177970-27-3

Upstream product

• 75-44-5 phosgene 
• 13091-43-5 2-amino-3-bromo-5-methylbenzoic acid 
• 2941-78-8 2-Amino-5-methylbenzoic acid 
• 32315-10-9 bis(trichloromethyl) carbonate 

Relevant academic research and scientific papers

Target protein degradation inducing compound, preparation method thereof and pharmaceutical composition for preventing or treating targeted protein related diseases containing the same as an active ingredient

The present invention relates to a degraducer for inducing the decomposition of target protein, a producing method thereof, and a pharmaceutical composition for preventing or treating target protein-related diseases by containing the degraducer as an active ingredient. A novel compound represented by chemical formula 1, ULB-L-PTM, by the present invention, as a degraducer compound inducing the decomposition of target protein using cereblon E3 ubiquitin ligase, is able to significantly achieve a target protein degradation-inducing activity with an excellent binding activity of a cereblon E3 ubiquitin ligase binder thereby, being able to achieve an excellent protein degradation activity by targeting protein or polypeptide related to various diseases. The bromodomain-containing pharmaceutical composition for preventing or treating protein-related diseases or conditions contains the novel compound represented by chemical formula 1 as an active ingredient and has a useful effect of providing a health functional food composition for prevention or improvement.(AA) Example 22 (nM, 24h)COPYRIGHT KIPO 2020

NOVEL PIPERIDINE-2,6-DIONE DERIVATIVE AND USE THEREOF

The present disclosure relates to a novel piperidine-2,6-dione derivative and a use thereof and, more specifically, to a piperidine-2,6-dione derivative compound having a structure of a thalidomide analog. A compound of chemical formula 1 according to the present disclosure specifically binds with CRBN protein, and is involved in functions thereof. Therefore, the compound of the present disclosure can be favorably used in the prevention or treatment of leprosy, chronic graft versus host disease, an inflammatory disease, or cancer, which are caused by actions of CRBN protein.

A simple heterocyclic fusion reaction and its application for expeditious syntheses of rutaecarpine and its analogs

In the search for new inhibitors of cholinesterases, a simple heterocyclic fusion reaction of isatoic anhydride 8 and 3,4-dihydroisoquinoline 22 was discovered which involves a spontaneous dehydrogenation upon heating. Applying the reaction, the bioactive natural alkaloid rutaecarpine and several substituted derivatives out of tryptamines and anthranilic acids or isatoic anhydrides, respectively, can be synthesized without tedious chromatographic purification. This provides simple and fast access to larger amounts of compounds with this privileged structure in medicinal chemistry.

The synthesis of C2-symmetric and axially chiral compounds for recognition and catalysis

Axially chiral amidines and guanidines, some possessing C2-symmetry, have been targeted as potential chiral catalysts for reactions of α,β-unsaturated carboxylic acids or esters. The key step in each synthesis required the coupling of two sterically demanding aromatic compounds to form atropisomeric biaryl species. (C) 2000 Elsevier Science Ltd.