58347-52-7Relevant academic research and scientific papers
CD73 INHIBITING 2,4-DIOXOPYRIMIDINE COMPOUNDS
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Paragraph 1155, (2021/11/06)
The present disclosure provides pyrimidine dione compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors. The compounds can be used alone or in combination with other anti-cancer agents.
BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
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Page/Page column 83-84, (2021/04/23)
The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer. Formula (I)
Compounds, Compositions, and Methods for Modulating CDK9 Activity
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Paragraph 0121-0122, (2020/05/14)
Inhibitors of CDK9 that are pyrazolo[1,5-a]pyrimidine derivatives and salts thereof, corresponding to formula (I):
LRRK2 INHIBITORS AND METHODS OF MAKING AND USING THE SAME
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, (2016/09/22)
Compounds having the formula (I), (II), (III) are provided. Compounds of the present disclosure are useful for the treatment of neurodegenerative diseases, such as Parkinson's Disease.
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; scheme or table, 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.
