IP Library Granted Patent US 7,649,098
Granted Patent B2
US 7,649,098 · App. 11/698,253 · Granted Jan 19, 2010

Imidazole-based compounds, compositions comprising them and methods of their use

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Quick Facts
Patent No.
US 7,649,098
App. No.
11/698,253
Granted
Jan 19, 2010
Kind
B2
Abstract

Imidazole-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula I:

Claims (30)

1. A compound of the formula:

wherein:

R 1 is hydrogen, alkyl or aryl;

R 3 is OR 3A , NHC(O)R 3A , NHSO 2 R 3A or hydrogen;

each R 3A is independently hydrogen or alkyl, aryl, alkylaryl, arylalkyl, heteroalkyl, heterocycle, alkylheterocycle, or heterocyclealkyl optionally substituted with halo;

R 6 is OR 6A or OC(O)R 6A ;

R 7 is OR 7A or OC(O)R 7A ;

R 8 is OR 8A or OC(O)R 8A ;

R 9 is hydrogen, CH 2 OR 9A or CH 2 OC(O)R 9A ; and

each of R 6A , R 7A , R 8A , and R 9A is independently hydrogen or lower alkyl.

2. The compound of claim 1 , which is of the formula:

3. The compound of claim 1 , which is of the formula:

4. The compound of claim 3 , which is of the formula:

5. The compound of claim 4 , wherein R 1 is lower alkyl.

6. The compound of claim 4 , wherein R 3 is OR 3A .

7. The compound of claim 4 , wherein R 3 is N(R 3A ) 2 or NHC(O)R 3A .

8. The compound of claim 4 , wherein R 3 is NHSO 2 R 3A .

9. The compound of claim 6 , wherein R 3A is hydrogen or lower alkyl.

10. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is lower alkyl;

R 3 is hydrogen, OR 3A , NHC(O)R 3A or NHSO 2 R 3A ;

R 9 is hydrogen or CH 2 OH; and

each R 3A is independently hydrogen or lower alkyl.

11. The compound of claim 10 , which is of the formula:

12. The compound of claim 11 , wherein R 3 is OR 3A .

13. The compound of claim 12 , wherein R 3A is hydrogen.

14. A compound, or a pharmaceutically acceptable salt thereof, wherein the compound is:

(E)-1-(4-((1R,2S ,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)-ethanone oxime.

15. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient or diluent.

Assignments (4)
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
CHANGE OF NAME Recorded Feb 24, 2022
From: LEXICON GENETICS INCORPORATED
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 059240/0463 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →