62492-54-0

Upstream product

• 7033-50-3 6-chloro-2-methyl-4H-benzo[d][1,3]oxazin-4-one 
• 5922-60-1 2-amino-5-chlorobenzonitrile 
• 2398-37-0 3-methoxyphenyl bromide 
• 635-21-2 5-chloroanthranilic acid 
• 62492-51-7 2-Acetylamino-5-chlor-3'-methoxy-benzophenon 

Downstream Products

• 62492-51-7 2-Acetylamino-5-chlor-3'-methoxy-benzophenon 
• 1332665-18-5 (RS)-3-(6-chloro-2-methyl-3-(2-(piperidin-1-yl)ethyl)-3,4-dihydroquinazolin-4-yl)phenol 
• 1332662-77-7 (RS)-6-chloro-4-(3-methoxyphenyl)-2-methyl-3-(2-(piperidin-1-yl)ethyl)-3,4-dihydroquinazoline 
• 1332673-50-3 C₂₃H₂₈ClN₃O₂ 
• 62492-58-4 2-amino-5-chloro-3'-hydroxybenzophenone 

Relevant academic research and scientific papers

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: Discovery, synthesis, and characterization of their binding mode by protein crystallography

Trypanothione reductase (TryR) is a genetically validated drug target in the parasite Trypanosoma brucei, the causative agent of human African trypanosomiasis. Here we report the discovery, synthesis, and development of a novel series of TryR inhibitors based on a 3,4-dihydroquinazoline scaffold. In addition, a high resolution crystal structure of TryR, alone and in complex with substrates and inhibitors from this series, is presented. This represents the first report of a high resolution complex between a noncovalent ligand and this enzyme. Structural studies revealed that upon ligand binding the enzyme undergoes a conformational change to create a new subpocket which is occupied by an aryl group on the ligand. Therefore, the inhibitor, in effect, creates its own small binding pocket within the otherwise large, solvent exposed active site. The TryR-ligand structure was subsequently used to guide the synthesis of inhibitors, including analogues that challenged the induced subpocket. This resulted in the development of inhibitors with improved potency against both TryR and T. brucei parasites in a whole cell assay.

SULPHONAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Disclosed are compounds having the general formula (I) as defined herein, the preparation thereof, and the use thereof for the prophylaxis or treatment of any disease involving a dysfunction associated with the orexin 2 receptor such as obesity, appetite or taste disorders including cachexia, anorexia and bulimia, diabetes, metabolic syndromes, vomiting and nausea, depression and anxiety, addictions, mood and behaviour disorders, schizophrenia, sleep disorders, restless legs syndrome, memory learning disorders, sexual and psychosexual dysfunctions, pain, visceral or neuropathic pain, hyperalgesia, allodynia, digestive disorders, irritable bowel syndrome, neuronal degenerescence, ischaemic or haemorrhagic attacks, Cushing's disease, Guillain-Barré syndrome, myotonic dystrophy, urinary incontinence, hyperthyroidism, pituitary function disorders, hypertension or hypotension.

Compounds and methods for inhibiting mitotic progression

This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treat