N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides

Patent metadata

Field	Value
Publication number	US-9616136-B2
Application number	US-201514951105-A
Country	US
Kind code	B2
Filing date	Nov 24, 2015
Priority date	Oct 15, 2010
Publication date	Apr 11, 2017
Grant date	Apr 11, 2017

Abstract

The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.

First claim

What is claimed is:

1. A method comprising administering to a mammal a compound having the following structure:

wherein:
Ar is aryl, optionally substituted with halo;
R 1 is lower alkyl;
the dotted line (“---”) represents a covalent bond;
X 1 is a spacer moiety; and
POLY 1 is a poly(alkylene oxide),

and pharmaceutically acceptable salts thereof.

2. The method of claim 1 , wherein the compound is encompassed within the formula:

wherein:
Ar is aryl, optionally substituted with halo;
R 1 is lower alkyl;
X 1 is a spacer moiety; and
POLY 1 is a poly(alkylene oxide),

and pharmaceutically acceptable salts thereof.

3. The method of claim 1 , wherein the compound is encompassed within the formula:

wherein:
Ar is aryl, optionally substituted with halo;
R 1 is lower alkyl;
X 1 is a spacer moiety; and
POLY 1 is a poly(alkylene oxide),

and pharmaceutically acceptable salts thereof.

4. The method of claim 1 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).

5. The method of any one of claims 1 , 3 and 4 , wherein the poly(alkylene oxide) has from about 2 to about 30 monomers.

6. The method of claim 5 , wherein the poly(alkylene oxide) has from about 2 to about 10 monomers.

7. The method of claim 1 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.

8. A method comprising administering to a mammal a compound selected from the group consisting of (2R) N-benzyl-2-carboxy mPEG 1 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 2 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 3 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 4 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 5 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 6 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 7 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 8 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 9 amino-3-methoxy propionamide, and pharmaceutically acceptable salts of each of the foregoing.

Assignees

• Nektar Therapeutics

Inventors

• Riggs-Sauthier Jennifer
• Zhang Wen

Classifications

• A61K47/60 Primary

  the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol · CPC title

• A61K31/165

  having aromatic rings, e.g. colchicine, atenolol, progabide · CPC title

• C07D235/22 Primary

  with hetero atoms directly attached to ring nitrogen atoms (C07D235/10 takes precedence) · CPC title

• A61P25/08

  Antiepileptics; Anticonvulsants · CPC title

• A61K47/48215 Primary

  Human Necessities · mapped topic