219963-60-7Relevant academic research and scientific papers
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: Identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134)
Bromidge, Steven M.,Clarke, Stephen E.,Gager, Tracey,Griffith, Kerry,Jeffrey, Phillip,Jennings, Andrew J.,Joiner, Graham F.,King, Frank D.,Lovell, Peter J.,Moss, Stephen F.,Newman, Helen,Riley, Graham,Rogers, Derek,Routledge, Carol,Serafinowska, Halina,Smith, Douglas R.
, p. 55 - 58 (2001)
Substituted N-phenyl-4-methoxy-3-piperazin-1-ylbenzenesulfonamides and conformationally restricted analogues have been identified as high affinity and selective 5-HT6 antagonists. Compounds from this series had a range of pharmacokinetic profiles in rat and in general there was a correlation between clearance and CNS penetration. Based on its overall biological profile 2 (SB-357134) was selected for further pre-clinical evaluation. (C) 2000 Elsevier Science Ltd.
Aromatic heterocyclic derivative and application thereof in medicine
-
Paragraph 0232; 0238-0241, (2020/02/08)
The invention provides aromatic heterocyclic derivatives or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, which are used for treating Alzheimer's disease. The invention also discloses pharmaceutical compositions containing the compounds and a method for treating Alzheimer's disease by using the compounds or the pharmaceutical compositions provided by the invention.
Indole derivatives and its application on the medicament
-
Paragraph 0222; 0232-0235, (2019/03/28)
The invention provides indole derivatives or stereisomers, tautomers, nitrogen oxides, solvate, metabolic products, pharmaceutically acceptable salts or prodrugs thereof for treating the alzheimer disease. The invention further discloses a pharmaceutical composition containing the compounds and a method of using the compounds or the pharmaceutical composition thereof to treat the alzheimer disease.
Substituted heteroaryl compounds and compositions and uses thereof
-
Paragraph 0154; 0164-0167, (2019/06/05)
The present invention relates to a novel heteroaromatic compound, and a pharmaceutical composition containing the compound. The heteroaromatic compound or pharmaceutical composition containing the compound can be used for exciting a melatonin receptor. The present invention also relates to a preparation method of the compound and pharmaceutical composition thereof, and application of the compound and pharmaceutical composition in treating central nervous system dysfunction of mammals especially human.
Aromatic heterocyclic derivative and its application on the medicament
-
Paragraph 0202; 0208-0211, (2019/06/27)
The invention provides aromatic heterocyclic derivatives or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, which are used for treating Alzheimer's disease. The invention also disclo
Indoline derivative and application of indoline derivative in medicine
-
Paragraph 0190; 0191; 0192; 0193, (2016/10/08)
The invention discloses an indoline derivative, or stereisomer, tautomer, nitric oxide, solvate, metabolite, pharmacy-acceptable salt or other prodrugs of the indoline derivative. The indoline derivative is used for resisting 5-HT6 receptors. The invention further relates to a method for preparing the compound and application of the compound in treating or preventing diseases related to 5-HT6 receptors.
AROMATIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS
-
Paragraph 00215, (2015/07/07)
Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and methods for using such compounds or pharmaceutical compositions thereof to treat Alzheimer's disease.
SULFONAMIDE DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF
-
Paragraph 00190, (2015/11/09)
Provided herein are sulfonamide derivatives or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and use of such compounds or pharmaceutical compositions thereof for managing or treating 5-HT6 receptor-mediated diseases, especially in the manufacture of a medicament for managing or treating Alzheimer's disease.
Synthesis and in vivo evaluation of [O-methyl-11C] N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl) benzenesulfonamide as an imaging probe for 5-HT6 receptors
Liu, Fei,Majo, Vattoly J.,Prabhakaran, Jaya,Milak, Matthew S.,John Mann,Parsey, Ramin V.,Dileep Kumar
, p. 5255 - 5259 (2011/10/09)
The serotonin receptor 6 (5-HT6) is implicated in the pathophysiology of cognitive diseases, schizophrenia, anxiety and obesity and in vivo studies of this receptor would be of value for studying the pathophysiology of these disorders. Therefor
