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, heteroarylalkanoyl, heterocyclylalkanoyl, heterocycylcarbonylalkanoyl, heteroarylaminocarbonylalkanoyl, heterocyclylaminocarbonylalkanoyl, cyanoaminocarbonylalkanoyl, alkylsulfonylaminocarbonylalkanoyl, arylsulfonylaminocarbonylalkanoyl, sulfoaminocarbonylalkanoyl, phosphonoaminocarbonylalkanoyl, phosphono, sulfo, phosphonoalkanoyl, sulfoalkanoyl, alkylsulfonylalkanoyl, and alkylphosphonoalkanoyl; R2 is selected from the group consisting of formyl, carboxyalkenyl, heteroaryl, CH2SR14, CH2SOR14, CH2SO2R14, R3 is hydrido, hydroxyl, isopropenyl, isopropyl, 1′-hydroxyisopropyl, 1′-haloisopropyl, 1′-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, 3′-haloisopropenyl, 3′-hydroxyisopropenyl, 3′-aminoisopropenyl, 3′-thioisopropenyl, 1′-alkoxyethyl, 1′-hydroxyiminoethyl, and 1′-alkoxyiminoethyl; 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; R5 is selected from the group consisting of C2-C20 alkyl, alkenyl, alkynyl, carboxy(C2-C20)alkyl, amino, aminoalkyl, dialkylamino, monoalkylaminoalkyl, dialkylaminoalkyl, alkoxyalkyl, cyanoalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, sulfo, phosphono, sulfoalkyl, phosphonoalkyl, alkylsulfonyl, alkylphosphono, alkanoylaminoalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, heterocyclylcarbonylalkyl, cycloalkycarbonylalkyl, heteroarylalkylaminocarbonyalkyl, arylalkylaninocarbonylalkyl, heterocyclylalkylaminocarbonylalkyl, carboxyalkylaminocarbonylalkyl, arylsulfonylaminocarbonylalkyl, alkylsulfonylaminocarbonylalkyl, arylphosphonoaminocarbonylalkyl, alkylphosphonoaminocarbonylalkyl, and hydroxyimrinoaminoalkyl; R6 is selected from the group consisting of hydrido, phosphono, sulfo, alkyl, sulfoalkyl, phosphonoalkyl, alkylsulfonyl, alkylphosphono, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl; CH2CONR7R8, trialkylsilyl, ethoxyethyl, and tetrahydropyranyl ether; R6 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, heteroarlsulfonyl, heterocyclylsulfonyl, and cycloalkyl, or R.sub.7 and R.sub.8 can together with the nitrogen atom to which they are attached form a heterocyclyl or heteroaryl group, wherein the heterocyclyl or heteroaryl can optionally include one or more heteroatoms selected from the group consisting of nitrogen, sulfur and oxygen; R9 is selected from the group consisting of hydrido, phosphono, sulfo, alkyl, alkenyl, trialkylsilyl, cycloalkyl, carboxyalkyl, alkoxycarbonloxyalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkoxyalkyl, cyanoalkyl, phosphonoalkyl, sulfoalkyl, alkylsulfonyl, alkylphosphono, aryl, heteroaryl, heterocyclyl, arylalkyl, heteroarylalkyl, heterocyclyalkyl, and dialkoxyalkyl; R12 and R13 independently selected from the group consisting of hydrido, alkyl, alkenyl, alkylamino, alkynyl, alkoxy, alkoxycarbonyl, alkoxyaminoalkyl, cycloalkyloxo, heterocyclylaminoalkyl, cycloalkyl, cyanoalkyl, cyano, sulfo, phosphono, sulfoalkyl, phosphonoalkyl, alkylsulfonyl, alkylphosphono, alkoxyalkyl, heteroaryl, heteroarylalkyl, dialkylaminoalkyl, and heterocyclylalkyl, or R12 and R13 can together with the nitrogen atom to which they are attached form a heterocyclyl group or a heteroaryl group, wherein the heterocyclyl or heteroaryl can optionally include one or more additional heteroatoms selected from the group consisting of nitrogen, sulfur and oxygen, or R12 and R13 can together with the nitrogen atom to which they are attached form an alkylazo group, and d is one to six; R14 is selected from the group consisting of hydrido, alkyl, alkenyl, arylalkyl, carboxyalkyl, carboxyalkenyl, alkoxycarbonylalkyl, alkenyloxycarbonylalkyl, cyanoalkyl, hydroxyalkyl, carboxybenzyl, and aminocarbonylalkyl; R18 and R19 are independently selected from the group consisting of hydrido, methyl and ethyl; d is one to six; and 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, R5, R6, R7, R8, R9, R12, R13, R18, R19, 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, amiino, azido, monoalkylamino, dialkylamino, cyano, acetyl, acetamido, C3-C7 cycloalkyl, C2-6 alkenyl, C2-C6 alkynl aryl, and heteroaryl; and R41 and R42 are independently selected from the group consisting of hydrido, alkyl, and alkenyl; with the proviso that when there is an unsaturation between carbons 18 and 19 then R4 is not present. |