191352-30-4

Upstream product

• 70886-35-0 N-(2-hydroxy-5-nitrophenyl)formamide 
• 21085-72-3 1-bromo-2,3,4-tri-O-acetyl-α-D-glucuronic acid methyl ester 
• 7355-18-2 (2S,3S,4S,5R,6S)-3,4,5,6-Tetraacetoxy-tetrahydro-pyran-2-carboxylic acid methyl ester 
• 191352-28-0 tert-butyl (2-hydroxy-5-nitrophenyl)(methyl)carbamate 
• 14703-72-1 2-(methylamino)-4-nitrophenol 
• 191352-29-1 (2S,3R,4S,5S,6S)-2-(2-((tert-butoxycarbonyl)(methyl)amino)-4-nitrophenoxy)-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate 

Downstream Products

• 355010-32-1 2-methylamino-4-nitrophenyl-β-D-glucopyranosiduronic acid 
• 496916-62-2 methyl {2-[({2-fluoro-4-[bis(2-chloroethyl)amino]phenoxy}carbonyl)methylamino]-4-nitrophenyl 2,3,4-tri-O-acetyl-β-D-glucopyranosid}uronate 
• 355010-40-1 2-methylamino-4-nitrophenyl-2,3,4-tri-O-(tert-butyldimethylsilyl)-β-D-glucopyranosiduronic acid 
• 355010-36-5 benzyl [2-methylamino-4-nitrophenyl-2,3,4-tri-O-(tert-butyldimethylsilyl)-β-D-glucopyranoside]uronate 
• 355010-37-6 benzyl [2-(N-chloroformyl-N-methylamino)-4-nitrophenyl-2,3,4-tri-O-(tert-butyldimethylsilyl)-β-D-glucopyranoside]uronate 
• 355010-33-2 2-(trimethylsilyl)ethyl [2-methylamino-4-nitrophenyl-2,3,4-tri-O-(tert-butyldimethylsilyl)-β-D-glucopyranoside]uronate 
• 355010-34-3 2-(trimethylsilyl)ethyl [2-(N-chloroformyl-N-methylamino)-4-nitrophenyl-2,3,4-tri-O-(tert-butyldimethylsilyl)-β-D-glucopyranoside]uronate 
• 191352-27-9 (2S,3S,4S,5R,6S)-6-[2-({4-[Bis-(2-chloro-ethyl)-amino]-phenoxycarbonyl}-methyl-amino)-4-nitro-phenoxy]-3,4,5-trihydroxy-tetrahydro-pyran-2-carboxylic acid 
• 191352-32-6 (2S,3S,4S,5R,6S)-6-[2-({4-[Bis-(2-chloro-ethyl)-amino]-phenoxycarbonyl}-methyl-amino)-4-nitro-phenoxy]-3,4,5-trihydroxy-tetrahydro-pyran-2-carboxylic acid methyl ester 

Relevant academic research and scientific papers

BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF

It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.

GLUCURONIDE PRODRUGS OF TOFACITINIB

The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula (I): (Formula (I)) where A1 and R1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

GLUCURONIDE PRODRUGS OF JANUS KINASE INHIBITORS

The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: where W1, R1 and A1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

Glucuronide prodrugs of hydroxy compounds for antibody directed enzyme prodrug therapy (adept): A phenol nitrogen mustard carbamate

A prodrug consisting of a β-D-glucuronic acid linked to a self-immolative spacer (a N-(ortho-hydroxyphenyl)-N-methylcarbamate) and a phenolic nitrogen mustard was synthesised. As this prodrug was easily cleaved by a β-glucuronidase enzyme and displayed lo