IP Library Granted Patent US 10,829,506
Granted Patent B2
US 10,829,506 · App. 15/851,676 · Granted Nov 10, 2020

Amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use

Inventors: Georg Schlechtingen (Dresden, DE); Hans-Joachim Knölker (Dresden, DE); Tim Friedrichson (Dresden, DE); Gary Jennings (Dresden, DE); Tobias Braxmeier (Kuppenheim, DE)
Assignee: GRI Bio, Inc.
C07F9/4006A61K31/205A61K31/4425A61K31/662C07C229/12C07C309/14C07D211/06C07D211/46C07D211/60C07D211/62C07D295/037C07F9/3808
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Quick Facts
Patent No.
US 10,829,506
App. No.
15/851,676
Granted
Nov 10, 2020
Kind
B2
Abstract

The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6 and their medical use, including their use in treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder.

Claims (15)

1. A compound of the following formula 1

or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein:

R 1 is a C 10-20 hydrocarbon group;

R 2 is a C 1-4 alkyl group, and R 3 is H;

R 4 is a C 1-6 hydrocarbon group;

R 5 is —SO 3 , —SO 3 H, —PO 3 2− , —PO 3 H 2 , —PO 2 (OC 1-3 alkyl), —PO 2 H(OC 1-3 alkyl), —PO(OC 1-3 alkyl) 2 , —CO 2 , —CO 2 H or —CO 2 (C 1-3 alkyl; and

X is N + .

2. The compound of claim 1 , wherein R 5 is —SO 3 or —SO 3 H.

3. The compound of claim 1 , wherein R 5 is —PO 3 2− ″, —PO 3 H − , or —PO 3 H 2 .

4. The compound of claim 1 , wherein R 4 is —(CH 2 ) 3 —.

5. The compound of claim 1 , wherein R 1 is a linear C 10-20 alkyl group, a linker C 10-20 alkenyl group, or a linear C 10-20 alkynyl group.

6. The compound of claim 1 , wherein R 1 is —(CH 2 ) 11 —CH 3 , —(CH 2 ) 13 —CH 3 , or —(CH 2 ) 15 —CH 3 .

7. The compound of claim 1 , wherein R 2 is methyl.

8. The compound of claim 1 , wherein the compound is a compound of any of the following formulae:

9. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

Assignments (4)
SECURITY INTEREST Recorded Dec 15, 2022
From: GRI BIO, INC.
To: ALTIUM GROWTH FUND, LP
Reel/Frame 062108/0599 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 30, 2020
From: SCHLECHTINGEN, GARY; KNOLKER, HANS-JOACHIM; FRIEDRICHSON, TIM; JENNINGS, GARY; BRAXMEIER, TOBIAS
To: GLYCOREGIMMUNE, INC.
Reel/Frame 053939/0334 →
CHANGE OF NAME Recorded Sep 30, 2020
From: GLYCOREGIMMUNE, INC.
To: GRI BIO, INC.
Reel/Frame 053953/0127 →
SECURITY INTEREST Recorded Nov 2, 2018
From: GRI BIO, INC.
To: TEP BIOTECH, LLC
Reel/Frame 047399/0239 →
Priority Claims (1)
EP 11167752 · May 26, 2011 · regional
Continuity (2)
Division 14403167
Related Publication 20180244703A1 · Aug 30, 2018