[EN] PROTEIN KINASE MKK4 INHIBITORS FOR PROMOTING LIVER REGENERATION OR REDUCING OR PREVENTING HEPATOCYTE DEATH<br/>[FR] INHIBITEURS DE PROTÉINE KINASE MKK4 POUR FAVORISER LA RÉGÉNÉRATION HÉPATIQUE OU POUR RÉDUIRE OU PRÉVENIR LA MORT DES HÉPATOCYTES
申请人:HEPAREGENIX GMBH
公开号:WO2019149738A1
公开(公告)日:2019-08-08
The invention relates to pyrazolo-pyridine compounds which inhibit mitogen-activated protein kinase kinase 4 (MKK4) and in particular, selectively inhibit MKK4 over protein kinases JNK1 and MKK7. The compounds are useful for promoting liver regeneration or reducing or preventing hepatocyte death. They are further useful for treating osteoarthritis or rheumatoid arthritis, or CNS-related diseases.
Abstract A simple and convenient method for the synthesis of thiophosphates by coupling of phosphites with thiols under mild conditions has been developed. The reactions were promoted by trichloroisocyanuricacid (TCCA) and were carried out at room temperature in a one-pot two-step procedure within 20 min. A variety of substrates was tolerated in this method. Notably, both aryl and alkyl thiols could
Reactions of Phosphonium Ylides with S<sub>8</sub>or Se in the Presence of Amines. Formation of Thioaldehydes or Selenoaldehydes
作者:Kentaro Okuma、Yasuo Komiya、Hiroshi Ohta
DOI:10.1246/cl.1988.1145
日期:1988.7.5
The reaction of phosphonium ylides with elemental sulfur gave thioaldehydes which were successfully changed to corresponding thioamides when treated with secondary amines. On the other hand, the reaction of selenoaldehydes with secondary amines afforded bis(dialkylamino)methanes in good yields.
[[(<i>tert</i>-Butyl)dimethylsilyl]oxy]methyl Group for Sulfur Protection
作者:Lihong Wang、Derrick L. J. Clive
DOI:10.1021/ol2002573
日期:2011.4.1
aliphatic thiols can be protected by reaction with t-BuMe2SiOCH2Cl in DMF in the presence of a base (2,6-lutidine or proton sponge); the resulting t-BuMe2SiOCH2SR or t-BuMe2SiOCH2SAr are deprotected by sequential treatment with Bu4NF and I2 to give symmetrical disulfides. Another mode of deprotection involves reaction with a sulfenyl chloride; this process gives an unsymmetricaldisulfide and was examined
Intramolecular Chalcogenylation of Isooxazolines Mediated by PhICl2 and Diorganyl Disulfides or Diselenides
作者:Fengxia Sun、Yunfei Du、Dongke Zhang、Jingran Zhang、Xiaoxian Li、Zhenyang Yu、Yadong Li
DOI:10.1055/s-0040-1719833
日期:2022.1
Reactive organosulfenyl chlorides (ArSCl) or selenenyl chlorides (ArSeCl), generated in situ from the reaction of PhICl2 with diorganyl disulfides or diselenides, enable the intramolecular oxidative cyclization/chalcogenylation of β,γ-unsaturated oximes, leading to the formation of a series of chalcogenylated isooxazolines in good to excellent yield.