702701-70-0

Upstream product

• 55489-58-2 triethylene glycol monobenzyl ether 
• 124-63-0 methanesulfonyl chloride 
• 96042-30-7 4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran 
• 112-27-6 2,2'-[1,2-ethanediylbis(oxy)]bisethanol 
• 100-39-0 benzyl bromide 

Downstream Products

• 1003598-44-4 2-{2-[2-(3,3,3-trifluoro-propoxy)-ethoxy]-ethoxy}-ethoxymethyl-benzene 
• 1003598-45-5 2-{2-[2-(4,4,4-trifluoro-butoxy)-ethoxy]-ethoxy}-ethoxymethyl-benzene 
• 423763-19-3 monobenzyl heptaethylene glycol 
• 86770-75-4 2-(2-(2-(benzyloxy)ethoxy)ethoxy)ethan-1-amine 
• 86770-70-9 ((2-(2-(2-azidoethoxy)ethoxy)ethoxy)methyl)benzene 
• 1273387-07-7 {2-[2-(2-hydroxyethoxy)ethoxy]ethyl} (6-{(pyridin-2-ylsulfonyl)[4-(thiazol-2-yl)benzyl]aminomethyl}pyridin-2-ylamino)acetate 
• 1273387-06-6 2-{2-[2-(benzyloxy)ethoxy]ethoxy}ethyl 2-({6-[(N-{[4-(1,3-thiazol-2-yl)phenyl]methyl}pyridine-2-sulfonamido)methyl]pyridin-2-yl}amino)acetate 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUND

It is to provide a novel heterocyclic compound which has the effect of inducing degradation of interleukin-1 receptor-associated kinase-M (IRAK-M) protein and is expected to be useful for the prevention/treatment of cancer, fibrosis, infectious diseases, etc. The present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.

HETEROCYCLIC COMPOUND

One of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity. Another of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity and exhibits a protein degradation induction activity. The present invention provides a compound represented by formula (I) (the symbols in the formula are as defined in the present Description) and salts thereof.

Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands

Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin ligase have emerged as a novel paradigm in drug development. Herein we found that linker attachment points of CRBN ligands highly affect their aqueous stability and neosubstrate degradation features. This work provides a blueprint for the assembly of future heterodimeric CRBN-based degraders with tailored properties.

A MedChem toolbox for cereblon-directed PROTACs

A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.

Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof

Disclosed are an antibody drug conjugate IB, which uses ether linkages for connection, and improves the water solubility, stability and cytotoxicity in vivo and in intro, and an intermediate, a pharmaceutical composition, and uses of the antibody drug conjugate. The antibody drug conjugate has simple synthetic steps and a high yield.

A new way to do an old reaction: highly efficient reduction of organic azides by sodium iodide in the presence of acidic ion exchange resin

Organic azides are readily reduced to the corresponding amines by treatment with sodium iodide in the presence of acidic ion exchange resin. The process, optimal when performed at 40 °C and 200 mbar pressure on a rotatory evaporator, is extremely efficient, clean, and tolerant of a variety of functional groups.

Bna Conjugates and Methods of Use

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, decreasing arterial blood pressure and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.

Ionic strength mediated hydrophobic force switching of CF 3-terminated ethylene glycol self-assembled monolayers (SAMs) on gold

We have synthesised novel oligo(ethylene glycol), CF3-terminated switching self-assembled monolayers, which allow the force experienced by a hydrophobic object to be controlled via the ionic strength of the environment. The Royal Society of Chemistry.