| 主权项 |
1. A compound of Formula I:or a pharmaceutically acceptable salt thereof, wherein:
Ar is H X is CH or N; Y is CH or N; R1 is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; wherein said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are each optionally substituted by 1, 2, 3, or 4 groups independently selected from halo, OH, CN, NR1aR2b, C1-6 alkoxy, and C1-6 haloalkoxy; each R1a and R2b is independently selected from H and C1-6 alkyl; or any R1a and R2b together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group, which is optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl; R2 is selected from halo, CN, C1-6 alkyl, C1-6 haloalkyl, -L-(C1-6 alkyl), -L-(C1-6 haloalkyl), and -L-(C1-4 alkylene)n-Cy2 and —(C1-4 alkylene)n-Cy2; wherein said C1-6 alkyl in said C1-6 alkyl and -L-(C1-6 alkyl) is optionally substituted by 1, 2, 3, or 4 independently selected R2a groups; L is O, NRB, S, S(O), S(O)2, C(O), C(O)NRB, S(O)NRB, S(O)2NRB, NRBC(O), NRBS(O), and NRBS(O)2; RA and RB are each independently selected from H and C1-6 alkyl; Cy2 is selected from C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, and 5-6 membered heteroaryl; each of which is substituted with p independently selected R2a groups; wherein p is 0, 1, 2, 3, or 4; each R2a is independently selected from OH, NO2, CN, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di(C1-6 alkyl)carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di(C1-6 alkyl)aminosulfonyl, amino sulfonylamino, C1-6 alkylaminosulfonylamino, di(C1-6 alkyl)aminosulfonylamino, amino carbonylamino, C1-6 alkylaminocarbonylamino, and di(C1-6 alkyl)aminocarbonylamino; R3 is halo, CN, NO2, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —(C1-4 alkylene)r-Cy3, ORn, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORb, NRfC(O)Rb, NRfC(O)ORb, NRcC(O)NRcRd, C(═NRe)Rb, C(═NRe)NRcRd, NRcC(═NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRfS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, or S(O)2NRcRd; wherein said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are each optionally substituted by 1, 2, 3, or 4 independently selected R3a groups; Cy3 is selected from C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, and 5-6 membered heteroaryl; each of which is optionally substituted with 1, 2, 3, or 4 independently selected R3a groups; provided that one of the following is true: (1) R3 is —(C1-4 alkylene)r-Cy3; or (2) R2 is selected from -L-(C1-4 alkylene)n-Cy2 and —(C1-4 alkylene)n-Cy2; or (3) R3 is —(C1-4 alkylene)r-Cy3; and R2 is selected from -L-(C1-4 alkylene)n-Cy2 and —(C1-4 alkylene)n-Cy2; each R3a is independently selected from halo, CN, NO2, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, (4-7 membered heterocycloalkyl)-C1-4 alkyl, phenyl-C1-4 alkyl, (5-6 membered heteroaryl)-C1-4 alkyl, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORb, NRcC(O)NRcRd, C(═NRe)Rb, C(═NRe)NRcRd, NRcC(═NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, and S(O)2NRcRd; wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, (4-7 membered heterocycloalkyl)-C1-4 alkyl, phenyl-C1-4 alkyl, and (5-6 membered heteroaryl)-C1-4 alkyl are each optionally substituted by 1, 2, 3, or 4 groups independently selected from OH, NO2, CN, halo, C1-6 alkyl, cyano-C1-6 alkyl, HO—C1-6 alkyl, C1-4 alkoxy-C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di(C1-6 alkyl)carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di(C1-6 alkyl)aminosulfonyl, amino sulfonylamino, C1-6 alkylaminosulfonylamino, di(C1-6 alkyl)aminosulfonylamino, amino carbonylamino, C1-6 alkylaminocarbonylamino, and di(C1-6 alkyl)aminocarbonylamino; R4 is selected from H, OH, NO2, CN, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, cyano-C1-6 alkyl, HO—C1-6 alkyl, C1-4 alkoxy-C1-6 alkyl, C3-7 cycloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di(C1-6 alkyl)carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di(C1-6 alkyl)aminosulfonyl, amino sulfonylamino, C1-6 alkylaminosulfonylamino, di(C1-6 alkyl)aminosulfonylamino, aminocarbonylamino, C1-6 alkylaminocarbonylamino, and di(C1-6 alkyl)aminocarbonylamino; R5 is selected from halo, OH, CN, C1-4 alkyl, C1-4 alkoxy, and C1-4 haloalkoxy; each Ra, Rc, and Rd is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, (4-7 membered heterocycloalkyl)-C1-4 alkyl, phenyl-C1-4 alkyl, and (5-6 membered heteroaryl)-C1-4 alkyl; wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, (4-7 membered heterocycloalkyl)-C1-4 alkyl, phenyl-C1-4 alkyl, and (5-6 membered heteroaryl)-C1-4 alkyl are each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from OH, NO2, CN, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, cyano-C1-6 alkyl, HO—C1-6 alkyl, C1-4 alkoxy-C1-6 alkyl, C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di(C1-6 alkyl)carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di(C1-6 alkyl)aminosulfonyl, aminosulfonylamino, C1-6 alkylaminosulfonylamino, di(C1-6 alkyl)aminosulfonylamino, aminocarbonylamino, C1-6 alkylaminocarbonylamino, and di(C1-6 alkyl)aminocarbonylamino; each Rb is independently selected from C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, (4-7 membered heterocycloalkyl)-C1-4 alkyl, phenyl-C1-4 alkyl, and (5-6 membered heteroaryl)-C1-4 alkyl; each optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from OH, NO2, CN, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, cyano-C1-6 alkyl, HO—C1-6 alkyl, C1-4 alkoxy-C1-6 alkyl, C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di(C1-6 alkyl)carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di(C1-6 alkyl)aminosulfonyl, aminosulfonylamino, C1-6 alkylaminosulfonylamino, di(C1-6 alkyl)aminosulfonylamino, aminocarbonylamino, C1-6 alkylaminocarbonylamino, and di(C1-6 alkyl)amino carbonylamino; each Re is independently selected from H, C1-4 alkyl, CN, OH, C1-4 alkoxy, C1-4 alkylsulfonyl, carbamyl, C1-4 alkylcarbamyl, di(C1-4 alkyl)carbamyl, and C1-4 alkylcarbonyl; each Rf is independently selected from C1-4 alkylsulfonyl, C1-4 alkylcarbonyl and C1-4 alkoxycarbonyl; n is 0 or 1; and r is 0 or 1. |
