61098-38-2Relevant academic research and scientific papers
MACROCYCLIC RIP2-KINASE INHIBITORS
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Page/Page column 31; 51-52, (2021/08/06)
The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2-kinase, and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
Pyrazolopyrimidines and related heterocycles as CK2 inhibitors
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Page/Page column 570, (2016/05/02)
The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula:
Pyrazolopyrimidin CK2 and related heterocyclic compound as an inhibitor
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Paragraph 0702, (2016/10/08)
The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula:
MK2 INHIBITORS AND USES THEREOF
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Paragraph 00791, (2014/10/03)
The present invention provides compounds, compositions thereof, and methods of using the same.
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: Discovery and in vivo activity of selective pyrazolo[1,5- a ]pyrimidine inhibitors using a focused library and structure-based optimization approach
Kosugi, Tomomi,Mitchell, Dale R.,Fujino, Aiko,Imai, Minoru,Kambe, Mika,Kobayashi, Shinji,Makino, Hiroaki,Matsueda, Yohei,Oue, Yasuhiro,Komatsu, Kanji,Imaizumi, Keiichiro,Sakai, Yuri,Sugiura, Satoshi,Takenouchi, Osami,Unoki, Gen,Yamakoshi, Yuko,Cunliffe, Vicky,Frearson, Julie,Gordon, Richard,John Harris,Kalloo-Hosein, Heidi,Le, Joelle,Patel, Gita,Simpson, Donald J.,Sherborne, Brad,Thomas, Peter S.,Suzuki, Naotaka,Takimoto-Kamimura, Midori,Kataoka, Ken-Ichiro
supporting information; experimental part, p. 6700 - 6715 (2012/09/25)
A novel class of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) inhibitors was discovered through screening a kinase-focused library. A homology model of MAPKAP-K2 was generated and used to guide the initial SAR studies and to rationalize the observed selectivity over CDK2. An X-ray crystal structure of a compound from the active series bound to crystalline MAPKAP-K2 confirmed the predicted binding mode. This has enabled the discovery of a series of pyrazolo[1,5-a]pyrimidine derivatives showing good in vitro cellular potency as anti-TNF-α agents and in vivo efficacy in a mouse model of endotoxin shock.
Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists
Saito, Tetsuji,Obitsu, Tetsuo,Minamoto, Chiaki,Sugiura, Tsuneyuki,Matsumura, Naoya,Ueno, Sonoko,Kishi, Akihiro,Katsumata, Seishi,Nakai, Hisao,Toda, Masaaki
scheme or table, p. 5955 - 5966 (2011/11/04)
To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a] pyrimidines, imidazo[1,2-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines were designed, synthesized and evaluated as CRF1 receptor antagonists. Compounds 2-27 showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound 5 was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chemical modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e] pyrimidines. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.
PHARMACEUTICALLY USEFUL HETEROCYCLE-SUBSTITUTED LACTAMS
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Page/Page column 139, (2011/04/18)
The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.
Methods for inhibiting protein kinases
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Page/Page column 110, (2010/11/26)
The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevent
Pyrazolopyrimidines as protein kinase inhibitors
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Page/Page column 47-48, (2010/11/26)
In its many embodiments, the present invention provides a novel class of amino-substituted pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including o
