22-07-2021 дата публикации
Номер: US20210220321A1
Polymorphic forms of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) and a metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) are disclosed and characterized. Compositions and method for treatment of Alzheimer's disease that includes the polymorphic forms and metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73). 1. A method of making a crystal form of ANAVEX2-73 , comprising crystallizing the ANAVEX2-73 in a supercritical fluid (SCF) environment.2. The method of claim 1 , wherein the supercritical fluid comprises supercritical carbon dioxide.3. The method of claim 1 , wherein the crystallizing comprises:a. making a solution of ANAVEX2-73 in a solvent;b. introducing the solution to the SCF;c. allowing crystallization of ANAVEX2-73 in the SCF environment to form crystals;d. isolating the crystals, thus obtaining the crystal form of ANAVEX2-73.4. The method of claim 3 , wherein the solvent comprises ethanol claim 3 , acetonitrile claim 3 , isopropyl alcohol claim 3 , trifluoroethanol claim 3 , acetone claim 3 , 3-methyl-I-butanol claim 3 , 2-ethoxyethanol claim 3 , 1-propanol claim 3 , dichloromethane claim 3 , dimethyl sulfoxide claim 3 , N claim 3 ,N′-dimethylacetamide claim 3 , dimethylformamide claim 3 , trifluoroethanol claim 3 , 1:9 v/v trifluoroethanol+ethanol claim 3 , 1:1 v/v acetone+ethanol claim 3 , 3-methyl-1-butanol claim 3 , N-methyl-2-pyrrolidone claim 3 , tert-butanol claim 3 , or a combination thereof.5. The method of claim 3 , wherein the SCF environment comprises pressure from about 85 bar to about 200 bar claim 3 , temperature ranging from about 40° C. to about 80° C. claim 3 , and TS flow ranging from about 0.1 g/min to about 1.7 g/min.6. A crystal form produced according to the method of claim 1 , substantially characterized by an X-ray diffraction pattern of claim 1 , claim 1 , or .7. The crystal form of claim 6 , further ...
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