92260-32-7

Upstream product

• 42869-47-6 6-bromo-2-methyl-1H-imidazo[4,5-b]pyridine 
• 74-88-4 methyl iodide 
• 70232-59-6 5-bromo-N-methyl-3-nitropyridin-2-amine 
• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 89415-54-3 5-bromo-N²-methylpyridine-2,3-diamine 
• 78-39-7 Triethyl orthoacetate 
• 1445-45-0 Trimethyl orthoacetate 
• 41231-05-4 2,3-Dimethylimidazo<4,5-b>pyridine 

Relevant academic research and scientific papers

OGA INHIBITOR COMPOUNDS

The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.

THERAPEUTIC COMPOUNDS

Compounds disclosed herein including compounds of formula I′: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

INHIBITORS OF HIV REPLICATION

Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.

1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES

The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c] quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H- imidazo[4,5-c] quinofinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c] quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H- imidazo[4,5-c] quinolinone derivatives; and a process for the preparation of the novel 1H- imidazo[4,5-c] quinolinone derivatives.

Halogenation of 2-unsubstituted and 2-methylimidazo[4,5-b]pyridine derivatives

Halogenation of 2-unsubstituted and 2-methylimidazo[4,5-b]pyridines and their N-methyl derivatives with bromine and chlorine in acetic acid takes different pathways, depending on the acetic acid concentration. The bromination in 50% aqueous acetic acid gives only 6-bromoimidazo[4,5-b]pyridines; bromination and chlorination of 2-unsubstituted imidazo[4,5-b]pyridines in glacial acetic acid leads to 5,6-dibromo(dichloro)imidazo[4,5-b]pyridin-2-ones, and bromination of 2-methylimidazo[4,5-b]pyridines in glacial acetic acid involves both the pyridine ring and the 2-methyl group to afford the corresponding 6-bromo-2-tribromomethylimidazo[4,5-b]pyridines.