| 主权项 |
1. A compound of formula (I): wherein: R1, R4 and R5 are independently selected from hydrogen, alkyl, aryl, aralkyl, —C(O)R9 or —C(O)N(R6)R7; one of R2 and R3 is selected from one of the following and the other is selected from the other two of the following: a) a bicyclic aryl of formula (II) or a bicyclic heteroaryl of formula (II): where:A is an alkylene chain containing six to eight carbons, an alkenylene chain containing six to eight carbons, or an alkynylene chain containing six to eight carbons, where one or two carbons of the alkylene, alkenylene or alkynylene chain is optionally replaced by —NR9—, ═N—, —O—, —S(O)p— (where p is 0, 1 or 2) or —P(O)p— (where p is 0, 1 or 2) and where each carbon in the alkylene chain, the alkenylene chain or the alkynylene chain is independently optionally substituted by one or two substituents selected from the group consisting of oxo, thioxo, cyano, nitro, halo, haloalkyl, alkyl, cycloalkyl, cycloalkylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, ═N—O—R6, —R10—OR9, —R10—O—R11—OR9, —R10—O—R11—O—R11—OR9, —R10—O—R11—CN, —R10—O—R11—C(O)OR9, —R10—O—R11—C(O)N(R6)R7, —R10—O—R11—S(O)pR9 (where p is 0, 1 or 2), —R10—O—R11—N(R6)R7, —R10—O—R11—C(NR12)N(R12)H, —R10—OC(O)—R9, —R10—N(R6)R7, —R10—C(O)R9, —R10—C(O)OR9, —R10—C(O)N(R6)R7, —R10—N(R6)C(O)OR8, —R10—N(R6)C(O)R9, —R10—N(R6)S(O)tR9 (where t is 1 or 2), —R10—S(O)tOR9 (where t is 1 or 2), —R10—S(O)pR9 (where p is 0, 1 or 2), and —R10—S(O)tN(R6)R7 (where t is 1 or 2); andB1, B2, B3 and B4 are each independently selected from the group consisting of ═C(R13)— and ═N—, provided that one of B1, B2, B3 and B4 is a carbon directly bonded to the nitrogen to which its corresponding R2 or R3 is attached; b) a polycyclic heteroaryl containing more than 14 ring atoms optionally substituted by one or more substituents selected from the group consisting of oxo, thioxo, cyano, nitro, halo, haloalkyl, alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, —R10—OR9, —R10—O—R11—OR9, —R10—O—R11—O—R11—OR9, —R10—O—R11—CN, —R10—O—R11—C(O)OR9, —R10—O—R11—C(O)N(R6)R7, —R10—O—R11—S(O)pR9 (where p is 0, 1 or 2), —R10—O—R11—N(R6)R7, —R10—O—R11—C(NR12)N(R12)H, —R10—OC(O)—R9, —R10—N(R6)R7, —R10—C(O)R9, —R10—C(O)OR9, —R10—C(O)N(R6)R7, —R10—N(R6)C(O)OR9, —R10—N(R6)C(O)R9, —R10—N(R6)S(O)tR9 (where t is 1 or 2), —R10—S(O)tOR9 (where t is 1 or 2), —R10—S(O)pR9 (where p is 0, 1 or 2), and —R10—S(O)tN(R6)R7 (where t is 1 or 2); or c) a bridged bicyclic aryl of formula (III) or a bridged bicyclic heteroaryl of formula (III): where:m and n are independently 1 to 4;q and r are independently 0 to 3;each A1, A3 and A4 is independently selected from the group consisting of C(R8)2, O, S(O)p (where p is 0, 1 or 2), P(O)p (where p is 0, 1 or 2) and N(R9);each A2 is independently selected from the group consisting of C(R8) and N; andB5, B6, B7 and B8 are each independently selected from the group consisting of ═C(R13)— and ═N—, provided that one of B5, B6, B7 and B8 is a carbon directly bonded to the nitrogen to which its corresponding R2 or R3 is attached; each R6 and R7 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, hydroxyalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted aralkenyl, optionally substituted aralkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted cycloalkylalkenyl, optionally substituted cycloalkylalkynyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heterocyclylalkenyl, optionally substituted heterocyclylalkynyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heteroarylalkenyl, optionally substituted heteroarylalkynyl, —R11—OR9, —R11—CN, —R11—NO2, —R11—N(R9)2, —R11—C(O)OR9 and —R11—C(O)N(R9)2, or any R6 and R7, together with the common nitrogen to which they are both attached, form an optionally substituted N-heteroaryl or an optionally substituted N-heterocyclyl; each R8 is independently selected from the group consisting of hydrogen, cyano, nitro, halo, haloalkyl, alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, —R10—OR9, —R10—O—R11—OR9, —R10—O—R11—O—R11—OR9, —R10—O—R11—CN, —R10—O—R11—C(O)OR9, —R10—O—R11—C(O)N(R6)R7, —R10—O—R11—S(O)pR9 (where p is 0, 1 or 2), —R10—O—R11—N(R6)R7, —R10—O—R11—C(NR12)N(R12)H, —R10—OC(O)—R9, —R10—N(R6)R7, —R10—C(O)R9, —R10—C(O)OR9, —R10—C(O)N(R6)R7, —R10—N(R6)C(O)OR9, —R10—N(R6)C(O)R9, —R10—N(R6)S(O)tR9 (where t is 1 or 2), —R10—S(O)tOR9 (where t is 1 or 2), —R10—S(O)pR9 (where p is 0, 1 or 2), and —R10—S(O)tN(R6)R7 (where t is 1 or 2), or two R8's on adjacent carbons can combine to form a double bond; each R9 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted aralkenyl, optionally substituted aralkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted cycloalkylalkenyl, optionally substituted cycloalkylalkynyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heterocyclylalkenyl, optionally substituted heterocyclylalkynyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heteroarylalkenyl, optionally substituted heteroarylalkynyl; each R10 is independently selected from the group consisting of a direct bond, an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain and an optionally substituted straight or branched alkynylene chain; each R11 is independently selected from the group consisting of an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain and an optionally substituted straight or branched alkynylene chain; each R12 is hydrogen, alkyl, cyano, nitro or —OR9; and each R13 is independently selected from the group consisting of hydrogen, cyano, nitro, halo, haloalkyl, alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, —R10—OR9, —R10—OC(O)—R9, —R10—N(R6)R7, —R10—C(O)R9, —R10—C(O)OR9, —R10—C(O)N(R6)R7, —R10—N(R6)C(O)OR9, —R10—N(R6)C(O)R9, —R10—N(R6)S(O)tR9 (where t is 1 or 2), —R10—S(O)tOR9 (where t is 1 or 2), —R10—S(O)pR9 (where p is 0, 1 or 2), and —R10—S(O)tN(R6)R7 (where t is 1 or 2);as an isolated stereoisomer or a mixture thereof, or as a pharmaceutically acceptable salt thereof. |
