1313236-75-7

Upstream product

• 16136-52-0 4-cyanoindole 
• 98-59-9 p-toluenesulfonyl chloride 
• 31271-86-0 1-[(4-methylphenyl)sulfonyl]-1H-indole-4-carbonitrile 
• 1145678-74-5 (1-tosyl-1H-indol-4-yl)methanamine 
• 1313236-71-3 tert-butyl 4-allyl-4-((1-tosyl-1H-indol-4-yl)methylamino)piperidine-1-carboxylate 
• 1313236-73-5 tert-butyl 4-allyl-4-(N-((1-tosyl-1H-indol-4-yl)methyl)acrylamido)piperidine-1-carboxylate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Downstream Products

• 1313236-98-4 9-(benzo[d]oxazol-2-yl)-1-((1-tosyl-1H-indol-4-yl)methyl)-1,9-diazaspiro[5.5]undecan-2-one 
• 1313236-77-9 tert-butyl 2-oxo-1-((1-tosyl-1H-indol-4-yl)methyl)-1,9-diazaspiro[5.5]undecane-9-carboxylate 
• 1313236-80-4 1-((1-tosyl-1H-indol-4-yl)methyl)-1,9-diazaspiro[5.5]undecan-2-one trifluoroacetate 
• 1313236-82-6 9-(quinoxalin-2-yl)-1-((1-tosyl-1H-indol-4-yl)methyl)-1,9-diazaspiro[5.5]undecan-2-one 
• 1373766-35-8 9-(4,6-dimethylpyrimidin-2-yl)-1-((1-tosyl-1Hindol-4-yl)methyl)-1,9-diazaspiro[5.5]undecan-2-one 

Relevant academic research and scientific papers

Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia

Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep disorders in several recent clinical trials in volunteers and primary insomnia patients. The relative contribution of antagonism of OX1R and OX2R for sleep induction is still a matter of debate. We therefore initiated a drug discovery project with the aim of creating both OX2R selective antagonists and DORAs. Here we report that the OX 2R selective antagonist 26 induced sleep in mice primarily by increasing NREM sleep, whereas the DORA suvorexant induced sleep largely by increasing REM sleep. Thus, OX2R selective antagonists may also be beneficial for the treatment of insomnia.

Diaza-spiro[5.5]undecanes

The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS

The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

DIAZA-SPIRO[5.5]UNDECANES AS OREXIN RECEPTOR ANTAGONISTS

The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.