31143-05-2

Upstream product

• 536-90-3 m-Anisidine 
• 555-31-7 aluminum isopropoxide 
• 67-63-0 isopropyl alcohol 
• 67-64-1 acetone 

Downstream Products

• 174181-29-4 N-isopropyl-N-(3-methoxyphenyl)bromoacetamide 
• 174181-28-3 3-(1-{[Isopropyl-(3-methoxy-phenyl)-carbamoyl]-methyl}-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-ylmethyl)-indazole-1-carboxylic acid tert-butyl ester 
• 174181-31-8 2-(-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydrobenzo[b][1,4]diazepin-1-yl)-N-isopropyl-N-(3-methoxy-phenyl)-acetamide 
• 174181-30-7 N-Isopropyl-N-(3-methoxy-phenyl)-2-(2-phenylamino-phenylamino)-acetamide 

Relevant academic research and scientific papers

Ion channel modulators and methods of use

In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels.

Optimization of 3-(1H-Indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists

We previously described a series of 3-(1H-indazol-3-ylmethyl)-1,5- benzodiazepine CCK-A agonists exemplified by compound 1 (GW 5823), which is the first reported binding selective CCK-A full agonist demonstrating oral efficacy in a rat feeding model. In this report we describe analogs of compound 1 designed to explore changes to the CS and N1 pharmacophores and their effect on agonist activity and receptor selectivity. Agonist efficacy in this series was affected by stereoelectronic factors within the C3 moiety. Binding affinity for the CCK-A vs CCK-B receptor showed little dependence on the structure of the C3 moiety but was affected by the nature of the second substituent at CS. Structure-activity relationships at the N1- anilidoacetamide 'trigger' moiety within the C3 indazole series were also investigated. Both agonist efficacy and binding affinity within this series were modulated by variation of substituents on the Nl-anilidoacetamide moiety. Evaluation of several analogs in an in vivo mouse gallbladder emptying assay revealed compound 1 to be the most potent and efficacious of all the analogs tested. The pharmacokinetic and pharmacodynamic profile of 1 in rats is also discussed.

ALCOHOLS AND ALUMINIUM ALKOXIDES IN THE PRESENCE OF RANEY-NICKEL AS ALKYLATING AGENTS. II. A KINETIC STUDY OF ALKYLATION OF AROMATIC AMINES

The kinetics of N-alkylation of substituted anilines with isopropanol and aluminium isopropoxide, catalysed by Raney-nickel, have been studied.The reaction proceeds according to a second-order equation.The formation of the Schiff's bases of the anilines along the reaction courses have been detected.The data reported also show that the reaction rates depend upon the nucleophilicity of the substrate to be alkylated.A possible mechanism is discussed.