CPC A61K 31/506 (2013.01) [A61J 1/035 (2013.01); A61K 31/404 (2013.01); A61K 31/415 (2013.01); A61K 31/44 (2013.01); A61K 31/4418 (2013.01); A61K 31/4439 (2013.01); A61K 31/444 (2013.01); A61K 31/4525 (2013.01); A61K 31/4545 (2013.01); A61K 31/4709 (2013.01); A61K 31/496 (2013.01); A61K 31/497 (2013.01); C07D 209/18 (2013.01); C07D 209/42 (2013.01); C07D 209/49 (2013.01); C07D 213/64 (2013.01); C07D 213/73 (2013.01); C07D 213/82 (2013.01); C07D 213/84 (2013.01); C07D 231/12 (2013.01); C07D 231/14 (2013.01); C07D 231/20 (2013.01); C07D 235/24 (2013.01); C07D 239/34 (2013.01); C07D 401/04 (2013.01); C07D 401/12 (2013.01); C07D 401/14 (2013.01); C07D 403/10 (2013.01); C07D 403/12 (2013.01); C07D 405/14 (2013.01); C07D 407/12 (2013.01); C07D 413/14 (2013.01); C07D 417/12 (2013.01)] | 46 Claims |
1. A compound of formula Ia:
![]() a deuterated derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein, independently for each occurrence:
Ring B is a C6-C10 aryl ring or C3-C10 heteroaryl or heterocyclic ring wherein anywhere from 1 to 4 ring atoms are independently O, S, N, or NR;
Ring C is a C6-C10 aryl ring, C3-C14 heteroaryl or heterocyclic ring wherein anywhere from 1 to 4 ring atoms are independently N, O, or S, or a C3-C10 cycloalkyl ring;
X is O or NR;
Y is CRR, CO, O, S, SO, SO2, S(O)NH or NR;
R1 is halo; CN; F5S; SiR3; OH; NRR; C1-C6 alkyl; C1-C6 fluoroalkyl; C1-C6 alkoxy; C1-C6 fluoroalkoxy; C2-C6 alkenyl; C2-C6 alkynyl; (C1-C9 alkylene)-R4 wherein up to four CH2 units are independently replaced with O, CO, S, SO, SO2 or NR; C6-C10 aryl; C3-C10 heteroaryl or heterocyclic ring wherein anywhere from 1 to 4 ring atoms are independently O, S, N, or NR; or C3-C10 cycloalkyl;
R2 is halo; OH; NRR; azide; CN; CO2R; C1-C6 alkyl; C1-C6 fluoroalkyl; C1-C6 alkoxy; C1-C6 fluoroalkoxy; C2-C6 alkenyl; C2-C6 alkynyl; C6-C10 aryl; C3-C13 heteroaryl or heterocyclic ring wherein anywhere from 1 to 4 ring atoms are independently O, S, N, or NR; C3-C10 cycloalkyl; or a (C1-C9 alkylene)-R4 wherein up to four CH2 units are independently replaced with O, CO, S, SO, SO2 or NR;
or two R2 may form a ═CH2 or ═O group;
R3 is halo; CN; CO2R; C1-C6 alkyl; C1-C6 fluoroalkyl; C2-C6 alkenyl; C2-C6 alkynyl; C1-C6 alkoxy; C1-C6 fluoroalkoxy; or C6-C10 aryl; C3-C10 heteroaryl or heterocyclic ring wherein anywhere from 1 to 4 ring atoms are independently O, S, N, or NR; C3-C10 cycloalkyl; or a (C1-C9 alkylene)-R4 wherein up to four CH2 units are independently replaced with O, CO, S, SO, SO2 or NR;
or two R3 may form a ═CH2 or ═O group;
R4 is H; azide; CF3; CHF2; OR; CCH; CO2R; OH; C6-C10 aryl, C3-C10 heteroaryl or heterocycloalkyl wherein anywhere from 1 to 4 ring atoms are independently O, S, N, or NR; C3-C10 cycloalkyl; NRR, NRCOR, CONRR, CN, halo, or SO2R;
R is independently H; OH; CO2H; CO2; C1-C6 alkyl; C1-C6 alkyl; C2-C6 alkenyl; C2-C6 alkynyl; C6-C10 aryl; C3-C10 heteroaryl or heterocycloalkyl wherein anywhere from 1 to 4 ring atoms are independently O, S, N, or NR; or C3-C10 cycloalkyl;
n is 0, 1, 2 or 3;
o is 0, 1, 2, 3, 4, or 5;
p is 0, 1, 2, or 3; and
q is 0, 1, 2, 3, 4, or 5.
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