Therapeutic and imaging compositions and uses thereof

Patent metadata

Field	Value
Publication number	US-10689462-B2
Application number	US-201815978872-A
Country	US
Kind code	B2
Filing date	May 14, 2018
Priority date	May 7, 2013
Publication date	Jun 23, 2020
Grant date	Jun 23, 2020

Abstract

Various embodiments of the present invention are directed to polyrotaxanes comprising a poloxamer core and at least one cyclodextrin and methods for treating Niemann-Pick type C (NPC) and imaging (e.g., MRI) using the polyrotaxanes various embodiments of the present invention.

First claim

What is claimed is:

1. A polyrotaxane comprising the general formula:

or a salt thereof,
wherein:
n is an integer from 1 to 30;
C and C′ are the same or different and represent endcapping groups of the formula:

wherein:
L 1 is a (C 1 -C 6 )hydrocarbylene group,
G 1 and G 2 , together, form a radical having the formula:

wherein each L 2 is independently a bond or acyl; each G 3 is a substituted or unsubstituted (C 6 -C 50 )hydrocarbyl group, interrupted by 0 to 5 groups chosen from —O—, —NH—, and —S—; and
each s is independently an integer from 1 to 5; and
t is an integer from 2 to 5:
B is a poly(ethylene glycol)-poly(propylene glycol)-poly(ethylene glycol) (PEG-PPG-PEG) triblock copolymer; and
A is a beta cyclodextrin;
wherein G 3 is not a substituted or unsubstituted (C 6 -C 12 )aryl group.

2. The polyrotaxane of claim 1 , wherein G 3 is a substituted or unsubstituted —O—(C 6 -C 50 )alkyl group.

3. The polyrotaxane of claim 1 , wherein G 3 is a cholesteryl group.

4. The polyrotaxane of claim 1 , wherein n is an integer from 5 to 15.

5. The polyrotaxane of claim 1 , wherein n is an integer from 3 to 11.

6. A pharmaceutical composition comprising the polyrotaxane of claim 1 and a pharmaceutically acceptable carrier.

7. The polyrotaxane of claim 1 , wherein the poly(ethylene glycol)-poly(propylene glycol)-poly(ethylene glycol) (PEG-PPG-PEG) triblock copolymer has the formula:

wherein each R 5 is methyl; d is an integer from about 100 to about 800; and q is an integer from about 100 to about 800.

8. The polyrotaxane of claim 7 , wherein d+q is from about 100 to about 800.

Assignees

• Purdue Research Foundation

Inventors

• Thompson David H
• Kulkarni Aditya
• Collins Christopher
• Mondjinou Yawo

Classifications

• C08L71/02

  Polyalkylene oxides · CPC title

• A61K51/065

  conjugates with carriers being macromolecules · CPC title

• A61K49/126

  Linear polymers, e.g. dextran, inulin, PEG · CPC title

• A61K49/085

  conjugated systems · CPC title

• C08L5/16

  Cyclodextrin; Derivatives thereof · CPC title