1258440-55-9Relevant academic research and scientific papers
S1P1 AGONIST AND APPLICATION THEREOF
-
Paragraph 0204-0207, (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.
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses
Demont, Emmanuel H.,Bailey, James M.,Bit, Rino A.,Brown, Jack A.,Campbell, Colin A.,Deeks, Nigel,Dowell, Simon J.,Eldred, Colin,Gaskin, Pam,Gray, James R. J.,Haynes, Andrea,Hirst, David J.,Holmes, Duncan S.,Kumar, Umesh,Morse, Mary A.,Osborne, Greg J.,Renaux, Jessica F.,Seal, Gail A. L.,Smethurst, Chris A.,Taylor, Simon,Watson, Robert,Willis, Robert,Witherington, Jason
, p. 1003 - 1020 (2016/02/23)
FTY720 is the first oral small molecule approved for the treatment of people suffering from relapsing-remitting multiple sclerosis. It is a potent agonist of the S1P1 receptor, but its lack of selectivity against the S1P3 receptor ha
Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists
Taylor, Simon J.,Demont, Emmanuel H.,Gray, James,Deeks, Nigel,Patel, Aarti,Nguyen, Dung,Taylor, Maxine,Hood, Steve,Watson, Robert J.,Bit, Rino A.,McClure, Fiona,Ashall, Holly,Witherington, Jason
, p. 8236 - 8256 (2015/11/09)
This article describes the finding of substantial upregulation of mRNA and enzymes of the cytochrome P450 1A family during a lead optimization campaign for small molecule S1P1 agonists. Fold changes in mRNA up to 10 000-fold for CYP1A1 in vivo
THIAZOLE OR THIADIZALOE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
-
Page/Page column 25-26, (2010/12/31)
Thiazole or thiadizaloe derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated
THIADIAZOLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF DISORDERS MEDIATED BY SLPL RECEPTORS
-
Page/Page column 32, (2010/12/31)
The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
S1P1 AGONISTS COMPRISING A BICYCLIC N-CONTAINING RING
-
Page/Page column 37-38, (2010/12/31)
The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
5-MEMBERED HETEROARYL DERIVATIVES USED AS SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONISTS
-
Page/Page column 39, (2011/01/12)
5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
5-MEMBERED HETEROARYL DERIVATIVES USED AS SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONISTS
-
Page/Page column 74, (2011/01/12)
5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
