POLYMER MICELLES CONTAINING SN-38 FOR THE TREATMENT OF CANCER

• US 20100278932A1
• Filed: 05/04/2010
• Published: 11/04/2010
• Est. Priority Date: 05/04/2009
• Status: Abandoned Application

• Current Assignee: Intezyne Technologies
• Original Assignee: Intezyne Technologies
• Inventors: Cardoen, Gregoire, Carie, Adam, Slama, Richard, Skaff, Habib, Sill, Kevin N., Rios-Doria, Jonathan
• Application Number:
  US12/773,702
• Publication Number:
  US 20100278932A1
• Time in Patent Office: Days
• US Class Current: 424/501
• CPC Class Codes: A61K 31/4375 the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 47/6907 the form being a microemulsion, nanoemulsion or micelle
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C08G 65/329 with organic compounds
• CPC Class Codes: C08G 65/33396 having oxygen in addition to nitrogen
• CPC Class Codes: C08G 69/10 Alpha-amino-carboxylic acids polysuccinimides C08G73/1092
• CPC Class Codes: C08G 69/40 Polyamides containing oxygen in the form of ether groups C08G69/12, C08G69/32 take precedence
• CPC Class Codes: C08G 69/48 Polymers modified by chemical after-treatment
• CPC Class Codes: C08L 2203/02 for biomedical use
• CPC Class Codes: C08L 2205/05 containing polymer components which can react with one another
• CPC Class Codes: C08L 2666/20 Macromolecular compounds having nitrogen in the main chain according to C08L75/00 - C08L79/00; Derivatives thereof
• CPC Class Codes: C08L 71/02 Polyalkylene oxides
• CPC Class Codes: C08L 77/00 Compositions of polyamides obtained by reactions forming a carboxylic amide link in the main chain of polyhydrazides C08L79/06; of polyamideimides or polyamide acids C08L79/08; Compositions of derivatives of such polymers
• CPC Class Codes: C08L 77/04 Polyamides derived from alpha-amino carboxylic acids C08L77/10 takes precedence

Abstract

The present invention provides micelles having SN-38 encapsulated therein.

Claims

1. A micelle, having SN-38 encapsulated therein, comprising a multiblock copolymer of formula I:

2. The micelle according to claim 1 wherein R¹ is —

OCH₃.

3. The micelle according to claim 2 wherein:

n is about 270;

m is 1;

x is about 10;

y is about 20; and

z is about 20.

4. The micelle according to claim 2 wherein:

y is 20±

5 and z is 20±

5.

5. The micelle according to claim 1 wherein, wherein R¹ is —

N₃.

6. The micelle according to claim 5 wherein:

n is about 270;

m is 1;

x is about 10;

y is about 20; and

z is about 20.

7. A crosslinked micelle, having SN-38 encapsulated therein, comprising a crosslinked multiblock polymer of formula X:

8. The micelle according to claim 7 wherein R^1a and R^1b are simultaneously —

OCH₃.

9. The micelle according to claim 8 wherein:

n is about 270;

m is 1;

x is about 10;

y is about 20; and

z is about 20.

10. The micelle according to claim 7 wherein R^1a and R^1b are simultaneously —

N₃.

11. The micelle according to claim 10 wherein:

n is about 270;

m is 1;

x is about 10;

y is about 20; and

z is about 20.

12. The micelle according to claim 7 wherein R^1a is —

OCH₃ and R^1b is

13. The micelle according to claim 7, wherein R^1a is —

OCH₃ and R^1b is —

OCH₃.

14. The micelle according to claim 7, wherein R^1a is —

OCH₃ and R^1b is —

N₃.

15. The micelle according to claim 12, wherein T is RGD or Her-2.