34682-99-0

Usage

Synthesis Reference(s)

Journal of Heterocyclic Chemistry, 11, p. 199, 1974 DOI: 10.1002/jhet.5570110217Synthesis, p. 301, 1975 DOI: 10.1055/s-1975-23738

InChI:InChI=1/C5H4N4OS/c10-5-8-4(11)7-3-1-2-6-9(3)5/h1-2H,(H2,7,8,10,11)

Upstream product

• 34683-00-6 ethyl N-[(1H-pyrazol-5-yl)carbamothioyl]carbamate 
• 1820-80-0 3-aminopyrazole 
• 16182-04-0 Ethoxycarbonyl isothiocyanate 
• 34683-00-6 N-[(1H-pyrazol-3-ylamino)thioxomethyl]carbamic acid ethyl ester 

Downstream Products

• 54346-18-8 2-(methylsulfanyl)-3H-pyrazolo[1,5-a][1,3,5]triazin-4-one 
• 54346-19-9 4-chloro-2-methylthiopyrazolo(1,5-a)-1,3,5-triazine 
• 1162654-55-8 4-(N-methyl-N-phenylamino)-2-(methylsulfonyl)pyrazolo[1,5-a]-1,3,5-triazine 
• 1358769-17-1 C₁₉H₂₆N₆O₂ 
• 1358769-19-3 C₂₄H₂₅Br₂N₇O 
• 1358769-23-9 C₂₄H₂₄Br₂ClN₇O 
• 54346-35-9 8-bromo-2-(methylsulfanyl)pyrazolo[1,5-a][1,3,5]triazin-4-ol 
• 54346-33-7 8-bromo-2-(methylthio)-4-chloropyrazolo<1,5-a>-1,3,5-triazine 
• 54346-18-8 2-(methylsulfanyl)pyrazolo[1,5-a][1,3,5]triazin-4-ol 
• 54346-35-9 8-bromo-2-(methylsulfanyl)pyrazolo[1,5-a][1,3,5]triazin-4(3H)-one 
• 1313036-71-3 4-(3-aminophenoxy)-N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a][1,3,5]triazin-2-amine 
• 1313036-70-2 N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)-4-(3-nitrophenoxy)pyrazolo[1,5-a][1,3,5]triazin-2-amine 

Relevant academic research and scientific papers

PYRAZOLOTRIAZINES

The present invention provides compounds of general formula (I), in which X, R1, R2 and R3 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.

IMIDAZOTRIAZINES ACTING ON CANCER VIA INHIBITION OF CDK12

The present invention provides compounds of general formula (I): in which X, R1, R2 and R3 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.

PYRAZOLOPYRAZINES ACTING ON CANCERS VIA INHIBITION OF CDK12

The present invention provides compounds of general formula (I) in which X, R1, R2 and R3 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.

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Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action

Despite the availability of hundreds of antibiotic drugs, infectious diseases continue to remain one of the most notorious health issues. In addition, the disparity between the spread of multidrug-resistant pathogens and the development of novel classes of antibiotics exemplify an important unmet medical need that can only be addressed by identifying novel targets. Herein we demonstrate, by the development of the first in vivo active DegS inhibitors based on a pyrazolo[1,5-a]-1,3,5-triazine scaffold, that the serine protease DegS and the cell envelope stress-response pathway σE represent a target for generating antibiotics with a novel mode of action. Moreover, DegS inhibition is synergistic with well-established membrane-perturbing antibiotics, thereby opening promising avenues for rational antibiotic drug design.

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HETEROARYL DERIVATIVES AS SEPIAPTERIN REDUCTASE INHIBITORS

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FUSED BICYCLIC HETEROAROMATIC DERIVATIVES AS KINASE INHIBITORS

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