the compound corresponds to formula (I):

B is selected from the group consisting of

A is thienyl;

as to R¹ and R²:

R¹ is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, —C(O)OR_a, —C(O)NR_aR_b, and R_1p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, or 2 substituents independently selected from the group consisting of cyano, formyl, halo, nitro, oxo, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b,—N(R_e)C(O)R_a, —N(R_e)C(O)OR_a, —N(R_e)C(O)NR_aR_b, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, —N═CR_jR_k, —C(R_e)═CR_jR_k, and R_1q; and

R² is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, or 2 substituents independently selected from the group consisting of cyano, formyl, halo, nitro, oxo, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)OR_a, —N(R_e)C(O)NR_aR_b, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, —N═CR_jR_k, and R_2q; or, alternatively,

R¹ and R², together with the carbon atom to which they are attached, form a monocyclic ring selected from the group consisting of cycloalkyl and cycloalkenyl, wherein:

each of the cycloalkyl and cycloalkenyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of halo, —OH, —O(alkyl), —NH₂, —N(H)(alkyl), —N(alkyl)₂, alkyl, and haloalkyl;

as to R³ and R⁴:

R³ is selected from the group consisting of hydrogen, cyano, formyl, halo, oxo, nitro, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, alkyl, alkenyl, alkynyl, and R_3p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, oxo, halo, nitro, —OR^a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_3q; and

R⁴ is selected from the group consisting of hydrogen, cyano, formyl, halo, oxo, nitro, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, alkyl, alkenyl, alkynyl, and R_4p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, oxo, halo, nitro, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_4q; or, alternatively,

R³ and R⁴, together with the carbon atoms to which they are attached, form a ring selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, and heterocycle, wherein:

each of the of aryl, heteroaryl, cycloalkyl, cycloalkenyl, and heterocycle is substituted with (R⁸)_m;

R⁵ is selected from the group consisting of —OR_d, —SR_d, —NR_dR_e, —N(H)C(O)R_d, —N(H)C(O)OR_d, —N(H)SO₂R_d, and —N(H)SO₂NR_dR_e;

R⁶ is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, and -alkylR₁₀₆;

R⁷ at each occurrence is independently selected from the group consisting of cyano, formyl, nitro, oxo, halo, alkyl, alkenyl, alkynyl, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OP(═O)(R_e)(OR_e), —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(═NH)R_e, —N(R_e)C(═Nalkyl)R_e, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(═S)NR_aR_b, —N(R_e)C(═S)N(R_e)C(O)R_a, —N(R_e)C(O)OR_a, —N(R_e)SOR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)R_a, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_7p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, oxo, nitro, halo, —N₃, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SOR_a, —N(R_e)SO_a2R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)R_a, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_7q;

R⁸ at each occurrence is independently selected from the group consisting of cyano, formyl, nitro, oxo, halo, alkyl, alkenyl, alkynyl, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_8p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, nitro, oxo, halo, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_8q;

R⁹ at each occurrence is independently selected from the group consisting of alkyl, alkenyl, alkynyl, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_9p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, nitro, oxo, halo, —OR_a, —OC(O)R_a, —OC(O)OR_a, —OC(O)NR_aR_b, —OSO₂R_a, —OSO₂NR_aR_b, —SR_a, —S(O)R_a, —SO₂R_a, —SO₂OR_a, —SO₂NR_aR_b, —NR_aR_b, —N(R_e)C(O)R_a, —N(R_e)C(O)NR_aR_b, —N(R_e)C(O)OR_a, —N(R_e)SO₂R_a, —N(R_e)SO₂NR_aR_b, —N(R_e)SO₂N(R_e)C(O)OR_a, —C(O)R_a, —C(O)OR_a, —C(O)NR_aR_b, and R_9q;

R¹⁰ is selected from the group consisting of hydrogen and alkyl;

R¹¹ is selected from the group consisting of hydrogen and alkyl;

as to R_aand R_b:

R_a at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, and R_p, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, oxo, halo, nitro, —OR_c, —OC(O)R_c, —OC(O)OR_c, —OC(O)NR_cR_d, —OSO₂R_c, —OSO₂NR_cR_d, —SR_c, —S(O)R_c, —SO₂R_c, —SO₂OR_c, —SO₂NR_cR_d, —NR_cR_d, —N(R_e)C(O)R_c, —N(R_e)C(O)NR_cR_d, —N(R_e)C(O)OR_c, —N(R_e)SO₂R_c, —N(R_e)SO₂NR_cR_d, —N(R_e)SO₂N(R_e)C(O)OR_c, —C(O)R_c, —C(O)OR_c, —C(O)NR_cR_d, —C(O)N(R_e)NR_cR_d, and R_q; and

R_b at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, R₁₀₆, haloalkyl, hydroxyalkyl, alkoxyalkyl, and -alkylR₁₀₆; or, alternatively,

R_a and R_b, together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of heterocycle and heteroaryl, wherein:

each of the heterocycle and heteroaryl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, cyano, formyl, halo, nitro, oxo, —OR_c, —OC(O)R_c, —OC(O)OR_c, —OC(O)NR_cR_d, —OSO₂R_c, —OSO₂NR_cR_d, —SR_c, —S(O)R_c, —SO₂R_c, —SO₂OR_c, —SO₂NR_cR_d, —NR_cR_d, —N(R_e)C(O)R_c, —N(R_e)C(O)NR_cR_d, —N(R_e)C(O)OR_c, —N(R_e)SO₂R_c, —N(R_e)SO₂NR_cR_d, —N(R_e)SO₂N(R_e)C(O)OR_c, —C(O)R_c, —C(O)OR_c, and —C(O)NR_cR_d, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, or 2 substituents independently selected from the group consisting of cyano, halo, nitro, oxo, —OR_c, —OC(O)R_c, —OC(O)OR_c, —OC(O)NR_cR_d, —OSO₂R_c, —OSO₂NR_cR_d, —SR_c, —S(O)R_c, —SO₂R_c, —SO₂OR_c, —SO₂NR_cR_d, —NR_cR_d, —N(R_e)C(O)R_c, —N(R_e)C(O)NR_cR_d, —N(R_e)C(O)OR_c, —N(R_e)SO₂R_c, —N(R_e)SO₂NR_cR_d, —N(R_e)SO₂N(R_e)C(O)OR_c, —C(O)R_c, —C(O)OR_c, —C(O)NR_cR_d, and R_q;

as to R_c and R_d:

R_c at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, and R₁₀₃, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, oxo, halo, nitro, —OR_f, —OC(O)R_f, —OC(O)OR_f, —OC(O)NR_fR_g, —OSO₂R_f, —OSO₂NR_fR_g, —SR_f, —S(O)R_f, —SO₂R_f, —SO₂OR_f, —SO₂NR_fR_g, —NR_fR_g, —N(R_e)C(O)R_f, —N(R_e)C(O)NR_fR_g, —N(R_e)C(O)OR_f, —N(R_e)SO₂R_f, —N(R_e)SO₂NR_fR_g, —N(R_e)SO₂N(R_e)C(O)OR_f, —C(O)R_f, —C(O)OR_f, —C(O)NR_fR_g, and R₁₀₃; and

R_d at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, R₁₀₆, haloalkyl, alkoxyalkyl, hydroxyalkyl, and -alkylR₁₀₆; or, alternatively,

R_c and R_d, together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of heterocycle and heteroaryl, wherein:

each of the heteroaryl and heterocycle is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, cyano, formyl, halo, nitro, oxo, —OR_f, —OC(O)R_f, —OC(O)OR_f, —OC(O)NR_fR_g, —OSO₂R_f, —OSO₂NR_fR_g, —SR_f, —S(O)R_f, —SO₂R_f, —SO₂OR_f, —SO₂NR_fR_g, —NR_fR_g, —N(R_e)C(O)R_f, —N(R_e)C(O)NR_fR_g, —N(R_e)C(O)OR_f, —N(R_e)SO₂R_f, —N(R_e)SO₂NR_fR_g, —N(E_e)SO₂N(R_e)C(O)OR_f, —C(O)R_f, —C(O)OR_f, and —C(O)NR_fR_g, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, halo, nitro, oxo, —OR_f, —OC(O)R_f, —OC(O)OR_f, —OC(O)NR_fR_g, —OSO₂R_f, —OSO₂NR_fR_g, —SR_f, —S(O)R_f, —SO₂R_f, —SO₂NR_fR_g, —NR_fR_g, —N(R_e)C(O)R_f, —N(R_e)C(O)NR_fR_g, —N(R_e)C(O)OR_f, —N(R_e)SO₂R_f, —N(R_e)SO₂NR_fR_g, —N(R_e)SO₂N(R_e)C(O)OR_f, —C(O)R_f, —C(O)OR_f, —C(O)NR_fR_g, and R₁₀₃;

R_e at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, R₁₀₆, haloalkyl, and alkylR₁₀₆;

as to R_f and R_g:

R_f at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, and R₁₀₃, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, nitro, halo, oxo, —OH, —O(alkyl), —O(cyanoalkyl), —O(haloalkyl), —O(R₁₀₆), —NH₂, —N(H)(alkyl), —N(alkyl)₂, —N(H)(R₁₀₆), —N(alkyl)(R₁₀₆), —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), —C(O)N(alkyl)₂, and R₁₀₃; and

R_g at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, R₁₀₆, haloalkyl, and -alkylR₁₀₆; or, alternatively,

R_f and R_g, together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of heterocycle and heteroaryl, wherein:

each of the heterocycle and heteroaryl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, cyano, formyl, halo, nitro, oxo, —OH, —O(alkyl), —O(cyanoalkyl), —O(haloalkyl), —OR₁₀₆, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —N(H)(R₁₀₆), N(alkyl)(R₁₀₆), C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), and —C(O)N(alkyl)₂, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, nitro, halo, oxo, —OH, —O(alkyl), —O(cyanoalkyl), —O(haloalkyl), —OR₁₀₆, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —N(H)(R₁₀₆), —N(alkyl)(R₁₀₆), —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), —C(O)N(alkyl)₂, and R₁₀₃;

as to R_j and R_k:

R_j at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, R₁₀₃, haloalkyl, and -alkylR₁₀₃; and

R_k at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; or, alternatively,

R_j and R_k, together with the carbon atom to which they are attached, form a ring selected from the group consisting of cycloalkyl, cycloalkenyl, heterocycle, aryl and heteroaryl, wherein:

each ring is substituted with 0, 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, nitro, cyano, formyl, halo, oxo, —OH, —O(alkyl), —O(cyanoalkyl), —O(haloalkyl), —OR₁₀₆, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —N(H)(R₁₀₆), —N(alkyl)(R₁₀₆), —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl) and —C(O)N(alkyl)₂, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, nitro, halo, oxo, —OH, —O(alkyl), —O(cyanoalkyl), —O(haloalkyl), —OR₁₀₆, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —N(H)(R₁₀₆), —N(alkyl)(R₁₀₆), —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), —C(O)N(alkyl)₂, and R₁₀₃;

m is selected from the group consisting of 0, 1, 2, 3, and 4;

n is selected from the group consisting of 0, 1, 2, 3, and 4;

p is selected from the group consisting of 0, 1, and 2;

t is selected from the group consisting of 0, 1, 2, 3, and 4;

R_p, R_q, R_1p, R_1q, R_2q, R_3p, R_3q, R_4p, R_4q, R_7p, R_7q, R_8p, R_8q, R_9p, and R_9q, at each occurrence, are independently selected from the group consisting of cycloalkyl, cycloalkenyl, aryl, heteroaryl, and heterocycle; wherein:

each of the cycloalkyl, cycloalkenyl, aryl, heteroaryl, and heterocycle is substituted with 0, 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, cyano, formyl, halo, nitro, oxo, —OR₁₀₁, —OC(O)R₁₀₁, —OC(O)OR₁₀₁, —OC(O)NR₁₀₁R₁₀₂, —OSO₂R₁₀₁, —OSO₂NR₁₀₁R₁₀₂, —SR₁₀₁, —S(O)R₁₀₁, —SO₂R₁₀₁, —SO₂OR₁₀₁, —SO₂NR₁₀₁R₁₀₂, —NR₁₀₁R₁₀₂, —N(R₁₀₂)C(O)R₁₀₁, —N(R₁₀₂)C(O)OR₁₀₁, —N(R₁₀₂)C(O)NR₁₀₁R₁₀₂, —N(R₁₀₂)SO₂R₁₀₁, —N(R₁₀₂)SO₂NR₁₀₁R₁₀₂, —N(R₁₀₂)SO₂N(R₁₀₂)C(O)OR₁₀₁, —C(O)R₁₀₁, —C(O)OR₁₀₁, and —C(O)NR₁₀₁R₁₀₂, wherein:

each of the alkyl, alkenyl, and alkynyl is substituted with 0, 1, 2, or 3 substituents independently selected from the group consisting of cyano, formyl, halo, nitro, oxo, —OR₁₀₁, —OC(O)R₁₀₁, —OC(O)OR₁₀₁, —OC(O)NR₁₀₁R₁₀₂, —OSO₂R₁₀₁, —OSO₂NR₁₀₁R₁₀₂, —SR₁₀₁, —S(O)R₁₀₁, —SO₂R₁₀₁, SO₂OR₁₀₁, —SO₂NR₁₀₁R₁₀₂, —NR₁₀₁R₁₀₂, —N(R₁₀₂)C(O)R₁₀₁, —N(R₁₀₂)C(O)OR₁₀₁, —N(R₁₀₂)C(O)NR₁₀₁R₁₀₂, —N(R₁₀₂)SO₂R₁₀₁, —N(R₁₀₂)SO₂NR₁₀₁R₁₀₂, —N(R₁₀₂)SO₂N(R₁₀₂)C(O)OR₁₀₁, —C(O)R₁₀₁, —C(O)OR₁₀₁, and —C(O)NR₁₀₁R₁₀₂;

as to R₁₀₁and R₁₀₂:

R₁₀₁ at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, R₁₀₃, -alkylR₁₀₃, -alkenylR₁₀₃, -alkynylR₁₀₃, haloalkyl, cyanoalkyl, -alkylC(O)R₁₀₄, -alkylC(O)OR₁₀₄, -alkylC(O)NR₁₀₄R₁₀₅, -alkyl-OR₁₀₄, -alkyl-OC(O)R₁₀₄, -alkyl-OC(O)OR₁₀₄, -alkylSR₁₀₄, -alkylS(O)R₁₀₄, -alkylSO₂R₁₀₄, -alkylSO₂OR₁₀₄, -alkylSO₂NR₁₀₄R₁₀₅, -alkylNR₁₀₄R₁₀₅, -alkylN(R₁₀₅)C(O)R₁₀₄, -alkylN(R₁₀₅)C(O)OR₁₀₄, -alkylN(R₁₀₅)C(O)NR₁₀₄R₁₀₅, -alkylN(R₁₀₅)SO₂R₁₀₄, and -alkylN(R₁₀₅)SO₂NR₁₀₄R₁₀₅; and

R₁₀₂ at each occurrence is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, and benzyl; or, alternatively,

R₁₀₁ and R₁₀₂, together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of heterocycle and heteroaryl, wherein:

each of the heterocycle or heteroaryl is substituted with 0, 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, nitro, formyl, halo, cyano, —OH, —Oalkyl, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), —C(O)N(alkyl)₂, —SH, —Salkyl, —S(O)alkyl, —SO₂alkyl, —C(O)alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, -alkylNH₂, -alkylN(H)(alkyl), -alkylN(alkyl)₂, -alkylC(O)OH, -alkylC(O)Oalkyl, -alkylC(O)NH₂, -alkylC(O)N(H)(alkyl), -alkylC(O)N(alkyl)₂, -alkylSH, -alkylSalkyl, -alkylS(O)alkyl, -alkylSO₂alkyl and -alkylC(O)alkyl;

R₁₀₃ at each occurrence is independently selected from the group consisting of cycloalkyl, cycloalkenyl, aryl, heteroaryl, and heterocycle, wherein:

each of the cycloalkyl, cycloalkenyl, aryl, heteroaryl and heterocycle is independently substituted with 0, 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, halo, nitro, cyano, oxo, formyl, haloalkyl, —OR₁₀₄, —OC(O)R₁₀₄, —OC(O)OR₁₀₄, —OC(O)NR₁₀₄R₁₀₅, —OSO₂NR₁₀₄R₁₀₅, —SO₂R₁₀₅, —S(O)R₁₀₄, —NR₁₀₄R₁₀₅, —N(R₁₀₅)C(O)NR₁₀₄R₁₀₅, —N(R₁₀₅)COR₁₀₄, —N(R₁₀₅)SO₂R₁₀₄, —N(R_105)SO2NR₁₀₄R₁₀₅, —C(O)R₁₀₄, —C(O)OR₁₀₄, —C(O)NR₁₀₄R₁₀₃, -alkylOR₁₀₄, -alkylOC(O)R₁₀₄, -alkylOC(O)OR₁₀₄, -alkylOC(O)NR₁₀₄R₁₀₅, -alkylOSO₂NR₁₀₄R₁₀₅, -alkylSO₂R₁₀₄, -alkylS(O)R₁₀₄, -alkylNR₁₀₄R₁₀₅, -alkylN(R₁₀₅)COR₁₀₄, -alkylN(R₁₀₅)SO₂R₁₀₄, -alkylN(R₁₀₄)C(O)NR₁₀₄R₁₀₅, -alkylN(R₁₀₅)SO₂NR₁₀₄R₁₀₅, -alkylC(O)R₁₀₄, -alkylC(O)OR₁₀₄, and -alkylC(O)NR₁₀₄R₁₀₅;

as to R₁₀₄ and R₁₀₅:

R₁₀₄and R₁₀₅, at each occurrence, are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, and benzyl; or, alternatively,

R₁₀₄and R₁₀₅, together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of heterocycle and heteroaryl, wherein:

each of the heterocycle or heteroaryl is substituted with 0, 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, nitro, formyl, halo, cyano, —OH, —Oalkyl, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), —C(O)N(alkyl)₂, —SH, —Salkyl, —S(O)alkyl, —SO₂alkyl, —C(O)alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, -alkylNH₂, -alkylN(H)(alkyl), -alkylN(alkyl)₂, -alkylC(O)OH, -alkylC(O)Oalkyl, -alkylC(O)NH₂, -alkylC(O)N(H)(alkyl), —alkylC(O)N(alkyl)₂, —alkylSH, -alkylSalkyl, -alkylS(O)alkyl, -alkylSO₂alkyl, and -alkylC(O)alkyl; and

R₁₀₆ at each occurrence is independently selected from the group consisting of aryl and heteroaryl, wherein:

each of the aryl and heteroaryl is substituted with 0, 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, nitro, formyl, halo, cyano, —OH, —Oalkyl, —NH₂, —N(H)(alkyl), —N(alkyl)₂, —C(O)OH, —C(O)Oalkyl, —C(O)NH₂, —C(O)N(H)(alkyl), —C(O)N(alkyl)₂, —SH, —Salkyl, —S(O)alkyl, —SO₂alkyl, —C(O)alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, -alkylNH₂, -alkylN(H)(alkyl), -alkylN(alkyl)₂, -alkylC(O)OH, -alkylC(O)Oalkyl, -alkylC(O)NH₂, -alkylC(O)N(H)(alkyl), -alkylC(O)N(alkyl)₂, —alkylSH, -alkylSalkyl, -alkylS(O)alkyl, -alkylSO₂alkyl, and alkylC(O)alkyl.