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CAPLUS COPYRIGHT 2013 ACS
||Preparation of tricyclic indole derivatives useful as endothelial lipase inhibitors
||Connelly, Margery A.; Greco, Michael; Ye, Hong
||Janssen Pharmaceutica, NV, Belg.
||U.S. Pat. Appl. Publ., 30pp. CODEN: USXXCO
The present invention is directed to tricyclic indole derivs. I [R1 = (CH2)a-Ph, (CH2)b-O-phenyl; a = 1-5; b = 1-4; Ph of group R1 can be optionally substituted with halo, alkyl, alkoxy; R2 = H, OH, OMe, NH2; ring A = 5-7 membered, satd. ring structure selected from II-VII; R3 = H, alkyl, alkyl-OH, etc.; with the provisos], pharmaceutical compns. contg. them and their use in the treatment of disorders and conditionsmodulated by endothelial lipase, for example, cardiovascular disorders. Over twenty compds. I were prepd. E.g., a multi-step synthesis of VIII, starting from 2-ethoxy-3-phenethyl-2-(trifluoromethyl)oxirane and 2,3,4,5-tetrahydro-1H-benzo[b]azepine, was described. Exemplified compds. I were tested in the endothelial lipase assay (data given).
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