Method of preparing dendritic drugs

摘要

Synthetic design of drug-incorporated novel dendrimer structures for quantitatively controlled drug delivery. The dendritic drugs have better control and thus a quantitative drug release can be obtained. There are no prior art dendritic drugs that control release both sequentially and quantitatively like the dendritic drugs disclosed herein. The dendritic drugs are formed by incorporating multiple same type drug units or more than two different drug types into a dendritic cascade structure to form a dendrimer drug.

主权项

1. A method of preparing a dendritic drug, the method comprising:
(I) providing a therapeutically active multifunctional drug, said drug having at least one reactive group capable of providing a linker site, said drug having at least one functional group capable of providing a starting point for the preparation of a dendritic structure; (II) chemically protecting any reactive group in the drug that is not capable of providing a linker site or providing a starting point for the preparation of a dendritic molecule; (III) chemically protecting any reactive groups capable of providing a linker site; (IV) chemically protecting any functional group capable of providing a starting point for the preparation of a dendritic molecule; (V) deprotecting any group formed in (III); (VI) reacting any group formed in (V) with a first linker group selected from the group consisting of:
(i) biologically compatible compounds,(ii) biologically inactive compounds,(iii) biologically active compounds,(iv) biologically compatible and bioactive compounds,(v) biologically compatible and biologically inactive compounds; (VII) reacting the first linker from (VI) with a second linker group selected from the group consisting of:
(i) biologically compatible compounds,(ii) biologically inactive compounds,(iii) biologically active compounds,(iv) biologically compatible and bioactive compounds,(v) biologically compatible and biologically inactive compounds; (VIII) coupling two units formed in (VI) through the first linker groups; (IX) deprotecting the groups formed in (IV) to yield a core molecule for the dendritic drug; (X) reacting a predetermined amount of the molecules formed in (VI) with each one equivalent of the molecule formed in (VIII), and deprotecting the protected groups formed in (IV); (XI) deprotecting any group in the molecule that is not capable of providing a linker site or providing a starting point for the preparation of a dendritic molecule to give a first generation dendritic drug.