1290127-51-3

Upstream product

• 1290127-88-6 C₂₀H₃₆O₈S₂ 
• 1190854-58-0 tert-butyl {3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl}carbamate 
• 1190854-64-8 6-methoxypyrazolo[5,1-b]thiazole-7-carboxylic acid 
• 1190854-60-4 ethyl 6-oxo-5,6-dihydropyrazolo[5,1-b][1,3]thiazole-7-carboxylate 
• 1190854-61-5 ethyl 6-methoxypyrazolo[5,1-b][1,3]thiazole-7-carboxylate 
• 1190854-62-6 6-methoxypyrazolo[5,1-b][1,3]thiazole 
• 1383482-44-7 C₂₀H₂₅N₃O₄S 
• 1383482-51-6 4-hydroxytetrahydro-2H-pyran-4-carbaldehyde 
• 1290127-90-0 C₆H₇N₃OS 
• 1190854-63-7 tert-butyl (6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl)carbamate 
• 1190854-65-9 tert-butyl (3-bromo-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl)carbamate 

Downstream Products

• 1290127-52-4 N-(cyclopropylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-N-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-amine 
• 1290127-53-5 cyclopropylmethyl-(3,6-dihydro-2H-pyran-4-ylmethyl)-[3-(2,6-dimethoxy-4-methoxymethyl-phenyl)-6-methoxy-pyrazolo[5,1-b][1,3]thiazol-7-yl]-amine 

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).

PYRAZOLOTHIAZOLE COMPOUND

A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C 1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group