57311-64-5Relevant academic research and scientific papers
α1b-adrenergic receptor antagonists
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Page/Page column 90, (2010/11/30)
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1is hydrogen etc., B is bond, or B—N—R1forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and α1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for α1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which α1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by α1B adrenoceptor.
CCR2B receptor antagonists: Conversion of a weak HTS hit to a potent lead compound
Forbes, Ian T,Cooper, David G.,Dodds, Emma K.,Hickey, Deirdre M.B.,Ife, Robert J.,Meeson, Malcolm,Stockley, Martin,Berkhout, Theo A.,Gohil, Jayneeta,Groot, Pieter H.E.,Moores, Kitty
, p. 1803 - 1806 (2007/10/03)
A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.
(2E,4E)-N-(4-(1H-indol-3-yl)piperidin-1-yl)alkyl-5-(substituted phenyl)-2,4-pentadienamides as antiallergic agents with antihistaminic and anti slow-reacting substance (SRS) activities
Shigenaga,Manabe,Matsuda,Fujii,Matsuo
, p. 3 - 10 (2007/10/02)
As an extension of our study aiming to discover a novel compound with dual activities against histamine and slow-reacting substance (SRS), we synthesized two types of indolylpiperidine derivatives, 3 and 4-20. Testing for in vivo antianaphylactic activity and for in vitro anti-SRS activity revealed that (2E,4E)-5-(3,5-dimethoxy-4-hydroxyphenyl)-N-(2-(4-(1H-indol-3-yl)piper idin-1-yl)ethyl)-2,4-pentadienamide (11) exhibited potent dual activities with ED50 = 0.89 mg/kg and IC50 = 1.43 μM, respectively. However, the plasma concentration of unchanged 11 was very low when administered orally in guinea pigs. This result can be explained by fast formation of a glucuronic acid conjugate.
Indolylpiperidine compounds, processes for the preparation thereof and pharmaceutical composition comprising the same
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, (2008/06/13)
The invention relates to novel indolylpiperidine compounds useful in the treatment of allergic disease and inflammation.
N-[ω-(4'-(3"-indolyl)-piperidino)-alkyl]-benzamides
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, (2008/06/13)
N-[ω-(4'-(3"-indolyl)-piperidino)-alkyl]-benzamides of the formula SPC1 Wherein R is selected from the group consisting of hydrogen and alkoxy of 1 to 3 carbon atoms, R1 and R2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, n is 2 or 3, X is selected from the group consisting of hydrogen and alkoxy of 1 to 3 carbon atoms, X1 is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, --NH2 and EQU1 and X2 is selected from the group consisting of hydrogen, chlorine and sulfamoyl and their non-toxic, pharmaceutically acceptable acid addition salts having neurosedative properties and their preparation.
