141642-82-2Relevant articles and documents
Discovery of β-Arrestin Biased Ligands of 5-HT7R
Kim, Youngjae,Kim, Hyunguk,Lee, Jieon,Lee, Jae Kyun,Min, Sun-Joon,Seong, Jihye,Rhim, Hyewhon,Tae, Jinsung,Lee, Hyunjoo Jenny,Choo, Hyunah
, p. 7218 - 7233 (2018)
Though many studies have been published about therapeutic potentials of selective 5-HT7R ligands, there have been few biased ligands of 5-HT7R. The development of potent and selective biased ligands of 5-HT7R would be of great help in understanding the relationship between pharmacological effects and G protein/β-arrestin signaling pathways of 5-HT7R. In order to identify 5-HT7R ligands with biased agonism, we designed and synthesized a series of tetrahydroazepine derivatives 1 and 2 with arylpyrazolo moiety or arylisoxazolo moiety. Through several biological evaluations such as binding affinity, selectivity profile, and functions in G protein and β-arrestin signaling pathways, 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine 1g was discovered as the β-arrestin biased ligand of 5-HT7R. In an electroencephalogram (EEG) test, 1g increased total non-rapid eye movement (NREM) sleep time and decreased total rapid eye movement (REM) sleep time.
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT7/2 inhibitors leading to the identification of a clinical candidate
Dvorak, Curt A.,Rudolph, Dale A.,Nepomuceno, Diane,Dvorak, Lisa,Lord, Brian,Fraser, Ian,Bonaventure, Pascal,Lovenberg, Timothy,Carruthers, Nicholas I.
supporting information, (2020/12/07)
We report here the synthesis and characterization of a dual 5-HT7 / 5-HT2 receptor antagonist 3-(4-Fluoro-phenyl)-2-isopropyl-2,4,5,6,7,8-hexahydro-1,2,6-triaza-azulene (4j). 4j is a high affinity 5-HT7 and 5-HT2A/su
PYRIMIDINE-BASED BICYCLES AS ANTIVIRAL AGENTS FOR THE TREATMENT AND PREVENTION OF HIV INFECTION
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Page/Page column 72; 73; 78-79; 81-83; 85-86; 88-89; 91-94; 96; ..., (2021/08/27)
This invention relates to pyrimidine derivatives, having HIV replication inhibiting. The present invention provides new pyrimidine compounds, designed for the treatment and prevention of HIV-mediated diseases. The invention further relates to pharmaceutical compositions and drugs contained in them. The invention also relates to the use of abovementioned compounds for the treatment and/or prevention of HIV in subjects with HIV-infection (human immunodeficiency virus) or having risk of getting HIV-infection.
DISUBTITUTED AZETIDINES, PYRROLIDINES, PIPERIDINES AND AZEPANES AS INHIBITORS OF MONOAMINE OXIDASE B FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Page/Page column 19, (2018/04/20)
This invention relates to new inhibitors of MAO-Bwith the general formula I, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the alleviation of symptoms and treatment of acute and chronic neurological disorders, cognitive and neurodegenerative diseases.