US 12,213,971 B2
Histone deacetylase inhibitors for immunomodulation in tumor microenvironment
Jia-Shiong Chen, Taipei (TW); Mu-Hsuan Yang, Taipei (TW); Yi-Hong Wu, Taipei (TW); Sz-Hao Chu, Taipei (TW); Cheng-Han Chou, Taipei (TW); Ye-Su Chao, Taipei (TW); and Chia-Nan Chen, Taipei (TW)
Assigned to GREAT NOVEL THERAPEUTICS BIOTECH & MEDICALS CORPORATION, Taipei (TW)
Filed by GREAT NOVEL THERAPEUTICS BIOTECH & MEDICALS CORPORATION, Taipei (TW)
Filed on May 1, 2023, as Appl. No. 18/310,387.
Application 18/310,387 is a division of application No. 17/243,378, filed on Apr. 28, 2021, granted, now 11,672,788.
Claims priority of provisional application 63/018,427, filed on Apr. 30, 2020.
Prior Publication US 2023/0263790 A1, Aug. 24, 2023
Int. Cl. A61K 31/444 (2006.01); A61K 31/44 (2006.01); A61K 31/4406 (2006.01); A61P 35/00 (2006.01); C07D 213/56 (2006.01); C07D 401/12 (2006.01)
CPC A61K 31/444 (2013.01) [A61K 31/44 (2013.01); A61K 31/4406 (2013.01); A61P 35/00 (2018.01); C07D 213/56 (2013.01); C07D 401/12 (2013.01)] 21 Claims
 
1. A method for epigenetic immunomodulation of tumor microenvironment (TME) and/or treatment of cancer in a subject in need thereof, the method comprising administrating an effective amount of a compound of formula (I) to the subject:

OG Complex Work Unit Chemistry
wherein W and Y are each independently selected from CH and N;
R1 is each independently selected from hydrogen, halogen, C1-C3 alkyl and halogenated C1-C3 alkyl, and can be mono-, di-, tri- or tetra-substitution;
C1 and C2 are C atoms linked by a double bond;
Ar is selected from the group consisting of the following:

OG Complex Work Unit Chemistry
wherein Ar is linked to C2 via the solid line;
R2 has the same meaning as described for R1; and
R3 is hydrogen or C1-C3 alkyl;
or a pharmaceutically acceptable salt, hydrate, stereoisomer or solvate thereof.