US 12,227,509 B2
Dihydropyrazolopyrazinone derivative having MGAT2 inhibitory activity
Yusuke Tateno, Osaka (JP); Manabu Katou, Toyonaka (JP); and Toshihiro Wada, Osaka (JP)
Assigned to SHIONOGI & CO., LTD., Osaka (JP)
Appl. No. 17/422,108
Filed by Shionogi & Co., Ltd., Osaka (JP)
PCT Filed Jan. 10, 2020, PCT No. PCT/JP2020/000553
§ 371(c)(1), (2) Date Jul. 9, 2021,
PCT Pub. No. WO2020/145369, PCT Pub. Date Jul. 16, 2020.
Claims priority of application No. 2019-003073 (JP), filed on Jan. 11, 2019.
Prior Publication US 2022/0135577 A1, May 5, 2022
Int. Cl. C07D 487/10 (2006.01); A61P 3/04 (2006.01); C07D 491/20 (2006.01)
CPC C07D 487/10 (2013.01) [A61P 3/04 (2018.01); C07D 491/20 (2013.01)] 28 Claims
 
1. A compound represented by formula (I):

OG Complex Work Unit Chemistry
wherein
R1 is hydrogen;
R2a and R2b are taken together with an adjacent carbon atom to form ring B;
ring B is represented by formula:

OG Complex Work Unit Chemistry
wherein R6s are each independently halogen, or substituted or unsubstituted alkyloxy, and
n is 1 or 2;
R3a is hydrogen;
R3b is hydrogen;
R4a is a group represented by formula:

OG Complex Work Unit Chemistry
wherein
L3 is a single bond or substituted or unsubstituted alkylene,
R7 is halogen, substituted or unsubstituted sulfamoyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted non-aromatic heterocyclyl, or a group represented by formula: —S(═O)(═N—RN)—RS1,
RN is hydrogen, and
RS1 is substituted or unsubstituted alkyl; and
R4b is substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl, or its pharmaceutically acceptable salt.