US 11,655,245 B2
Oxadiazole transient receptor potential channel inhibitors
Jack Alexander Terrett, South San Francisco, CA (US); Huifen Chen, South San Francisco, 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, Montreal (CA); Matthew Volgraf, South San Francisco, CA (US); and Elisia Villemure, South San Francisco, CA (US)
Assigned to Genentech, Inc., South San Francisco, CA (US)
Filed by Genentech, Inc., South San Francisco, CA (US)
Filed on Jun. 16, 2020, as Appl. No. 16/903,020.
Application 16/903,020 is a division of application No. 16/355,352, filed on Mar. 15, 2019, granted, now 10,710,994.
Claims priority of provisional application 62/644,987, filed on Mar. 19, 2018.
Claims priority of provisional application 62/676,057, filed on May 24, 2018.
Claims priority of provisional application 62/725,488, filed on Aug. 31, 2018.
Claims priority of provisional application 62/812,806, filed on Mar. 1, 2019.
Prior Publication US 2020/0308161 A1, Oct. 1, 2020
Int. Cl. A61K 31/427 (2006.01); A61P 11/00 (2006.01); A61P 23/00 (2006.01); A61P 25/00 (2006.01); A61P 29/00 (2006.01); C07D 513/04 (2006.01); C07D 473/30 (2006.01); C07D 487/04 (2006.01); C07D 498/04 (2006.01); C07D 471/04 (2006.01); C07D 413/14 (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)] 48 Claims
 
1. A method for treating a disease or condition in a mammal in need thereof, the disease or condition selected from pain, migraine, asthma, chronic obstructive pulmonary disease, cough, and itch, the method comprising administering to the mammal a therapeutically effective amount of a compound of formula (I):

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: a bond; C1-4 alkylene; —O—; —S—; —SO2—; or —N(Ra)—;
n is: 0, 1, 2 or 3;
Ra is H or —C1-6 alkyl, which may be unsubstituted or substituted one or more times with halo;
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 C3-6cycloalkyl fused to a substituted or unsubstituted phenyl; substituted or unsubstituted heteroaryl; or substituted or unsubstituted naphthyl.