179686-64-7

Upstream product

• 88-72-2 1-methyl-2-nitrobenzene 
• 5680-79-5 glycine ethyl ester hydrochloride 
• 3958-60-9 2-nitrophenylmethyl bromide 
• 552-89-6 2-nitro-benzaldehyde 
• 219782-24-8 {[1-(2-Nitro-phenyl)-meth-(Z)-ylidene]-amino}-acetic acid methyl ester 

Downstream Products

• 345201-60-7 methyl N-(2-nitrobenzyl)-N-(thymin-1-ylacetyl)glycinate 
• 85313-33-3 methyl N-(2-nitrobenzyl)glycinate hydrochloride 
• 1174568-18-3 methyl N-(tert-butoxycarbonyl)-N-(2-nitrobenzyl)glycinate 
• 5946-39-4 2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine 
• 1824-72-2 1,3,4,5-tetrahydro-2H-benzo[e][1,4]diazepin-2-one 
• 179686-66-9 tert-butyl 2-oxo-1,2,3,5-tetrahydro-4H-1,4-benzodiazepine-4-carboxylate 
• 179686-65-8 methyl N-(2-aminobenzyl)-N-(tert-butoxycarbonyl)glycinate 
• 345201-73-2 {[2-(2-{(2-tert-butoxycarbonylamino-ethyl)-[(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-acetyl]-amino}-acetylamino)-benzyl]-[(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-acetyl]-amino}-acetic acid methyl ester 
• 345201-78-7 {[2-(2-{(2-tert-butoxycarbonylamino-ethyl)-[(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-acetyl]-amino}-acetylamino)-benzyl]-[(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-acetyl]-amino}-acetic acid 
• 345201-64-1 methyl N-(2-aminobenzyl)-N-(thymin-1-ylacetyl)glycinate 

Relevant academic research and scientific papers

HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS

The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Design, synthesis, and pharmacological evaluation of fused β-homophenylalanine derivatives as potent DPP-4 inhibitors

Dipeptidyl peptidase-4 (DPP-4) inhibitors are accepted as a favorable class of agents for the treatment of type 2 diabetes. Herein, a series of fused β-homophenylalanine derivatives as novel DPP-4 inhibitors were designed, synthesized, and evaluated for their inhibitory activities against DPP-4. Most of them displayed excellent DPP-4 inhibitory activities and good selectivity. Among them, 9aa, 18a, and 18m also showed good efficacy in an oral glucose tolerance test (OGTT) in ICR mice. Moreover, when dosed 8 h prior to glucose challenge, 18m showed significantly greater potency than sitagliptin. It thus provides potential candidates for the further development into potent drugs targeting DPP-4.

NOVEL HETEROCYCLIC COMPOUNDS

The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relat

Backbone modifications of aromatic peptide nucleic acid (APNA) monomers and their hybridization properties with DNA and RNA

Aromatic peptide nucleic acid (APNA) monomers containing N-(2-aminobenzyl)-glycine, N-(2-aminobenzyl)-(R)- or -(S)-alanine, and N-(2-aminobenzyl)-β-alanine moieties as part of their backbone were synthesized. These novel analogues were incorporated as a single "point mutation" in PNA hexamers, and their physicochemical properties were investigated by UV thermal denaturation and CD experiments. Destabilization in triplex formation between the PNA-APNA chimeras and complementary DNA or RNA oligomers was observed, as compared to the PNA control. The APNA monomer composed of the N-(2-aminobenzyl)-glycine backbone led to the smallest decrease in the thermal stability of the triplexes formed with DNA and RNA, while maintaining selectivity for base-pairing recognition. Since the PNA-APNA chimeras are more lipophilic than the corresponding PNA homopolymers, these oligomers may also exhibit better cell membrane permeability properties.