| 主权项 |
1. A compound according to formula I: or a pharmaceutically acceptable salt, tautomer, or ester thereof, wherein: Y is a linker selected from the group consisting of a covalent bond, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, heterocyclyl, carbocyclyl, carbonyl, iminyl, diazenyl, O, S, SO, SO2, carboxyalkyl, carboxyalkenyl, carboxyalkynyl, and N—R39; X is a linker selected from the group consisting of a covalent bond, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, carbonyl, iminyl, diazenyl, O, S, SO, SO2, and N—R39, m is an integer from one to six; n is an integer from zero to five; q is one or two; R1 is selected from the group consisting of C3-C20 alkanoyl, carboxyalkanoyl, carboxyalkenoyl, alkoxycarbonylalkanoyl, alkenyloxycarbonylalkanoyl, cyanoalkanoyl, hydroxyalkanoyl, aminocarbonylalkanoyl, hydroxyaminocarbonylalkanoyl, monoalkylaminocarbonylalkanoyl, dialkylaminocarbonylalkanoyl, heterocyclylalkanoyl, heterocycyl carbonylalkanoyl, heteroarylaminocarbonylalkanoyl, heterocyclylaminocarbonylalkanoyl, cyanoaminocarbonylalkanoyl, alkyl sulfonylaminocarbonylalkanoyl, aryl sulfonylaminocarbonylalkanoyl, sulfoaminocarbonylalkanoyl, phosphonoaminocarbonylalkanoyl, phosphono, sulfo, phosphonoalkanoyl, sulfoalkanoyl, alkyl sulfonylalkanoyl, and alkylphosphonoalkanoyl; R2 is selected from the group consisting of R3 is hydrido, hydroxyl, isopropenyl, isopropyl, 1′-hydroxyisopropyl, 1′-haloisopropyl, thioisopropyl, 1′-trifluoromethylisopropyl, 2′-hydroxyisopropyl, 2′-haloisopropyl, 2′-thioisopropyl, 2′-trifluoromethylisopropyl, 1′-hydroxyethyl, 1′-(alkoxy)ethyl, 1′-(alkoxyalkoxy)ethyl, 1′-(arylalkoxy)ethyl; 1′-(arylcarbonyloxy)ethyl, acetyl, 1′-(hydroxyl)-1′-(hydroxyalkyl)ethyl, (2′-oxo)tetrahydrooxazolyl, 1′,2′-epoxyisopropyl, 2′-haloisopropenyl, 2′-hydroxyisopropenyl, 2′-aminoisopropenyl, 2′-thioisopropenyl, 3′-haloisopropenyl, 3′-hydroxyisopropenyl, 3′-aminoisopropenyl, 3′-thioisopropenyl, 1′-alkoxyethyl, 1′-hydroxyiminoethyl, 1′-alkoxyiminoethyl, and wherein m2 is 0 to 3; wherein Y2 is —SR33 or —NR33R34; R32 is hydrido or hydroxy; R33 and R34 are independently selected from the group consisting of hydrido, alkyl, alkanoyl, arylalkyl, heteroarylalkyl, arylsulfonyl and arylaminocarbonyl; or R33 and R34 taken together with the nitrogen to which they are attached form a heterocycle, wherein the heterocycle optionally includes one or more heteroatoms selected from the group consisting of nitrogen, sulfur and oxygen; R4 is hydrido; or R3 and R4 are taken together to form a radical selected from the group consisting of oxo, alkylimino, alkoxyimino and benzyloxyimino; R7 and R8 are independently selected from the group consisting of hydrido, alkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, carboxyalkyl, alkoxyalkyl, alkoxyalkoxyalkyl, alkoxycarbonylaminoalkoxyalkyl, alkoxycarbonylaminoalkyl, aminoalkoxyalkyl, alkylcarbonylaminoalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, arylcarbonylaminoalkyl, alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, heterocyclylsulfonyl, and cycloalkyl, or R7 and R8 together with the nitrogen atom to which they are attached form a heterocyclyl or heteroaryl group, wherein the heterocyclyl or heteroaryl optionally includes one or more additional heteroatoms selected from the group consisting of nitrogen, sulfur and oxygen; R10 and R11 are independently selected from the group consisting of hydrido, alkyl, amino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, carboxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, hydroxyalkyl, cyanoalkyl, alkoxyalkoxyalkyl, alkoxycarbonylaminoalkoxyalkyl, alkoxycarbonylaminoalkyl, alkoxycarbonylalkyl, hydroxyalkoxyalkyl, aminoalkoxyalkyl, alkylcarbonylaminoalkyl, heterocyclyl, heterocyclylalkyl, aryl, heteroarylalkyl, arylalkyl, arylcarbonylaminoalkyl, alkyl sulfonyl, aryl sulfonyl, alkyl sulfonylaminoalkyl, aryl sulfonylaminoalkyl, cycloalkyl, and alkyl interrupted by one or more oxygen atoms, or R10 and R11 together with the nitrogen atom to which they are attached form a heterocyclyl group, wherein the heterocyclyl optionally includes one or more additional heteroatoms selected from the group consisting of nitrogen, sulfur and oxygen; R15 and R16 are independently selected from the group consisting of hydrido, alkyl, alkoxycarbonyl, alkoxyaminoalkyl, cyclooxoalkyl, cycloalkylcarbonyl, heterocyclylaminoalkyl, cycloalkyl, cyanoalkyl, cyano, sulfo, phosphono, sulfoalkyl, phosphonoalkyl, alkylsulfonyl, alkylphosphono, alkoxyalkyl, and heterocyclylalkyl, or R15 and R16 together with the nitrogen atom to which they are attached form a heterocyclyl group, wherein the heterocyclyl optionally includes one or more additional heteroatoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, or R15 and R16 together with the nitrogen atom to which they are attached form an alkylazo group; R17 is selected from the group consisting of hydrido, alkyl, perhaloalkyl, alkoxy, alkenyl, carboxyalkyl, amino, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkoxyalkyl, alkoxycarbonyl, cyanoalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, alkanoylaminoalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, heterocyclylcarbonylalkyl, cycloalkylcarbonylalkyl, heteroarylalkylaminocarbonylalkyl, arylalkylaminocarbonylalkyl, heterocyclylalkylaminocarbonylalkyl, carboxyalkylaminocarbonylalkyl, aryl sulfonylaminocarbonylalkyl, alkyl sulfonylaminocarbonylalkyl, and hydroxyiminoaminoalkyl; and R20 is selected from the group consisting of hydrido, C1-C6 alkyl, and aryl; R21, R22, R23, R24, R25, R26, R27, R28, R29, and R31 are independently selected from the group consisting of hydrido, halo, C1-C6 alkyl, hydroxyl, alkoxy, carboxy, amino, azido, monoalkylamino, dialkylamino, cyano, acetyl, acetamido, C3-C7 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, aryl, and heteroaryl; R35 and R36, are radicals independently selected from the group consisting of hydrido, chloro, bromo, fluoro, iodo, hydroxyl, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, C1-C6 alkoxy, and amino; or R35 and R36 are taken together to form a carbonyl; R37 and R38 are radicals independently selected from the group consisting of hydrido, chloro, bromo, fluoro, iodo, hydroxyl, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, C1-C6 alkoxy, and amino; or where R37 and R38 are taken together to form a carbonyl; R39 is a radical selected from the group consisting of hydrido, chloro, bromo, fluoro, iodo, hydroxyl, alkyl, alkanoyl, alkylsulfonyl, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, C1-C6 alkoxy, and amino; wherein any hydrido of Y, R1, R2, R3, R4, R7, R8, R10, R11, R15, R16, R17, R20, R32, R33, R34, R35, R36, R37, R38, or R39 is independently, optionally replaced with one or more moieties selected from the group consisting of halo, C1-C6 alkyl, hydroxyl, alkoxy, carboxy, amino, azido, monoalkylamino, dialkylamino, cyano, acetyl, acetamido, C3-C7 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, aryl, and heteroaryl; and R41 and R42 are independently selected from the group consisting of hydrido, alkyl, and alkenyl; with the proviso that when q is 1 then R4 is alkyl or alkenyl, R41 and R42 are hydrido, the bond between carbons 12 and 13 is fully saturated; and the bond between carbons 18 and 19 is fully saturated; with the proviso that when q is 2 and the bond between carbons 12 and 13 is unsaturated then R4 and R41 are methyl, R42 is hydrido, and the bond between carbons 18 and 19 is fully saturated; with the proviso that when q is 2 and either the bond between carbons 18 and 19 is unsaturated or the bond between carbons 12 and 13 is unsaturated; then R4 is hydrido, and; R41 and R42 are methyl; and, with the proviso that when there is an unsaturation between carbons 18 and 19 then R4 is not present. |
