| 主权项 |
1. A compound of Formula I:or a pharmaceutically acceptable salt or solvate thereof, wherein:
Q is oxygen (O) or sulfur (S); A1 is C(O)OH, or C(O)R7; or is selected from R1A is selected from R1A1,
C1-6 alkyl substituted with 1-3 R8,C2-6 alkenyl substituted with 1-2 R8,C2-6 alkynyl substituted with 1-2 R8,C3-8 cycloalkyl substituted with 1-2 R8,5-6 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 1-2 R8; R1A1 is C2-6 alkyl, C3-6 alkenyl, or C3-8 cycloalkyl wherein: (a) each of which has at least one CH2 moiety replaced with O, S, S(O), S(O)2, S(O)2NH, S(O)2NR9A, C(O), C(O)NH, C(O)NR9A, NH, or NR9A; and (b) remaining CH2 or CH substituted with 1-2 R8; R2, R3, R4 and R5 are independently selected from hydrogen (H), alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, halo, —NH2, —CN, —NO2, —C(O)OH, —C(O)OR9, —OCF3, —OR9, —OH, —SH, —SR9, —S(O)3H, —P(O)3H2, —C(O)NH2, —C(O)NHR9, —C(O)NR9R9, —NHR9, —NR9R9, —S(O)2NHR9, —S(O)2NR9R9, —NHS(O)2CF3, —NR9S(O)2CF3, —C(O)NHS(O)2R9, —C(O)NR9S(O)2R9, —S(O)2NHC(O)OR9, —S(O)2NR9C(O)OR9, —S(O)2NHC(O)NHR9, —S(O)2NHC(O)NR9R9, —S(O)2NR9C(O)NHR9, —C(O)H, —S(O)2NR9C(O)NR9R9, —C(O)NHS(O)2CF3, —C(O)NR9S(O)2CF3, —C(O)R9, —NR9C(O)H, —NHC(O)R9, —NR9C(O)R9, —OC(O)R9, —OC(O)NH2, —OC(O)NHR9, —OC(O)NR9R9, —C(NH)NH2, —C(NH)NHR9, —C(NH)NR9R9, —C(NR9)NH2, —C(NR9)NHR9, —NHC(NR9)NR9R9, —S(O)R9, —S(O)2R9, —NHC(O)OR9, —NR9C(O)OR9, —NHS(O2)R9 and —NR9S(O2)R9, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl groups are each optionally substituted with one, two, three, four, or five substituents independently selected from R10;
optionally one of R2 and R3, R3 and R4 or R4 and R5 may be taken together to form a 5-10 membered carbocyclyl, a 5-10 membered heterocyclyl, an aryl or a 5-7 membered heteroaryl ring, each of which may optionally be substituted by one two, three, four, or five of alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, halo, —NH2, —CN, —NO2, —C(O)OH, —C(O)OR9, —OCF3, —OR9, —OH, —SH, —SR9, —S(O)3H, —P(O)3H2, —C(O)NH2, —C(O)NHR9, —C(O)NR9R9, —NHR9, —NR9R9, —S(O)2NHR9, —S(O)2NR9R9, —NHS(O)2CF3, —NR9S(O)2CF3, —C(O)NHS(O)2R9, —C(O)NR9S(O)2R9, —S(O)2NHC(O)OR9, —S(O)2NR9C(O)OR9, —S(O)2NHC(O)NHR9, —S(O)2NHC(O)NR9R9, —S(O)2NR9C(O)NHR9, —C(O)H, —S(O)2NR9C(O)NR9R9, —C(O)NHS(O)2CF3, —C(O)NR9S(O)2CF3, —C(O)R9, —NR9C(O)H, —NHC(O)R9, —NR9C(O)R9, —OC(O)R9, —OC(O)NH2, —OC(O)NHR9, —OC(O)NR9R9, —C(NH)NH2, —C(NH)NHR9, —C(NH)NR9R9, —C(NR9)NH2, —C(NR9)NHR9, —NHC(NR9)NR9R9, —S(O)R9, —S(O)2R9, —NHC(O)OR9, —NR9C(O)OR9, —NHS(O2)R9 and —NR9S(O2)R9, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl groups are each optionally substituted with one, two, three, four, or five substituents independently selected from R10; R7 is selected from —COOH, —COOR9, —NHS(O)2CF3, —NR12S(O)2CF3, —NHC(O)H, —NR12C(O)H, —NHC(O)R9, —NR12C(O)R9, —NHC(O)OR9, —NR12C(O)OR9, —NHS(O2)R9 and —NR12S(O2)R; R8 is selected from cycloalkyl, heterocyclyl, aryl, heteroaryl, each of which may optionally be substituted by one or more of R11, halo, —NH2, —CN, —NO2, —C(O)OH, —C(O)OR11, —OCF3, —OR11, —OH, —SH, —SR11, —C(O)NH2, —C(O)NHR11, —C(O)NR11R12, —NHR11, —NR11R12, —S(O)2NHR11, —S(O)2NR11R12, —NHS(O)2CF3, —NR12S(O)2CF3, —C(O)NHS(O)2R1, —C(O)NR12S(O)2R11, —S(O)2NHC(O)OR11, —S(O)2NR12C(O)OR11, —S(O)2NHC(O)NHR11, —S(O)2NHC(O)NR11R12, —S(O)2NR12C(O)NHR11, —C(O)H, —S(O)2NR12C(O)NR11R12, —C(O)NHS(O)2CF3, —C(O)NR12S(O)2CF3, —C(O)R11, —NR12C(O)H, —NHC(O)R11, —NR12C(O)R1, —OC(O)R11, —OC(O)NH2, —OC(O)NHR11, —OC(O)NR11R12, —C(NH)NH2, —C(NH)NHR11, —C(NH)NR11R12, —C(NR12)NH2, —C(NR12)NHR11, —NHC(NR12)NR11R12, —S(O)R11, —S(O)2R, —NHC(O)OR11, —NR12C(O)OR11, —NHS(O2)R11 and —NR12S(O2)R11; R9 is selected from alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, aryl, heteroaryl, each of which may optionally be substituted by one or more of R11, halo, —NH2, —CN, —NO2, —C(O)OH, —C(O)OR12, —OCF3, —OR12, —OH, —SH, —SR12, —C(O)NH2, —C(O)NHR12, —C(O)NR12R12, —NHR12, —NR12R12, —S(O)2NHR12, —S(O)2NR12R12, —NHS(O)2CF3, —NR12S(O)2CF3, —C(O)H, —C(O)R12, —NHC(O)H, —NR12C(O)H, —NHC(O)R12, —NR12C(O)R12, —S(O)R12, —S(O)2R12, —NHC(O)OR12, —NR12C(O)OR12, —NHS(O2)R12 and —NR12S(O2)R12; R9A is C1-4 alkyl; R10 is selected from alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, aryl, heteroaryl, halo, —NH2, —CN, —NO2, —C(O)OH, —OCF3, —OR13, —OH, —SH, —SR13, —C(O)NH2, —C(O)NHR13, —C(O)NR9AR13, —NHR13, —NR9AR13, —S(O)2NHR13, —S(O)2NR9AR13, —NHS(O)2CF3, —C(O)H, —C(O)R13, —NHC(O)R13, —NR9A C(O)R13, —S(O)R13, —S(O)2R13, —NHC(O)OR13, —NR9A C(O)OR13, —NHS(O2)R13 and —NR9A S(O2)R13, wherein said alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, aryl, and heterocyclyl groups are each optionally substituted with one or more R14; R11 is selected from C1-4 alkyl, C1-4 alkyloxy, C1-4 haloalkyl, 3-6 membered cycloalkyl, 3-6 membered heterocyclyl, aryl, heteroaryl, each of which may optionally be substituted by one or more of R9A, NH2, —CN, —NO2, —C(O)OH, —OCF3, —OR13, —OH, —SH, —SR13, —C(O)NH2, —C(O)NHR9A, —NHR9A, —S(O)2NHR9A, —NHS(O)2CF3, —C(O)H, —C(O)R9A, —S(O)R9A, —S(O)2R9A, —NHC(O)R9A, —NHC(O)OR9A, and —NHS(O2)R13; R12 is selected from C1-4 alkyl, C1-4 alkyloxy, C1-4 haloalkyl, 3-6 membered cycloalkyl, 3-6 membered heterocyclyl, aryl, and heteroaryl; R13 is selected from C1-4 alkyl which may optionally be substituted by one or more of halo, —CF3, —NH2, —CN, —C(O)OH, —OCF3, —OR9A, —OH, —SH, —SR9A, —C(O)NH2, —C(O)NHR9A, and —NHR9A; R14 is selected from halo, —CF3, —NH2, —CN, —C(O)OH, —OCF3, —OR9A, —OH, —SH, —SR9A, —C(O)NH2, —C(O)NHR9A, and —NHR9A; provided that when RIA is methylene then R8 is not an aryl moiety. |
