445441-58-7

Upstream product

• 366-99-4 3-fluoro-4-methoxyaniline 
• 321-17-5 1-bromo-4,5-difluoro-2-nitrobenzene 
• 445441-57-6 1-bromo-4-fluoro-5-methoxy-2-nitrobenzene 
• 348-61-8 1-bromo-3,4-difluorobenzene 

Downstream Products

• 661463-25-8 5-({[2-bromo-5-fluoro-4-(methyloxy)phenyl]amino}methylidene)-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 864292-37-5 2,4-dichloro-7-fluoro-6-methoxyquinazoline 
• 1279093-79-6 C₁₈H₂₄FNO₃ 
• 1279093-80-9 C₂₀H₂₃F₄NO₄ 

Relevant academic research and scientific papers

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase

G9a-like protein (GLP) and G9a are highly homologous protein lysine methyltransferases (PKMTs) sharing approximately 80% sequence identity in their catalytic domains. GLP and G9a form a heterodimer complex and catalyze mono- and dimethylation of histone H3 lysine 9 and nonhistone substrates. Although they are closely related, GLP and G9a possess distinct physiological and pathophysiological functions. Thus, GLP or G9a selective small-molecule inhibitors are useful tools to dissect their distinct biological functions. We previously reported potent and selective G9a/GLP dual inhibitors including UNC0638 and UNC0642. Here we report the discovery of potent and selective GLP inhibitors including 4 (MS0124) and 18 (MS012), which are >30-fold and 140-fold selective for GLP over G9a and other methyltransferases, respectively. The cocrystal structures of GLP and G9a in the complex with either 4 or 18 displayed virtually identical binding modes and interactions, highlighting the challenges in structure-based design of selective inhibitors for either enzyme.

N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR

The present invention relates to the use compounds of formula I which are antagonists of the 5-HT 6 receptor, for treating a cognitive disorder selected from the group consisting of age-related cognitive decline, mild cognitive impairment and dementia

HSP-90 BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND THEIR USE IΝ THE TREATMENT AND PREVENTION OF FUNGAL INFECTIONS

The invention relates to therapeutic compounds that bind to HSP90. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating or preventing fungal infections.

HSP-90 BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND THEIR USE FN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES

The invention relates to therapeutic compounds that bind to HSP90. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating diseases and disorders such as cancer, autoimmune disease and other diseases.

AMINOCYCLOHEXENE QUINOLINES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY

Cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.