| 主权项 |
1. A compound of Formula I, or a pharmaceutically acceptable salt thereof: wherein: R1 is selected from NH and N; the dashed line (- - - -), in conjunction with the solid line to which it is parallel, represents an optional double bond; R2 is selected from oxo or NH2, with the proviso that, when R2 is oxo, R1 and the bond represented by the dashed line (- - - -), in conjunction with the solid line to which it is parallel, is a single bond; and with the proviso that, when R2 is NH2, R1 is N and the bond represented by the dashed line (- - - -), in conjunction with the solid line to which it is parallel, is a double bond; R3 is selected from the group of H, F, CH2F, CHF2, and CF3; R5 is selected from the group of CN; unsubstituted C1-C4 alkyl; C1-C4 alkyl substituted with 1, 2, or 3 halogens; C1-C4 alkyl substituted with 1 substituent selected from —S—CH3 and —O—CH3; C2-C4 alkenyl; C2-C4 alkynyl; unsubstituted C3-C6 cycloalkyl; and C3-C6 cycloalkyl substituted by 1, 2, or 3 substituents selected from F and CH3; R4′ is selected from the group of H, —C(═O)R6, —C(═O)OR6, and —C(═O)NR6R7;
R4 is selected from the group of H, —C(═O)R6, —C(═O)OR6, and —C(═O)NR6R7; or
a) R4 is a group of the formula: wherein:each Y is O, S, NR, +N(O)(R), N(OR), +N(O)(OR), or N—NR2; andW1 and W2, when taken together, are —Y3(C(Ry)2)3 Y3—;or one of W1 or W2 together with R4′ is —Y3— and the other of W1 or W2 is Formula Ia;or W1 and W2 are each, independently, a group of the Formula Ia: wherein:each Y1 is, independently, O, S, NR, +N(O)(R), N(OR), +(N)(O)(OR), or N—NR2;each Y2 is independently a bond, O, CR2, —O—CR2—, NR, +N(O)(R), N(OR), +N(O)(OR), N—NR2, S, S—S, S(O), or S(O)2;each Y3 is a single bond;M1 is 0, 1, 2, or 3;each Rx is independently Ry or the formula: wherein:each M2a, M2b, and M2c is independently 0 or 1;M2d is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12;each Ry is independently H, F, Cl, Br, I, OH, R, —C(═Y1)R, —C(═Y1)OR, —C(═Y1)N(R)2, —N(R)2, —+N(R)3, —SR, —S(O)R, —S(O)2R, —S(O)(OR), —S(O)2(OR), —OC(═Y1)R, —OC(═Y1)OR, —OC(═Y1)(N(R)2), —SC(═Y1)R, —SC(═Y1)OR, —SC(═Y1)(N(R)2), —N(R)C(═Y1)R, —N(R)C(═Y1)OR, —N(R)C(═Y1)N(R)2, —SO2NR2, —CN, —N3, —NO2, —OR, or W3;or when taken together, two Ry on the same carbon atom form a carbocyclic ring having 3, 4, 5, 6, or 7 carbon ring atoms;or when taken together, two Ry on the same carbon atom form along with the carbon atom a heterocycle having 3, 4, 5, 6, or 7 ring atoms wherein one ring atom is selected from O or N and all other ring atoms are carbon;each R is independently H, (C1-C8) alkyl, (C1-C8) substituted alkyl, (C2-C8)alkenyl, (C2-C8) substituted alkenyl, (C2-C8) alkynyl, (C2-C8) substituted alkynyl, C6-C10 aryl, C6-C10 substituted aryl, a 3- to 10-membered heterocycle, a substituted 3- to 10-membered heterocycle, a 5- to 12-membered heteroaryl, a substituted 5- to 12-membered heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, or substituted heteroarylalkyl; andW3 is W4 or W5;W4 is R, —C(Y1)Ry, —C(Y1)W5, —SO2Ry, or —SO2W5;W5 is selected from phenyl, naphthyl, a C3-C8 carbocycle, or a 3- to 10-membered heterocycle, wherein W5 is independently substituted with 0, 1, 2, 3, 4, 5, or 6 Ry groups;each R6 and R7 is independently H, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C4-C8)carbocyclylalkyl, C6-C10 aryl, C6-C10 substituted aryl, 5- to 10-membered heteroaryl, substituted 5- to 10-membered heteroaryl, —C(═O)(C1-C8)alkyl, —S(O)n(C1-C8)alkyl or aryl(C1-C8)alkyl;or R6 and R7 taken together with a nitrogen to which they are both attached form a 3- to 7-membered heterocycle wherein any one ring carbon atom of said heterocycle can optionally be replaced with —O—, —S—or —NRa—;and wherein each (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl(C1-C8)alkyl of each R6 or R7 is, independently, optionally substituted with one, two, three, or four substituents selected from halo, hydroxy, CN, N3, N(Ra)2 or ORa; and wherein one, two, or three of the non-terminal carbon atoms of each said (C1-C8)alkyl may be optionally replaced with —O—, —S— or —NRa—; or
b) R4 is a group selected from: wherein:
R8 is selected from phenyl, 1-naphthyl, 2-naphthyl, R9 is selected from H and CH3;R10 is selected from H or C1-C6 alkyl;R10′ is selected from H or C1-C6 alkyl;or R10 and R10′, together with the carbon atom to which they are bound, form a 3-, 4-, 5-, or 6-membered spirocycle wherein all ring atoms of the spirocycle are carbon;or Rl0 and R10′, together with the carbon atom to which they are bound, form a 3-, 4-, 5-, or 6-membered spirocycle wherein 1 or 2 of the ring atoms of the spirocycle are selected from the group of O, S, and N, and all other ring atoms of the spirocycle are carbon;R11 is selected from H, C1-C8 alkyl, benzyl, C3-C6 cycloalkyl, —CH2—C3-C6 cycloalkyl, —CH2CH2—S—C(O)—C3-C6 alkyl, R7′ is selected from C1-C8 alkyl, —O—C1-C8 alkyl, benzyl, —O-benzyl, —CH2—C3-C6 cycloalkyl, and CF3; or
c) R4 and R4′ combine to form the structure selected from: |
