1453186-95-2Relevant academic research and scientific papers
CDK KINASE INHIBITOR, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATION
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, (2022/02/24)
Disclosed in the present invention are a CDK kinase inhibitor, a preparation method therefor, a pharmaceutical composition, and an application. The present invention provides a compound as represented by formula I-a, a cis-trans isomer thereof, a pharmaceutically acceptable salt thereof, a solvate of the pharmaceutically acceptable salt thereof, a tautomer thereof, or a polymorph thereof. The compound of the present invention has good CDK7 inhibitory activity, cell activity, and tumor growth inhibitory activity.
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
CDK kinase inhibitor as well as preparation method, pharmaceutical composition and application thereof
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, (2021/01/04)
The invention provides a CDK kinase inhibitor as well as a preparation method, a pharmaceutical composition and an application thereof. The compound as shown in the formula I, the stereoisomer or thepharmaceutically acceptable salt of the compound have higher bioavailability, longer in-vivo half-life period and better in-vivo efficacy when being used as a CDK kinase inhibitor.
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.
PYRAZOLO - TRIAZINE DERIVATIVES AS SELECTIVE CYCLIN- DEPENDENT KINASE INHINITORS
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, (2013/09/12)
The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE DERIVATIVES
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, (2013/09/12)
The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors
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Paragraph 0247; 0248, (2013/09/12)
The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhinitors
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Paragraph 0260, (2013/09/12)
The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
