US2009227599A1PendingUtilityA1
Sulfonyl-substituted bicyclic compounds as modulators of ppar
Est. expiryMar 30, 2018(expired)· nominal 20-yr term from priority
Inventors:Stewart A. NobleGuy OshiroJames W. MalechaCunxiang ZhaoSergio G. DuronAndrew LindstromAndrew K. ShiauBoliang LouSteven P. GovekDavid J. Thomas
C07D 295/26C07D 257/04C07D 209/26C07D 405/04C07D 209/08C07D 333/60C07D 213/74C07D 409/12C07D 211/96C07D 401/04C07D 487/08C07D 241/04C07D 401/12C07D 317/66
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Claims
Abstract
Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Claims
exact text as granted — not AI-modified1 - 13 . (canceled)
14 . A method of modulating a peroxisome proliferator-activated receptor (PPAR) function comprising contacting said PPAR with 4-[2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid.
15 . The method as recited in claim 24 , contacting said PPAR with a single enantiomer of 4-[cis-2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid substantially free of the other enantiomer.
16 . The method as recited in claim 24 wherein said modulation is selective for PPARδ over PPARγ or PPARα.
17 . The method as recited in claim 26 wherein said selectivity is 100-fold or greater.
18 . A method for treating scarring in a patient in need thereof comprising
i. identifying a patient in need of such treatment; and ii. administering to said patient a therapeutically effective amount of a therapeutically effective amount of 4-[2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid.
19 . A method for treating scarring in a patient in need thereof comprising
i. identifying a patient in need of such treatment; and ii. administering to said patient a therapeutically effective amount of a single enantiomer of 4-[cis-2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid substantially free of the other enantiomer.
20 . A method of wound healing in a patient in need thereof comprising
i. identifying a patient in need of wound healing; and ii. administering to said patient a therapeutically effective amount of 4-[2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid.
21 . A method of wound healing in a patient in need thereof comprising
i. identifying a patient in need of wound healing; and ii. administering to said patient a therapeutically effective amount of a single enantiomer of 4-[cis-2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid substantially free of the other enantiomer.
22 . A method for treating an inflammatory disease in a patient in need thereof comprising
i. identifying a patient in need of such treatment; and ii. administering to said patient a therapeutically effective amount of 4-[2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid.
23 . The method as recited in claim 22 , wherein said disease is selected from the group consisting of asthma, rheumatoid arthritis, osteoarthritis, inflammatory response to tissue injury, psoriasis, ulcerative colitis, dermatitis, and autoimmune disease.
24 . The method as recited in claim 23 , wherein said disease is inflammatory response to tissue injury.
25 . A method for treating an inflammatory disease in a patient in need thereof comprising
i. identifying a patient in need of such treatment; and ii. administering to said patient a therapeutically effective amount of a single enantiomer of 4-[cis-2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid substantially free of the other enantiomer.
26 . The method as recited in claim 25 , wherein said disease is selected from the group consisting of asthma, rheumatoid arthritis, osteoarthritis, inflammatory response to tissue injury, psoriasis, ulcerative colitis, dermatitis, and autoimmune disease.
27 . The method as recited in claim 26 , wherein said disease is inflammatory response to tissue injury.
28 . A method for treating, in a patient in need thereof, a disease selected from the group consisting of diabetes, obesity, metabolic syndrome, and insulin resistance, comprising
iii. identifying a patient in need of such treatment; and iv. administering to said patient a therapeutically effective amount of a therapeutically effective amount of 4-[2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid.
29 . The method as recited in claim 28 wherein said disease is diabetes.
30 . The method as recited in claim 28 wherein said disease is obesity.
31 . The method as recited in claim 28 wherein said disease is metabolic syndrome.
32 . The method as recited in claim 28 wherein said disease is insulin resistance.
33 . A method for treating, in a patient in need thereof, a disease selected from the group consisting of diabetes, obesity, metabolic syndrome, and insulin resistance, comprising
iii. identifying a patient in need of such treatment; and iv. administering to said patient a therapeutically effective amount of a single enantiomer of 4-[cis-2,6-dimethyl-4-(4-trifluoromethoxy-benzyl)-piperazine-1-sulfonyl]-indan-2-carboxylic acid substantially free of the other enantiomer.
34 . The method as recited in claim 33 wherein said disease is diabetes.
35 . The method as recited in claim 33 wherein said disease is obesity.
36 . The method as recited in claim 33 wherein said disease is metabolic syndrome.
37 . The method as recited in claim 33 wherein said disease is insulin resistance.Cited by (0)
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