5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists
Novel 5-cyclic amine-3-arylsulfonylindazoles were prepared, and several analogues within this class have been identified as high-affinity 5-HT 6 receptor ligands with improved pharmacokinetic and pharmacological properties. One selected example, 18b, showed good brain penetrability and a generally favorable pharmacokinetic profile with procognitive efficacy in the rat novel object recognition assay. The synthesis and structure-activity relationship of this potent class are discussed.
Haydar, Simon N.,Yun, Heedong,Andrae, Patrick M.,Mattes, James,Zhang, Jean,Kramer, Angela,Smith, Deborah L.,Huselton, Christine,Graf, Radka,Aschmies, Suzan,Schechter, Lee E.,Comery, Thomas A.,Robichaud, Albert J.
supporting information; scheme or table
p. 2521 - 2527
(2010/08/22)
Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.
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(2008/06/13)
SUBSTITUTED N-ARYLHETEROCYCLES, METHOD FOR PRODUCTION AND USE THEREOF AS MEDICAMENTS
The invention relates to N-arylheterocycles and the physiologically-acceptable salts and physiologically-functional derivatives thereof. Compounds of formula (I), where the groups have the given meanings, the N-oxides and the physiologically-acceptable salts and methods for production thereof are disclosed. The compounds are suitable as anorectics for example.
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Page/Page column 107
(2010/02/08)
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