US2009227599A1PendingUtilityA1

Sulfonyl-substituted bicyclic compounds as modulators of ppar

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Assignee: KALYPSYS INCPriority: Mar 30, 1998Filed: Mar 3, 2009Published: Sep 10, 2009
Est. expiryMar 30, 2018(expired)· nominal 20-yr term from priority
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-modified
1 - 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.

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