Crystalline forms of therapeutic compounds and uses thereof
First Claim
1. A method of inhibiting growth factor signaling comprising administering to a subject in need thereof a therapeutically effective amount of a crystalline form of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one comprising:
- (i) crystalline Form II having an X-ray powder diffraction (XRPD) pattern with peaks at about 8.44, 10.57, 14.92, 17.22, 21.26 and 22.42±
0.2 degrees two theta, or 10.47, 8.36, 5.93, 5.15, 4.18 and 3.96±
0.2 Å
in d-spacing;
or(ii) crystalline Form III having an XRPD pattern with peaks at about 9.60, 10.45, 19.30, 19.71, 21.84, and 23.42±
0.2 degrees two theta or 9.21, 8.46, 4.60, 4.50, 4.07 and 3.80±
0.2 Å
in d-spacing.
6 Assignments
0 Petitions
Accused Products
Abstract
Described herein is certain crystalline forms of Compound 5, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.
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Citations
15 Claims
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1. A method of inhibiting growth factor signaling comprising administering to a subject in need thereof a therapeutically effective amount of a crystalline form of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one comprising:
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(i) crystalline Form II having an X-ray powder diffraction (XRPD) pattern with peaks at about 8.44, 10.57, 14.92, 17.22, 21.26 and 22.42±
0.2 degrees two theta, or 10.47, 8.36, 5.93, 5.15, 4.18 and 3.96±
0.2 Å
in d-spacing;
or(ii) crystalline Form III having an XRPD pattern with peaks at about 9.60, 10.45, 19.30, 19.71, 21.84, and 23.42±
0.2 degrees two theta or 9.21, 8.46, 4.60, 4.50, 4.07 and 3.80±
0.2 Å
in d-spacing. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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9. A method of inhibiting growth factor signaling comprising administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising:
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a plurality of coated particles, comprising; a core particle comprising a crystalline form of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one, wherein the crystalline form constitutes at least about 80 wt % of the core particle; and a coating comprising one or more surface-altering agents surrounding the core particle; wherein the crystalline form is; (i) crystalline Form II having an X-ray powder diffraction (XRPD) pattern with peaks at about 8.44, 10.57, 14.92, 17.22, 21.26 and 22.42±
0.2 degrees two theta, or 10.47, 8.36, 5.93, 5.15, 4.18 and 3.96±
0.2 Å
in d-spacing;
or(ii) crystalline Form III having an XRPD pattern with peaks at about 9.60, 10.45, 19.30, 19.71, 21.84, and 23.42±
0.2 degrees two theta or 9.21, 8.46, 4.60, 4.50, 4.07 and 3.80±
0.2 Å
in d-spacing. - View Dependent Claims (10, 11, 12, 13, 14, 15)
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Specification