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CAPLUS COPYRIGHT 2012 ACS
|Patent Number: ||WO 2012143813 |
|Title: ||Preparation of spiro[indazole-5,4'-piperidin]-1'-yl compounds as acetyl-CoA carboxylase inhibitors |
|Inventor(s): ||Dow, Robert Lee; Edmonds, David James; Griffith, David Andrew; Southers, James Alfred, Jr. |
|Patent Assignee(s): ||Pfizer Inc., USA |
|Source: ||U.S. Pat. Appl. Publ., 73pp. CODEN: USXXCO |
|Language: ||English |
Title compds. I and II [R1 = alkyl or cylcoalkyl; R2 = (un)substituted indolyl, indazolyl, pyrrolopyridinyl, pyrazolopyridinyl, quinolinyl or benzoimidazolyl; R3 = H or alkyl], and their pharmaceutically acceptable salts, are prepared as acetyl-CoA carboxylase (ACC) inhibitors. Thus, e.g., compound III was prepared by the coupling reaction of 1-isopropyl-4,6-dihydrospiro[indazole-5,4'-piperidin]-7(1H)-one (preparation given) with 3-carbamoyl-1H-indole-6-carboxylic acid (preparation given). Compound III exhibited inhibitory activity against recombinant human ACC1 and ACC2 with IC50 values of 6.0 nM and 1.4 nM, resp. The invention compds. are useful for the treatment of acetyl-CoA carboxylase associated diseases such as type 2 diabetes and nonalcoholic fatty liver disease (NAFLD).
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Note: Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced the abstract using additional information found in the patent. The title of the PCT patent publication is Substituted acetyl-CoA carobxylase inhibitors.