US 8,344,007 B2Granted

Water-soluble polymer-based cantharimides as potentially selective anti-tumor agents

AssigneeThe Hong Kong Polytechnic University

InventorsJohnny Cheuk-on Tang, Albert Sun-chi Chan, Kim-hung Lam, Chung-hin Chui, Stanton Hon Lung Kok, Marcus Chun Wah Yuen, Sau Hing Chan, Chor Hing Cheng, Filly Cheung

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Abstract

A cantharimide compound may include the backbone of formula (1). R1, R2, R3, and R4 may be independently selected from the group consisting of H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O)R10, N—R11R12, O—R13, S—R14, P(O)(OR15)(OR16), As(O)(OR17)(OR18), SO2R19, SO3R20, and B(OR21). X1 to X4 may be independently selected from the group consisting of nitrogen and carbon, such that X1 to X4 are not all hydrogen. Y1, Y2 and R5 to R21 may be independently selected from the group consisting of hydrogen, C1-12-alkyl, -aryl, heteroaryl, and a bioactive polymer.

Claims19

Dependent claims

A cantharimide compound, comprising the background of formula (1):

wherein, R1, R2, R3, and R4 are independently selected from the group consisting of H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O)R10, N—R11R12, O—R13, S—R14, P(O)(OR15)(OR16), As(O)(OR17)(OR18), SO2R19, SO3R20, and B(OR21),
wherein the R1 to R4 are not all hydrogen with the proviso that R3 is not hydrogen;
wherein the X1 to X4 are carbon;
and
wherein the Y1, Y2 and R5 to R21 are independently selected from the group consisting of hydrogen, C1-12-alkyl, aryl, heteroaryl, and a bioactive polymer comprising:
(i) a polymer moiety from 2 to 300 monomer units;
and
(ii) a terminal moiety connected to the polymer moiety at the ω-position, provided that the cantharimide compound is neither
and a pharmaceutically acceptable salt, solvate or hydrate thereof.

6 more elements

Dependencies are inferred from the claim text.