US 11,787,798 B2
Aryl piperidines as monoacylglycerol lipase modulators
Michael K. Ameriks, San Diego, CA (US); Cynthia B. Berry, Poway, CA (US); Krisztián Biró, Budapest (HU); Pablo Garcia-Reynaga, San Diego, CA (US); Andrew V. Samant, Cardiff, CA (US); and Warren S. Wade, San Diego, CA (US)
Assigned to Janssen Pharmaceutica NV, Beerse (BE)
Filed by Janssen Pharmaceutica NV, Beerse (BE)
Filed on Mar. 25, 2021, as Appl. No. 17/212,274.
Claims priority of provisional application 63/000,282, filed on Mar. 26, 2020.
Prior Publication US 2022/0363679 A1, Nov. 17, 2022
Int. Cl. C07D 401/06 (2006.01); C07D 413/06 (2006.01); C07D 413/14 (2006.01); C07D 471/04 (2006.01); C07D 417/14 (2006.01)
CPC C07D 471/04 (2013.01) [C07D 401/06 (2013.01); C07D 413/06 (2013.01); C07D 413/14 (2013.01); C07D 417/14 (2013.01)] 18 Claims
 
1. A compound of Formula (I):

OG Complex Work Unit Chemistry
wherein
X is CH2 or O;
R2a and R2b are each independently selected from H and C1-4alkyl;
R3 is selected from:
(a) phenyl; phenyl substituted with one, two or three members each independently selected from: halo, C1-6alkyl, C1-6haloalkyl, C(CH3)2OH, OC1-6alkyl, OC1-6haloalkyl, SCH3, SF5, Si(CH3)3, N(CH3)2, C3-6cycloalkyl, OC3-6cycloalkyl, phenyl, O-phenyl, O-pyridyl and C3-6cycloalkyl substituted with CH3; and
(b) pyridyl substituted with C1-6alkyl; naphthyl;

OG Complex Work Unit Chemistry
R4 is selected from: H, F, and C1-3alkyl; and
R5a and R5b are each independently selected from H and CH3;
or a pharmaceutically acceptable salt, isotope, N-oxide, solvate, or stereoisomer thereof.