911124-07-7

Upstream product

• 911124-06-6 (4-amino-3-fluoro-5-vinylbenzyl)carbamic acid t-butyl ester 
• 124-63-0 methanesulfonyl chloride 
• 953090-83-0 tert-butyl 3-fluoro-5-iodo-4-(methylsulfonamido)-benzylcarbamate 
• 7486-35-3 tri-n-butyl(vinyl)tin 

Downstream Products

• 1005172-74-6 N-(4-aminomethyl-2-fluoro-6-vinyl-phenyl)-methanesulfonamide hydrochloride 
• 1204387-46-1 tert-butyl 3-cyclopropyl-5-fluoro-4-(methylsulfonamido)benzylcarbamate 
• 911124-08-8 N-(4-aminomethyl-2-fluoro-6-vinylphenyl)methanesulfonamide 

Relevant academic research and scientific papers

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.

NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1 )antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.