High-molecular weight conjugate of combretastatins

Details High-molecular weight conjugate of combretastatins High-molecular weight conjugate of combretastatins

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61P 9/00 (2006.01) A61P 35/00 (2006.01) C08G 81/00 (2006.01)

Patent

CA 2658100

A novel derivative of a combretastatin which has water solubility and is capable of releasing a drug independent of biological enzymes in which individual differences are likely caused and whose effective therapeutic effect can be expected has been demanded.A polymer conjugate of a combretastatin, characterized by having a structure in which a hydroxy group of a combretastatin is linked via an ester bond to a carboxylic acid group of the following polymer moiety in a block copolymer of a polyethylene glycol structure moiety with a polymer moiety having two of more carboxylic acid groups such as polyaspartic acid or polyglutamic acid is provided.

La présente invention concerne un dérivé innovant d'une combrétastatine qui est soluble dans l'eau et qui est capable de libérer, indépendamment des enzymes biologiques dans lesquelles des différences individuelles existent vraisemblablement, un médicament dont on peut attendre un effet thérapeutique efficace. L'invention concerne un conjugué polymère d'une combrétastatine, caractérisé par une structure dans laquelle un groupe hydroxyle d'une combrétastatine est lié par une liaison ester à un groupe acide carboxylique du fragment de polymère suivant dans un copolymère séquencé d'un fragment à structure de polyéthylène glycol avec un fragment polymère ayant deux ou plusieurs groupes acide carboxylique tels qu'un acide polyaspartique ou un acide polyglutamique.

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