| 主权项 |
1. A method for treating sickle cell disease comprising administering to a subject having sickle cell disease an effective amount of a fucose analog selected from the group consisting of one of the following formulae (I) or (II): or a pharmaceutically acceptable salt or solvate form thereof, wherein each of formula (I) or (II) can be the alpha or beta anomer or the corresponding aldose form; each of R1, R2, R2a, R3, R3a and R4 is independently selected from OH, a hydrolyzable ester group, a hydrolyzable ether group, and a small electron withdrawing group; R5 is a member selected from the group consisting of —CH3, —CHX2, —CH2X, —CH(X)—C1-C4 alkyl unsubstituted or substituted with halogen, —CH(X′)—C2-C4 alkene unsubstituted or substituted with halogen, —CH(X′)—C2-C4 alkyne unsubstituted or substituted with halogen, —CH═C(R10)(R11), —C(CH3)═C(R12)(R13), —C(R14)═C═C(R15)(R16), —C3 carbocycle unsubstituted or substituted with methyl or halogen, —CH(X′)—C3 carbocycle unsubstituted or substituted with methyl or halogen, C3 heterocyle unsubstituted or substituted with methyl or halogen, —CH(X′)—C3 heterocycle unsubstituted or substituted with methyl or halogen, —CH2N3, —CH2CH2N3, and benzyloxymethyl, or R5 is a small electron withdrawing group; wherein
R10 is hydrogen or C1-C3 alkyl unsubstituted or substituted with halogen;R11 is C1-C3 alkyl unsubstituted or substituted with halogen;R12 is hydrogen, halogen or C1-C3 alkyl unsubstituted or substituted with halogen; andR13 is hydrogen, or C1-C3 alkyl unsubstituted or substituted with halogen;R14 is hydrogen or methyl;R15 and R16 are independently selected from hydrogen, methyl and halogen;X is halogen; andX′ is halogen or hydrogen; and additionally, each of R1, R2, R2a, R3 and R3a are optionally hydrogen; optionally two R1, R2, R2a, R3 and R4 on adjacent carbon atoms are combined to form a double bond between said adjacent carbon atoms; and provided that at least one of R1, R2, R2a, R3, R3a, R4 and R5 is a small electron withdrawing group, or R5 comprises a halogen, site of unsaturation, carbocycle, heterocycle or azide. |
