1074764-35-4

Upstream product

• 221185-05-3 (3S)-N,N-dibenzyl-5-(4-methylpiperazin-1-yl)chroman-3-amine 
• 1369501-50-7 (S)-N,N-dibenzyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)chroman-3-amine 
• 1369501-48-3 (3S)-3-[(tert-butoxycarbonyl)amino]-3,4-dihydro-2H-chromen-5-yl trifluoromethanesulfonate 
• 221360-35-6 (3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-amine 
• 851175-96-7 2-(2,4-dimethylphenyl)-5-methyl-2H-1,2,3-triazole-4-carboxylic acid 
• 1369922-92-8 (3S)-3-amino-3,4-dihydro-2H-chromen-5-ol 

Relevant academic research and scientific papers

Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers

Recent findings showing a relation between mutations in the Na V1.7 channel in humans and altered pain sensation has contributed to increase the attractiveness of this ion channel as target for development of potential analgesics. Amido chromanes 1 and 2 were identified as blockers of the NaV1.7 channel and analogues with modifications of the 5-substituent and the carboxamide part of the molecule were prepared to establish the structure-activity relationship. Compounds 13 and 29 with good overall in vitro and in vivo rat PK profile were identified. Furthermore, 29 showed in vivo efficacy in a nociceptive pain model.

NEW COMPOUNDS 807

The present invention relates to new compounds. The present invention relates to new compounds, to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.