TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
申请人:Arvinas, Inc.
公开号:US20180125821A1
公开(公告)日:2018-05-10
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME
申请人:Arvinas, Inc.
公开号:US20180215731A1
公开(公告)日:2018-08-02
The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ENHANCER OF ZESTE HOMOLOG 2 POLYPEPTIDE
申请人:Arvinas, Inc.
公开号:US20180177750A1
公开(公告)日:2018-06-28
The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand 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.
A facile one-step synthesis of monoazacrownethers by treatment of dialkanolamines with oligothylene glycol di(toluene-p-sulphonates) or dichlorides in ButOM–ButOH (M = Na, K) is described.
SEALING AGENT FOR PHOTOELECTRIC CONVERSION ELEMENT AND PHOTOELECTRIC CONVERSION ELEMENT USING THE SAME
申请人:NIPPON KAYAKU KABUSHIKI KAISHA
公开号:EP1598897A1
公开(公告)日:2005-11-23
A sealing agent for a photoelectric conversion device which comprises one or more of a compound having a glycidyl structure, a compound having a cyclohexene oxide structure, a compound having an oxetane structure and a compound having a vinyl ether structure, and a cationic polymerization initiator; a photoelectric conversion device using the sealing agent; and a solar cell comprising the photoelectric conversion device. The sealing agent for a photoelectric conversion device can be used for pasting together upper and lower electroconductive glass substrates at an ordinary temperature in the manufacture of a photoelectric conversion device, and is excellent with respect to adhesion strength and the reliability in moisture resistance.