IP Library Granted Patent US 6,924,311
Granted Patent B2
US 6,924,311 · App. 09/982,544 · Granted Aug 2, 2005

Methods for affecting various diseases utilizing LXR compounds

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Quick Facts
Patent No.
US 6,924,311
App. No.
09/982,544
Granted
Aug 2, 2005
Kind
B2
Abstract

The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXRβ selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXRα-selective antagonist.

Claims (25)

1. A method for treating diabetes in a mammal, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist, wherein said treatment decreases hyperglycemia.

2. The method of claim 1 further comprising administering to said mammal a thiazolidinedione as an additional active agent.

3. The method of claim 1 wherein said LXR agonist is a pan LXR agonist.

4. The method of claim 1 wherein said LXR agonist is a LXRβ agonist.

5. The method of claim 4 wherein said LXRβ agonist is a partial agonist or agonist that exhibits about 2 to about 10 fold preference for LXRβ compared to LXRα.

6. The method of claim 1 wherein said agonist is in a composition comprising an additional active agent for treating diabetes.

7. The method of claim 6 wherein said active agent decreases hyperglycemia.

8. The method of claim 7 wherein said agent modulates diabetes or treats diabetes and its related symptoms, complications, and disorders.

9. The method of claim 1 wherein said agonist is N-(2,2,2-trifluoroethyl)-N-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethylethyl)-phenyl]-benzene sulfonamide.

10. A method for treating type II diabetes in a mammal, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist, wherein said treatment decreases hyperglycemia.

11. The method of claim 10 wherein said LXR agonist is a pan LXR agonist.

12. The method of claim 10 wherein said LXR agonist is a LXRβ agonist.

13. The method of claim 12 wherein said LXRβ agonist is a partial agonist or agonist that exhibits about 2 to about 10 fold preference for LXRβ compared to LXRα.

14. The method of claim 10 wherein said agonist is in a composition comprising an additional active agent for treating type II diabetes.

15. The method of claim 14 wherein said active agent decreases hyperglycemia.

16. The method of claim 15 wherein said agent modulates diabetes or treats diabetes and its related symptoms, complications, and disorders.

17. The method of claim 10 wherein said agonist is N-(2,2,2-trifluoroethyl)-N-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethylethyl)-phenyl]-benzene sulfonamide.

18. A method for treating type II diabetes in a mammal and reducing the cardiovascular complications of type II diabetes, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist, wherein said treatment decreases hyperglycemia.

19. A method for decreasing hyperglycemia in a mammal comprising administering to said mammal a therapeutically-effective amount of an LXR agonist.

20. A method for treating diabetes in a mammal, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist, wherein said treatment decreases insulin resistance.

21. A method for treating type II diabetes in a mammal, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist, wherein said treatment decreases insulin resistance.

22. A method for treating type II diabetes in a mammal and reducing the cardiovascular complications of type II diabetes, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist wherein said treatment decreases insulin resistance.

23. The method of claim 22 further comprising administering to said mammal a thiazolidinedione as an additional active agent.

24. A method for decreasing insulin resistance in a mammal comprising administering to said mammal a therapeutically-affective amount of an LXR agonist.

25. A method for improving the control of glucose homeostasis in a mammal, said method comprising administering to said mammal a therapeutically-effective amount of an LXR agonist, wherein the control of glucose homeostasis is improved by decreasing hyperglycemia or reducing insulin resistance.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 27, 2022
From: EXELIXIS PATENT COMPANY LLC
To: EXELIXIS, INC.
Reel/Frame 059752/0813 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2011
From: EXELIXIS, INC.
To: EXELIXIS PATENT COMPANY LLC
Reel/Frame 026138/0390 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 24, 2011
From: X-CEPTOR THERAPEUTICS, INC.
To: EXELIXIS, INC.
Reel/Frame 026015/0141 →
RELEASE OF SECURITY Recorded Aug 16, 2005
From: COMERICA BANK
To: X-CEPTOR THERAPEUTICS, INC.
Reel/Frame 016641/0184 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 23, 2005
From: SCHULMAN, IRA G.; BISCHOFF, ERIC D.; TANGIRALA, RAJENDRA K.
To: X-CEPTOR THERAPEUTICS, INC.
Reel/Frame 016730/0589 →
SECURITY AGREEMENT Recorded Sep 3, 2004
From: X-CEPTOR THERAPEUTICS, INC.
To: COMERICA BANK
Reel/Frame 015074/0913 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 14, 2002
From: SCHULMAN, IRA G.; BISCHOFF, ERIC D.; TANGIRALA, RAJENDRA K.
To: X-CEPTOR THERAPEUTICS, INC.
Reel/Frame 012578/0968 →