Claims for Patent: 10,959,994

Summary for Patent: 10,959,994

Title:	Solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
Abstract:	The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.
Inventor(s):	Luke George P., Sheth Pratik
Assignee:	FORMA Therapeutics, Inc.
Application Number:	US16693642
Patent Claims:	1. An oral unit dosage form comprising:an active pharmaceutical ingredient (API) consisting essentially of a Type A solid form of (S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile, wherein the solid form is characterized by a differential scanning calorimetry (DSC) thermogram with an endothermic event at about 256.6° C., andone or more excipients selected from the group consisting of a filler, a disintegrant, a lubricant, and a glidant.2. The oral unit dosage form of claim 1 , wherein the oral unit dosage form comprises one or more of: (a) about 5 wt % croscarmellose sodium claim 1 , (b) about 60 wt % microcrystalline cellulose claim 1 , and (c) about 1 wt % magnesium stearate.3. An oral unit dosage form comprising:(a) a Type A solid form of (S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile; and(b) one or more components selected from the group consisting of microcrystalline cellulose, croscarmellose sodium, and magnesium stearate.5. The oral unit dosage form of claim 4 , wherein the excipients comprise a filler claim 4 , a disintegrant claim 4 , and a lubricant; and wherein the solid form of Compound 1 is characterized by an X-ray Powder Diffraction (XRPD) having diffractions at angles (2 theta±0.2) of 6.3 claim 4 , 12.8 claim 4 , 13.8 claim 4 , 23.6 claim 4 , and 27.8 claim 4 , corresponding to d-spacing (angstroms±0.2) of 14.0 claim 4 , 6.9 claim 4 , 6.4 claim 4 , 3.8 claim 4 , and 3.2 claim 4 , respectively.6. The oral unit dosage form of claim 5 , wherein the solid form of Compound 1 is characterized by an X-ray Powder Diffraction (XRPD) having diffractions at angles (2 theta±0.2) of 5.7 claim 5 , 6.3 claim 5 , 8.5 claim 5 , 10.6 claim 5 , 12.8 claim 5 , 13.8 claim 5 , 17.3 claim 5 , 22.0 claim 5 , 22.8 claim 5 , 23.6 claim 5 , and 27.8.7. The oral unit dosage form of claim 4 , wherein the solid form of Compound 1 is characterized by an X-ray Powder Diffraction (XRPD) having further diffractions at angles (2 theta±0.2) of 5.7 claim 4 , 8.5 claim 4 , 10.6 claim 4 , 17.3 claim 4 , 22.0 claim 4 , and 22.8 corresponding to d-spacing (angstroms±0.2) of 15.4 claim 4 , 10.4 claim 4 , 8.4 claim 4 , 5.1 claim 4 , 4.0 claim 4 , and 3.9 claim 4 , respectively.9. The oral unit dosage form of claim 4 , wherein the solid form of Compound 1 is characterized by a differential scanning calorimetry (DSC) thermogram with an endothermic event at about 256.6° C.10. The oral unit dosage form of claim 4 , wherein the solid form of Compound 1 is characterized by a dynamic vapor sorption (DVS) showing maximum water uptake of 0.25% w/w at 25° C./90% RH.11. The oral unit dosage form of claim 4 , wherein the oral unit dosage form is a capsule comprising a total of 50 mg of Compound 1.12. The oral unit dosage form of claim 4 , wherein the oral unit dosage form is a capsule comprising a total of 150 mg of Compound 1.13. The oral unit dosage form of claim 4 , wherein the one or more excipients comprise microcrystalline cellulose claim 4 , croscarmellose sodium claim 4 , and magnesium stearate in a weight ratio of about 61:5:1.14. The oral unit dosage form of claim 4 , wherein the oral unit dosage form is a capsule comprising Compound 1 and the excipients in a weight ratio of about 33:67.16. The oral unit dosage form of claim 1 , wherein the one or more excipients comprise one or more of: (a) microcrystalline cellulose; (b) croscarmellose sodium; and (c) magnesium stearate.17. The oral unit dosage form of claim 16 , wherein the composition comprises the olutasidenib and the filler in a weight ratio of about 1:2.18. The oral unit dosage form of claim 17 , wherein the composition comprises the olutasidenib and the filler in a weight ratio of about 33:61.19. The oral unit dosage form of claim 1 , comprising about 30-35% by weight of olutasidenib.21. The unit dosage form of claim 20 , wherein the unit dosage form comprises 50-150 mg olutasidenib.22. The unit dosage form of claim 21 , wherein the unit dosage form comprises 50 mg olutasidenib.23. The unit dosage form of claim 22 , wherein the unit dosage form is a tablet.24. The unit dosage form of claim 22 , wherein the unit dosage form is a capsule.25. The unit dosage form of claim 21 , wherein the unit dosage form comprises 150 mg olutasidenib.26. The unit dosage form of claim 25 , wherein the unit dosage form is a tablet.27. The unit dosage form of claim 25 , wherein the unit dosage form is a capsule.28. The unit dosage form of claim 20 , wherein the one or more excipients are selected from the group consisting of a filler claim 20 , a disintegrant claim 20 , a lubricant claim 20 , and a glidant.29. The unit dosage form of claim 20 , wherein the one or more excipients are selected from the group consisting of (a) microcrystalline cellulose; (b) croscarmellose sodium; and (c) magnesium stearate.30. The unit dosage form of claim 20 , comprising micronized olutasidenib.31. The unit dosage form of claim 30 , wherein the unit dosage form is a tablet comprising 150 mg olutasidenib.32. The unit dosage form of claim 31 , wherein about 33% w/w of the tablet is olutasidenib.