Zentiva K.s.

Ustav Makromolekularni Chemie Av Cr, V.v.i.

Mikrobiologicky Ustav Av Cr, V.v.i.

Petr Chytil

Karel Ulbrich

Blanka Rihova

Tomas Etrych

Jiri Strohalm

Tomas Mrkvan

Martin Studenovsky

Michal Pechar

The present invention relates to water-soluble high-molecular-weight polymer drug carriers and their conjugates with drugs, derived from dendrimers of the amidoamine and 2,2-bis(hydroxymethyl)propanoic types, the amino and hydroxy end groups of which are attached to semitelechelic copolymers of N-(2 hydroxypropyl)methacrylamide (HPMA) through biodegradable spacers. The polymer carriers and conjugates enable targeted transport notably of anticancer drugs into solid tumors in which biodegradation, the associated controlled drug release and subsequent elimination of polymer carrier from the organism are provided. The polymer carrier conjugated with a cancerostatic for use in targeted therapy of human tumors.

Dendritic high-molecular-weight polymer drug carriers and their conjugates with drugs especially for treatment of solid tumours

A polymeric drug, in which a cancerostatic connected via spacers containing hydrolytically cleavable hydrazone bonds is bound to a water-soluble polymeric carrier prepared on the basis of a N-(2-hydroxypropyl)methacrylamide copolymer, wherein the structure of the polymeric drug consists of the main chain of N-(2-hydroxypropyl)methacrylamide carrying the cancerostatic and another chain of N-(2-hydroxypropyl)methacrylamide&#x2014;a graft, which may also carry a cancerostatic, said grafts being bound to the main chain by a bond that is stable in the body and/or by a bond cleavable in the body, especially by an oligopeptide spacer selected from the series of GlyLeuGly (SEQ ID. NO. 1), GlyPheGly (SEQ ID. NO. 2), GlyPheLeuGly (SEQ ID. NO. 3) and GlyLeuPheGly (SEQ ID. NO. 4), and a method of its preparation.

Grafted macromolecular conjugates of doxorubicin with anticancer activity and method of their preparation

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Kladno, Czechia

Petr Chytil