[EN] 3,3-DIFLUOROPIPERIDINE CARBAMATE HETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES 3,3-DIFLUOROPIPÉRIDINE CARBAMATE UTILISÉS EN TANT QU'ANTAGONISTES DES RÉCEPTEURS NMDA NR2B
申请人:RUGEN HOLDINGS (CAYMAN) LTD
公开号:WO2016196513A1
公开(公告)日:2016-12-08
Disclosed are chemical entities of Formula (I), wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
[EN] GAMMA-AMINOAMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY<br/>[FR] MODULATEURS GAMMA-AMINOAMIDES DE L'ACTIVITE DE RECEPTEUR DE CHIMIOKINE
申请人:MERCK & CO INC
公开号:WO2004041279A1
公开(公告)日:2004-05-21
The present invention is directed to compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
[EN] DISCOVERY, TOTAL SYNTHESIS, AND BIOACTIVITY OF DOSCADENAMIDES<br/>[FR] DÉCOUVERTE, SYNTHÈSE TOTALE ET BIOACTIVITÉ DE DOSCADENAMIDES
申请人:UNIV FLORIDA
公开号:WO2021021629A1
公开(公告)日:2021-02-04
The invention is directed towards compounds (e.g., Formulae (I)-(IX)), their mechanism of action, processes to prepare the compounds, methods of activating quorum sensing signaling activity, and methods of treating diseases and disorders using the compounds described herein (e.g., Formulae (I)-(IX)).
Concise asymmetric routes to 2,2,4-trisubstituted tetrahydrofurans via chiral titanium imide enolates: Key intermediates towards synthesis of highly active azole antifungals SCH 51048 and SCH 56592
作者:Anil K Saksena、Viyyoor M Girijavallabhan、Haiyan Wang、Yi-Tsung Liu、Russel E Pike、Ashit K Ganguly
DOI:10.1016/0040-4039(96)01203-8
日期:1996.8
approaches to the key (−)-(2R)-cis-tosylate 1 and its (+)-(2S)-enantiomer 15 via generation of chiralimideenolates having a 2,2-disubstituted olefin functionality in the β-position, are described. In a “protecting group free” sequence, reaction of the titanium enolate generated from (4R)-benzyl-2-oxazolidinone derived imide 5b with s-trioxane provided a convenient intermediate 19 which could be directly
Studies on the Total Synthesis of Formamicin: Synthesis of the C(1)−C(11) Fragment
作者:Noel A. Powell、William R. Roush
DOI:10.1021/ol0069610
日期:2001.2.1
[figure: see text] An efficient and highly concise synthesis of 6, corresponding to the C(1)-C(11) fragment of formamicin (1), has been accomplished by a route utilizing a diastereoselective lactate aldol reaction to set the C(6) tertiary ether and the TES-OTf mediated transketalization of the C(6) tertiary methoxymethyl ether and the C(25) PMB ether to set the seven-membered methylene acetal unit