87808-48-8

Usage

InChI:InChI=1/C9H9FO2/c1-6-3-4-7(5-8(6)10)9(11)12-2/h3-5H,1-2H3

Upstream product

• 99-75-2 4-methyl-benzoic acid methyl ester 
• 350-28-7 3-fluoro-4-methyl-benzoic acid 
• 77-78-1 dimethyl sulfate 
• 67-56-1 methanol 
• 59189-97-8 3-fluoro-4-methylbenzoic acid chloride 
• 186581-53-3 diazomethane 
• 74-88-4 methyl iodide 

Downstream Products

• 128577-47-9 methyl 4-(bromomethyl)-3-fluorobenzoate 
• 1134777-51-7 4-dibromomethyl-3-fluorobenzoic acid methyl ester 
• 1389311-89-0 C₁₀H₁₂ClF 
• 1379326-22-3 2-(3-fluoro-4-methylphenyl)propan-2-ol 
• 193290-36-7 methyl 4-(cyanomethyl)-3-fluorobenzoate 
• 74733-25-8 methyl 3-fluoro-4-formylbenzoate 
• 1402345-20-3 3-fluoro-4-[(E)-3-oxo-3-(2-phenylamino-pyridin-3-yl)-propenyl]-benzoic acid methyl ester 
• 1402345-21-4 3-fluoro-4-[3-oxo-3-(2-phenylamino-pyridin-3-yl)-propyl]-benzoic acid methyl ester 
• 1402345-22-5 3-fluoro-4-{3-[2-(methoxyoxalyl-phenyl-amino)-pyridin-3-yl]-3-oxo-propyl}-benzoic acid methyl ester 
• 1402345-23-6 3-(4-carboxy-2-fluoro-benzyl)-4-oxo-1-phenyl-1,4-dihydro-[1,8]naphthyridine-2-carboxylic acid methyl ester 

Relevant academic research and scientific papers

Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model

Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of neurodegenerative disorders. SW-100 (1a), a phenylhydroxamate-based HDAC6 inhibitor (HDAC6i) bearing a tetrahydroquinoline (THQ) capping group, is a highly potent and sel

A scalable and safe continuous flow procedure for in-line generation of diazomethane and its precursor MNU

Diazomethane is a valuable C1-building block for organic synthesis. Due to its intrinsic reactivity and instability, handling of this reagent is associated with serious safety hazards. Herein we present a simple and robust continuous flow process, allowing a safe and on-demand generation of diazomethane with a productivity of 95-117 mmol h-1. The developed two-step process starts from non-hazardous N-methylurea, and generates and consumes N-methyl-N-nitrosourea (MNU) and diazomethane, thus enabling a safe and convenient scale-up to a multi-gram scale in a conventional synthesis laboratory.

TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS

Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, tr

3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

Synthesis of novel 3-substituted benzamides related to imatinib

Twelve new 3-substituted benzamide derivatives structurally related to tyrosine kinase inhibitor imatinib have been synthesised by a Cu(I)-catalysed coupling of three previously synthesised (5-iodo-2-methylphenyl)-[4-(pyridin-3-yl)-6-perfluoroalkylpyrimidin-2-yl]amines with four synthesised 3-substituted 4-(4-methylpiperazin-1-ylmethyl)benzamides.

Development of Fluorine-18 Labeled Metabolically Activated Tracers for Imaging of Drug Efflux Transporters with Positron Emission Tomography

Increased activity of efflux transporters, e.g., P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), at the blood-brain barrier is a pathological hallmark of many neurological diseases, and the resulting multiple drug resistance represents a major clinical challenge. Noninvasive imaging of transporter activity can help to clarify the underlying mechanisms of drug resistance and facilitate diagnosis, patient stratification, and treatment monitoring. We have developed a metabolically activated radiotracer for functional imaging of P-gp/BCRP activity with positron emission tomography (PET). In preclinical studies, the tracer showed excellent initial brain uptake and clean conversion to the desired metabolite, although at a sluggish rate. Blocking with P-gp/BCRP modulators led to increased levels of brain radioactivity; however, dynamic PET did not show differential clearance rates between treatment and control groups. Our results provide proof-of-concept for development of prodrug tracers for imaging of P-gp/BCRP function in vivo but also highlight some challenges associated with this strategy.

PROTEIN KINASE INHIBITORS

The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.

AZAINDOLE DERIVATIVES AS MULTI KINASE INHIBITORS

The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.

AZAINDOLE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES

The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus a

NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.