High-molecular weight conjugate of podophyllotoxins

C - Chemistry – Metallurgy – 08 – G

Patent

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Details

C08G 81/00 (2006.01) A61K 31/365 (2006.01) A61K 31/7048 (2006.01) A61K 47/34 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01) C08G 85/00 (2006.01)

Patent

CA 2652656

A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded. A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/ polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin are linked via an ester bond is provided.

La présente invention concerne un nouveau dérivé de podophyllotoxine, qui est capable de libérer un médicament indépendamment d'enzymes biologiques et on peut s'attendre à ce qu'il ait un effet thérapeutique efficace et soit soluble dans l'eau. On propose également un polymère ayant un motif structural polyéthylène-glycol et deux ou plusieurs motifs structuraux monoamide succinique, en particulier un conjugué polymère d'une podophyllotoxine dans lequel un groupe acide carboxylique d'un copolymère polyéthylène-glycol/acide polyaspartique et un groupe hydroxyle de la podophyllotoxine sont liés par l'intermédiaire d'une liaison ester.

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