55656-32-1

Upstream product

• 140-89-6 potassium ethyl xanthogenate 
• 20348-16-7 2-amino-3-hydroxy-6-methylpyridine 
• 15128-90-2 6-methyl-2-nitropyridin-3-ol 
• 75-15-0 carbon disulfide 

Downstream Products

• 78757-34-3 1-Cyclohexyl-3-(3-hydroxy-6-methyl-pyridin-2-yl)-thiourea 
• 78771-20-7 N-(6-Methyl-3-hydroxy-2-pyridyl)-N-benzylthiourea 

Relevant academic research and scientific papers

Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria

The discovery and development of new antibiotics capable of curing infections due to multidrug-resistant and pandrug-resistant Gram-negative bacteria are a major challenge with fundamental importance to our global healthcare system. Part of our broad program at Novartis to address this urgent, unmet need includes the search for new agents that inhibit novel bacterial targets. Here we report the discovery and hit-to-lead optimization of new inhibitors of phosphopantetheine adenylyltransferase (PPAT) from Gram-negative bacteria. Utilizing a fragment-based screening approach, we discovered a number of unique scaffolds capable of interacting with the pantetheine site of E. coli PPAT and inhibiting enzymatic activity, including triazolopyrimidinone 6. Structure-based optimization resulted in the identification of two lead compounds as selective, small molecule inhibitors of bacterial PPAT: triazolopyrimidinone 53 and azabenzimidazole 54 efficiently inhibited E. coli and P. aeruginosa PPAT and displayed modest cellular potency against the efflux-deficient E. coli ΔtolC mutant strain.

ANTIPRURITIC AGENT

An antipruritic which exerts an antipruritic effect based on a novel action mechanism and is effective for pruritus. The antipruritic contains as an effective ingredient a compound which activates a central type nicotinic acetylcholine receptor.

NOVEL PIPERAZINES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF

Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are phannaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.

AZABENZOXAZOLES FOR THE TREATMENT OF CNS DISORDERS

The present invention relates to a7 nicotinic receptor agonists of formula (la) or (lb) as described herein and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal an a7 nicotinic receptor agonist of formula (la) or (lb). It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant a7nicotinic receptor agonist of formula (la) or (lb).

Anilide compounds and drugs containing the same

The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or Ar represents an aryl group which may or may not have a substituent; X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15. The inventive compounds are useful in the form of pharmaceutical composition, specifically as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitor.

Pharmaceutical compositions for CNS and other disorders

The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist.

PREPARATION OF 5-METHYL-3H-OXAZOLOPYRIDINE-2-THIONE AND ITS REACTION WITH AMINES

5-Methyl-3H-oxazolopyridine-2-thione, which exists in the dipolar form, was obtained by the reaction of 6-methyl-2-amino-3-hydroxypyridine with potassium ethylxanthate.The reaction of the product with amines leads to the corresponding thioureas.