54346-18-8Relevant academic research and scientific papers
Microwave-assisted sequential one-pot synthesis of 8-substituted pyrazolo[1,5-a][1,3,5]triazines
Besson, Thierry,Elie, Jonathan,Fruit, Corinne
, (2021/06/30)
This paper reports a convenient sequential one-pot approach for the synthesis of an array of 14 pyrazolo[1,5-a][1,3,5]triazines, substituted in C8 by halogen (Br), various functions (CN and CO2Et)2 and alkyl or (het)aryl groups. This study conf
PYRAZOLOTRIAZINES
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, (2021/06/22)
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
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, (2021/09/11)
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
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, (2021/09/11)
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.
Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action
Bongard, Jens,Schmitz, Anna Laura,Wolf, Alex,Zischinsky, Gunther,Pieren, Michel,Schellhorn, Birgit,Bravo-Rodriguez, Kenny,Schillinger, Jasmin,Koch, Uwe,Nussbaumer, Peter,Klebl, Bert,Steinmann, J?rg,Buer, Jan,Sanchez-Garcia, Elsa,Ehrmann, Michael,Kaiser, Markus
supporting information, p. 1074 - 1078 (2019/05/07)
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.
INDOLE AHR INHIBITORS AND USES THEREOF
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, (2018/11/22)
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
FUSED BICYCLIC HETEROAROMATIC DERIVATIVES AS KINASE INHIBITORS
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, (2016/04/26)
A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, inc
CALCIUM CHANNEL AGONISTS
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, (2014/12/12)
Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel agonists, are disclosed. The disclosed calcium channel agonists and corresponding salt forms have a structure according to general formula I wherein each bond depicted as " " is a single bond or a double bond as needed to satisfy valence requirements; Z1, Z2, Z3, Z4, and Z5 independently are nitrogen or carbon; R1 and R3 are alkyl; R2 is alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and R4 is alkyl or hydroxyalkyl.
COMPOUNDS WITH ANTIBACTERIAL ACTIVITY AGAINST CLOSTRIDIUM
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, (2013/05/09)
The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for prepar
COMPOUNDS WITH ANTIBACTERIAL ACTIVITY AGAINST CLOSTRIDIUM
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, (2012/02/15)
The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for prepar
