610797-50-7Relevant academic research and scientific papers
HETEROCYCLIC GROUP CONTAINED AMINO-METHANOL DERIVATIVE, AND SALT, SYNTHETIC METHOD AND USE THEREOF
-
, (2015/04/15)
The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection, or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis.
HETEROCYCLIC GROUP CONTAINED AMINO-METHANOL DERIVATIVE, AND SALT, SYNTHETIC METHOD AND USE THEREOF
-
, (2015/04/22)
The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection , or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis.
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P3-sparing S1P1 agonists
Asano, Masayoshi,Nakamura, Tsuyoshi,Sekiguchi, Yukiko,Mizuno, Yumiko,Yamaguchi, Takahiro,Tamaki, Kazuhiko,Shimozato, Takaichi,Doi-Komuro, Hiromi,Kagari, Takashi,Tomisato, Wataru,Inoue, Ryotaku,Yuita, Hiroshi,Oguchi-Oshima, Keiko,Kaneko, Reina,Nara, Futoshi,Kawase, Yumi,Masubuchi, Noriko,Nakayama, Shintaro,Koga, Tetsufumi,Namba, Eiko,Nasu, Hatsumi,Nishi, Takahide
scheme or table, p. 3083 - 3088 (2012/06/04)
We have previously disclosed 1,2,4-oxadiazole derivative 3 as a potent S1P3-sparing S1P1 agonist. Although compound 3 exhibits potent and manageable immunosuppressive efficacy in various in vivo models, recent studies have revealed that its 1,2,4-oxadiazole ring is subjected to enterobacterial decomposition. As provisions for unpredictable issues, a series of alternative compounds were synthesized on the basis of compound 3. Extensive SAR studies led to the finding of 1,3-thiazole 24c with the EC50 value of 3.4 nM for human S1P1, and over 5800-fold selectivity against S1P3. In rat on host versus graft reaction (HvGR), the ID50 value of 24c was determined at 0.07 mg/kg. The pharmacokinetics in rat and monkey is also reported. Compared to compound 3, 24c showed excellent stability against enterobacteria.
Ruthenium olefin metathesis catalysts with modified styrene ethers: Influence of steric and electronic effects
Zaja, Mirko,Connon, Stephen J.,Dunne, Aideen M.,Rivard, Michael,Buschmann, Nicole,Jiricek, Jan,Blechert, Siegfried
, p. 6545 - 6558 (2007/10/03)
A series of olefin metathesis catalysts with modified isopropoxybenzylidene ligands were synthesised, and the effects of ligands on the rate of metathesis investigated. Increased steric hinderance ortho to the isopropoxy group enhanced reaction rates. In the case of N-heterocyclic carbene complexes, decreasing electron density at both the chelating oxygen atom and the Ru=C bond accelerated reaction rates appreciably. Catalysts containing a tricyclohexylphosphane ligand, followed the same trend with regard to benzylidene electrophilicity, while higher electron density at oxygen enhanced reaction rates.
