US 11,872,224 B2
Amorphous solid dispersion formulation
Chi-Feng Yen, Taipei (TW); and Fang-Wei Tien, Taipei (TW)
Assigned to TaiGen Biotechnology Co., Ltd., Taipei (TW); and TaiGen Biopharmaceuticals Co. (Beijing), Ltd., Beijing (CN)
Filed by TaiGen Biotechnology Co., Ltd., Taipei (TW); and TaiGen Biopharmaceuticals Co. (Beijing), Ltd., Beijing (CN)
Filed on Dec. 29, 2021, as Appl. No. 17/564,418.
Claims priority of provisional application 63/131,886, filed on Dec. 30, 2020.
Prior Publication US 2022/0202817 A1, Jun. 30, 2022
Int. Cl. A61K 31/495 (2006.01); A61K 31/5025 (2006.01); A61K 47/10 (2017.01); A61K 47/32 (2006.01); A61K 47/38 (2006.01)
CPC A61K 31/5025 (2013.01) [A61K 47/10 (2013.01); A61K 47/32 (2013.01); A61K 47/38 (2013.01)] 16 Claims
 
1. An amorphous solid dispersion comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable polymer;

OG Complex Work Unit Chemistry
wherein
G is hydrogen or —C(R2R2′) —O—C═O)—R3, in which each of R2 and R2′independently is hydrogen or C1-4 alkyl; R3 is C1-4 alkyl;
R1 is halogen, deuterium, or C1-4 alkyl;
m is an integer of 1 to 9; and
the star (*) indicates a chiral center:,
wherein the pharmaceutically acceptable polymer is polyvinylpyrrolidone/vinyl acetate copolymer, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, methacrylic acid and methyl methacrylate copolymer, hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose acetate succinate (HPMCAS), hydroxypropyl methyl cellulose phthalate (HPMCP), Polyethylene glycol (PEG), or Kollidon SR; and
wherein the weight ratio of the compound of Formula (I) or a pharmaceutically acceptable salt thereof to the pharmaceutically acceptable polymer is in a range between about 1:1 to about 1:5.