US 12,202,824 B2
Oxadiazole transient receptor potential channel inhibitors
Jack Alexander Terrett, San Francisco, CA (US); Huifen Chen, Burlingame, CA (US); Lea Constantineau-Forget, Montreal (CA); Robin Larouche-Gauthier, Montreal (CA); Luce Lépissier, Montreal (CA); Francis Beaumier, Montreal (CA); Martin Déry, Montreal (CA); Chantal Grand-Maître, Montreal (CA); Claudio Sturino, L'ile-Bizard (CA); Matthew Volgraf, Oakland, CA (US); and Elisia Villemure, Oakland, CA (US)
Assigned to Genentech, Inc., South San Francisco, CA (US)
Filed by Genentech, Inc., South San Francisco, CA (US)
Filed on Aug. 2, 2022, as Appl. No. 17/816,855.
Application 16/903,020 is a division of application No. 16/355,352, filed on Mar. 15, 2019, granted, now 10,710,994, issued on Jul. 14, 2020.
Application 17/816,855 is a continuation of application No. 16/903,020, filed on Jun. 16, 2020, granted, now 11,655,245.
Claims priority of provisional application 62/812,806, filed on Mar. 1, 2019.
Claims priority of provisional application 62/725,488, filed on Aug. 31, 2018.
Claims priority of provisional application 62/676,057, filed on May 24, 2018.
Claims priority of provisional application 62/644,987, filed on Mar. 19, 2018.
Prior Publication US 2023/0121700 A1, Apr. 20, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 413/14 (2006.01); A61K 31/427 (2006.01); A61K 31/437 (2006.01); A61K 31/4375 (2006.01); A61K 31/4985 (2006.01); A61K 31/5025 (2006.01); A61K 31/519 (2006.01); A61K 31/522 (2006.01); A61K 31/53 (2006.01); A61P 11/00 (2006.01); A61P 19/02 (2006.01); A61P 23/00 (2006.01); A61P 25/00 (2006.01); A61P 29/00 (2006.01); C07D 471/04 (2006.01); C07D 473/08 (2006.01); C07D 473/30 (2006.01); C07D 487/04 (2006.01); C07D 498/04 (2006.01); C07D 513/04 (2006.01)
CPC C07D 413/14 (2013.01) [A61K 31/427 (2013.01); A61P 11/00 (2018.01); A61P 23/00 (2018.01); A61P 25/00 (2018.01); A61P 29/00 (2018.01); C07D 471/04 (2013.01); C07D 473/30 (2013.01); C07D 487/04 (2013.01); C07D 498/04 (2013.01); C07D 513/04 (2013.01)] 17 Claims
 
1. A compound of formula (II)

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
A is: substituted or unsubstituted 6-6 fused bicyclic heteroaryl which may be partially saturated; substituted or unsubstituted 5-6 fused bicyclic heteroaryl which may be partially saturated; or substituted and unsubstituted 6-5 fused bicyclic heteroaryl which may be partially saturated;
X is methylene;
R1 is: H; or C1-6alkyl; and
R4 is: substituted or unsubstituted phenyl; substituted or unsubstituted heteroaryl; or substituted or unsubstituted naphthyl;
or R1 and R4 may together form an unsubstituted or substituted C3-6cylcoalkyl fused to a substituted or unsubstituted phenyl; substituted or unsubstituted heteroaryl; or substituted or unsubstituted naphthyl.