935534-40-0Relevant articles and documents
STING PYRAZOLE AGONISTS AND USES THEREOF
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, (2020/07/14)
The present invention provides compounds, compositions thereof, and methods of using the same for the modulation of STING, and the treatment of STING-mediated disorders.
Novel 3H-[1,2,3]triazolo[4,5-c]pyridine derivatives as GPR119 agonists: Synthesis and structure-activity/solubility relationships
Matsuda, Daisuke,Kobashi, Yohei,Mikami, Ayako,Kawamura, Madoka,Shiozawa, Fumiyasu,Kawabe, Kenichi,Hamada, Makoto,Nishimoto, Shinichi,Kimura, Kayo,Miyoshi, Masako,Takayama, Noriko,Kakinuma, Hiroyuki,Ohtake, Norikazu
, p. 4339 - 4354 (2017/07/22)
We previously reported a novel series of 1H-pyrazolo[3,4-c]pyridine derivatives and the identification of compound 4b as a highly potent GPR119 agonist. However, the advancement of preclinical evaluations of compound 4b is expected to be difficult because of the compound's significantly poor aqueous solubility (0.71?μM at pH6.8). In this article, we describe the further optimization of compound 4b focusing on the improvement of its aqueous solubility. Optimization of the central spacer, left-hand aryl group and right-hand piperidine N-capping group led to the identification of a potent GPR119 agonist, 3H-[1,2,3]triazolo[4,5-c]pyridine derivative 32o, with improved solubility (15.9?μM at pH6.8).
PESTICIDALLY ACTIVE BI- OR TRICYCLIC HETEROCYCLES WITH SULFUR CONTAINING SUBSTITUENTS
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, (2015/01/16)
Pesticidally active bi-or tricyclic heterocycles with sulphur-containing substituents, stereoisomers and tautomeric forms thereof that can be used as insecticides and can be prepared in a manner known per se.