1253197-29-3

Upstream product

• 81593-57-9 7-methoxy-3-(4-methylphenylsulfonyl)-2,3,4,5-tetrahydro-3-benzazepin-1-one 
• 2645-02-5 methyl tosylglycinate 
• 177259-98-2 2-[(3-(benzyloxy)phenyl)]ethan-1-ol 
• 2039-67-0 2-(3-methoxyphenyl)-1-ethanamine 
• 98-59-9 p-toluenesulfonyl chloride 
• 1253197-27-1 7-hydroxy-3-(4-tosyl)-2,3,4,5-tetrahydro-3-benzazepine-1-one 
• 64880-89-3 N-[(3-methoxyphenyl)ethyl]-4′′-methylbenzenesulfonamide 
• 1253197-28-2 7-benzyloxy-3-(4-tosyl)-2,3,4,5-tetrahydro-3-benzazepine-1-one 

Downstream Products

• 1253197-26-0 (+/-)-7-benzyloxy-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-30-6 (+/-)-WMS-1418 
• 1253197-31-7 (+/-)-7-benzyloxy-3-[3-(phenylsulfonyl)propyl]-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-32-8 (+/-)-7-benzyloxy-3-[3-(phenylsulfanyl)propyl]-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-33-9 (+/-)-7-(benzyloxy)-3-(3-[2-(4-fluorophenyl)-5,5-dimethyl-1,3-dioxan-2-yl]propyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-34-0 (+/-)-trans-7-(benzyloxy)-3-(4-phenylcyclohexyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-35-1 (+/-)-cis-7-(benzyloxy)-3-(4-phenylcyclohexyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1257108-44-3 (+/-)-7-(benzyloxy)-3-(3-phenylbenzyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-37-3 (+/-)-7-benzyloxy-3-(1,4-dioxaspiro[4.5]decan-8-yl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 
• 1253197-38-4 (+/-)-WMS-1410 
• 1253197-39-5 (+/-)-N-benzyl-2-[7-(benzyloxy)-1-hydroxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl]-N-methylacetamide 
• 1253197-40-8 (+/-)-N-benzyl-2-(1,7-dihydroxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl)-N-methylacetamide 
• 1253197-41-9 (+/-)-cis-3-(4-phenylcyclohexyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-1,7-diol 
• 1253197-43-1 (+/-)-7-benzyloxy-3-(3-phenoxypropyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol 

Relevant academic research and scientific papers

Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies

To analyze the N-methyl-d-aspartate (NMDA) receptor distribution in the central nervous system, fluorinated ligands that selectively address the ifenprodil binding site of GluN2B-subunit-containing NMDA receptors were developed. Various strategies to introduce a fluorine atom into the potent GluN2B ligand 2 (3-(4-phenylbutyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1,7-diol) were pursued, including replacement of the benzylic OH moiety with a fluorine atom (13) and introduction of fluoroethoxy moieties at various positions (14 (7-position), 17 (9-position), 18a–c (1-position)). With respect to GluN2B affinity and selectivity over related receptors, the fluoroethoxy derivatives 14 and 18a are the most promising ligands. Radiosynthesis of fluoroethoxy derivative [18F]14 was performed by nucleophilic substitution of the phenol 2 with 2-[18F]fluoroethyl tosylate. On rat brain slices the fluorinated PET tracer [18F]14 accumulated in regions with high density of NMDA receptors containing GluN2B subunits. The bound radioactivity could not be replaced by (S)-glutamate. However, the GluN2B ligands eliprodil, Ro 25-6981, and the non-labeled 3-benzazepine 14 were able to abolish the specific binding of [18F]14.

NR2B SELECTIVE NMDA-RECEPTOR ANTAGONISTS FOR TREATMENT OF IMMUNE-MEDIATED INFLAMMATORY DISEASES

The present invention provides novel means and methods for treatment auf immunemediated inflammatory diseases.

Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols

NR2B selective NMDA receptor antagonists with tetrahydro-3-benzazepine-1,7- diol scaffold have been designed by formal cleavage and reconstitution of the piperidine ring of the lead compound ifenprodil (1). The secondary amine 10 represents the central bu

NR2B-SELECTIVE NMDA-RECEPTOR ANTAGONISTS

The present invention relates to compounds according to general formula (I) and pharmaceutical compositions comprising compounds according to general formula (I).