| 主权项 |
1. A non-agonist PPARG modulatory compound of formula (IA) or (IB), or a pharmaceutically acceptable salt thereof: wherein: R2 is H or (C1-C4)alkyl; R3 is optionally mono- or multi-substituted (C1-C8)alkyl, (C1-C8)alkenyl, (C1-C8)alkynyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, heterocyclyl, cycloalkylalkyl, or heterocyclylalkyl; wherein if present each substituent on R3 is independently selected from the group consisting of (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C1o)aryl, (C3-C9)cycloalkyl, 3-9 membered mono- and bicyclic heterocyclyl, 3-9 membered mono- and bicyclic heteroaryl, halo, haloalkyl, haloalkoxy, nitro, cyano, CO2R′, methylenedioxy, OR′, N(R′)2, (C1-C4)alkyl-S(O)q, SO2NR′2, and (C1-C6)alkoxyl, wherein R′ is independently H, (C1-C6)alkyl, (C1-C6)haloalkyl, or (C3-C9)cycloalkyl, or wherein two R′ bonded to an atom together with the atom form a 3-8 membered ring optionally further comprising a heteroatom selected from the group consisting of O, NR′, and S(O)q, and wherein alkyl, alkenyl, alkynyl, aryl, arylalkyl, or cycloalkyl is optionally mono- or independently multi-substituted with (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, halo, OR′, N(R′)2, aryl, or aroyl; and wherein an alkyl or an alkyl group of a cycloalkylalkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl can be substituted with oxo; each X1-X4 is independently N or is C substituted with an independently selected R7 or with Z, provided that no more than one of X1-X4 is N, and provided that there is one and only one Z group present in the ring comprising X1, Z is a group of formulawherein a wavy line indicates a point of attachment, each X5-X7 is independently N or is C substituted with an independently selected H or R4; provided that that no more than one of X5-X7 is N;
R4 is H, halo, CO2R′, CN, OR′, N(R′)2, (C1-C4)alkyl optionally mono- or multi-substituted with halo, OR′ or N(R′)2 or a combination thereof, C-bonded tetrazolyl, R′S(O)2NHC(O), R′C(O)NHS(O)2, or (C1-C4)alkyl-S(O)q; or R4 is —(C(R′)2)mCO2R′ or is —O(C(R′)2)mCO2R′, wherein m is 1, 2, or 3; R is H or (C1-C6)alkyl; q is 0, 1 or 2; R5 is H or (C1-C4)alkyl; R6 is R7; or R5 and R6 taken together form a —CH2CH2— group; and, R7 is H, halo, CO2R′, CN, OR′, N(R′)2, (C1-C4)alkyl or (C1-C4)fluoroalkyl optionally substituted with OR′ or N(R′)2, C-bonded tetrazolyl, or (C1-C4)alkyl-S(O)q; or R7 is —(C(R′)2)mCO2R′ or is —O(C(R′)2)mCO2R′, wherein m is 1, 2, or 3. |
