895534-29-9Relevant academic research and scientific papers
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism
Harris III, Ralph N.,Stabler, Russel S.,Repke, David B.,Kress, James M.,Walker, Keith A.,Martin, Renee S.,Brothers, Julie M.,Ilnicka, Mariola,Lee, Simon W.,Mirzadegan, Tara
scheme or table, p. 3436 - 3440 (2010/07/16)
A series of 5-HT6 ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT6 for antagonism.
ARYLSULFONAMIDYL TETRALIN DERIVATIVES AND USES THEREOF
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, (2008/06/13)
Compounds of the formula I or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.
TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
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, (2008/06/13)
Compounds of the formula I, II or III; or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.
TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
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Page/Page column 100; 101, (2008/06/13)
Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein R2 is (CR3R4)n-NR5R6 and m, p, q, Ar, R1, R3, R4, R5 and R6 are as defined in the claims, which are selective antagonists of 5-HT6 and/or 5-HT2A. Also provided are compositions comprising these compounds and their use in the preparation of medicaments for treating central nervous system disease states selected from psychoses, schizophrenia, manic depressions, neurological disorders, memory disorders, attention deficit disorder, Parkinson’s disease, amyotrophic lateral scierosis, Alzheimer’s disease, food uptake disorders and Huntington’s disease.
