7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT6 receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with reduced hERG liability. An advanced analog tested in rat social recognition model showed significant activity suggesting potential utility in the enhancement of short-term memory.
Sundar, Babu G.,Bailey, Thomas R.,Dunn, Derek D.,Bacon, Edward R.,Salvino, Joseph M.,Morton, George C.,Aimone, Lisa D.,Zeqi, Huang,Mathiasen, Joanne R.,Dicamillo, Amy,Huffman, Mark J.,McKenna, Beth A.,Kopec, Karla,Lu, Lily D.,Brown, Rebecca,Qian, Jie,Angeles, Thelma,Connors, Thomas,Spais, Chrysanthe,Holskin, Beverly,Galinis, Deborah,Duzic, Emir,Schaffhauser, Herve,Rosse, Gerard C.
scheme or table
p. 120 - 123
(2012/03/10)
AURONE DERIVATIVE-CONTAINING COMPOSITION FOR DIAGNOSIS
The present invention provides a composition for diagnosing amyloid-related diseases, comprising a compound represented by general formula (I): wherein X represents O or the like; R1, R3, R4, R5, R6,
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(2009/12/04)
NOVEL COMPOUNDS AS PHARMACEUTICAL AGENTS
The current invention relates to compounds of the formula:(Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.
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Page 46
(2010/02/07)
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