Anionic or cationic dendrimer antimicrobial or antiparasitic compositions

• US 20030129158A1
• Filed: 08/26/2002
• Published: 07/10/2003
• Est. Priority Date: 09/14/1998
• Status: Active Grant

• Current Assignee: Starpharma Pty Ltd. (Starpharma Holdings Ltd.)
• Original Assignee: Starpharma Pty Ltd. (Starpharma Holdings Ltd.)
• Inventors: Matthews, Barry Ross, Holan, George
• Granted Patent: US 7,572,459 B2
• Time in Patent Office: Days
• US Class Current: 424/78.17
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

To inhibit, prophylactically or therapeutically, a bacterial, yeast, fungal, or parasitic agent in a patient, an effective amount of a dendrimer is administered to the patient, which dendrimer has a plurality of terminal groups, at least one of which has an anionic- or cationic-moiety covalently bonded or linked thereto. The anionic-containing moiety is not a disaccharide or oligosaccharide moiety, and, where the anionic-containing moiety is a neuraminic- or sialic acid-containing moiety, it is modified in the 4-position by substitution with an amino, amido, cyano, azido or guanido group, or is unsaturated.

Claims

1. A method of treatment or prevention of a parasitic infection in a human or non-human animal patient, which comprises administration to the patient of an effective amount of a dendrimer having a plurality of terminal groups wherein at least one of said terminal groups has an anionic- or cationic-containing moiety covalently bonded or linked thereto.

2. A method according to claim 1, wherein said compound is a dendrimer which comprises a polyvalent core covalently bonded to at least two dendritic branches, and extends through at least two generations.

3. A method according to claim 2 wherein said dendrimer is a polyamidoamine dendrimer based on an ammonia core.

4. A method according to claim 2 wherein said dendrimer is a polyamidoamine dendrimer based on an ethylene diamine core.

5. A method according to claim 2 wherein said dendrimer is a polylysine dendrimer based on a benzhydrylamine or other suitable core.

6. A method according to claim 2 wherein said dendrimer is a poly(propyleneimine) dendrimer.

7. A method according to claim 2 wherein said compound is a polyionic dendriner of the general formula I:

8. A method according to any of claim 1 wherein in said compound said anionic- or cationic-containing moiety or moieties are bonded to amine, sulfhydryl, hydroxy or other reactive terminal groups of the dendrimer by amide, thiourea, urea, amide, alkylamine, ether, thioether, carbamate, ester, or other suitable linkages.

9. A method according to claim 1, wherein in said compound said anionic- or cationic-containing moieties are selected from the group consisting of sulfonic acid-containing moieties, carboxylic acid-containing moieties (including neuraminic and sialic acid-containing moieties and modified neuraminic and sialic acid-containing moieties), boronic acid-containing moieties, phosphoric and phosphonic acid-containing moieties (including esterified phosphoric and phosphonic acid-containing moieties), primary, secondary, tertiary or quaternary amino-containing moieties, pyridinium-containing moieties, guanidinium-containing moieties, amidinium-containing moieties, phenol-containing moieties, heterocycles possessing acidic or basic hydrogens, and zwitterionic-containing moieties.

10. A method according to claim 1, wherein in said compound the moiety or moieties which are bonded to amino or other reactive terminal groups of the dendrimer are selected from the following groups, in which n is zero or an integer of from 1 to 20:

12. A method according to claim 1, wherein said treatment comprises inhibition of parasitic pathogens.

13. A method according to claim 12, wherein said treatment comprises inhibition of internal parasitic pathogens.

14. A method according to claim 13, wherein said treatment comprises inhibition of parasitic worms.

15. A method according to claim 14, said parasitic worms are selected from the group consisting of nematodes, trematodes and cestodes.