Biotin tethered homotryptamine derivatives: High affinity probes of the human serotonin transporter (hSERT)
摘要:
Quantum dot conjugates of compounds capable of inhibiting the serotonin transporter (SERT) could form the basis of fluorescent probes for live cell imaging of membrane bound SERT. Additionally, quantum dot-SERT antagonist conjugates may be amenable to fluorescence-based, high-throughput assays for this transporter. This Letter describes the synthesis of SERT-selective ligands amenable to conjugation to quantum dots via a biotin-streptavidin binding interaction. SERT selectivity and affinity were incorporated into the ligand via a tetrahydropyridine or cyclohexylamine derivative and the affinity of these compounds for SERT was measured by their ability to produce SERT-dependent currents in Xenopus laveis oocytes. (C) 2011 Elsevier Ltd. All rights reserved.
Novel 2,4-Dianilinopyrimidine Derivatives, the Preparation Thereof, Their Use as Medicaments, Pharmaceutical Compositions and, in Particular, as IKK Inhibitors
The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Substituted benzamide compounds corresponding to formula (I)
in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
[EN] AZAINDOLE ACETIC ACID DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS D'ACIDE AZA-INDOL-ACÉTIQUE ET LEUR UTILISATION COMME MODULATEURS DES RÉCEPTEURS DE LA PROSTAGLANDINE D2
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2015140684A1
公开(公告)日:2015-09-24
The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
A compound of formula (I) is described: wherein R1 and R2 are as defined in the text and wherein the compounds are intended for use in treating medical conditions characterized by an imbalance in dopamine receptor activity.
CYCLOALKANE[B]AZAINDOLE ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
申请人:Hutchinson John Howard
公开号:US20100113503A1
公开(公告)日:2010-05-06
Described herein are compounds that are antagonists of PGD
2
receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD
2
receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD
2
-dependent or PGD
2
-mediated conditions or diseases.