Oligomer-containing benzamide-based compounds

Patent metadata

Field	Value
Publication number	US-9375486-B2
Application number	US-201314428816-A
Country	US
Kind code	B2
Filing date	Sep 17, 2013
Priority date	Sep 17, 2012
Publication date	Jun 28, 2016
Grant date	Jun 28, 2016

Abstract

The invention relates to (among other things) oligomer-containing benzamide-based compounds. A compound of the invention 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:
R 2 is lower alkyl;
(a) is an integer in the range of from 1 to 4 inclusive;
Y is either O or S;
R 3 is lower alkyl;
R 4 is selected from the group consisting of hydrogen, halo, lower alkoxy, amino, and lower alkylamino;
R 5 is selected from the group consisting of hydrogen, halo, lower alkoxy, amino, and lower alkylamino;
R 6 is selected from the group consisting of hydrogen, halo, lower alkoxy, amino, and lower alkylamino;
X is a stable or releasable linkage; and
POLY is a water-soluble, non-peptidic oligomer having a number of repeating monomers in the range of from 2 to 30,

and pharmaceutically acceptable salts thereof.

2. The compound of claim 1 , wherein the linkage is a stable linkage.

3. The compound of claim 1 , wherein the linkage is a degradable linkage.

4. The compound of claim 1 , wherein the linkage is selected from the group consisting of amine, urea, carbamate and ether.

5. The compound of claim 1 , wherein the weight average molecular weight of the water-soluble, non-peptidic oligomer is less than 400 Daltons.

6. The compound of claim 1 , having the following structure:

wherein n is in the range of 2 to 30, and pharmaceutically acceptable salts thereof.

7. The compound of claim 1 , wherein the water-soluble, non-peptidic oligomer is a poly(alkylene oxide).

8. The compound of claim 7 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).

9. The compound of claim 1 , wherein the water-soluble, non-peptidic oligomer has a number of repeating monomers in the range of from 2 to 10.

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

11. A composition comprising a compound of claim 1 , and (ii) optionally, a pharmaceutically acceptable excipient.

12. A composition of matter comprising a compound of claim 1 , wherein the compound is present in a dosage form.

Assignees

• Nektar Therapeutics

Inventors

• Cheng Lin
• Riggs-Sauthier Jennifer
• Anand Neel K

Classifications

• A61P1/04

  for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants · CPC title

• A61K31/166

  having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol · CPC title

• C07C237/44 Primary

  having carbon atoms of carboxamide groups, amino groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring · CPC title

• A61K47/60

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

• A61K47/59 Primary

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes · CPC title