TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
申请人:Arvinas, Inc.
公开号:US20180155322A1
公开(公告)日:2018-06-07
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
[EN] GLYCOSIDE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE GLYCOSIDE ET UTILISATIONS DE CEUX-CI
申请人:NOVARTIS AG
公开号:WO2011048112A1
公开(公告)日:2011-04-28
This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.
Stereospecificannulation of hydroxyvinylethers in the presence of triflic anhydride and tertiary amines and its syntheticapplication are described. Each 1-hydroxy-2-oxabicyclo[n.4.0]alkane, 2-oxabicyclo[n.4.0]alk-1(6)-ene and 2-oxabicyclo[n.4.0]alk-1(6+n)-ene is stereoselectively synthesized from the same hydroxyvinylether depending on the choice of the reaction conditions (temperature, solvent
描述了在三氟甲磺酸酐和叔胺存在下的羟基乙烯基醚的立体定向环氧化及其合成应用。每个1-羟基-2-氧杂双环[n.4.0]烷烃,2-氧杂双环[n.4.0] alk-1(6)-烯和2-氧杂双环[n.4.0] alk-1(6 + n)-烯根据反应条件(温度,溶剂和叔胺)的选择,由相同的羟基乙烯基醚立体选择性地合成。这些化合物导致多官能化的环状化合物和一些天然产物。我们提出,这种环化反应是通过纯S N 2样机理进行的。
Pyridinium Chlorochromate in Organic Synthesis. A Facile and Selective Oxidative Cleavage of Enol Ethers
Pyridinium chlorochromate (PCC) has been found to be selective reagent for the oxidative cleavage of enol ethers to esters or keto lactones in high yields.