IP Library Granted Patent US 8,288,438
Granted Patent B2
US 8,288,438 · App. 11/908,952 · Granted Oct 16, 2012

Methods for avoiding edema in the treatment or prevention of PPARγ-responsive diseases, including cancer

Assignees: Metabolex, Inc.; Dia Tex, Inc.
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Quick Facts
Patent No.
US 8,288,438
App. No.
11/908,952
Granted
Oct 16, 2012
Kind
B2
Abstract

Compounds, compositions, and methods of avoiding edema while treating or preventing PPARγ-mediated diseases, including cancer, using derivatives and prodrugs are provided.

Claims (18)

1. A method of treating edema in a subject with a PPARγ-responsive condition or disease, comprising administering to the subject a therapeutically effective amount of an edema-sparing PPARγ modulator wherein the modulator is a compound of Formula I:

wherein R is a member selected from the group consisting of a hydroxy, alkoxy, heteroalkoxy, aryloxy, heteroaryloxy, lower aralkoxy, di-lower alkylamino-lower alkoxy, lower alkanamido lower alkoxy, benzamido-lower alkoxy, ureido-lower alkoxy, N′-lower alkyl-ureido-lower alkoxy, carbamoyl-lower alkoxy, halophenoxy substituted lower alkoxy, carbamoyl substituted phenoxy, carbonyl-lower alkylamino, N,N-di-lower alkylamino-lower alkylamino, halo substituted lower alkylamino, hydroxy substituted lower alkylamino, lower alkanolyloxy substituted lower alkylamino, ureido, arylsulfonamido, alkylsulfonamido and lower alkoxycarbonylamino; and each X is independently a halogen;

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the administering is systemic.

3. The method of claim 1 , wherein the administering is local.

4. The method of claim 1 , wherein the administering is by the intravenous, oral, or rectal routes.

5. The method of claim 1 , wherein the administering is topical.

6. The method of claim 1 , wherein the condition is osteoporosis.

7. The method of claim 1 , wherein the condition is inflammation or allergy.

8. The method of claim 1 , wherein the condition is eczema, acne vulgaris, or psoriasis.

9. The method of claim 1 , wherein the condition is cachexia, irritable bowel syndrome, inflammatory bowel disease, including Crohn's disease and ulcerative colitis, pancreatitis, abdominal obesity, neurodegenerative disease, or retinopathy.

10. The method of claim 1 , wherein the subject is human.

11. The method of claim 1 , wherein the subject is human and the compound is administered as a (−) enantiomer which is substantially free of its (+) enantiomer.

12. The method of claim 11 , wherein the compound is halofenate.

13. The method of claim 1 , wherein the administering is chronic.

14. The method of claim 10 , wherein the subject has heart failure, congestive heart failure, or hypertension.

15. The method of claim 12 , wherein the compound is administered in an amount from 100 to 800 mg per day by the oral route.

16. The method of claim 15 , wherein the daily dosage is from about 200 mg to about 600 mg.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2016
From: CYMABAY THERAPEUTICS, INC.
To: DIATEX, INC.
Reel/Frame 039045/0152 →
RELEASE OF SECURITY INTEREST Recorded Aug 7, 2015
From: SILICON VALLEY BANK; OXFORD FINANCE LLC
To: CYMABAY THERAPEUTICS, INC.
Reel/Frame 036307/0406 →
SECURITY AGREEMENT Recorded Nov 22, 2013
From: CYMABAY THERAPEUTICS, INC.
To: SILICON VALLEY BANK; OXFORD FINANCE LLC
Reel/Frame 031710/0508 →
CHANGE OF NAME Recorded Oct 30, 2013
From: METABOLEX, INC.
To: CYMABAY THERAPEUTICS, INC.
Reel/Frame 031516/0970 →
CORRECTIVE ASSIGNMENT TO CORRECT THE NATURE OF CON Recorded Jul 16, 2009
From: METABOLEX, INC.
To: DIATEX, INC.
Reel/Frame 022973/0618 →
LICENSE Recorded Jun 17, 2009
From: METABOLEX, INC.
To: DIATEX, INC.
Reel/Frame 022835/0388 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 7, 2008
From: SANDERS, MARTIN E.; KARPF, DAVID B.
To: METABOLEX, INC.
Reel/Frame 020764/0334 →
Continuity (3)
Provisional Application 60663977 · Mar 21, 2005
Provisional Application 60664515 · Mar 22, 2005
Related Publication 20080269189A1 · Oct 30, 2008