5900-13-0

Usage

Uses

Used in Pharmaceutical Industry:
5-BROMO-3-METHOXYPYRAZIN-2-YLAMINE is used as a chemical intermediate for the development of N-pyrazinylbenzenesulfonamides, which are crucial in the treatment of chemokine mediated diseases such as asthma. Its role in the synthesis process is vital for creating effective medications that can help manage and alleviate the symptoms of these conditions.

InChI:InChI=1/C5H6BrN3O/c1-10-5-4(7)8-2-3(6)9-5/h2H,1H3,(H2,7,8)

Upstream product

• 124-41-4 sodium methylate 
• 24241-18-7 2-amino-3,5-dibromopyrazine 
• 67-56-1 methanol 
• 4774-10-1 2-amino-3-methoxypyrazine 
• 87444-39-1 5-bromo-3-methylsulfonylpyrazin-2-amine 

Downstream Products

• 94139-36-3 4-amino-N-(5-bromo-3-methoxy-pyrazin-2-yl)-benzenesulfonamide 
• 95516-10-2 4-acetylamino-N-(5-bromo-3-methoxy-pyrazin-2-yl)-benzenesulfonamide 
• 4774-10-1 2-amino-3-methoxypyrazine 
• 566203-88-1 2,3-dichloro-N-(3-methoxypyrazin-2-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Synthesis and cytotoxicity evaluation of novel indolylpyrimidines and indolylpyrazines as potential antitumor agents

Novel indolylpyrimidines and indolylpyrazines have been synthesized as potential antitumor agents. They were screened in a panel of 60 human tumor cell lines in vitro. Compounds 7, 9, 10, 15, 21 exhibited efficiently cytotoxic activities with GI50 values in the low micromolar range against a variety of human cancer cell lines. 2,4-Bis(3′-indolyl)pyrimidine 8 displayed selective cytotoxic activity against IGROV1 tumor cell line with the GI50 value below 0.01 μM.

INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS

Provided herein are compounds of formula (V) that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.

Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators

The evolution of gamma-secretase modulators (GSMs) through the introduction of novel heterocycles with the goal of aligning activity for reducing the levels of Aβ42 and properties consistent with a drug-like molecule are described. The insertion of a methoxypyridine motif within the tetracyclic scaffold provided compounds with improved activity for arresting Aβ42 production as well as improved properties, including solubility. In vivo pharmacokinetic analysis demonstrated that several compounds within the novel series were capable of crossing the BBB and accessing the therapeutic target. Treatment with methoxypyridine-derived compound 64 reduced Aβ42 levels in the plasma of J20 mice, in addition to reducing Aβ42 levels in the plasma and brain of Tg2576 mice.

PYRIDINYL AND PYRAZINYL-(AZA)INDOLSULFONAMIDES

The present invention relates to pyridinyl and pyrazinyl-(aza)indolsulfonamides having GPR17 modulator activity. The compounds have utility in the treatment of a variety of GPR17-associated disorders.

Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists

N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent sta

Carbonylation as a novel method for the assembly of pyrazine based oligoamide alpha-helix mimetics

The design and synthesis of oligoamide α-helix peptidomimetics is reported. The oligoamide type systems are prepared in a modular fashion by coupling the monomers using palladium-catalyzed carbonylation chemistry. This enabled us to use substrates with a low nucleophilicity, leading to previously unreported pyrazine based oligoamide α-helix mimetics. The proof of principle is given by synthesizing a small set of compounds. Various end-capping groups were introduced and also a mixed multimer was successfully prepared.

N-SUBSTITUTED 4-AMINOPHENOLS AND CORRESPONDING QUINONE IMINES

Compounds of formula I or formula II, wherein Q1Q3 and R1-R5 are as defined in the claims, exhibit CytC derived peroxidase inhibiting activity and are thus useful as CytC derived peroxidase inhibiting agents.

Necrosulfonamide inhibits necroptosis by selectively targeting the mixed lineage kinase domain-like protein

Through high-throughput screening of 200000 compounds and subsequent structure-activity relationship (SAR) studies we identified necrosulfonamide (NSA) as a potent small molecule inhibitor for necroptosis, induced by a combination of TNF-a, Smac mimetic, and z-VAD-fmk (T/S/Z). Applying a forward chemical genetic approach, we utilized an NSA based chemical probe to further reveal that NSA selectively targeted the Mixed Lineage Kinase Domain-like Protein (MLKL) to block the necrosome formation.

Novel Heterocyclic Compounds and Uses Thereof

New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

NOVEL HETEROCYCLIC COMPOUNDS AND USES THEROF

New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.