US 12,240,825 B2
Oxexin 1 receptor antagonists
Giles Albert Brown, Cambridge (GB); Miles Stuart Congreve, Cambridge (GB); John Andrew Christopher, Cambridge (GB); Nigel Alan Swain, Cambridge (GB); Sarah Joanne Bucknell, Cambridge (GB); Anne Mary Stephenson, Cambridge (GB); Benjamin Gerald Tehan, Cambridge (GB); Geraint Jones, Nottingham (GB); Mark Mills, Nottingham (GB); Anil Patel, Nottingham (GB); and Andrew William Phillips, Nottingham (GB)
Assigned to NXERA PHARMA UK LIMITED, Cambridge (GB)
Appl. No. 17/426,301
Filed by Heptares Therapeutics Limited, Cambridge (GB)
PCT Filed Jan. 28, 2020, PCT No. PCT/GB2020/050182
§ 371(c)(1), (2) Date Jul. 28, 2021,
PCT Pub. No. WO2020/157474, PCT Pub. Date Aug. 6, 2020.
Claims priority of application No. 1901142 (GB), filed on Jan. 28, 2019.
Prior Publication US 2022/0098165 A1, Mar. 31, 2022
Int. Cl. C07D 401/04 (2006.01); C07D 401/14 (2006.01)
CPC C07D 401/04 (2013.01) [C07D 401/14 (2013.01)] 20 Claims
 
1. A compound of formula (1):

OG Complex Work Unit Chemistry
or a salt thereof, wherein
V is N, CH or CF;
W is N, CH or CF;
X is N, CH or CF;
Y is CH2;
Z is N, CH or CF;
R1 is selected from the group consisting of H, C(O)R6, and C1-6 alkyl, wherein the C1-6 alkyl is optionally substituted with one or more halogens or hydroxy groups;
R2 is a 5 or 6-membered heteroaryl ring containing two or three nitrogen atoms, and is optionally substituted with one or more fluorine atoms;
R3 is H or C1-3 alkyl;
R4 is H or a halogen;
R5 is H or a halogen;
R6 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy and C3-6 cycloalkyl, each of which is optionally substituted with —OMe or one or more fluorine atoms.