Nova Patents
IL276876A

Digital asset custodial system

Abstract

This record has no abstract on file.

IL276876A, drawing sheet 1
Sheet 1 of 2

Term

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61 claims: 41 independent, 20 dependent

  1. 1
    20443-0537WO1 // INCY0243-WO1 What is claimed is:1. A compound of Formula (I): (I) or a pharmaceutically acceptable salt thereof;wherein: X is CR3;R1 is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl;R2 is selected from H, D, halo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C614 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa2, SRa2, NHORa2, C(O)Rb2, C(O)NRc2Rd2, C(O)NRc2(ORa2), C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, C(=NRe2)Rb2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2C(=NRe2)Rb2, NRc2S(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)(=NRe2)Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, S(O)2NRc2Rd2, OS(O)(=NRe2)Rb2, OS(O)2Rb2, SF5, P(O)Rf2Rg2, OP(O)(ORh2)(ORi2), P(O)(ORh2)(ORi2), and BRj2Rk2, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of R2 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RC substituents;R3 is selected from H, D, halo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C614 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa3, SRa3, NHORa3, C(O)Rb3, C(O)NRc3Rd3, C(O)NRc3(ORa3), C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3C(=NRe3)Rb3, NRc3S(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)(=NRe3)Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3, OS(O)(=NRe3)Rb3, OS(O)2Rb3, SF5, P(O)Rf3Rg3, 238 20443-0537WO1 // INCY0243-WO1 OP(O)(ORh3)(OR13), P(O)(ORh3)(ORi3), and BRj3Rk3, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of R3 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 Independently selected RD substituents;Cy1 is C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, or 4-14 membered heterocycloalkyl, wherein the C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, or 4-14 membered heterocycloalkyl is optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RE or RM substituents;Cy2 is C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, or 4-14 membered heterocycloalkyl, wherein the C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, or 4-14 membered heterocycloalkyl is optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RF substituents;each Ra2, Rc2, Rd2, Ra3, Rc3, and Rd3 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 414 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra2, Rc2, Rd2, Ra3, Rc3, and Rd3 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RG substituents;or any Rc2 and Rd2 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;or any Rc3 and Rd3 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;each Rb2 and Rb3 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 239 20443-0537WO1 // INCY0243-WO1 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb2 and Rb3are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RG substituents;each Re2 and Re3 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rf2, Rg2, Rf3, and Rg3 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rh2, Ri2, Rh3, and Ri3 is independently selected from H, C1-6 alkyl, C1 -6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj2, Rk2, Rj3, and Rk3 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or any Rj2 and Rk2 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;or any Rj3 and Rk3 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RC, RD, RE, RM, RF, and RG is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa4, SRa4, NHORa4, C(O)Rb4, C(O)NRc4Rd4, C(O)NRc4(ORa4), C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)ORa4, NRc4C(O)NRc4Rd4, C(=NRe4)Rb4, C(=NRe4)NRc4Rd4, NRc4C(=NRe4)NRc4Rd4, NRc4C(=NRe4)Rb4, NRc4S(O)Rb4, NRc4S(O)NRc4Rd4, NRc4S(O)2Rb4, NRc4S(O)(=NRe4)Rb4, NRc4S(O)2NRc4Rd4, S(O)Rb4, 240 20443-0537WO1 // INCY0243-WO1 S(O)NRc4Rd4, S(O)2Rb4, S(O)2NRc4Rd4, OS(O)(=NRe4)Rb4, OS(O)2Rb4, SF5, P(O)Rf4Rg4, OP(O)(ORh4)(OR4), P(O)(ORh4)(ORi4), and BRj4Rk4, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RC, RD, RE, RM, RF, and RG are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RH substituents;each Ra4, Rc4, and Rd4 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra4, Rc4, and Rd4 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RH substituents;or, any Rc4 and Rd4 attached to the same N atom, together with the N atom to which they are attached, optionally form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RH substituents;each Rb4is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb4 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RH substituents;each Re4 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;241 20443-0537WO1 // INCY0243-WO1 each Rf4 and Rg4 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh4 and Ri4 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj4 and Rk4 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj4 and Rk4 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RH is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa5, SRa5, NHORa5, C(O)Rb5, C(O)NRc5Rd5, C(O)NRc5(ORa5), C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, C(=NRe5)Rb5, C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5C(=NRe5)Rb5, NRc5S(O)Rb5, NRc5S(O)NRc5Rd5, NRc5S(O)2Rb5, NRc5S(O)(=NRe5)Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, S(O)2NRc5Rd5, OS(O)(=NRe5)Rb5, OS(O)2Rb5, SF5, P(O)Rf5Rg5, OP(O)(ORh5)(ORi5), P(O)(ORh5)(ORi5), and BRj5Rk5, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RH are each optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;each Ra5, Rc5, and Rd5 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered 242 20443-0537WO1 // INCY0243-WO1 heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra5, Rc5, and Rd5 are each optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;or any Rc5 and Rd5 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;each Rb5 is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 arylC1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C614 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb5 are each optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;each Re5 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rf5 and Rg5 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh5 and Ri5 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj5 and Rk5 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj5 and Rk5 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RI is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered 243 20443-0537WO1 // INCY0243-WO1 heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa6, SRa6, NHORa6, C(O)Rb6, C(O)NRc6Rd6, C(O)NRc6(ORa6), C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)ORa6, NRc6C(O)NRc5Rd6, C(=NRe6)Rb6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, NRc6C(=NRe6)Rb6, NRc6S(O)Rb6, NRc6S(O)NRc6Rd6, NRc6S(O)2Rb6, NRc6S(O)(=NRe6)Rb6, NRc6S(O)2NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, S(O)2NRc6Rd6, OS(O)(=NRe6)Rb6, OS(O)2Rb6, SF5, P(O)Rf6Rg6, OP(O)(ORh6)(ORi6), P(O)(ORh6)(ORi6), and BRj6Rk6, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RI are each optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;each Ra6, Rc6, and Rd6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra6, Rc6, and Rd6 are each optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;or any Rc6 and Rd6 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;each Rb6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb6 are each optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;each Re6 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 244 20443-0537WO1 // INCY0243-WO1 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rf6 and Rg6 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh6 and Ri6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj6 and Rk6 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj6 and Rk6 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RJ is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa7, SRa7, NHORa7, C(O)Rb7, C(O)NRc7Rd7, C(O)NRc7(ORa7), C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)ORa7, NRc7C(O)NRc7Rd7, C(=NRe7)Rb7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, NRc7C(=NRe7)Rb7, NRc7S(O)Rb7, NRc7S(O)NRc7Rd7, NRc7S(O)2Rb7, NRc7S(O)(=NRe7)Rb7, NRc7S(O)2NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, S(O)2NRc7Rd7, OS(O)(=NRe7)Rb7, OS(O)2Rb7, SF5, P(O)Rf7Rg7, OP(O)(ORh7)(ORi7), P(O)(ORh7)(ORi7), and BRj7Rk7, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RJ are each optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;each Ra7, Rc7, and Rd7 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- wherein the C1-6 245 20443-0537WO1 // INCY0243-WO1 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra7, Rc7, and Rd7 are each optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;or any Rc7 and Rd7 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;each Rb7is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb7 are each optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;each Re7 is independently selected from H, OH, CN, C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, C1-6haloalkyl, C1-6haloalkoxy, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, and 4-14 membered heterocycloalkyl;each Rf7 and Rg7 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh7 and Ri7 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj7 and Rk7 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj7 and Rk7 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RK is independently selected from H, D, OH, halo, oxo, CN, C(O)OH, NH2, NO2, SF5, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6246 20443-0537WO1 // INCY0243-WO1 14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;and wherein any heteroaryl group of any of the above-recited substituents optionally comprises an N-oxide on any ring-forming nitrogen.
  2. 2
    A compound of Formula (I):or a pharmaceutically acceptable salt thereof;wherein: X is N;R1 is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl;R2 is selected from H, D, halo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C614 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa2, SRa2, NHORa2, C(O)Rb2, C(O)NRc2Rd2, C(O)NRc2(ORa2), C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, C(=NRe2)Rb2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2C(=NRe2)Rb2, NRc2S(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)(=NRe2)Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, S(O)2NRc2Rd2, OS(O)(=NRe2)Rb2, OS(O)2Rb2, SF5, P(O)Rf2Rg2, OP(O)(ORh2)(ORi2), P(O)(ORh2)(ORi2), and BRj2Rk2, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of R2 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RC substituents;Cy1 is C6-14 aryl, C3-14 cycloalkyl, or 5-14 membered heteroaryl, wherein the C6-14 aryl, C3-14 cycloalkyl, or 5-14 membered heteroaryl is optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RE or RM substituents;Cy2 is C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, or 4-14 membered heterocycloalkyl, wherein the C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, or 4-14 247 20443-0537WO1 // INCY0243-WO1 membered heterocycloalkyl is optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RF substituents;each Ra2, Rc2, and Rd2 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra2, Rc2, and Rd2 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RG substituents;or any Rc2 and Rd2 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;each Rb2 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb2 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RG substituents;each Re2 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rf2 and Rg2 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;248 20443-0537WO1 // INCY0243-WO1 each Rh2 and R12 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj2 and Rk2 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or any Rj2 and Rk2 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RC, RE, RM, RF, and RG is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa4, SRa4, NHORa4, C(O)Rb4, C(O)NRc4Rd4, C(O)NRc4(ORa4), C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)ORa4, NRc4C(O)NRc4Rd4, C(=NRe4)Rb4, C(=NRe4)NRc4Rd4, NRc4C(=NRe4)NRc4Rd4, NRc4C(=NRe4)Rb4, NRc4S(O)Rb4, NRc4S(O)NRc4Rd4, NRc4S(O)2Rb4, NRc4S(O)(=NRe4)Rb4, NRc4S(O)2NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, S(O)2NRc4Rd4, OS(O)(=NRe4)Rb4, OS(O)2Rb4, SF5, P(O)Rf4Rg4, OP(O)(ORh4)(ORi4), P(O)(ORh4)(ORi4), and BRj4Rk4, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RC, RE, RM, RF, and RG are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RH substituents;each Ra4, Rc4, and Rd4 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra4, Rc4, and Rd4 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RH substituents;or, any Rc4 and Rd4 attached to the same N atom, together with the N atom to which they are attached, optionally form a 5- or 6-membered heteroaryl or a 4-14 membered 249 20443-0537WO1 // INCY0243-WO1 heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RH substituents;each Rb4is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb4 are each optionally substituted with 1, 2, 3, 4, 5, 6, 7, or 8 independently selected RH substituents;each Re4 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rf4 and Rg4 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh4 and Ri4 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj4 and Rk4 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj4 and Rk4 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RH is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa5, SRa5, NHORa5, C(O)Rb5, C(O)NRc5Rd5, C(O)NRc5(ORa5), C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, 250 20443-0537WO1 // INCY0243-WO1 NRc5Rd5, NRc5NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, C(=NRe5)Rb5, C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5C(=NRe5)Rb5, NRc5S(O)Rb5, NRc5S(O)NRc5Rd5, NRc5S(O)2Rb5, NRc5S(O)(=NRe5)Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, S(O)2NRc5Rd5, OS(O)(=NRe5)Rb5, OS(O)2Rb5, SF5, I’(O)RR, OP(O)(ORh5)(ORi5), P(O)(ORh5)(ORi5), and BRj5Rk5, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RH are each optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;each Ra5, Rc5, and Rd5 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra5, Rc5, and Rd5 are each optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;or any Rc5 and Rd5 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;each Rb5 is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 arylC1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C614 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb5 are each optionally substituted with 1, 2, 3, or 4 independently selected RI substituents;each Re5 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;251 20443-0537WO1 // INCY0243-WO1 each Rf5 and Rg5 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh5 and Ri5 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj5 and Rk5 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj5 and Rk5 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RI is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa6, SRa6, NHORa6, C(O)Rb6, C(O)NRc6Rd6, C(O)NRc6(ORa6), C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)ORa6, NRc6C(O)NRc5Rd6, C(=NRe6)Rb6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, NRc6C(=NRe6)Rb6, NRc6S(O)Rb6, NRc6S(O)NRc6Rd6, NRc6S(O)2Rb6, NRc6S(O)(=NRe6)Rb6, NRc6S(O)2NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, S(O)2NRc6Rd6, OS(O)(=NRe6)Rb6, OS(O)2Rb6, SF5, P(O)Rf6Rg6, OP(O)(ORh6)(ORi6), P(O)(ORh6)(ORi6), and BRj6Rk6, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RI are each optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;each Ra6, Rc6, and Rd6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered 252 20443-0537WO1 // INCY0243-WO1 heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra6, Rc6, and Rd6 are each optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;or any Rc6 and Rd6 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;each Rb6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb6 are each optionally substituted with 1, 2, 3, or 4 independently selected RJ substituents;each Re6 is independently selected from H, OH, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rf6 and Rg6 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh6 and Ri6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj6 and Rk6 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj6 and Rk6 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RJ is independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered 253 20443-0537WO1 // INCY0243-WO1 heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa7, SRa7, NHORa7, C(O)Rb7, C(O)NRc7Rd7, C(O)NRc7(ORa7), C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)ORa7, NRc7C(O)NRc7Rd7, C(=NRe7)Rb7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, NRc7C(=NRe7)Rb7, NRc7S(O)Rb7, NRc7S(O)NRc7Rd7, NRc7S(O)2Rb7, NRc7S(O)(=NRe7)Rb7, NRc7S(O)2NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, S(O)2NRc7Rd7, OS(O)(=NRe7)Rb7, OS(O)2Rb7, SF5, P(O)Rf7Rg7, OP(O)(ORh7)(ORi7), P(O)(ORh7)(ORi7), and BRj7Rk7, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of RJ are each optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;each Ra7, Rc7, and Rd7 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Ra7, Rc7, and Rd7 are each optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;or any Rc7 and Rd7 attached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14 membered heterocycloalkyl group, wherein the 5- or 6-membered heteroaryl or 4-14 membered heterocycloalkyl group is optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;each Rb7is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- of Rb7 are each optionally substituted with 1, 2, 3, or 4 independently selected RK substituents;254 20443-0537WO1 // INCY0243-WO1 each Re7 is independently selected from H, OH, CN, C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, C1-6haloalkyl, C1-6haloalkoxy, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, and 4-14 membered heterocycloalkyl;each Rf7 and Rg7 is independently selected from H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkylC1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C16 alkyl-;each Rh7 and Ri7 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;each Rj7 and Rk7 is independently selected from OH, C1-6 alkoxy, and C1-6 haloalkoxy;or, any Rj7 and Rk7 attached to the same B atom, together with the B atom to which they are attached, form a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from C1-6 alkyl and C1-6haloalkyl;each RK is independently selected from H, D, OH, halo, oxo, CN, C(O)OH, NH2, NO2, SF5, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C614 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;and wherein any heteroaryl group of any of the above-recited substituents optionally comprises an N-oxide on any ring-forming nitrogen.
  3. 4
    The compound of any one of claims 1-3, or a pharmaceutically acceptable salt thereof; wherein:each RI Is Independently selected from D, halo, oxo, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, CN, NO2, ORa6, SRa6, NHORa6, C(O)Rb6, C(O)NRc6Rd6, C(O)NRc6(ORa6), C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)ORa6, NRc6C(O)NRc5Rd6, C(=NRe6)Rb6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, NRc6C(=NRe6)Rb6, NRc6S(O)Rb6, NRc6S(O)NRc6Rd6, NRc6S(O)2Rb6, NRc6S(O)(=NRe6)Rb6, NRc6S(O)2NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, S(O)2NRc6Rd6, OS(O)(=NRe6)Rb6, OS(O)2Rb6, SF5, P(O)Rf6Rg6, OP(O)(ORh6)(OR16), P(O)(ORh6)(OR16), and BRj6Rk6;each Ra6, Rc6, and Rd6 Is Independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-;or any Rc6 and Rd6 attached to the same N atom, together w1th the N atom to wh1ch they are attached, form a 5- or 6-membered heteroaryl or a 4 membered heterocycloalkyl group;and 256 20443-0537WO1 // INCY0243-WO1 each Rb6 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-14 aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6alkyl-, C3-14cycloalkyl-C1-6alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-.
  4. 5
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein Cy1 is C6-14 aryl, wherein the C6-14 aryl is optionally substituted with 1, 2, 3, or 4 independently selected RE substituents.
  5. 6
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein Cy1 is C3-14 cycloalkyl, wherein the C3-14 cycloalkyl is optionally substituted with 1, 2, 3, or 4 independently selected RE substituents.
  6. 7
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein Cy1 is 5-14 membered heteroaryl, wherein the 5-14 membered heteroaryl is optionally substituted with 1, 2, 3, or 4 independently selected RE substituents.
  7. 8
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein Cy1 is 4-14 membered heterocycloalkyl, wherein the 4-14 membered heterocycloalkyl is optionally substituted with 1, 2, 3, or 4 independently selected RE substituents.
  8. 9
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein Cy1 is phenyl or 5-10 membered heteroaryl, wherein the phenyl or 5-10 membered heteroaryl is optionally substituted with 1, 2, 3, or 4 independently selected RE substituents.
  9. 10
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein Cy1 is selected from phenyl, pyridinyl, furanyl, benzofuranyl, and pyrazolyl, each of which is optionally substituted with 1, 2, or 3 substituents selected from C1-3 alkyl, halo, CN, and C1-3 alkoxy.
  10. 11
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein the optionally substituted Cy1 is selected from cyanophenyl, 257 20443-0537WO1 // INCY0243-WO1 cyanofluorophenyl, 2,3-dihydro-1 H-pyrrolo[2,3,- b ]pyridine, phenyl, methoxyphenyl, fluorophenyl, pyridinyl, methylfUranyl, benzofUranyl, and methyl-1 H-pyrazolyl.
  11. 12
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein the optionally substituted Cy1 is selected from 2-cyanophenyl, 3cyanophenyl, 3-cyano fluorophenyl, 2,3-dihydro-1 H-pyrrolo[2,3,-b ]pyridine, phenyl, 3methoxyphenyl, 2-fluorophenyl, pyridine yl, 2-methylfuran yl, benzofuran yl, and 1methyl-1H-pyrazol yl.
  12. 13
    The compound of any one of claims 1-4, or a pharmaceutically acceptable salt thereof, wherein the optionally substituted Cy1 is selected from 3-cyanophenyl and phenyl.
  13. 14
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is C6-14 aryl, wherein the C6-14 aryl is optionally substituted with 1, 2, 3, or 4 independently selected RF substituents.
  14. 15
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is C3-14 cycloalkyl, wherein the C3-14 cycloalkyl is optionally substituted with 1, 2, 3, or 4 independently selected RF substituents.
  15. 16
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is 5-14 membered heteroaryl, wherein the 5-14 membered heteroaryl is optionally substituted with 1, 2, 3, or 4 independently selected RF substituents.
  16. 17
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is 4-14 membered heterocycloalkyl, wherein the 4-14 membered heterocycloalkyl is optionally substituted with 1, 2, 3, or 4 independently selected RF substituents.
  17. 18
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is selected from C3-6 cycloalkyl, phenyl, 5-10 membered heteroaryl, and 5-10 membered heterocycloalkyl;wherein the 5-10 membered heteroaryl and 5-10 membered heterocycloalkyl each comprise one, two, or three nitrogen atoms as ring-forming heteroatoms, wherein one of the 258 20443-0537WO1 // INCY0243-WO1 one or two nitrogen atoms is optionally an N-oxide, and wherein a ring-forming carbon atom is optionally substituted by oxo;and wherein the C3-6 cycloalkyl, phenyl, 5-10 membered heteroaryl, and 5-10 membered heterocycloalkyl are each optionally substituted with 1, 2, or 3 substituents selected from C1-3 alkyl, C1-3 alkyl-OH, halo, CN, C1-3 alkoxy, and C(O)NH2.
  18. 19
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is selected from pyridinyl, tetrahydropyridinyl, piperidinyl, pyridine-Noxide, oxo-dihydropyridinyl, phenyl, pyrazolo[1,5-a]pyridin yl, pyrazolo[1,5-b]pyridazinyl, pyrazolyl, pyrimidinyl, quinolinyl, oxazolyl, 2,3-dihydro-[1,4]dioxino[2,3-b]pyridin yl, and triazolyl each of which is optionally substituted with 1, 2, or 3 substituents selected from C1-3 alkyl, C1-3 alkyl-OH, halo, CN, C1-3 alkoxy, and C(O)NH2.
  19. 20
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein Cy2 is cyclopropyl optionally substituted with 1, 2, or 3 substituents selected from C1-3 alkyl, halo, CN, C1-3 alkoxy, and C(O)NH2.
  20. 21
    The compound of any one of claims 1-13, or a pharmaceutically acceptable salt thereof, wherein the optionally substituted Cy2 is selected from 2,6-dimethylpyridin yl, pyridin yl, 2-methylpyridin yl, 1-carbamoyl-1,2,3,6-tetrahydropyridin yl, 1carbamoylpiperidin yl, 2-methoxypyridin yl, 2-methoxy methylpyridin yl, 2,6dimethylpyridin yl oxide, 1-ethyl oxo-1,6-dihydropyridin yl, 3-methylpyridin yl, 3-fluoropyridin yl, 3-chloropyridin yl, 3-methoxypyridin yl, 3-cyanopyridin yl, 4carbamoylphenyl, pyrazolo[1,5-a ]pyridin yl, pyrazolo[1,5-b]pyridazin yl, 5-methyl-1Hpyrazol yl, 1-ethyl-1H-pyrazol yl, 1-isopropyl-1H-pyrazol yl, 1-propyl-1H-pyrazol-5yl, pyrimidin yl, 2,3-dihydro-[1,4]dioxino[2,3-b]pyridin yl, quinolin yl, 5fluoropyrimidin yl, oxazol yl, 4-methyloxazol yl, 4-ethyloxazol yl, 4(hydroxymethyl) methyloxazol yl, 4-(methoxymethyl) methyloxazol yl, 4(hydroxymethyl) methyloxazol yl, 1-ethyl-1H-1,2,3-triazol yl, and cyclopropyl.
  21. 22
    The compound of any one of claims 1-21, or a pharmaceutically acceptable salt thereof, wherein R1 is selected from H and C1-6 alkyl. 259 20443-0537WO1 // INCY0243-WO1
  22. 23
    The compound of any one of claims 1-21, or a pharmaceutically acceptable salt thereof, wherein R1 is H or C1-3 alkyl.
  23. 24
    The compound of any one of claims 1-21, or a pharmaceutically acceptable salt thereof, wherein R1 is H or ethyl.
  24. 25
    The compound of any one of claims 1-21, or a pharmaceutically acceptable salt thereof, wherein R1 is H.
  25. 26
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein R2 is selected from H, C1-6 alkyl, C6-14aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, ORa2, NRc2Rd2, C(O)Rb2, C(O)NRc2Rd2, and C(O)ORa2, wherein the C1-6 alkyl, C6-14aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14 cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, are each optionally substituted with 1, 2, or 3 independently selected RC substituents.
  26. 27
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein R2 is selected from H, C1-6 alkyl, C6-14aryl, C3-14cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, ORa2, NRc2Rd2, C(O)Rb2, C(O)NRc2Rd2, and C(O)ORa2, wherein the C1-6 alkyl, C6-14aryl, C3-14 cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C6-14 aryl-C1-6 alkyl-, C3-14cycloalkyl-C1-6 alkyl-, (5-14 membered heteroaryl)-C1-6 alkyl-, and (4-14 membered heterocycloalkyl)-C1-6 alkyl-, are each substituted with 1, 2, or 3 independently selected RC substituents.
  27. 28
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein R2 is selected from H, phenyl, 5-6 membered heteroaryl, C(O)Rb2, C(O)NRc2Rd2, and C(O)ORa2, wherein the phenyl and 5-6 membered heteroaryl are each optionally substituted with 1 or 2 independently selected RC substituents. 260 20443-0537WO1 // INCY0243-WO1
  28. 29
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein R2 is selected from H, C(O)OEt, CONH2, and C(O)NHEt.
  29. 30
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein R2 selected from phenyl and 5-6 membered heteroaryl, each of which is optionally substituted with C(O)OMe.
  30. 31
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein R2 is on or .
  31. 32
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein the optionally substituted R2 is selected from pyridinylmethyl, hydroxy(phenyl)methyl, hydroxyethylamino(phenyl)ethyl, cyclohexylmethyl, fluorobenzyl, hydroxy(fluorophenyl)methyl, (methylpyridinyl)methyl, (fluoropyridinyl)methyl, (trifluoromethylpyridinyl)methyl, ((hydroxymethyl)pyridinyl)methyl, (methoxypyridinyl)methyl, (methylpyrazolyl)benzyl, (methylpyrazolyl)methyl, benzoisoxazolylmethyl, (methylindazolyl)methyl, (hydroxyazetidinyl)methyl, benzoyl, phenylcyclopropyl, (cyano(phenyl)methyl)amino, tetrahydrofuranyl, phenyl(pyridinyloxy)methyl, fluoro ((fluorohydroxypyrrolidinyl)methyl)benzyl, ((carboxypiperidinyl)methyl)fluorobenzyl, fluoro((Nmethylmethylsulfonamido)methyl)benzyl, ((dioxoimidazolidinyl)methyl)fluorobenzyl, (difluorophenyl)(hydroxy)methyl, (pyridinyl-1H-tetrazolyl)methyl, (pyrazolyl-1Htetrazolyl)methyl, (thiazolyl-1H-tetrazolyl)methyl, (methyltrifluoromethylpyrazolyl)methyl, ((1,1 -dioxidoisothiazolidinyl)methyl)fluorobenzyl, ((methyl-2,5 dioxoimidazolidinyl)methyl)benzyl, and (cyanophenoxy)methyl.
  32. 33
    The compound of any one of claims 1-25, or a pharmaceutically acceptable salt thereof, wherein the optionally substituted R2 is selected from pyridin ylmethyl, hydroxy(phenyl)methyl, (2-hydroxyethylamino)(phenyl)methyl, cyclohexylmethyl, 2fluorobenzyl, (2-fluorophenyl)(hydroxy)methyl, (6-methylpyridin yl)methyl, (3fluoropyridin yl)methyl, (3-methoxypyridin yl)methyl, 2-(1-methyl-1H-pyrazol-4yl)benzyl, benzo[d]isoxazol ylmethyl, (1-methyl-1H-indazol yl)methyl, (3- 261 20443-0537WO1 // INCY0243-WO1 hydroxyazetidin yl)methyl, benzoyl, 1-phenylcyclopropyl, (cyano(phenyl)methyl)amino, tetrahydrofuran yl, phenyl(pyridin yloxy)methyl, 2-fluoro (((3R,4R) fluoro-4hydroxypyrrolidin yl)methyl)benzyl, 2-((4-carboxypiperidin yl)methyl) fluorobenzyl, 2-fluoro ((N-methylmethylsulfonamido)methyl)benzyl, 2-((2,5-dioxoimidazolidin-1yl)methyl) fluorobenzyl, (2,6-difluorophenyl)(hydroxy)methyl, (5-(pyridin yl)-1Htetrazol-1 -yl)methyl, (5-(1H-pyrazol-1 -yl)-1H-tetrazol yl)methyl, (5-(thiazol yl)-1Htetrazol-1 -yl)methyl, (5 -methyl-3 -(trifluoromethyl)-1H-pyrazol-1 -yl)methyl, (3 methylpyridin yl)methyl, 2-((1,1-dioxidoisothiazolidin yl)methyl) fluorobenzyl, 2fluoro ((3-methyl-2,5-dioxoimidazolidin yl)methyl)benzyl, (6-(trifluoromethyl)pyridin-2yl)methyl, (3-(hydroxymethyl)pyridin yl)methyl, (1-methyl-1H-pyrazol yl)methyl, and (2-cyanophenoxy)methyl, (3-methylpyridin yl)methoxy, (6-methylpyridin yl)methoxy, and ((3-methylpyridin yl)methyl)amino.
  33. 34
    The compound of any one of claims 1-28, or a pharmaceutically acceptable salt thereof, wherein each RC is independently selected from halo, C1-6 alkyl, C6-14 aryl, 5-14 membered heteroaryl, (4-14 membered heterocycloalkyl)-C1-6 alkyl-, ORa4, C(O)ORa4, and NRc4Rd4, wherein the C1-6 alkyl, 5-14 membered heteroaryl, and (4-14 membered heterocycloalkyl)-C1-6 alkyl- are optionally substituted with 1, 2, or 3 independently selected RH substituents.
  34. 35
    The compound of any one of claims 1-28 and 34, or a pharmaceutically acceptable salt thereof, wherein each RH is independenty selected from halo, oxo, C1-6 alkyl, C1-6 haloalkyl, ORa5, C(O)ORa5, and NRc5S(O)2Rb5.
  35. 36
    The compound of any one of claims 1 and 3-35, or a pharmaceutically acceptable salt thereof, wherein R3 is selected from H, halo, C1-6 alkyl, C6-14aryl, 5-14 membered heteroaryl, CN, and ORa3, wherein the C1-6 alkyl, C6-14 aryl, and 5-14 membered heteroaryl are each optionally substituted with 1, 2, or 3 independently selected RD substituents.
  36. 37
    The compound of any one of claims 1 and 3-35, or a pharmaceutically acceptable salt thereof, wherein R3 is selected from H, C1-3 alkyl, halo, CN, morpholinomethyl, 4ethoxyphenyl, 2-hydroxyethoxy, and pyridinyl. 262 20443-0537WO1 // INCY0243-WO1
  37. 38
    The compound of any one of claims 1 and 3-35, or a pharmaceutically acceptable salt thereof, wherein R3 is selected from H, methyl, bromo, CN, morpholinomethyl, 4ethoxyphenyl, 2-hydroxyethoxy, and pyridinyl.
  38. 46
    A pharmaceutical composition comprising a compound of any one of claims 1-45, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient or carrier.
  39. 47
    A method of inhibiting an activity of an adenosine receptor, comprising contacting the receptor with a compound of any one of claims 1-45, or a pharmaceutically acceptable salt thereof.
  40. 48
    A method of treating a disease or disorder in a patient, wherein the disease or disorder is associated with abnormal expression of A2A or A2B receptors, comprising administering to said patient a therapeutically effective amount of a compound of any one of claims 1-45, or a pharmaceutically acceptable salt thereof. 276 20443-0537WO1 // INCY0243-WO1
  41. 61
    A method of treating or preventing atherosclerotic plaque formation in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound of any one of claims 1-45, or a pharmaceutically acceptable salt thereof. 278
Independent claims41