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

Patent metadata

Field	Value
Publication number	US-9907855-B2
Application number	US-201715445381-A
Country	US
Kind code	B2
Filing date	Feb 28, 2017
Priority date	Oct 15, 2010
Publication date	Mar 6, 2018
Grant date	Mar 6, 2018

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 of Formula I-C:

wherein:
Ar is benzyl, phenyl, naphthyl, biphenyl, or phenanthrenyl;
R 1 is methyl, ethyl, n-butyl, i-butyl, or t-butyl;
X 1 is a single bond, —O—, —S—, —NH—, or —NHC(O)—; and
POLY 1 is a poly(ethylene oxide) oligomer having from 1 to 15 monomers;

and pharmaceutically acceptable salts thereof.

2. The compound of claim 1 , according to Formula I-C(R):

and pharmaceutically acceptable salts thereof.

3. The compound of claim 1 , according to Formula I-C(S):

and pharmaceutically acceptable salts thereof.

4. The compound of claim 1 , wherein POLY 1 is end-capped with hydroxy, methoxy, ethoxy, or benzyloxy.

5. The compound of claim 1 , wherein POLY 1 is end-capped with methoxy.

6. The compound of claim 1 , wherein X 1 is —NHC(O)—.

7. The compound of claim 1 , wherein Ar is phenyl.

8. The compound of claim 1 , wherein R 1 is methyl.

9. The compound of claim 1 , according to formula:

wherein n is 1, 2, 3, 4, 5, 6, 7, 8, or 9; and pharmaceutically acceptable salts thereof.

10. A composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient.

Assignees

• Nektar Therapeutics

Inventors

• Riggs Sauthier Jennifer
• Zhang Wen

Classifications

• C07D235/22 Primary

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

• A61P25/08

  Antiepileptics; Anticonvulsants · CPC title

• A61K47/60 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

• A61K47/48215 Primary

  Human Necessities · mapped topic