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US 2003/0153606 A1Published application
Thiazolidinedione derivatives for the treatment of diabetes and other diseases
AssigneeMaxia Pharmaceuticals, Inc.
InventorsMagnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P.M. Pleynet, Lyle W. Spruce
Life of this patent
Estimating the term…
Abstract
The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease. 1
Claims32
A compound of the formula:
- 60
- wherein:
- R1 and R2 together with the aromatic ring bonded thereto comprise a cycloalkyl or cycloalkenyl ring having 3 to 8 carbon atoms that optionally comprises 1 or 2 heteroatoms selected from O, S, NH or N-alkyl, and wherein the cycloalkyl or cycloalkenyl ring is optionally further substituted with one or more groups independently selected from halogen, alkyl, hydroxyl, alkoxy, substituted alkoxy, carboxy, carboalkoxy, alkylcarboxamide, substituted alkylcarboxamide, dialkylcarboxamide, substituted dialkylcarboxamide, amino, mono-substituted amino or di-substituted amino;
- R3 and R4 are independently or together hydrogen, halogen, alkyl, substituted alkyl, haloalkyl, alkoxy, substituted alkoxy, amino, mono-substituted amino, di-substituted amino or haloalkoxy;
- Ar is Formula (VI), (VII) or (VIII):
- 61
- wherein:
- R8 is alkyl, substituted alkyl, alkenyl, haloalkyl, hydroxy, acyloxy, halogen, alkoxy, substituted alkoxy, amino, mono-substituted amino, di-substituted amino, alkylamide or haloalkoxy;
- and
- R9 and R10 are independently or together hydrogen, halogen, alkyl, substituted alkyl, haloalkyl, alkenyl, substituted alkenyl, alkoxy, hydroxyl, amino, mono-substituted amino, di-substituted amino, alkylamide or haloalkoxy;
- R5 is hydrogen, or alkyl;
- — represents a bond present or absent;
- and
- W, X, Y and Z together form a 2,4-thiazolidinedione or a 2-thioxo-4-thiazolidinedione;
- or a pharmaceutically acceptable salt thereof.
12 more elements
Dependencies are inferred from the claim text.