IP Library Granted Patent US 7,825,142
Granted Patent B2
US 7,825,142 · App. 12/545,954 · Granted Nov 2, 2010

Heterocyclic compounds, compositions comprising them and methods of their use

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Quick Facts
Patent No.
US 7,825,142
App. No.
12/545,954
Granted
Nov 2, 2010
Kind
B2
Abstract

Heterocyclic 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 (35)

1. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

X is N or NR 9 ;

Y is CR 4 , N, NR 9 , O or S;

Z is CR 4 , CHR 4 , N, NR 9 , O or S;

R 1 is hydrogen or optionally substituted lower alkyl;

each R 4 is independently OR 4A , OC(O)R 4A , hydrogen, halogen, or optionally substituted alkyl, aryl, alkylaryl, arylalkyl, heteroalkyl, heterocycle, alkylheterocycle, or heterocyclealkyl;

R 5 is OR 5A or OC(O)R 5A ;

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

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

R 8 is hydrogen, CH 2 OR 8A or CH 2 OC(O)R 8A ;

each R 9 is independently hydrogen or optionally substituted alkyl, aryl, alkylaryl, arylalkyl, heteroalkyl, heterocycle, alkylheterocycle, or heterocyclealkyl; and

each of R 4A , R 5A , R 6A , R 7A and R 8A is independently hydrogen or lower alkyl.

2. The compound of claim 1 , wherein X is N.

3. The compound of claim 1 , wherein Y is O.

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

5. The compound of claim 1 , wherein one or more of R 5 , R 6 , R 7 , and R 8 is hydroxyl or acetate.

6. The compound of claim 5 , wherein all of R 5 , R 6 , and R 7 are hydroxyl.

7. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

X is CR 4 , CHR 4 , N, NR 9 , O or S;

Y is CR 4 , CHR 4 , N, NR 9 , O or S;

Z is CR 4 , CHR 4 , N, NR 9 , O or S;

R 1 is hydrogen or optionally substituted lower alkyl; and

R 3 is optionally substituted alkyl;

each R 4 is independently OR 4A , OC(O)R 4A , hydrogen, halogen, or optionally substituted alkyl, aryl, alkylaryl, arylalkyl, heteroalkyl, heterocycle, alkylheterocycle, or heterocyclealkyl;

R 5 is OR 5A or OC(O)R 5A ;

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

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

R 8 is hydrogen, CH 2 OR 8A or CH 2 OC(O)R 8A ;

each R 9 is independently hydrogen or optionally substituted alkyl, aryl, alkylaryl, arylalkyl, heteroalkyl, heterocycle, alkylheterocycle, or heterocyclealkyl; and

each of R 4A , R 5A , R 6A , R 7A and R 8A is independently hydrogen or lower alkyl.

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

9. The compound of claim 7 , wherein one or more of R 5 , R 6 , R 7 , and R 8 is hydroxyl or acetate.

10. The compound of claim 9 , wherein all of R 5 , R 6 , and R 7 are hydroxyl.

Assignments (3)
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
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 →