191352-28-0

Upstream product

• 14703-72-1 2-(methylamino)-4-nitrophenol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 70886-35-0 N-(2-hydroxy-5-nitrophenyl)formamide 
• 99-57-0 2-hydroxy-5-nitroaniline 

Downstream Products

• 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 
• 191352-30-4 (2S,3S,4S,5R,6S)-2-(methoxycarbonyl)-6-(2-(methylamino)-4-nitrophenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate 
• 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 
• 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 
• 191352-31-5 (2S,3S,4S,5R,6S)-3,4,5-Triacetoxy-6-[2-({4-[bis-(2-chloro-ethyl)-amino]-phenoxycarbonyl}-methyl-amino)-4-nitro-phenoxy]-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.

Prodrugs for the therapy of tumors and inflammatory disorders

Compounds of the formula Iglycosyl-Y[--C( Y)--X--] p --W(R) n --Z--C( Y)-active compound (I)are described which are suitable for the treatment of carcinomatous diseases, autoimmune diseases and chronic inflammatory diseases such as rheumatoid arthritis.

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