439291-60-8Relevant articles and documents
Process for the preparation of N-(phenylethyl) anilines salts and solvates thereof useful as serotonin 5-HT6 antagonists
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Page/Page column 37-38, (2009/10/01)
The invention relates to a process for preparing N-(1-phenylethyl)anilines, salts, and solvates thereof, to novel intermediates, and to the use of the intermediates in the preparation of serotonin 5-HT6 antagonists.
Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Page/Page column 14, (2010/02/11)
Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.
2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: The discovery of α10 subtype selective 2′-alkylsulfonyl-substituted analogues
Hodson, Stephen J.,Bishop, Michael J.,Speake, Jason D.,Navas III, Frank,Garrison, Deanna T.,Bigham, Eric C.,Saussy Jr., David L.,Liacos, James A.,Irving, Paul E.,Jeffrey Gobel,Sherman, Bryan W.
, p. 2229 - 2239 (2007/10/03)
A series of 2′-alkylthio-2-(anilinomethyl)imidazolines were prepared to examine the effect of the alkyl group size, sulfur oxidation state, and phenyl ring substitution on ligand binding and agonism of α-adrenergic receptor subtypes α1a, α1b, α1d, α2a, and α2c. Binding at all receptor subtypes decreased for compounds in the sulfone oxidation state as compared to their sulfide analogues. While sulfides were generally potent, nonselective agonists, sulfones exhibited α1a subtype selectivity in a cell-based functional assay. Sulfone (32) was 250-7000-fold selective for α1a vs all other subtypes.
