1190854-75-1

Upstream product

• 1190854-65-9 tert-butyl (3-bromo-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl)carbamate 
• 1190854-63-7 tert-butyl (6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl)carbamate 
• 1290127-90-0 C₆H₇N₃OS 
• 1190854-62-6 6-methoxypyrazolo[5,1-b][1,3]thiazole 
• 1190854-61-5 ethyl 6-methoxypyrazolo[5,1-b][1,3]thiazole-7-carboxylate 
• 1190854-60-4 ethyl 6-oxo-5,6-dihydropyrazolo[5,1-b][1,3]thiazole-7-carboxylate 
• 1190854-64-8 6-methoxypyrazolo[5,1-b]thiazole-7-carboxylic acid 
• 1190854-58-0 tert-butyl {3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl}carbamate 
• 1290127-88-6 C₂₀H₃₆O₈S₂ 
• 29943-42-8 Tetrahydro-4H-pyran-4-one 

Relevant academic research and scientific papers

Design, synthesis, and structure-activity relationships of novel pyrazolo[5,1-b]thiazole derivatives as potent and orally active corticotropin-releasing factor 1 receptor antagonists

This paper describes the design, synthesis, and structure-activity relationships of a novel series of 7-dialkylamino-3-phenyl-6-methoxy pyrazolo[5,1-b]thiazole derivatives for use as selective antagonists of the corticotropin-releasing factor 1 (CRF1) receptor. The most promising compound, N-butyl-3-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-6-methoxy-N- (tetrahydro-2H-pyran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine (6t), showed high affinity (IC50 = 70 nM) and functional antagonism (IC50 = 7.1 nM) for the human CRF1 receptor as well as dose-dependent inhibition of the CRF-induced increase in the plasma adrenocorticotropic hormone (ACTH) concentration at a dose of 30 mg/kg (po). Further, in the light/dark test in mice, the compound 6t showed anxiolytic activity at a dose of 30 mg/kg (po).

3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUNDS

A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.