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Last Updated: December 23, 2024

Claims for Patent: 11,254,652

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Summary for Patent: 11,254,652

Title:	Crystalline forms of N-(4-(4-(cyclopropymethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfon- amide
Abstract:	Provided herein are amorphous and crystalline hemisulfate salt forms of the formula (I). Also provided are pharmaceutical compositions comprising the amorphous and crystalline hemisulfate salt forms, methods for their manufacture, and uses thereof for treating conditions associated with pyruvate kinase such as e.g., pyruvate kinase deficiency. ##STR00001##
Inventor(s):	Sizemore; Jacob P. (Cambridge, MA), Guo; Liting (Suzhou, CN), Mirmehrabi; Mahmoud (Halifax, CA), Su; Yeqing (Halifax, CA)
Assignee:	Agios Pharmaceuticals, Inc. (Cambridge, MA)
Application Number:	16/765,456
Patent Claims:	1. A crystalline form of a compound having the formula: ##STR00031## wherein the crystalline form is crystalline Form A characterized by x-ray powder diffraction peaks at 2.THETA. angles (.+-.0.2.degree.) 9.9.degree., 15.8.degree., and 22.6.degree.. 2. The crystalline form of claim 1, wherein the compound is a solvate. 3. The crystalline Form A of claim 1, wherein the crystalline form is characterized by x-ray powder diffraction peaks at 2.THETA. angles (.+-.0.2.degree.) 9.9.degree., 15.8.degree., and 22.6.degree.; and at least one, at least two, or at least three additional x-ray powder diffraction peak at 2.THETA. angles (.+-.0.2.degree.) selected from 15.0.degree., 17.1.degree., 21.3.degree., and 21.9.degree.. 4. The crystalline Form A of claim 3, wherein the crystalline form is characterized by x-ray powder diffraction peaks at 2.THETA. angles (.+-.0.2.degree.) 9.9.degree., 11.4.degree., 15.0.degree., 15.3.degree., 15.8.degree., 17.1.degree., 17.7.degree., 21.3.degree., 21.9.degree., 22.6.degree., and 23.5.degree.. 5. The crystalline Form A of claim 4, wherein the crystalline form is characterized by x-ray powder diffraction peaks at 2.THETA. angles (.+-.0.2.degree.) 4.9.degree., 9.9.degree., 11.0.degree., 11.4.degree., 11.7.degree., 12.3.degree., 12.8.degree., 13.6.degree., 13.9.degree., 14.2.degree., 15.0.degree., 15.3.degree., 15.8.degree., 17.1.degree., 17.4.degree., 17.7.degree., 18.8.degree., 19.1.degree., 19.8.degree., 21.3.degree., 21.9.degree., 22.6.degree., 23.0.degree., 23.2.degree., 23.5.degree., 23.8.degree., 24.1.degree., 24.5.degree., 25.3.degree., 25.6.degree., 26.1.degree., 27.1.degree., 28.1.degree., and 29.8.degree.. 6. A pharmaceutical composition comprising the crystalline form of claim 1; and a pharmaceutically acceptable carrier. 7. A tablet composition comprising the crystalline form of claim 1; and a pharmaceutically acceptable carrier. 8. A method of forming crystalline Form A of claim 1, the method comprising reacting a compound of Formula 1: ##STR00032## with H.sub.2SO.sub.4 in an alcoholic solution.

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