Cationic polyphosphazene compound, polyphosphazenes-drug conjugate compound and method for preparing same
AssigneeCnpharm Co., Ltd.
InventorsYoun Soo Sohn, Yong Joo Jun, Prakash Gouda Avaji
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Abstract
The present invention relates to a new class of cationic linear polyphosphazenes bearing as side groups a hydrophilic poly(ethylene glycol) and a spacer group selected from the group consisting of lysine, oligopeptides containing lysine, amino-ethanol, amino-propanol, amino-butanol, amino-pentanol and amino-hexanol, and the polyphosphazene-drug conjugates comprising hydrophobic anticancer drugs by covalent bonding and the preparation methods thereof. The present polyphosphazene-drug conjugates exhibit outstanding tumor selectivity and low toxicity.
Claims8
A method of delivering a drug to a patient or a living object in need thereof, the method comprising:
- administering to the patient or the living object a linear polyphosphazene-drug conjugate compounds represented by the following chemical formula 2:
- wherein, in chemical formula 2, n is an integer from 3 to 300;
- MPEG represents methoxy poly(ethylene glycol);
- S is a spacer group selected from the group consisting of lysine, arginine, glutamine, asparagine, tyrosine, lysine-containing oligopeptide, arginine-containing oligopeptide, glutamine-containing oligopeptide, asparagine-containing oligopeptide, tyrosine-containing oligopeptide, amino-ethanol, amino-propanol, amino-butanol, amino-pentanol, and amino-hexanol;
- D is a hydrophobic molecule as a drug;
- L is a linker to connect the spacer group (S) and the hydrophobic molecule (D), wherein the hydrophobic molecule (D) has at least one functional group of hydroxyl or amine;
- x and y are independently in the range of 0-0.5;
- z is in the range of 0-1;
- and
- x+y+z=1.
A method of delivering a drug to a patient or a living object in need thereof, the method comprising:
- administering to the patient or the living object a linear polyphosphazene-drug conjugate compounds represented by the following chemical formula 2:
- wherein, in chemical formula 2, n is an integer from 3 to 300;
- MPEG represents methoxy poly(ethylene glycol);
- S is a spacer group;
- D is a hydrophobic molecule as a drug;
- L is a linker to connect the spacer group (S) and the hydrophobic molecule (D), wherein the hydrophobic molecule (D) has at least one functional group of hydroxyl or amine;
- x and y are independently in the range of 0-0.5;
- z is in the range of 0-1;
- and
- x+y+z=1, wherein spacer group (S) is aminoethanol or aminopropanol.
Dependencies are inferred from the claim text.