| 主权项 |
1. A compound of Formula I: wherein: when b represents a double bond, D represents —CH2— or Q, Ra and Rb are both not present; when b represents a single bond, D represents —C(O)—, —CH2— or Q, Ra and Rb are either both H or both —OH; G represents 0 or a direct bond; Q represents a structural fragment of formula Ig or Ih, where either (i) R1 represents —(CH2)a—C(R3)═C(R4)—(CH2)v—X, or —(CH2)w—C≡C—(CH2)x—X; the sum of w and x is from 2 to 10; the sum of u and v is from 2 to 6; X represents —C(O)-L1, —OH, —CN, —SH, —NHR3a, halo, phosphoramidityl, N-hydroxy succinimidyl ester, sulfo-N-hydroxy succinimidyl ester, fluorophenyl esters, isothiocyanato, iodoacetamidyl, maleimidyl, aryl or hetroaryl which latter two groups are substituted by one or more groups selected from —C(O)-L1, —OH, a sulfonyl ester, —NO2, —CHO, —N3, —CN, —SH, —NHR3a, halo, phosphoramidityl, N-hydroxy succinimidyl ester, sulfo-N-hydroxy succinimidyl ester, fluorophenyl esters, isothiocyanato, iodoacetamidyl and maleimidyl; L1 represents —OH or —O—C(O)—R5, or —C(O)-L1 represents a carboxylic acid functional group activated by a carbodiimide; R2 represents alkyl, cycloalkyl, alkylenyl, alkynyl, aryl, benzyl, heteroaryl wherein the latter three groups are substituted by one or more groups selected from —OH, —NH2 or a C1 to C6 alkyl substituted by one or more halo atoms independently substituted by one or more linear or branched oligo or poly-ethyleneoxy groups wherein the total number of oligo or poly-ethyleneoxy groups is from 2 to 100, or R2 represents —NR6(R7) or —N(R6a)—(CH2)—SO3−E+; R3 to R5 and R3a independently represent C1 to C6 alkyl or C1 to C6 alkyl substituted by one of more groups selected from —OH and halo R6 and R7 independently represent —(CH2)z—NR8(R9) or —(CH2)z—N+R8(R9)(R10)A−, provided that at least one of R6 and R7 is not H; R6a represents H or C1 to C3 alkyl or C1 to C3 substituted by one or more groups selected from —OH or halo; z represents 1 to 10; R8 to R10 independently represents H, alkyl or alkenyl or either alkylor alkenyl substituted by one or more groups selected from —OH and halo; A− represents I−, Cl− or Br−; and E+ represents a cationic group; (ii) R1 represents a structural fragment of formula Ia, Ib, Ic, Id, Ie, If: wherein the dashed lines indicate the point of attachment to the rest of the molecule, or R1 represents —(CH2)t—Z, —(CH2)u—C(R3)═C(R4)—(CH2)v—Z, or —(CH2)w—C≡C—(CH2)x—Z; R11 represents H, alkyl, alkyl substituted by one or more groups selected from —OH, halo or linear or branched ethyleneoxy groups wherein the total number of oligo or poly-ethyleneoxy groups is from 2 to 100; R12 to R14 independently represent H or C1 to C6 alkyl or C1 to C6 alkyl substituted by one or more groups selected from —OH, halo and linear or branched ethyleneoxy groups wherein the total number of oligo or poly-ethyleneoxy groups is from 2 to 100; r represents I−, Cl−, or Br−; t represents 1 to 20; the sum of w and x is from 2 to 6; the sum of u and v is from 2 to 15; Z represents —C(O)O−E+, —SO3−E+, a quarternary ammonium salt, a structural fragment of formulae Ia to If, or Z represents aryl, benzyl, heteroaryl (wherein the latter three groups may be substituted by one or more groups selected from —OH, —NH2 or a C1 to C6 alkyl substituted by one or more halo atoms) substituted by one or more —C(O)O−E+ groups, —SO3−E+ groups, a quarternary ammonium salt, a pyridinium ion or linear or branched oligo or poly-ethyleneoxy groups wherein the total number of oligo or poly-ethyleneoxy groups is from 2 to 100; E+ represents a cationic group; R2 represents —C(O)-L3, phosphoramidityl, N-hydroxy succinimidyl ester, sulfo-N-hydroxy succinimidyl ester, fluorophenyl esters, isothiocyanato, iodoacetamidyl, maleimidyl; L3 represents —OH or —O—C(O)—R15, halo, an activated ester such as 1-oxybenzotriazoyl or an aryloxy group optionally substituted with one or more subsistent selected from nitro, fluoro, chloro, cyano and trifluoromethyl, and R15 represents C1 to C6 alkyl or C1 to C6 alkyl substituted by one or more groups selected from —OH and halo; or a pharmaceutically-acceptable salt or solvate thereof. |
