October 21, 2013

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The following patent record is from the CAplusSM database.

CAPLUS COPYRIGHT 2013 ACS

Patent Number: WO 2013123277
Title: Preparation of tricyclic indole derivatives useful as endothelial lipase inhibitors
Inventor(s): Connelly, Margery A.; Greco, Michael; Ye, Hong
Patent Assignee(s): Janssen Pharmaceutica, NV, Belg.
Source: U.S. Pat. Appl. Publ., 30pp. CODEN: USXXCO
Language: English

Abstract:
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).

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention.

 View the full-text here.

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