Oligomer-containing benzamide-based compounds

Patent metadata

Field	Value
Publication number	US-10434181-B2
Application number	US-201815908286-A
Country	US
Kind code	B2
Filing date	Feb 28, 2018
Priority date	Sep 17, 2012
Publication date	Oct 8, 2019
Grant date	Oct 8, 2019

Abstract

The invention relates to (among other things) oligomer-containing benzamide-based compound 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 method of treating gastroparesis or arrhythmia comprising administering to a subject in need thereof an effective amount of 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 method of claim 1 , wherein the compound has the structure:

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

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

4. The method of claim 3 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).

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

6. The method of claim 3 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxyl end-capping moiety.

7. The method of claim 1 , wherein administering comprises administering the compound by a mode of administration selected from the group consisting of parenteral, oral, and transdermal.

8. The method of claim 1 , wherein the therapeutically effective dose of the compound is about 0.001 mg to 1000 mg.

9. The method of claim 1 , wherein said administering comprises administering the compound five times a day, four times a day, three times a day, twice daily, once daily, three times weekly, twice weekly, or once weekly.

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

• 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

• C07C231/12

  by reactions not involving the formation of carboxamide groups · 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