1609393-90-9

Basic information

• Product Name: 2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline
• Synonyms: 2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline
• CAS NO: 1609393-90-9
• Molecular Weight: 249.118
• Mol File: 1609393-90-9.mol
• Article Data: 14

Chemical Properties

• CAS DataBase Reference: 2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline(CAS DataBase Reference)
• NIST Chemistry Reference: 2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline(1609393-90-9)
• EPA Substance Registry System: 2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline(1609393-90-9)

Safety Data

• Hazardous Substances Data: 1609393-90-9(Hazardous Substances Data)

Upstream product

• 13073-25-1 2-bromo-6-nitro-phenol 
• 98775-19-0 2-bromo-6-nitrophenyl methyl ether 
• 116557-46-1 3-bromo-2-methoxyphenylamine 
• 73183-34-3 bis(pinacol)diborane 
• 28165-50-6 2-amino-6-bromophenol 

Relevant articles and documents

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2

A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clinical Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-membered heteroaryl groups in place of the N-methyl triazolyl moiety in 6. The X-ray co-crystal structure of an early lead (12) revealed a potential new binding pocket. Exploration of the new pocket resulted in two frontrunners for a clinical candidate. The potential hydrogen bonding interaction with Thr599 in the pocket was achieved with a tertiary amide moiety, confirmed by the X-ray co-crystal structure of 29. When the diversity search was extended to nicotinamides, a single fluorine atom addition was found to significantly enhance the permeability, which directly led to the discovery of 7 (BMS-986202) as a clinical Tyk2 inhibitor that binds to Tyk2 JH2. The preclinical studies of 7, including efficacy studies in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus, will also be presented.

SUBSTITUTED PYRIDINES FOR THE TREATMENT OF INFLAMMATORY DISEASES

Compounds having the structure of Formula (I) or pharmaceutically acceptable isomers, racemates, hydrates, solvates or salts thereof, where A, R1, R2a, R2b, R2c and R3 are as defined herein, are usefu

SUBSTITUTED N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE OR N-(METHYL-D3)-NICOTINAMIDE COMPOUNDS AS IL-12, IL-23 AND/OR IFNALPHA MODULATORS

There are disclosed compounds of the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating inflammatory and autoimmune diseases or disorders.