IP Library Granted Patent US 9,102,636
Granted Patent B2
US 9,102,636 · App. 13/043,159 · Granted Aug 11, 2015

Analgesic compounds, compositions, and uses thereof

Inventors: James C. Mannion (Plainsboro, NJ); Scott L. Dax (Landenberg, PA)
Assignee: Galleon Pharmaceuticals, Inc.
C07D277/18
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Quick Facts
Patent No.
US 9,102,636
App. No.
13/043,159
Granted
Aug 11, 2015
Kind
B2
Abstract

The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described.

Claims (8)

1. A compound according to Formula I or a salt thereof:

wherein in Formula I:

R 1 and R 2 are independently hydrogen or alkyl, or R 1 and R 2 form together a radical according to the formula (CH 2 ) n , wherein n is selected from the group consisting of 2, 3, 4, 5 and 6;

R 3 is, independently at each occurrence, hydrogen, alkyl, substituted alkyl, alkenyl, alkynyl, halogen, phenyl, substituted phenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, hydroxyl, alkoxy, cyano, nitro, acyl, carboxy, carboxyalkyl, or amido;

R 4 is hydrogen, alkyl, substituted alkyl, or acyl; and

W is carboxy, or carboxyalkyl.

2. The compound of claim 1 , wherein R 1 and R 2 are CH 3 .

3. A compound selected from the group consisting of (S)-2-(2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (R)-2-(2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (R)-2-(2-Hydroxy-4-methoxyphenylamino)-thiazoline-4-carboxylic acid, (R)-2-(4-Fluoro-2-hydroxyphenylamino)-thiazoline-4-carboxylic acid, (R)-2-(3,5-Dichloro-2-hydroxy-4-methylphenylamino)-thiazoline-4-carboxylic acid, (R)-2-(5-tert-Butyl-2-hydroxyphenylamino)-thiazoline-4-carboxylic acid, (R)-2-(2-Hydroxy-4-methoxycarbonylphenylamino)-thiazoline-4-carboxylic acid, (R)-2-(5-Ethanesulfonyl-2-hydroxy-phenylamino)-thiazoline-4-carboxylic acid, (R)-2-(4-Chloro-2-hydroxyphenylamino)-thiazoline-4-carboxylic acid, (R)-2-(2-Hydroxy-5-methoxyphenylamino)-thiazoline-4-carboxylic acid, (S)-2-(2-Hydroxy-5-chlorophenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (S)-2-(2-Hydroxy-5-chlorophenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (S)-2-(2-Hydroxy-5-methylphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (S)-2-(2-Hydroxy-5-methylphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (S)-2-(2-Hydroxy-4-methoxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (S)-2-(2-Hydroxy-4-methoxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (S)-2-(4-Chloro-2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (S)-2-(2-Hydroxy-5-nitrophenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (S)-2-(2-Hydroxy-5-nitrophenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (S)-2-(5-Ethanesulfonyl-2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (S)-2-(5-Ethanesulfonyl-2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid, (R)-2-(2-hydroxyphenylamino)-thiazoline-4-carboxylic acid methyl ester, (S)-2-(2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (R)-2-(4-chloro-2-hydroxyphenylamino)-thiazoline-4-carboxylic acid methyl ester, (S)-2-(4-chloro-2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, (R)-2-(4-chloro-2-hydroxyphenylamino)-thiazoline-4-carboxylic acid, and (R)-2-(2-hydroxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid methyl ester, mixtures thereof and salts thereof.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Jun 25, 2020
From: OXFORD FINANCE LLC
To: GALLEON PHARMACEUTICALS, INC.
Reel/Frame 053034/0805 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2017
From: GALLEON (ASSIGNMENT FOR THE BENEFIT OF CREDITORS), LLC
To: CERSCI THERAPEUTICS, INC.
Reel/Frame 042442/0617 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 2, 2016
From: GALLEON PHARMACEUTICALS, INC.
To: GALLEON (ASSIGNMENT FOR THE BENEFIT OF CREDITORS), LLC
Reel/Frame 039902/0442 →
SECURITY INTEREST Recorded Mar 3, 2016
From: GALLEON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC
Reel/Frame 037885/0614 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 23, 2011
From: MANNION, JAMES C.; DAX, SCOTT L.
To: GALLEON PHARMACEUTICALS, INC.
Reel/Frame 026325/0006 →
Continuity (4)
Provisional Application 61312482 · Mar 10, 2010
Provisional Application 61378781 · Aug 31, 2010
Related Publication 20110224269A1 · Sep 15, 2011
Related Publication 20120202860A2 · Aug 9, 2012