bis-(phosphine sulfide) (4) have been synthesized. A single crystal X-ray diffraction study was carried out for bis(phosphine oxide) 3, which revealed a pinched cone conformation for the calixarene core. In the solid state, each calixarene is linked to two other calixarenes via hydrogen bonds involving the phosphoryl groups as well as two of the four hydroxyl groups, thereby generating a supramolecular polymeric
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.
[EN] MTORC MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS DE MTORC ET LEURS UTILISATIONS
申请人:AEOVIAN PHARMACEUTICALS INC
公开号:WO2020154447A1
公开(公告)日:2020-07-30
Novel rapamycin analogs and uses thereof are disclosed herein. The rapamycin analogs of the present disclosure show increased mTORC1 specificity and lowered mTORC2 specificity relative to rapamycin.
NON-IONIC ARYL KETONE BASED POLYMERIC PHOTO-ACID GENERATORS
申请人:International Business Machines Corporation
公开号:US20180044459A1
公开(公告)日:2018-02-15
Non-ionic photo-acid generating (PAG) polymerizable monomers were prepared that contain a side chain sulfonate ester of an alpha-hydroxy aryl ketone. The aryl ketone group has a perfluorinated substituent alpha to the ketone carbonyl. The sulfur of the sulfonate ester is also directly linked to a fluorinated group. PAG polymers prepared from the PAG monomers release a strong sulfonic acid when exposed to high energy radiation such as deep UV or extreme UV light. The photo-generated sulfonic acid has a low diffusion rate in an exposed resist layer subjected to a post-exposure bake (PEB) at 100° C. to 150° C., resulting in formation of good line patterns after development.
The nucleophilic addition of methanol and other alcohols to 1,1-diphenylethylene (1) and styrene (6) into the Markovnikov- and anti-Markovnikov-type products was selectively achieved with 1-(N,N-dimethylamino)pyrene (Py) and 1,7-dicyanoperylene-3,4:9,10-tetracarboxylic acid bisimide (PDI) as photoredox catalysts. The regioselectivity was controlled by the photocatalyst. For the reductive mode towards