IP Library Granted Patent US 8,153,804
Granted Patent B2
US 8,153,804 · App. 11/497,539 · Granted Apr 10, 2012

Aryl pyridines and methods of their use

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Quick Facts
Patent No.
US 8,153,804
App. No.
11/497,539
Granted
Apr 10, 2012
Kind
B2
Abstract

Aryl pyridines, compositions comprising them, and methods of their use for the treatment, prevention and management of a variety of diseases and disorders are disclosed.

Claims (32)

1. A compound of formula I:

or a pharmaceutically acceptable salt or solvate thereof, wherein:

A is

R a is hydrogen, halogen or optionally substituted alkyl;

R b is hydrogen, halogen or optionally substituted alkyl;

each of R 1 , R 2 , R 3 , R 4 , R 5 is independently hydrogen, halogen, or optionally substituted heterocycle; or R 1 and R 2 , R 2 and R 3 , R 3 and R 4 , or R 4 and R 5 , together with the carbon atoms to which they are attached, form a pyrrolidinone ring;

each of R 6 and R 7 is independently hydrogen, halogen or optionally substituted alkyl; and

R 8 is an optionally substituted heterocycle or —NR c R d , —C(O)NR c R d , or —C(O)R e ,

wherein each of R c , R d and R e is independently hydrogen or optionally substituted alkyl;

provided that if each of R a , R b and R 1 -R 7 is hydrogen, then R 8 is not NH 2 .

2. The compound of claim 1 , wherein R 1 is the same as R 5 .

3. The compound of claim 1 , wherein R 1 is the same as R 4 and R 5 .

4. The compound of claim 1 , wherein R 1 is hydrogen.

5. The compound of claim 1 , wherein R 2 is an optionally substituted Heterocycle.

6. The compound of claim 1 , wherein R 3 is hydrogen.

7. The compound of claim 1 , wherein R 4 is hydrogen.

8. The compound of claim 1 , wherein R 5 is hydrogen.

9. The compound of claim 1 , wherein R 6 is the same as R 7 .

10. The compound of claim 1 , wherein R 6 is hydrogen.

11. The compound of claim 1 , wherein R 7 is hydrogen.

12. The compound of claim 1 , wherein R 8 is —C(O)NH 2 .

13. The compound of claim 1 , wherein R 8 is —C(O)-alkyl.

14. The compound of claim 1 , wherein R 8 is tetrazole.

15. A compound of formula II:

or a pharmaceutically acceptable salt or solvate thereof, wherein:

R a is hydrogen, halogen or optionally substituted alkyl;

R b is hydrogen, halogen or optionally substituted alkyl;

each of R 1 , R 2 , R 3 , R 4 , R 5 is independently hydrogen, halogen, or optionally substituted heterocycle; or R 1 and R 2 , R 2 and R 3 , R 3 and R 4 , or R 4 and R 5 , together with the carbon atoms to which they are attached, form a pyrrolidinone ring;

each of R 6 and R 7 is independently hydrogen, halogen or optionally substituted alkyl; and

R 8 is an optionally substituted heterocycle or —NR c R d , —C(O)NR c R d , or —C(O)R e ,

wherein each of R c , R d and R e is independently hydrogen or optionally substituted alkyl;

provided that if each of R a , R b and R 1 -R 7 is hydrogen, then R 8 is not NH 2 .

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 →