US 9,434,822 B2 · Block copolymer, micelle preparation, and anticancer agent containing the same as active ingredient

Abstract

A medicinal preparation is desired which has no harmful side effects such as hypersensitive reaction, heightens the water solubility of a sparingly water-soluble anticancer agent, maintains a high drug concentration in the blood, accumulates a drug in a tumor tissue at a high concentration, heightens the pharmacological effect of the sparingly water-soluble anticancer agent, and diminishes the side effects of the anticancer agent. Provided are: a novel block copolymer which can be a drug carrier having no harmful side effects such as hypersensitive reaction; a micelle preparation in which micelles are formed and which contains a sparingly water-soluble anticancer agent, especially paclitaxel, incorporated in the micelles in an amount necessary for a disease treatment without bonding it to the block copolymer and which can heighten the solubility of the drug in water; and an anticancer agent which comprises the micelle preparation as a medical ingredient, maintains a high concentration in the blood, has more potent drug activity, and is reduced in toxicity.

Claims8

Dependent claims

A block copolymer represented by the following general formula (3):

wherein R1 represents a hydrogen atom or a (C1 to C5) alkyl group, R2 represents a (C1 to C5) alkylene group, R3 represents a methylene group or an ethylene group, R4 represents a hydrogen atom or a (C1 to C4) acyl group, R5 represents a hydroxyl group, an optionally substituted aryl (C1 to C8) alkoxy group or —N(R6)-CO—NHR7, R6 and R7 may be the same or different and each represents a (C3 to C6) cyclic alkyl group or a (C1 to C5) alkyl group optionally substituted with a tertiary amino group;
n represents 5 to 1000, m represents 2 to 300, x′ represents 0 to 300 and y′ represents 0 to 300, provided that the sum of x′ and y′ is 1 or and less than m;
and R5 is a hydroxyl group at a ratio 0% relative to m, an optionally substituted aryl (C1 to C8) alkoxy group at a ratio of 10-80% relative to m, and —N(R6)-CO—NHR7 at a ratio of 11-30% relative to m.

Dependencies are inferred from the claim text.

Block copolymer, micelle preparation, and anticancer agent containing the same as active ingredient

Life of this patent

Block copolymer, micelle preparation, and anticancer agent containing the same as active ingredient

Life of this patent

Abstract

Claims8