Benzylamine derivatives which are useful in treating psychiatric
申请人:Akzo Nobel, N.V.
公开号:US06080773A1
公开(公告)日:2000-06-27
The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
申请人:Renz Martin
公开号:US20100331320A1
公开(公告)日:2010-12-30
This invention relates to novel compounds of the Formula Ik, Im
1
, Im
2
, Im
5
, In
1
, In
2
, In
5
, Io
1
, Io
2
, Io
5
, Ip
1
, Ip
3
, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Evidence and isolation of tetrahedral intermediates formed upon the addition of lithium carbenoids to Weinreb amides and N-acylpyrroles
作者:Laura Castoldi、Wolfgang Holzer、Thierry Langer、Vittorio Pace
DOI:10.1039/c7cc05215d
日期:——
The tetrahedralintermediates generated upon the addition of halolithium carbenoids (LiCH2X and LiCHXY) to Weinreb amides have been intercepted and fully characterized as O-TMS heminals. The commercially available N-trimethylsilyl imidazole is the ideal trapping agent whose employment, combined with a straightforward neutral Alox chromatographic purification, enables the isolation of such labile species
straightforward flow synthesis of α-chloro aldehydes has been developed. The strategy involves, for the first time, the thermal unstable chloroiodomethyllithium carbenoid and carbonyl compounds. A batch versus flow comparativestudy showcases the superb capability of flow technology in prolonging the lifetime of the lithiated carbenoid, even at -20 °C. Remarkably, the high chemoselectivity realized in flow
[EN] METHOD OF TREATING RHEUMATOID ARTHRITIS USING NF-kB INHIBITORS<br/>[FR] METHODE PERMETTANT DE TRAITER L'ARTHRITE RHUMATOIDE A L'AIDE D'INHIBITEURS DE NF-KB
申请人:WYETH CORP
公开号:WO2005039583A1
公开(公告)日:2005-05-06
The present invention concerns a method of treating rheumatoid arthritis by diagnosing that a person is in need of treatment for rheumatoid arthritis and administering a therapeutically effective amount of a ligand which modulates NF-kB transcription factor by interaction with estrogen receptor ER-α, estrogen receptor ER-β, or both ER-α and ER- β estrogen receptors with a substantial absence of creatine kinase stimulation. In certain embodiments, the administration is with a substantial absence of uterotropic activity.