220286-47-5

Upstream product

• 99-27-4 dimethyl 5-aminoisophthalate 
• 1955-46-0 5-nitro-1,3-benzenedicarboxylic acid, monomethyl ester 
• 13292-87-0 dimethylsulfide borane complex 
• 53732-08-4 3-hydroxymethyl-5-nitrobenzoic acid methyl ester 
• 7439-89-6 iron 
• 144-55-8 sodium hydrogencarbonate 

Downstream Products

• 307353-32-8 3-bromo-5-hydroxymethylbenzoic acid methyl ester 
• 177734-81-5 5-Hydroxymethyl-3-iodobenzoic acid methyl ester 
• 1310822-75-3 3-azido-5-hydroxymethylbenzoic acid methyl ester 
• 1310822-76-4 3-azido-5-azidomethylbenzoic acid methyl ester 
• 1310822-77-5 3-azido-5-(azidomethyl)-benzoic acid 
• 1310822-79-7 7-({5-[4-(3-azido-5-azidomethylbenzoylamino)phenyl]isoxazole-3-carbonyl}amino)heptanoic acid methyl ester 
• 1310822-87-7 7-{1-[4-(3-azido-5-azidomethylbenzoylamino)benzyl]-1H-pyrazol-4-ylcarbamoyl}heptanoic acid methyl ester 
• 1310822-89-9 5-[4-(3-azido-5-azidomethylbenzoylamino)phenyl]isoxazole-3-carboxylic acid (6-hydroxycarbamoylhexyl)amide 
• 1310822-94-6 octanedioic acid {1-[4-(3-azido-5-azidomethylbenzoylamino)benzyl]-1H-pyrazol-4-yl}amide hydroxyamide 
• 1639866-74-2 methyl 3-(bromomethyl)-5-((tert-butoxycarbonyl)amino)benzoate 
• 1639866-75-3 methyl 3-[(tert-butoxycarbonyl)amino]-5-(3-(trimethylsilyl)prop-2-yn-1-yl)benzoate 
• 1639866-76-4 tert-butyl {3-hydroxymethyl-5-[3-(trimethylsilyl)prop-2-yn-1-yl]phenyl}carbamate 
• 1639866-77-5 3-[(tert-butoxycarbonyl)amino]-5-[3-(trimethylsilyl)prop-2-yn-1-yl]benzoic acid 
• 1639866-78-6 3-amino-5-[3-(trimethylsilyl)prop-2-yn-1-yl]benzoic acid 

Relevant academic research and scientific papers

Preparation of new alkyne-modified ansamitocins by mutasynthesis

The preparation of alkyne-modified ansamitocins by mutasynthetic supplementation of Actinosynnema pretiosum mutants with alkyne-substituted aminobenzoic acids is described. This modification paved the way to introduce a thiol linker by Huisgen-type cycloaddition which can principally be utilized to create tumor targeting conjugates. In bioactivity tests, only those new ansamitocin derivatives showed strong antiproliferative activity that bear an ester side chain at C-3.

Bioreduction of aryl azides during mutasynthesis of new ansamitocins

Supplementing a culture of a mutant strain of Actinosynnema pretiosum that is unable to biosynthesize aminohydroxy benzoic acid (AHBA), with 3-azido-5-hydroxy-benzoic acid and 3-azido-5-amino-benzoic acid, unexpectedly yielded anilino ansamitocins instead

Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes

The design, synthesis, docking, and biological evaluation of novel potent HDAC3 and HDAC8 isoxazole- and pyrazole-based diazide probes suitable for binding ensemble profiling with photoaffinity labeling (BEProFL) experiments in cells is described. Both the isoxazole- and pyrazole-based probes exhibit low nanomolar inhibitory activity against HDAC3 and HDAC8, respectively. The pyrazole-based probe 3f appears to be one of the most active HDAC8 inhibitors reported in the literature with an IC50 of 17 nM. Our docking studies suggest that unlike the isoxazole-based ligands the pyrazole-based ligands are flexible enough to occupy the second binding site of HDAC8. Probes/inhibitors 2b, 3a, 3c, and 3f exerted the antiproliferative and neuroprotective activities at micromolar concentrations through inhibition of nuclear HDACs, indicating that they are cell permeable and the presence of an azide or a diazide group does not interfere with the neuroprotection properties, or enhance cellular cytotoxicity, or affect cell permeability.

NK-1 AND SEROTONIN TRANSPORTER INHIBITORS

The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.

Biphenylamidine derivatives

The present invention is a biphenylamidine derivative represented by the formula (1) or a pharmaceutically acceptable derivative thereof: and the biphenylamidine derivative or the pharmaceutically acceptable derivative thereof is a novel compound which can be used as a clinically applicable FXa inhibitor.

Pyrimidin derivatives

The invention relates to new pharmaceutically active compounds which are are P2-purinoceptor 7-transmembrane (TM) G-protein coupled receptor antagonists, compositions containing them and processes for their preparation.