1122089-67-1Relevant articles and documents
S1P1 AGONIST AND APPLICATION THEREOF
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, (2021/10/02)
The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.
Synthetic method of novel feed additive
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Paragraph 0025; 0026; 0027, (2017/12/06)
The invention discloses a synthetic method of a novel feed additive and belongs to the technical field of synthesis of feed additives. The novel feed additive has the structure shown in the specification, wherein R1 is an oxygen atom or a nitrogen atom, R2 is cyclopentane, cyclobutane or cyclopropane, and R3 is methyl, ethyl or phenyl. The invention further discloses a preparation method of the novel feed additive. The novel feed additive is synthesized with the novel method, operation is simple and easy to perform in the reaction process, raw materials are low in price and easy to obtain, the reaction efficiency is relatively high, the repetition is relatively good, and the novel feed additive has a good growth promoting function on grow-finishing pigs.
Novel S1P1 receptor agonists - Part 5: From amino-to alkoxy-pyridines
Bolli, Martin H.,Lescop, Cyrille,Birker, Magdalena,De Kanter, Ruben,Hess, Patrick,Kohl, Christopher,Nayler, Oliver,Rey, Markus,Sieber, Patrick,Velker, J?rg,Weller, Thomas,Steiner, Beat
supporting information, p. 326 - 341 (2016/04/19)
In a previous communication we reported on the discovery of aminopyridine 1 as a potent, selective and orally active S1P1 receptor agonist. More detailed studies revealed that this compound is phototoxic in vitro. As a result of efforts aiming at eliminating this undesired property, a series of alkoxy substituted pyridine derivatives was discovered. The photo irritancy factor (PIF) of these alkoxy pyridines was significantly lower than the one of aminopyridine 1 and most compounds were not phototoxic. Focused SAR studies showed, that 2-, 3-, and 4-pyridine derivatives delivered highly potent S1P1 receptor agonists. While the 2-pyridines were clearly more selective against S1PR3, the corresponding 3- or 4-pyridine analogues showed significantly longer oral half-lives and as a consequence longer pharmacological duration of action after oral administration. One of the best compounds, cyclopentoxy-pyridine 45b lacked phototoxicity, showed EC50 values of 0.7 and 140 nM on S1PR1 and S1PR3, respectively, and maximally reduced the blood lymphocyte count for at least 24 h after oral administration of 10 mg/kg to Wistar rats.