R¹ is:

(1) —C_1-6 alkyl,

(2) —C_1-6 alkyl substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —SO₂R^A, —SO₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)SO₂R^B, —N(R^A)SO₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B,

(3) —C_3-8 cycloalkyl, which is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

(4) —C_1-6 alkyl substituted with C_3-8 cycloalkyl, wherein the C_3-8 cycloalkyl is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

(5) heteroaryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of substituents (1) to (26) as defined below in part (i) of Part B of the definition of R^J,

(6) —C_1-6 alkyl substituted with R^J, wherein R^J is:

(A) aryl which is:

(i) optionally substituted with from 1 to 5 substituents each of which is independently:

(1) —C_1-6 alkyl, which is optionally substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —SO₂R^A, —SO₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)SO₂R^B, —N(R^A)SO₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B,

(2) —O—C_1-6 alkyl,

(3) —C_1-6 haloalkyl,

(4) —O—C_1-6 haloalkyl,

(5) —OH,

(6) halogen,

(7) —CN,

(8) —NO₂,

(9) —N(R^A)R^B,

(10) —C(O)N(R^A)R^B,

(11) —C(O)R^A,

(12) —CO₂R^A,

(13) —SR^A,

(14) —S(O)R^A,

(15) —SO₂R^A,

(16) —SO₂N(R^A)R^B,

(17) —N(R^A)SO₂R^B,

(18) —N(R^A)SO₂N(R^A)R^B,

(19) —N(R^A)C(O)R^B,

(20) —N(R^A)C(O)—C(O)N(R^A)R^B, or

(21) —N(R^A)CO₂R^B, and

(ii) optionally substituted with 1 or 2 substituents each of which is independently:

(1) —C_3-8 cycloalkyl,

(2) aryl,

(3) —C_1-6 alkyl substituted with aryl, —C_3-8 cycloalkyl, HetA, or HetB,

(4) -HetA,

(5) —C(O)-HetA; or

(6) -HetB;

wherein:

 each cycloalkyl is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

 each aryl is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J,

 each HetA is independently (i) a —C_4-7 azacycloalkyl or oxacycloalkyl or thiacycloalkyl or (ii) a —C_3-6 diazacycloalkyl or oxazacycloalkyl or thiazacycloalkyl, wherein the S in the thiacycloalkyl or thiazacycloalkyl is optionally oxidized to S(O) or SO₂, and wherein any of the rings defined in (i) or (ii) is optionally substituted with from 1 to 4 substituents each of which is independently oxo, —C_1-6 alkyl, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, or —S(O)₂R^A; and

 each HetB is independently a 5- or 6-membered heteroaromatic ring containing from 1 to 4 heteroatoms independently selected from N, O and S, wherein the heteroaromatic ring is optionally substituted with from 1 to 4 substituents each of which is independently any one of the substituents (1) to (26) as defined below in part (i) of Part B of the definition of R^J, or

(B) heteroaryl which is:

(i) optionally substituted with from 1 to 6 substituents each of which is independently:

(1) —C_1-6 alkyl,

(2) —C_1-6 alkyl substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —S(O)₂R^A, —S(O)₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)S(O)₂R^B, —N(R^A)S(O)₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B,

(3) —O—C_1-6 alkyl,

(4) —C_1-6 haloalkyl,

(5) —O—C_1-6 haloalkyl,

(6) —OH,

(7) -oxo,

(8) halogen,

(9) —CN,

(10) —NO₂,

(11) —N(R^A)R^B,

(12) —C(O)N(R^A)R^B,

(13) —C(O)R^A,

(14) —C(O)—C_1-6 haloalkyl,

(15) —C(O)OR^A,

(16) —OC(O)N(R^A)R^B,

(17) —SR^A,

(18) —S(O)R^A,

(19) —S(O)₂R^A,

(20) —S(O)₂N(R^A)R^B,

(21) —N(R^A)S(O)₂R^B,

(22) —N(R^A)S(O)₂N(R^A)R^B,

(23) —N(R^A)C(O)R^B,

(24) —N(R^A)C(O)N(R^A)R^B,

(25) —N(R^A)C(O)—C(O)N(R^A)R^B, or

(26) —N(R^A)CO₂R^B, and

(ii) optionally substituted with 1 or 2 substituents each of which is independently:

(1) —C_3-8 cycloalkyl,

(2) aryl,

(3) —C_1-6 alkyl substituted with aryl, —C_3-8 cycloalkyl, HetA, or HetB,

(4) -HetA,

(5) —C(O)-HetA; or

(6) -HetB;

wherein:

 each cycloalkyl is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

 each aryl is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J,

 each HetA is independently as defined in Part (A)(ii) of the definition of R^J, and

 each HetB is independently as defined in Part (A)(ii) of the definition of R^J;

(7) aryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J;

R² is:

(1) —H,

(2) —C_1-6 alkyl,

(3) —C_1-6 haloalkyl,

(4) —C_1-6 alkyl substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —SO₂R^A, —SO₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)SO₂R^B, —N(R^A)SO₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B, or

(5) —C_1-6 alkyl substituted with HetC, —C(O)-HetC, —SO₂-HetC, —N(R^A)C(O)-HetC, or —N(R^A)C(O)C(O)-HetC;

wherein HetC is a 4- to 7-membered, saturated or mono-unsaturated heterocyclic ring containing from 1 to 3 heteroatoms independently selected from 1 to 3 N atoms, zero to 1 O atom, and zero to 1 S atom, where the S is optionally oxidized to S(O) or S(O)₂, with the proviso that the ring is attached to the rest of the molecule via a ring N atom, and wherein the saturated or mono-unsaturated heterocyclic ring is optionally substituted with from 1 to 4 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, oxo, —C(O)R^A, —CO₂R^A, —S(O)R^A, —SR^A, —S(O)₂R^A, —CH₂—CH═CH₂, —O—C_1-6 alkyl, —C_1-6 haloalkyl, —C_1-6 alkylene-CN, —C_1-6 alkylene-OH, or —C_1-6 alkylene-O—C_1-6 alkyl;

or alternatively R¹ and R² together with the ring nitrogen to which R¹ is attached and the ring carbon to which R² is attached form a 5- to 7-membered, saturated heterocyclic ring in which the portion of the ring formed from R¹ and R² is a 3- to 5-membered methylene chain in which one of the methylene moieties is optionally replaced with N(H), wherein the chain is optionally substituted with from 1 to 3 substituents each of which is independently —C_1-6 alkyl, —OH, or oxo;

R³ is:

(1) —H,

(2) —C_1-6 alkyl,

(3) —C_1-6 haloalkyl,

(4) —C_1-6 alkyl substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —SO₂R^A, —SO₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)SO₂R^B, —N(R^A)SO₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B,

(5) —C_1-6 alkyl substituted with HetD, —C(O)-HetD, —SO₂-HetD, —N(R^A)C(O)-HetD, or —N(R^A)C(O)C(O)-HetD,

(6) CycM, AryM, or HetM, or

(7) —C_1-6 alkyl substituted with CycM, AryM, or HetM;

wherein:

HetD independently has the same definition as HetC;

CycM is —C_3-8 cycloalkyl which is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl;

AryM is aryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J; and

HetM is heteroaryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (26) as defined above in part (i) of Part B of the definition of R^J;

or alternatively R² and R³ together with the carbon atoms to which they are attached form:

(i) a 3- to 8-membered saturated carbocyclic ring which is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

(ii) a benzene ring, which is optionally substituted with from 1 to 4 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J,

(iii) a 4- to 7-membered, saturated or mono-unsaturated heterocyclic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, where each S is optionally oxidized to S(O) or S(O)₂, and wherein the saturated or mono-unsaturated heterocyclic ring is optionally substituted with from 1 to 4 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, oxo, —C(O)R^A, —CO₂R^A, —S(O)R^A, —SR^A, —S(O)₂R^A, —CH₂—CH═CH₂, —O—C_1-6 alkyl, —C_1-6 haloalkyl, —C_1-6 alkylene-CN, —C_1-6 alkylene-OH, or —C_1-6 alkylene-O—C_1-6 alkyl, or

(iv) a 5- or 6-membered heteroaromatic ring, which is optionally substituted with from 1 to 3 substituents each of which is independently any one of the substituents (1) to (26) as defined above in part (i) of Part B of the definition of R^J;

wherein R⁶ and R⁷ are absent, when R² and R³ together with the carbon atoms to which they are attached form a benzene ring or a heteroaromatic ring;

R⁴ is:

(1) —H,

(2) —C_1-6 alkyl,

(3) —C_1-6 haloalkyl,

(4) —C_1-6 alkyl substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —SO₂R^A, —SO₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)SO₂R^B, —N(R^A)SO₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B,

(5) —OH,

(6) —O—C_1-6 alkyl,

(7) —O—C_1-6 haloalkyl,

(8) —CN,

(9) —NO₂,

(10) —N(R^C)R^D,

(11) —C(O)N(R^C)R^D,

(12) —C(O)R^A,

(13) —CO₂R^A,

(14) —SR^A,

(15) —S(O)R^A,

(16) —SO₂R^A,

(17) —SO₂N(R^A)R^B,

(18) —N(R^A)C(O)R^B,

(19) —N(R^A)CO₂R^B,

(20) —N(R^A)SO₂R^B,

(21) —N(R^A)SO₂N(R^A)R^B,

(22) —OC(O)N(R^A)R^B,

(23) —N(R^A)C(O)N(R^A)R^B,

(24) —N(R^A)C(O)C(O)N(R^A)R^B,

(25) halogen,

(26) —S—C(O)N(R^C)R^D,

(27) —N═C(R^A)—N(R^C)R^D,

(28) —C(O)N(R^A)—C_1-6 alkylene-N(R^C)R^D,

(29) —C(O)—C_1-6 alkylene-N(R^C)R^D,

(30) —C(O)N(R^A)—C_1-6 alkylene-C_1-6 haloalkyl,

(31) —C(O)—C_1-6 alkylene-C_1-6 haloalkyl,

(32) —N(SO₂R^A)—V,

(33) —N[C(O)R^A]—V,

(34) —C_1-6 alkyl substituted HetE, —C(O)-HetE, —SO₂-HetE, —N(R^A)C(O)-HetE, or —N(R^A)C(O)C(O)-HetE,

(35) —C_1-6 alkyl substituted with CycL, AryL, HetL, or HetS, or

(36) —T—R^L,

wherein:

T is a single bond, O, C(O), C(O)N(R^A), N(R^A)C(O), S, S(O), S(O)₂, N(R^A)S(O)₂, S(O)₂N(R^A), O—C_1-6 alkylene, C(O)—C_1-6 alkylene, C(O)N(R^A)—C_1-6 alkylene, N(R^A)C(O)—C_1-6 alkylene, S—C_1-6 alkylene, S(O)—C_1-6 alkylene, S(O)₂—C_1-6 alkylene, C_1-6 alkylene-S, C_1-6 alkylene-S(O), C_1-6 alkylene-S(O)₂, C_1-6 alkylene-O, C_1-6 alkylene-C(O), C_1-6 alkylene-C(O)N(R^A), C_1-6 alkylene-N(R^A)C(O), C_1-6 alkylene-N(R^A)S(O)₂, or C_1-6 alkylene-S(O)₂N(R^A);

V is (i) —CH₂—C_2-6 alkenyl or (ii) —C_1-6 alkyl substituted with C(O)N(R^C)R^D, CycL, AryL, HetL, or HetS; and

R^L is CycL, AryL, HetL, or HetS;

CycL is —C_3-8 cycloalkyl which is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl;

AryL is aryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J;

HetE independently has the same definition as HetC;

HetL is heteroaryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (26) as defined above in part (i) of Part B of the definition of R^J;

HetS is a 4- to 7-membered, saturated or mono-unsaturated heterocyclic ring containing at least one carbon atom and from 1 to 4 heteroatoms independently selected from N, O and S, where each S is optionally oxidized to S(O) or S(O)₂, with the proviso that HetS is attached to the rest of the molecule via a ring carbon atom; and wherein the saturated or mono-unsaturated heterocyclic ring is optionally substituted with from 1 to 4 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, oxo, —C(O)R^A, —CO₂R^A, —S(O)R^A, —SR^A, —S(O)₂R^A, —CH₂—CH═CH₂, —O—C_1-6 alkyl, —C_1-6 haloalkyl, —C_1-6 alkylene-C(O)N(R^A)R^B, —C_1-6 alkylene-CN, —C_1-6 alkylene-OH, or —C_1-6 alkylene-O—C_1-6 alkyl;

R⁵ is:

(1) —C_1-6 alkyl,

(2) —C_1-6 alkyl substituted with —OH, —O—C_1-6 alkyl, —O—C_1-6 haloalkyl, —CN, —NO₂, —N(R^A)R^B, —C(O)N(R^A)R^B, —C(O)R^A, —CO₂R^A, —SR^A, —S(O)R^A, —SO₂R^A, —SO₂N(R^A)R^B, —N(R^A)C(O)R^B, —N(R^A)CO₂R^B, —N(R^A)SO₂R^B, —N(R^A)SO₂N(R^A)R^B, —OC(O)N(R^A)R^B, —N(R^A)C(O)N(R^A)R^B, or —N(R^A)C(O)C(O)N(R^A)R^B,

(3) —C_3-8 cycloalkyl, which is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

(4) —C_1-6 alkyl substituted with —C_3-8 cycloalkyl, wherein the —C_3-8 cycloalkyl is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl,

(5) heteroaryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (26) as defined above in part (i) of Part B of the definition of R^J,

(6) —C_1-6 alkyl substituted with R^K, wherein R^K independently has the same definition as R^J as set forth above in the definition of R¹, or

(7) aryl, which is optionally substituted with from 1 to 5 substituents each of which is independently any one of the substituents (1) to (21) as defined above in part (i) of Part A of the definition of R^J;

and with the proviso that R⁵ is —C_1-6 alkyl substituted with R^K, when R¹ is other than —C_1-6 alkyl substituted with R^J;

R⁶ and R⁷ are each independently —H or —C_1-6 alkyl;

or alternatively R³ and R⁷ together with the carbon atom to which they are attached form (i) a 3- to 8-membered saturated carbocyclic ring which is optionally substituted with from 1 to 6 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, —O—C_1-6 alkyl, —C_1-6 haloalkyl, or —O—C_1-6 haloalkyl or (ii) a 4- to 7-membered, saturated or mono-unsaturated heterocyclic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, where each S is optionally oxidized to S(O) or S(O)₂, and wherein the saturated or mono-unsaturated heterocyclic ring is optionally substituted with from 1 to 4 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, oxo, —C(O)R^A, —CO₂R^A, —S(O)R^A, —SR^A, —S(O)₂R^A, —CH₂—CH═CH₂, —O—C_1-6 alkyl, —C_1-6 haloalkyl, —C_1-6 alkylene-CN, —C_1-6 alkylene-OH, or —C_1-6 alkylene-O—C_1-6 alkyl,

each aryl is independently (i) phenyl, (ii) a 9- or 10-membered bicyclic, fused carbocyclic ring system in which at least one ring is aromatic, or (iii) an 11- to 14-membered tricyclic, fused carbocyclic ring system in which at least one ring is aromatic;

each heteroaryl is independently (i) a 5- or 6-membered heteroaromatic ring containing from 1 to 4 heteroatoms independently selected from N, O and S, wherein each N is optionally in the form of an oxide, or (ii) a 9- or 10-membered bicyclic, fused ring system containing from 1 to 4 heteroatoms independently selected from N, O and S, wherein either one or both of the rings contain one or more of the heteroatoms, at least one ring is aromatic, each N is optionally in the form of an oxide, and each S in a ring which is not aromatic is optionally S(O) or S(O)₂;

each R^A is independently —H or —C_1-6 alkyl;

each R^B is independently —H or —C_1-6 alkyl;

each R^C is independently —H or —C_1-6 alkyl; and

each R^D is independently —H or —C_1-6 alkyl;

or alternatively R^C and R^D together with the N to which they are both attached form a 4- to 7-membered, saturated or mono-unsaturated heterocyclic ring containing the N to which they are both attached and optionally containing 1 or 2 additional heteroatoms independently selected from N, O and S, where each S is optionally oxidized to S(O) or S(O)₂, and wherein the saturated or mono-unsaturated heterocyclic ring is optionally substituted with from 1 to 4 substituents each of which is independently halogen, —CN, —C_1-6 alkyl, —OH, oxo, —C(O)R^A, —CO₂R^A, —S(O)R^A, —SR^A, —S(O)₂R^A, —CH₂—C_2-6 alkenyl, —O—C_1-6 alkyl, —C_1-6 haloalkyl, —C_1-6 alkylene-CN, —C_1-6 alkylene-OH, or —C_1-6 alkylene-O—C_1-6 alkyl.