279261-59-5

Upstream product

• 279263-09-1 methyl 7-(4-methylphenyl)-2,3-dihydro-1-benzothiepine-4-carboxylate 
• 15084-55-6 7-bromo-3,4-dihydro-1-benzothiepin-5(2H)-one 
• 15115-76-1 4-[(4-bromophenyl)thio]butanoic acid 
• 15085-43-5 4-(4-bromophenylsulfanyl)butyric acid ethyl ester 
• 106-53-6 para-bromobenzenethiol 
• 677707-97-0 7-(4-methylphenyl)-3,4-dihydro-1-benzothiepin-5(2H)-one 
• 677707-98-1 methyl 7-(4-methylphenyl)-5-oxo-2,3,4,5-tetrahydro-1-benzothiepine-4-carboxylate 

Downstream Products

• 279261-60-8 7-(4-methylphenyl)-1,1-dioxo-2,3-dihydro-1-benzothiepine-4-carboxylic acid 

Relevant academic research and scientific papers

Synthesis of 1-benzothiepine and 1-benzazepine derivatives as orally active CCR5 antagonists

Quaternary ammonium benzocycloheptene compound 1 has previously been reported as a clinical candidate for an injectable CCR5 antagonist. In order to develop an orally active CCR5 antagonist, derivatives of tertiary amine benzocycloheptene 2, the chemical precursor to 1, were investigated. The benzocycloheptene ring was converted to benzothiepine and benzazepine rings and it was found that these changes could enhance the potency of tertiary amine derivatives. In particular, the 1-benzothiepine-1,1-dioxide 11b and the N-methyl-1-benzazepine 18 showed increased activity and good preliminary pharmacokinetic properties. The synthesis of 1-benzothiepine and 1-benzazepine derivatives and their activity are described.

Anilide derivative, production and use thereof

This invention is to provide a compound of the formula: wherein R1is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula: ?wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5and R6are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5and R6may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.