1354787-44-2

Upstream product

• 20781-20-8 2,4-Dimethoxybenzylamine 
• 163133-86-6 pyrimidin-4-amine 
• 613-45-6 2,4-Dimethoxybenzaldehyde 
• 1275930-89-6 6-chloro-N-(2,4-dimethoxybenzylamino)pyrimidin-4-amine 

Downstream Products

• 1354787-42-0 tert-butyl 4-(4-(4-(2-chloro-4-(N-(2,4-dimethoxybenzyl)-N-(pyrimidin-4-yl)sulfamoyl)-5-fluorophenoxy)-4'-(trifluoromethyl)biphenyl-3-yl)pyridin-2-yl)piperazine-1-carboxylate 
• 1354787-43-1 5-chloro-N-[(2,4-dimethoxyphenyl)methyl]-2,4-difluoro-N-(pyrimidin-4-yl)benzene-1-sulfonamide 
• 1450596-84-5 N-(2,4-dimethoxybenzyl)-2,5-difluoro-4-{[(1S,2R)-2-(1-methyl-1H-pyrazole-5-yl)cyclopentyl]oxy}-N-(pyrimidine-4-yl)benzenesulfonamide 
• 1432674-74-2 N-[(2,4-dimethoxyphenyl)methyl]-2,4,5-trifluoro-N-(pyrimidin-4-yl)benzene-1-sulfonamide 
• 1450597-07-5 N-(2,4-dimethoxybenzyl)-2,4-difluoro-5-methyl-N-(pyrimidin-4-yl)benzenesulfonamide 
• 1450596-69-6 3-chloro-N-(2,4-dimethoxybenzyl)-4-fluoro-N-(pyrimidin-4-yl)benzenesulfonamide 
• 1450598-94-3 5-chloro-N-[(2,4-dimethoxyphenyl)methyl]-2-fluoro-4-{[(1S,2R)-2-(1-methyl-1H-pyrazol-5-yl)cyclohexyl]oxy}-N-(pyrimidin-4-yl)benzene-1-sulfonamide 
• 1450596-82-3 N-[(2,4-dimethoxyphenyl)methyl]-2,3,4-trifluoro-N-(pyrimidin-4-yl)benzene-1-sulfonamide 
• 1450597-35-9 5-bromo-N-(2,4-dimethoxybenzyl)-2,4-difluoro-N-(pyrimidin-4-yl)benzenesulfonamide 
• 1450596-77-6 N-[(2,4-dimethoxyphenyl)methyl]-2,4,6-trifluoro-N-(pyrimidin-4-yl)benzene-1-sulfonamide 
• 1450597-72-4 3-chloro-N-(2,4-dimethoxybenzyl)-2,4-difluoro-N-(pyrimidin-4-yl)benzenesulfonamide 
• 1450596-75-4 3-cyano-N-(2,4-dimethoxybenzyl)-4-fluoro-N-(pyrimidin-4-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor

A highly potent, selective NaV1.7 inhibitor, DS-1971a, has been discovered. Exploration of the left-hand phenyl ring of sulfonamide derivatives (I and II) led to the discovery of novel series of cycloalkane derivatives with high NaV1.7 inhibitory potency in vitro. As the right-hand heteroaromatic ring affected the mechanism-based inhibition liability of CYP3A4, replacement of this moiety resulted in the generation of 4-pyrimidyl derivatives. Additionally, GSH adducts formation, which can cause idiosyncratic drug toxicity, was successfully avoided by this modification. An additional optimization led to the discovery of DS-1971a. In preclinical studies, DS-1971a demonstrated highly potent selective in vitro profile with robust efficacy in vivo. DS-1971a exhibited a favorable toxicological profile, which enabled multiple-dose studies of up to 600 mg bid or 400 mg tid (1200 mg/day) administered for 14 days to healthy human males. DS-1971a is expected to exert potent efficacy in patients with peripheral neuropathic pain, with a favorable safety profile.

BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/or epileptic seizure disorders.

METHOD FOR REMOVING DIMETHOXYBENZYL GROUP

In a method for producing a de-dimethoxybenzylated compound by removing a dimethoxybenzyl group from a compound containing a dimethoxybenzyl group bonded to a nitrogen atom in the presence of an acid, the de-dimethoxybenzylated compound is obtained by rem

DRUG FOR RESPIRATORY DISEASES

It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a pharmaceutical comprising a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; n: an integer of 1 to 3; and the heteroaryl or aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-C1-C3 alkylamino group, and when the heteroaryl or aryl group has two such groups, the two groups are the same as or different from each other.

Cycloalkane Derivatives

Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease. The present invention provides compounds represented by the following formula (I) or pharmacologically acceptable salts thereof:

BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain

Chemical Compounds

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.