911124-05-5

Upstream product

• 849353-46-4 4-amino-3-fluoro-5-iodo-benzonitrile 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1165739-58-1 4-(aminomethyl)-2-fluoro-6-iodoaniline hydrochloride 

Downstream Products

• 911124-06-6 (4-amino-3-fluoro-5-vinylbenzyl)carbamic acid t-butyl ester 
• 953090-83-0 tert-butyl 3-fluoro-5-iodo-4-(methylsulfonamido)-benzylcarbamate 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists

We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC50 of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described.

Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists

Structural optimization of multiple H-bonding region and structure-activity relationship of diarylalkyl amides/thioamides as novel TRPV1 antagonists are described. In particular, we identified amide 34o and thioamides 35o and 35r, of which antagonistic activities were highly enhanced by an incorporation of cyano or vinyl-substituent to the multiple H-bonding region. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron with IC50s of 25, 32 and 28 nM, respectively.

Novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and a pharmaceutical composition containing the same

This present invention relates to compounds of formula (I), in which R3 represents C2-C5 alkenyl or C2-C5 alkynyl and the other variables are as defined in the claims, isomers thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonists; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating pain, inflammatory disease of the joints, urinary bladder hypersensitivity including urinary incontinence, stomach duodenal ulcer, irritable bowel syndrome, inflammatory bowel disease, neurotic/allergic/inflammatory skin disease, psoriasis, asthma, chronic obstructive pulmonary disease, pruritus or prurigo.