1346556-73-7Relevant articles and documents
Ring derivative of inhibitor for bromodomains in bromodomain and extra-teminal domain (BET) family, and preparation method and pharmaceutical application of ring derivative
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Paragraph 0356; 0359; 0365-0369, (2021/02/24)
The invention relates to a compound as shown in a general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or an eutectic crystal thereof, an intermediate and a preparation method of the compound or the stereoisomer, the deuterated compound, the solvate, the prodrug, the metabolite, the pharmaceutically acceptable salt orthe eutectic crystal thereof, and application of the compound or the stereoisomer, the deuterated compound, the solvate, the prodrug, the metabolite, the pharmaceutically acceptable salt or the eutectic crystal thereof in inhibiting or degrading diseases related to the bromodomains in the BET family. The formula (I) is B-L-K.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00920; 002104; 002107-02108, (2021/01/23)
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists
Matsuda, Daisuke,Kawamura, Madoka,Kobashi, Yohei,Shiozawa, Fumiyasu,Suga, Youichirou,Fusegi, Keiko,Nishimoto, Shinichi,Kimura, Kayo,Miyoshi, Masako,Takayama, Noriko,Kakinuma, Hiroyuki,Ohtake, Norikazu
, p. 1832 - 1847 (2018/03/01)
The design and synthesis of a novel class of 7-azaspiro[3.5]nonane GPR119 agonists are described. In this series, optimization of the right piperidine N-capping group (R2) and the left aryl group (R3) led to the identification of compound 54g as a potent GPR119 agonist. Compound 54g showed a desirable PK profile in Sprague-Dawley (SD) rats and a favorable glucose lowering effect in diabetic rats.