| 主权项 |
1. A compound of formula (I): or a salt thereof, wherein: R1 is CN, S(O)jAr1, S(O)k(C1-6 alkylene)Ar1; —NO2, —C(O)R1A; —C(O)OR1B or —C(O)NR1CR1D; j is 0, 1 or 2; k is 0, 1 or 2; each Ar1 is independently C6-10 aryl or 5-10 membered heteroaryl, each of which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from Cy1, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, C1-6 haloalkyl, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(═NRe1)NRc1Rd1, NRc1C(═NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 and S(O)2NRc1Rd1; each Cy1 is independently C6-10 aryl, C3-10 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl, each of which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(═NRe1)NRc1Rd1, NRc1C(═NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, S(O)2NRc1Rd1 and oxo; R1A is H, R1E, C2-6 alkenyl, C2-6 alkynyl, Ar1 or (C1-6 alkylene)Ar1; R1B is H, R1E, C2-6 alkenyl, C2-6 alkynyl, Ar1, (C1-6 alkylene)Ar1, —N(C1-6 alkyl)2, —CH(R1F)—CH2—S(O)m(C1-6 alkyl); —CH(R1F)—CH2—N(R1F)C(O)O(C1-6 alkyl) or —CH(R1F)—CH2—OC(O)CH(R1G)NH2; R1C is H, R1E, C2-6 alkenyl, C2-6 alkynyl, Ar1 or (C1-6 alkylene)Ar1; R1D is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Ar1 or (C1-6 alkylene)Ar1; or R1C and R1D, together with the N atom to which they are attached, form a 5-, 6-, or 7-membered heterocycloalkyl group, which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(═NRe1)NRc1Rd1, NRc1C(═NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, S(O)2NRc1Rd1, oxo, Ar1, (C1-6 alkylene)Ar1 or C(O)Ar1; each R1E is independently unsubstituted C1-6 alkyl or C1-6 alkyl substituted by 1, 2 or 3 substituents independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(═NRe1)NRc1Rd1, NRc1C(═NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, S(O)2NRc1Rd1 and oxo; each R1F is independently H or C1-6 alkyl; R1G is H, C1-6 alkyl; —((C1-C6)alkylene)-OR1H, —((C1-C6)alkylene)-NR1H2, —((C1-C6)alkylene)-SR1H, —((C1-C6)alkylene)-C(═O)OR1H2, —((C1-C6)alkylene)-C(═O)NR1H2, —((C1-C6)alkylene)-C(═NR1H)NR1H2, —((C1-C6)alkylene)-OC(═O)R1H, —((C1-C6)alkylene)-NR1HC(═O)R1H, —((C1-C6)alkylene)-NRHC(═NRH)NR4a2, Ar1G and —((C1-C6)alkylene)Ar1G; each Ar1G is independently unsubstituted phenyl or phenyl which is substituted by 1, 2, 3, 4 or 5 substituents independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, C1-6 haloalkyl, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(═NRe1)NRc1Rd1, NRc1C(═NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, and S(O)2NRc1Rd1; each R1H is independently H or C1-6 alkyl; m is 0, 1 or 2; A is NR2B, O or S(O)n; n is 0, 1 or 2; R2A is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Ar2 or (C1-6 alkylene)Ar2; R2B is H, C1-6 alkyl, C(O)C1-6 alkyl, Cy2A, C(O)Cy2A, (C1-6 alkylene)Cy2A and C(O)(C1-6 alkylene)Cy2A; or R2A and R2B, together with the N atom to which they are attached, form a 5-, 6-, or 7-membered heterocycloalkyl group, which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from RCy2, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(═NRe2)NRc2Rd2, NRc2C(═NRe2)NRc2Rd2 NRc2Rd2 NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, S(O)2NRc2Rd2 and oxo; Ar2 is C6-10 aryl or 5-10 membered heteroaryl, each of which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from Cy2B, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(═NRe2)NRc2Rd2, NRc2C(═NRe2)NRc2Rd2 NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2 and S(O)2NRc2Rd2; Cy2A is C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl, or 5-10 heterocycloalkyl, each of which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from Cy2B, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(═NRe2)NRc2Rd2, NRc2C(═NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, S(O)2NRc2Rd2 and oxo; each Cy2B is independently C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl, or 5-10 heterocycloalkyl, each of which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(═NRe2)NRc2Rd2, NRc2C(═NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2Nc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, S(O)2NRc2Rd2 and oxo; R3A is H, Cy3A1 or C1-6 alkyl, C2-6 alkenyl, C1-6 alkynyl, wherein said C1-6 alkyl forming R3A is optionally substituted with 1, 2, or 3 substituents independently selected from Cy3A2, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(═NRd3)NRc3Rd3, NRc3C(═NRd3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3 and oxo; R3B is H, Cy3B1 or C1-6 alkyl, C2-6 alkenyl, C1-6 alkynyl, wherein said C1-6 alkyl forming R3B is optionally substituted with 1, 2, or 3 substituents independently selected from Cy3B2, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(═NRd3)NRc3Rd3, NRc3C(═NRd3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3 and oxo; each Cy3A1, Cy3A2, Cy3B1 and Cy3B2 is, independently, C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl, or 5-10 heterocycloalkyl, each of which is unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents independently selected from RCy3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(═NRe3)NRc3Rd3, NRc3C(═NRe3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3 and oxo; or R3A and R3B, together with the N atom to which they are attached, form a 5-, 6-, or 7-membered heterocycloalkyl group, which is unsubstituted or substituted by 3, 4 or 5 substituents independently selected from RCy3, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(═NRe3)NRc3Rd3, NRc3C(═NRe3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3 and oxo; each RCy3 is independently selected from C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl, 5-10 heterocycloalkyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, C1-6 haloalkyl, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(═NRe3)NRc3Rd3, NRc3C(═NRe3)NRc3Rd3 NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3 and oxo; wherein each of said C6-10 aryl, C3-7 cycloalkyl, 5-10 membered heteroaryl and 5-10 heterocycloalkyl forming RCy3 is independently unsubstituted or substituted by 1, 2, or 3 substituents independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, C1-6 haloalkyl, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(═NRe3)NRc3Rd3, NRc3C(═NRe3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, S(O)2NRc3Rd3 and oxo; each Ra1, Rb1, Rc1, Rd1, Ra2, Rb2, Rc2, Rd2, Ra3, Rb3, Rc3 and Rd3 is independently selected from H, C1-6 alkyl, C1-4 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, C3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkyl, C3-10 cycloalkyl-C1-4 alkyl, (5-10 membered heteroaryl)-C1-4 alkyl or (4-10 membered heterocycloalkyl)-C1-4 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, C3-10 cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkyl, C3-10 cycloalkyl-C1-4 alkyl, (5-10 membered heteroaryl)-C1-4 alkyl and (4-10 membered heterocycloalkyl)-C1-4 alkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from C1-4 alkyl, C1-4 haloalkyl, halo, CN, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(═NRe4)NRc4Rd4, NRc4C(═NRe4)NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4, NRc4S(O)2NRc4Rd4 and S(O)2NRc4Rd4; or any Rc1 and Rd1 attached to the same N atom, any Rc2 and Rd2 attached to the same N atom, any Rc3 and Rd3 attached to the same N atom, or any Rc4 and Rd4 attached to the same N atom, together with the N atom to which they are attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2 or 3 substituents independently selected from C1-6 alkyl, C3-7 cycloalkyl, 3-7 membered heterocycloalkyl, C6-10 aryl, 5-6 membered heteroaryl, C1-6 haloalkyl, halo, CN, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(═NRe4)NRc4Rd4, NRc4C(═NRe4)NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4, NRc4S(O)2NRc4Rd4 and S(O)2NRc4Rd4; each Ra4, Rb4, Rc4 and Rd4 is independently selected from H, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl and C2-4 alkynyl, wherein said C1-4 alkyl, C2-4 alkenyl, and C2-4 alkynyl, is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino, di(C1-4 alkyl)amino, C1-4 haloalkyl, and C1-4 haloalkoxy; or any Rc4 and Rd4 attached to the same N atom, together with the N atom to which they are attached, form a 3-, 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino, di(C1-4 alkyl)amino, C1-4 haloalkyl and C1-4 haloalkoxy; and each Re1, Re2, Re3 and Re4 is independently selected from H, C1-4 alkyl and CN; with the proviso that the compound is other than the following compounds, and salts thereof: 3-(4-methylamino-2-methanesulfanyl-pyrimidin-5-yl)-acrylonitrile; 3-(4-ethylamino-2-phenylamino-pyrimidin-5-yl)acrylonitrile; 3-(4-amino-2-methanesulfanyl-pyrimidin-5-yl)-acrylic acid and esters thereof; 3-(4-methylamino-2-methanesulfanyl-pyrimidin-5-yl)-acrylic acid and esters thereof; 3-(4-ethylamino-2-methanesulfanyl-pyrimidin-5-yl)-acrylic acid and esters thereof; 3-(4-cyclopropylamino-2-methanesulfanyl-pyrimidin-5-yl)acrylic acid and esters thereof; 3-(4-cyclopentylamino-2-methanesulfanyl-pyrimidin-5-yl)acrylic acid and esters thereof; 3-(4-cyclohexylamino-2-methanesulfanyl-pyrimidin-5-yl)acrylic acid and esters thereof; 3-(4-methoxybenzylamino-2-methanesulfanyl-pyrimidin-5-yl)acrylic acid and esters thereof; 3-2-methanesulfanyl-4-phenylamino-pyrimidin-5-yl)acrylic acid and esters thereof; 3-(4-amino-2-phenylamino-pyrimidin-5-yl)acrylic acid and esters thereof; and 3-(4-ethylamino-2-phenylamino-pyrimidin-5-yl)acrylic acid and esters thereof. |
