161455-95-4

Upstream product

• 104-94-9 4-methoxy-aniline 
• 16495-67-3 4-(isopropylamino)anisole 
• 161455-96-5 2-bromo-N-isopropyl-N-(4-methoxy-phenyl)-acetamide 
• 534-85-0 N-phenyl-1,2-benzenediamine 

Downstream Products

• 1026677-37-1 6-Fluoro-3-(1-{[isopropyl-(4-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 
• 1027220-55-8 7-Fluoro-3-(1-{[isopropyl-(4-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 
• 1027995-85-2 3-(1-{[Isopropyl-(4-methoxy-phenyl)-carbamoyl]-methyl}-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-ylmethyl)-pyrazolo[3,4-b]pyridine-1-carboxylic acid tert-butyl ester 
• 1025841-15-9 3-(1-{[Isopropyl-(4-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 
• 174180-79-1 2-[2,4-Dioxo-5-phenyl-3-(4,5,6,7-tetrahydro-1-benzyl-1H-indazol-3-ylmethyl)-2,3,4,5-tetrahydro-benzo[b][1,4]diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)-acetamide 

Relevant academic research and scientific papers

Novel benzodiazepine photoaffinity probe stereoselectively labels a site deep within the membrane-spanning domain of the cholecystokinin receptor

An understanding of the molecular basis of drug action provides opportunities for refinement of drug properties and for development of more potent and selective molecules that act at the same biological target. In this work, we have identified the active

Use of 1,5-benzo?b!1,4-diazepines to control gastric emptying

A method of controlling gastric emptying in patients having an early non-insulin-dependent diabetic condition and exhibiting rapid gastric emptying comprising the administration of an effective gastric emptying controlling amount of a compound of Formula

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.