229005-68-9

Upstream product

• 229007-09-4 4-[N-methyl-N-(tetrahydro-2H-pyran-4-yl)aminomethyl]aniline 
• 259739-46-3 7-(4-methylphenyl)-2,3-dihydro-1-benzothiepine-4-carboxylic acid 
• 106-53-6 para-bromobenzenethiol 
• 79-37-8 oxalyl dichloride 
• 677707-98-1 methyl 7-(4-methylphenyl)-5-oxo-2,3,4,5-tetrahydro-1-benzothiepine-4-carboxylate 
• 279263-09-1 methyl 7-(4-methylphenyl)-2,3-dihydro-1-benzothiepine-4-carboxylate 
• 677707-97-0 7-(4-methylphenyl)-3,4-dihydro-1-benzothiepin-5(2H)-one 
• 15085-43-5 4-(4-bromophenylsulfanyl)butyric acid ethyl ester 
• 15115-76-1 4-[(4-bromophenyl)thio]butanoic acid 
• 15084-55-6 7-bromo-3,4-dihydro-1-benzothiepin-5(2H)-one 

Downstream Products

• 229005-74-7 dimethyl-(N-(7-(4-methylphenyl)-2,3-dihydro-1-benzothiepine-4-carbonyl)-4-aminobenzyl)-N-(4-tetrahydropyranyl)ammonium iodide 

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.

Quaternary ammonium salts and their use

This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: wherein R1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is -CH2-, -S- or -O-; and R2, R3 and R4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.

Anilide derivative, production and use thereof

This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.