53732-08-4

Upstream product

• 1955-04-0 methyl 5-nitro-3-chloroformylbenzoate 
• 1955-46-0 5-nitro-1,3-benzenedicarboxylic acid, monomethyl ester 
• 13290-96-5 dimethyl 5-nitroisophthalate 

Downstream Products

• 199536-04-4 3-Amino-5-hydroxymethyl-benzoic acid methyl ester; hydrochloride 
• 172899-78-4 methyl 3-formyl-5-nitrobenzoate 
• 167215-63-6 3-methanesulfonyloxymethyl-5-nitrobenzoic acid methyl ester 
• 220286-47-5 3-Amino-5-hydroxymethylbenzoic acid methyl ester 
• 167215-64-7 3-azidomethyl-5-nitrobenzoic acid methyl ester 
• 913077-69-7 3-[(tert-butyloxycarbonyl)aminomethyl]-5-nitrobenzoic acid methyl ester 
• 209604-83-1 3-[(tert-butyloxycarbonyl)aminomethyl]-5-nitrobenzoic acid 
• 209604-82-0 3-aminomethyl-5-nitrobenzoic acid methyl ester 
• 602280-55-7 [6-[3-amino-5-(methoxycarbonyl)phenyl]-5-chloro-3-(isopropylamino)-2-oxopyrazin-1(2H)-yl]acetic acid 
• 602280-49-9 methyl 3-{1-[2-(benzyloxy)-2-oxoethyl]-3,5-dichloro-6-oxo-1,6-dihydropyrazin-2-yl}-5-nitrobenzoate 
• 602280-54-6 methyl 3-[1-[2-(benzyloxy)-2-oxoethyl]-3-chloro-5-(isopropylamino)-6-oxo-1,6-dihydropyrazin-2-yl]-5-nitrobenzoate 
• 609345-95-1 methyl 3-amino-5-[1-(2-{[4-((Z)-amino{[(benzyloxy)carbonyl]imino}methyl)benzyl]amino}-2-oxoethyl)-3-chloro-5-(isopropylamino)-6-oxo-1,6-dihydropyrazin-2-yl]benzoate 
• 199536-09-9 methyl 3-({[(tert-butoxycarbonyl)amino][(tert-butoxycarbonyl)imino]methyl}amino)-5-formylbenzoate 
• 199536-07-7 methyl 3-({[(tert-butoxycarbonyl)amino][(tert-butoxycarbonyl)imino]methyl}amino)-5-(hydroxymethyl)benzoate 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents

A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a, 9b, 12a-12c, 14 and 15) were designed and synthesized. Their antitubercular activities were evaluated in vitro against M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 μg mL?1 and 6g was the most active compound (MIC = 0.625 μg mL?1). Compounds 6g and 7a also showed potent inhibitory activity against M. tuberculosis H37Rv (MIC = 0.39 μg mL?1) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.125 μg mL?1). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They exhibited low cytotoxicity against HepG2 and RAW264.7 cell lines. The results demonstrated m-amidophenol as an attractive scaffold for the development of new antitubercular agents.

UREA DERIVATIVES USEFUL AS KINASE INHIBITORS

There are provided compounds of formula I, wherein R1, R1A, R1C to R1E, Ra, Rb, X1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

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

QUINAZOLINONE DERIVATIVES HAVING B-RAF INHIBITORY ACTIVITY

The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C

Protein kinase C (PKC) is a widely studied molecular target for the treatment of cancer and other diseases. We have approached the issue of modifying PKC function by targeting the C1 domain in the regulatory region of the enzyme. Using the X-ray crystal structure of the PKC δ C1b domain, we have discovered conveniently synthesizable derivatives of dialkyl 5-(hydroxymethyl)isophthalate that can act as potential C1 domain ligands. Structure-activity studies confirmed that the important functional groups predicted by modeling were indispensable for binding to the C1 domain and that the modifications of these groups diminished binding. The most promising compounds were able to displace radiolabeled phorbol ester ([3H]PDBu) from PKC α and δ at Ki values in the range of 200-900 nM. Furthermore, the active isophthalate derivatives could modify PKC activation in living cells either by inducing PKC-dependent ERK phosphorylation or by inhibiting phorbol-induced ERK phosphorylation. In conclusion, we report here, for the first time, that derivatives of isophthalic acid represent an attractive novel group of C1 domain ligands that can be used as research tools or further modified for potential drug development.

Macrocyclic Compounds Useful as Bace Inhibitors

The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS

The invention relates to novel macrocyclic compounds of the Formula (I) in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS

The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

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.