4031-84-9

Upstream product

• 83909-55-1 methyl 2-(N-morpholino)-5-nitrobenzoate 
• 2965-22-2 methyl 2-fluoro-5-nitro-benzoate 
• 110-91-8 morpholine 
• 56741-34-5 methyl 5-amino-2-fluorobenzoate 
• 6307-82-0 2-chloro-5-nitro-benzoic acid methyl ester 
• 2516-96-3 2-chloro-5-nitrobenzoic acid 

Downstream Products

• 759456-60-5 (5-amino-2-morpholinophenyl)methanol 
• 1116688-69-7 methyl 5-(3-(thiophen-2-yl)propiolamido)-2-morpholinobenzoate 
• 1116688-83-5 (E)-methyl 5-(3-(thiophen-2-yl)allylamino)-2-morpholinobenzoate 
• 847467-59-8 methyl 5-((4'-methoxybenzyl)amino)-2-morpholinobenzoate 
• 767347-26-2 methyl 5-((3'-methoxybenzyl)amino)-2-morpholinobenzoate 
• 766527-32-6 methyl 5-((4′-bromobenzyl)amino)-2-morpholinobenzoate 
• 767347-36-4 methyl 5-((3′-chlorobenzyl)amino)-2-morpholinobenzoate 

Relevant academic research and scientific papers

Development of 2-Morpholino-N-hydroxybenzamides as anti-proliferative PC-PLC inhibitors

Phosphatidylcholine-specific phospholipase C (PC-PLC) is a key enzyme involved in the metabolism of the mammalian phospholipid phosphatidylcholine into secondary messengers diacylglycerol (DAG) and phosphocholine. DAG and phosphocholine have been identifi

Incorporation of a nitric oxide donating motif into novel pc-plc inhibitors provides enhanced anti-proliferative activity

Inhibition of phosphatidylcholine-specific phospholipase C (PC-PLC) has previously been shown to be a potential target for novel cancer therapeutics. One downstream consequence of PC-PLC activity is the activation of NF-κB, a nuclear transcription factor

EIF4E INHIBITORS AND USES THEREOF

The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.

Development, synthesis and biological investigation of a novel class of potent PC-PLC inhibitors

Phospholipases are enzymes that are involved in the hydrolysis of acyl and phosphate esters of phospholipids, generating secondary messengers that have implications in various cellular processes including proliferation, differentiation and motility. As such inhibitors of phospholipases have been widely studied for their use as anti-cancer therapeutics. Phosphatidylcholine-specific phospholipase C (PC-PLC) is implicated in the progression of a number of cancer cell lines including aggressing triple-negative breast cancers. Most current studies on PC-PLC have utilised D609 as the standard inhibitor however it is known to have multiple failings, including poor stability in aqueous media. 2-Morpholinobenzoic acids were recently identified using vHTS as a potential class of lead compounds, with improvements over D609. In this work 129 analogues in this class were prepared and their PC-PLC inhibitory activity was assessed. It was found that the majority of these novel compounds had improved activity when compared to D609 with the most potent inhibitors completely inhibiting enzyme activity. It was determined that the best compound/s contained a morpholino and 2-substituted N-benzyl moieties with these findings explained using molecular modelling. The compounds reported here will allow for improved study of PC-PLC activity.

Synthesis and structure activity relationship studies of novel Staphylococcus aureus Sortase A inhibitors

Synthetic methods have been developed for lead Sortase A inhibitors identified from previous studies. Several derivatives of the lead inhibitor were synthesized to derive preliminary structure activity relationships (SAR). Different regions of the lead in

MACROCYCLIC INDOLES AS HEPATITIS C VIRUS INHIBITORS

The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, formula (I), wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.

Identification of novel inhibitors of bacterial surface enzyme Staphylococcus aureus Sortase A

In-silico virtual screening of bacterial surface enzyme Staphylococcus aureus Sortase A against commercial compound libraries using FlexX software package has led to the identification of novel inhibitors. Inhibition of enzyme catalytic activity was deter

Further studies on hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors toward improved replicon cell activities: Benzimidazole and structurally related compounds bearing the 2-morpholinophenyl moiety

Following the discovery of JTK-109 (1) as a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase, [(a) Hirashima, S.; Suzuki, T.; Ishida, T.; Noji, S.; Yata, S.; Ando, I.; Komatsu, M.; Ikeda, S.; Hashimoto, H. J. Med. Chem. 2006, 49, 4721. (b) Hashimoto, H.; Mizutani, K.; Yoshida, A. Int. Patent Appl. WO 01/47883, 2001.] further studies toward the improvement of the cellular potency have been performed. A greater than 40-fold improvement was achieved through replacing the biphenyl moiety with a 2-morpholinophenyl group and the benzimidazole ring with the tetracyclic scaffold to afford compound 7 with an excellent replicon potency (EC50 = 7.6 nM).

5-5-MEMBERED FUSED HETEROCYCLIC COMPOUND AND USE THEREOF AS HCV POLYMERASE INHIBITOR

The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and