavelength 1.54059 Å.
Cu Kα XRPD-defined non-solvate non-hydrate crystalline form by selected 2-theta values or d-spacing values
A non-solvate non-hydrate crystalline form of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate wherein the non-solvate non-hydrate crystalline form exhibits at least one of an XRPD pattern comprising at least five 2-theta values selected from specified peak lists, wherein the XRPD is measured using an incident beam of Cu Kα radiation, or an XRPD pattern comprising at least five d-spacing values selected from specified peak lists.
Across the independent claims provided, coverage is directed to specific hydrates and specific non-solvate non-hydrate crystalline forms of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate. The main inventive basis is an XRPD fingerprint defined by at least five specified 2-theta values, and in one claim also at least five specified d-spacing values, with XRPD measured using Cu Kα radiation (wavelength 1.54059 Å).
Stated Advantages
Not explicitly described in patent.
Documented Applications
Pharmaceutical composition containing the mono- or di-anion (depending on the hydrate/crystalline form and refinement).
Treating or controlling edema in a human by administering the hydrate or the non-solvate non-hydrate crystalline form.
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