| 主权项 |
1. A compound of formula (I): wherein: R1 is H or glycosyl, provided that if R1 is glycosyl then R2 and R3 are both OH and R4 is CH2OH; R2 is selected from the group consisting of H, OH, F and OR10, provided that if R2 is H, F or OR10, then R1 is H, R3 is OH and R4 is CH2OH; R3 is selected from the group consisting of H, OH, F and OR10; provided that if R3 is H, F or OR10, then R1 is H, R2 is OH and R4 is CH2OH; R4 is CH3, CH2OH, CH2OCOR11, CH2OR10, CH2OR11, CH2OS03H, CH2SH, CH2SR11, CH2SOR11, CH2S02R11, CH2P03H2, CH2OP(0)(OH)2, CH2OP(0)(OH)(OR11), CH2OP(0)(OR11)2, CO211, CH2NHCOR11, CH2NHC02R11, CH2NHCONH2, CH2NHCONHR11, CH2NHCON(R11)2, CH2N(R11)2, CH2NHSO2R11; provided that if R4 is other than CH2OH, then R1 is H and R2 and R3 are OH; R5 is 11; or R5 is a radical of formula (i): wherein Y is a radical of formula: each E1, the same or different, is independently selected from the group consisting of H, alkyl, alkoxy, halogen, nitroaryl; or, together with the ring to which it is attached, forms a fused bicyclic aryl group; p is an integer from 1 to 4; t is an integer from 1 to 2; Alk1 is C1-C4 straight chain alkyl; wherein when Y is a radical of formula (a) or (b) then Z is: or wherein when Y is a radical of formula (c), (d), (e), or (j) then Z is: u is 1 or 2; each A1, the same or different, is independently selected from the group consisting of: alkyl which may be optionally substituted with one or more substituents selected from the group consisting of (OCH2CH2)mOMe, NHC(O)OR14 alkoxyimino, oxo, halogen, alkoxy, NHCOCH2(OCH2CH2)mOMe, alkenyl which may be optionally substituted with one or more substituents selected from the group consisting of (OCH2CH2)mOMe, alkoxyimino, oxo, halogen and alkoxy; aryl which may be optionally substituted with one or more substituents selected from the group consisting of (OCH2CH2)mOMe, alkyl, alkoxy, dialkylamino, nitro, halogen; or aralkyl which may be optionally substituted with one or more substituents selected from the group consisting of (OCH2CH2)mOMe, alkoxyimino, oxo, halogen, alkyl, alkoxy, dialkylamino and nitro; m is an integer from 10 to 1500; E2 and A2 are each independently selected from H and A1; A4 is selected from the group consisting of H, methyl, CH2CH2CH2NHC(═NH)NH2, CH2C(═O)NH2, CH2C(═O)OH, CH2SH, CH2CH2C(═O)OH, CH2CH2C(═O)NH2, CH2(CH2)3NH2, CH2CH2SCH3, CH2OH, or A4, together with the carbon to which it is attached and the nitrogen adjacent to that carbon, forms a pyrrolidine ring; A5 is H or benzyloxycarbonyl; R6 is OR12, OH or H; R7 is OR12, OH or H; provided that at least one of R6 and R7 is OR12; wherein when R6 is OR12, R7 is H, R8 is Ci.Ci5 alkyl and X is O, then denotes an optional double bond linking the carbon adjacent to R7 with the carbon adjacent to R8; R8 is H or C1-C15 alkyl having a straight or branched carbon chain, wherein the carbon chain optionally incorporates one or more double bonds, one or more triple bonds, one or more oxygen atoms and/or a terminal or non-terminal optionally substituted aryl group; R10 is glycosyl; R11 is lower alkyl, lower alkenyl or aralkyl; R12 is C6-C30 acyl having a straight or branched carbon chain optionally substituted with one or more hydroxy groups at positions 2 and/or 3 of the acyl group and/or an optionally substituted chain terminating aryl group and which optionally incorporates one or more double bonds, one or more triple bonds, and/or one or more optionally substituted arylene groups and wherein the carbon chain is optionally substituted with one or more deuterium atoms; wherein the optional substituents on the aryl and arylene groups may be selected from halogen, cyano, dialkylamino, C1-C6 amide, nitro, C1-C6 alkoxy, C1-C6 acyloxy and C1-C6 thioalkyl; R14 is an optionally substituted alkyl, aryl or aralkyl group; X is O, CH2 or S; n is 1 when X is O or S; or n is 0 or 1 when X is CH2; wherein where X is CH2 then the following must all be true: the stereochemistry of the 6-membered sugar ring in formula (1) is α-D-galacto; R1 is H; R2 and R3 are both OH; R4 is CH2OH, CH2OR10 or CH2OR11; and: R6 is OH and R7 is OR12 and the stereochemistry at carbon atoms 2, 3 and 4 is (2S, 3S, 4R), (2S, 3S, 4S), (2R, 3S, 4S), (2R, 3S, 4R) or (2S, 3R, 4S); or R6 is OR12 and R7 is H, and R8 is C13H27 and the stereochemistry at carbon atoms 2 and 3 is (2S, 3S); wherein where X is S then the following must all be true: the stereochemistry of the 6-membered sugar ring in formula (I) is α-D-galacto; R1 is H; R2 and R3 are both OH; R4 is CH2OH, CH2OR10, CH2OR11 or C02H; and: R6 is OH and R7 is OR12 and the stereochemistry at carbon atoms 2, 3 and 4 is (2S, 3S, 4R) or R6 is OR12 and R7 is H and the stereochemistry at the carbon atoms 2 and 3 is (2S, 3S); or a pharmaceutically acceptable salt thereof. |
