864866-47-7

Upstream product

• 64169-34-2 5-bromophthalide 
• 75-31-0 isopropylamine 
• 78471-43-9 methyl 4-bromo-2-(bromomethyl)benzoate 
• 888030-75-9 N-isopropyl-4-bromo-2-hydroxymethylbenzamide 
• 99548-55-7 4-bromo-2-methyl-benzoic acid methyl ester 
• 68837-59-2 4-bromo-2-methylbenzoic acid 
• 888030-82-8 (5-bromo-3H-isobenzofuran-1-ylidene)-isopropyl-amine 

Downstream Products

• 1295301-37-9 1-(4-(2-isopropyl-1-oxoisoindolin-5-yl)benzyl)-3-methylimidazolidine-2,4-dione 

Relevant academic research and scientific papers

Efficient synthesis of 1,4-diaryl-5-methyl-1,2,3-triazole, a potential mglur1 antagonist, and the risk assessment study of arylazides

A concise and practical synthesis of a 1,4-diaryl-5-methyl-1,2,3-triazole is described. A mGluR1 antagonist 1 was prepared with one-pot operation by the Negishi coupling reaction between two building blocks, 5-bromophthalimidine (2) and 1-aryl-5-methyl-4-

Synthesis and biological evaluation of aryl isoxazole derivatives as metabotropic glutamate receptor 1 antagonists: A potential treatment for neuropathic pain

Glutamate is the major excitatory neurotransmitter and known to activate the metabotropic and ionotropic glutamate receptors in the brain. Among these glutamate receptors, metabotropic glutamate receptor 1 (mGluR1) has been implicated in various brain disorders including anxiety, schizophrenia and chronic pain. Several studies demonstrated that the blockade of mGluR1 signaling reduced pain responses in animal models, suggesting that mGluR1 is a promising target for the treatment of neuropathic pain. In this study, we have developed mGluR1 antagonists with an aryl isoxazole scaffold, and identify several compounds that are orally active in vivo. We believe that these compounds can serve as a useful tool for the investigation of the role of mGluR1 and a promising lead for the potential treatment of neuropathic pain.

Fused Pyrazoles as FGFR Inhibitors

The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: A potential treatment for psychotic disorders

We describe here the discovery and biological profile of a series of isoindolinone derivatives as developed mGluR1 antagonists. Our combined strategy of rapid parallel synthesis and conventional medicinal optimization successfully led to N-cyclopropyl 22 and N-isopropyl isoindolinone analogs 21 and 23 with improved in vivo DMPK profiles. Moreover the most advanced analog 23 showed an oral antipsychotic-like effect at a dose of 1 mg/kg in an animal model.

A short and efficient synthesis of isoindolin-1-ones

Here, we report a short and efficient synthesis of isoindolin-1-ones. Base-induced cyclization of o-hydroxymethyl-benzamides, which was easily prepared from the corresponding phthalides and amines, led predominantly to N-alkylation in good yield. The reaction proceeded under mild conditions and bromine and nitrile substituents were tolerated. The selectivity is explained by HASB theory. Georg Thieme Verlag Stuttgart.

DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE

The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X 1 represents oxygen atoms and the like, X 2 represents nitrogen atoms and the like, X 3 represents nitrogen atoms and the like, X 4 represents nitrogen atoms and the like, R 1 represents formula (II-1): wherein X 5 represents sulfur atoms and the like, A 1 represents carbon atoms and the like, A 2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.