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

Patent metadata

Field	Value
Publication number	US-9226971-B2
Application number	US-201113879603-A
Country	US
Kind code	B2
Filing date	Oct 14, 2011
Priority date	Oct 15, 2010
Publication date	Jan 5, 2016
Grant date	Jan 5, 2016

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 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 compound of claim 1 , 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 compound of claim 1 , 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 compound of claim 1 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).

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

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

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

8. 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.

9. A composition of matter comprising a compound encompassed within claim 8 or 1 , wherein the compound is present in a dosage form.

10. A composition comprising a compound encompassed within claim 8 or 1 , and optionally, a pharmaceutically acceptable excipient.

Assignees

• Riggs-Sauthier Jennifer
• Zhang Wen
• Nektar Therapeutics

Inventors

• Riggs-Sauthier Jennifer
• Zhang Wen

Classifications

• A61P25/08

  Antiepileptics; Anticonvulsants · CPC title

• 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

• A61K47/48215 Primary

  Human Necessities · mapped topic