US 11,952,346 B2
Modulators of mas-related G-protein receptor X2 and related products and methods
Marion Lanier, San Diego, CA (US); Marcus Boehm, San Diego, CA (US); Liming Huang, San Diego, CA (US); Esther Martinborough, San Diego, CA (US); Marcos Sainz, San Diego, CA (US); Brandon Selfridge, San Diego, CA (US); and Adam Yeager, San Diego, CA (US)
Assigned to Escient Pharmaceuticals, Inc., San Diego, CA (US)
Filed by Escient Pharmaceuticals, Inc., San Diego, CA (US)
Filed on Dec. 8, 2021, as Appl. No. 17/545,494.
Claims priority of provisional application 63/123,411, filed on Dec. 9, 2020.
Prior Publication US 2022/0340530 A1, Oct. 27, 2022
Int. Cl. C07D 209/08 (2006.01); C07C 255/60 (2006.01); C07D 213/73 (2006.01); C07D 231/14 (2006.01); C07D 239/48 (2006.01); C07D 239/94 (2006.01); C07D 277/56 (2006.01); C07D 277/62 (2006.01); C07D 401/12 (2006.01); C07D 403/04 (2006.01); C07D 405/04 (2006.01); C07D 471/04 (2006.01)
CPC C07D 213/73 (2013.01) [C07C 255/60 (2013.01); C07D 209/08 (2013.01); C07D 231/14 (2013.01); C07D 239/48 (2013.01); C07D 239/94 (2013.01); C07D 277/56 (2013.01); C07D 277/62 (2013.01); C07D 401/12 (2013.01); C07D 403/04 (2013.01); C07D 405/04 (2013.01); C07D 471/04 (2013.01)] 11 Claims
 
1. A compound having structure (Ib):

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt, stereoisomer, hydrate, solvate or isotope thereof, wherein:
R1 is aryl or heteroaryl, wherein R1 is optionally substituted with one or more Rq1;
each Rq1 is independently H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, cycloalkyl, heteroaryl, heterocyclyl, —OR, —O(CH2)nR, haloalkoxy, —C(O)OR, —C(O)R, —OC(O)R, halo, haloalkyl, —CN, —N(R)2, —N(R)C(═NH)N(R)2, —N(R)C(O)R, —N(R)S(O)2R, S(O)2R, —C(H)Q′R, or —(CH2)nQ′ where Q′ is selected from C1-6 alkyl, aryl, cycloalkyl, heterocyclyl, OR′, —C(O)OR′, —OC(O)R′, haloalkyl, —CN, —N(R′)2, —N(R′)C(O)R′, and —N(R′)S(O)2R′;
each R is independently H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, —C(O)NHR′, amino, —(CH2)nR′, halo, aryl, cycloalkyl, heteroaryl or heterocyclyl, or two R groups taken together with the atom to which they are attached form a carbocyle or heterocycle;
each R′ is independently H, C1-6 alkyl, haloalkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, cycloalkyl, heteroaryl, or heterocyclyl;
Rd is —CN;
Rw is H;
Rz is H;
R2 is H; and
each R3 is H.