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US 12,433,868 B2Granted
Polymorphic forms of ST-246 and methods of preparation
AssigneeSiga Technologies, Inc.
InventorsShanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
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Abstract
Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindo1-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
Claims8
A unit dosage form comprising a pharmaceutical composition formulated for oral administration, wherein:
- (a) said pharmaceutical composition comprises a polymorph Form I of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop [f] isoindol-2 (1H)-benzamide which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of about
- 7.63, 10.04, 11.47, 14.73, 15.21, 15.47, 16.06, 16.67, 16.98, 18.93, 19.96, 20.52, 20.79, 22.80, 25.16, 26.53, 27.20, 27.60, 29.60, 30.23, 30.49, 30.68, 31.14, 33.65, 34.33, 35.29, 35.56, 36.30, 37.36, 38.42, 38.66
- degrees and further comprises one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers, excipients, diluents, additives, fillers, lubricants and binders;
- and
- (b) said polymorph Form I has a D90% particle size diameter of up to about 300 microns.
2 more elements
A unit dosage form for oral administration comprising:
- (a) about 200 mg of ST-246, wherein ST-246 is polymorph Form I of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop [f] isoindol-2 (1H)-yl)-benzamide which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of about
- 7.63, 10.04, 11.47, 14.73, 15.21, 15.47, 16.06, 16.67, 16.98, 18.93, 19.96, 20.52, 20.79, 22.80, 25.16, 26.53, 27.20, 27.60, 29.60, 30.23, 30.49, 30.68, 31.14, 33.65, 34.33, 35.29, 35.56, 36.30, 37.36, 38.42, 38.66 degrees;
- (b) about 33.15 mg of lactose monohydrate;
- (c) about 42.90 mg of croscarmellose sodium;
- (d) about 1.95 mg of colloidal silicon dioxide;
- (e) about 13.65 mg of hydroxypropoyl methylcellulose;
- (f) about 7.8 mg of sodium lauryl sulfate;
- (g) about 1.95 mg of magnesium stearate;
- and
- (h) a quantity of microcrystalline cellulose up to about 88.60 mg such that the total weight of the dosage form is about 390 mg.
7 more elements
Dependencies are inferred from the claim text.