769858-09-5

Usage

Uses

Used in Pharmaceutical Industry:
2,3,4,5-tetrahydro-1λ6,4-benzothiazepine 1,1-dioxide is used as a pharmaceutical compound for its potential activity in the central nervous system. It acts as a calcium channel blocker, which is beneficial in the treatment of cardiovascular diseases and hypertension.
Used in Medicinal Chemistry:
2,3,4,5-tetrahydro-1λ6,4-benzothiazepine 1,1-dioxide is used as a valuable compound in medicinal chemistry due to its unique chemical structure and properties. It serves as a promising candidate for drug development, with potential applications in the field of pharmacology and therapy.

Upstream product

• 14953-97-0 2,3,4,5-tetrahydro-5H-1,4-benzothiazepine hydrochloride 
• 147-93-3 Thiosalicylic acid 
• 4892-02-8 Methyl thiosalicylate 
• 14944-00-4 3,4-dihydro-1,4-benzothiazepin-5(2H)-one 
• 1422496-40-9 1-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)ethanone 
• 58980-39-5 2,3,4,5-Tetrahydro-1,4-benzothiazepine 
• 930-69-8 sodium thiophenolate 
• 2014-75-7 2-(phenylthio)ethanamine 
• 2014-72-4 N-[2-(phenylsulfanyl)ethyl]acetamide 

Relevant academic research and scientific papers

Discovery of Benzoazepinequinoline (BAQ) Derivatives as Novel, Potent, Orally Bioavailable Respiratory Syncytial Virus Fusion Inhibitors

A novel benzoazepinequnoline (BAQ) series was discovered as RSV fusion inhibitors. BAQ series originated from compound 2, a hit from similarity-based virtual screening. In SAR exploration, benzoazepine allowed modifications in the head moiety. Benzylic sulfonyl on benzoazepine and 6-Me on quinoline were crucial for good anti-RSV activity. Although the basic amine in the head portion was crucial for anti-RSV activity, the attenuated basicity was required to reduce Vss. Introducing oxetane to the head portion led to discovery of compound 1, which demonstrated single-digit nM anti-RSV activity against different RSV strains, reasonable oral exposure in plasma, and 78-fold higher exposure in lung. Compound 1 also displayed 1 log viral reduction in a female BALB/c mice RSV model by b.i.d. oral dosing at 12.5 mg/kg. A single resistant mutant at L138F in fusion protein proved compound 1 to be a RSV fusion inhibitor.

PROCESS FOR THE PREPARATION OF N-[(3-AMINOOXETAN-3-YL)METHYL]-2-(1,1-DIOXO-3,5-DIHYDRO-1,4-BENZOTHIAZEPIN-4-YL)-6-METHYL-QUINAZOLIN-4-AMINE

The present invention relates to a novel process for the preparation of a compound of the formula (I): and pharmaceutically acceptable acid addition salts thereof, which is useful for prophylaxis and treatment of respiratory syncytial virus (RSV) infection in mammal or human being.

PROCESS FOR THE PREPARATION OF N-[(3-AMINOOXETAN-3-YL)METHYL]-2-(1,1-DIOXO-3,5-DIHYDRO-1,4-BENZOTHIAZEPIN-4-YL)-6-METHYL-QUINAZOLIN-4-AMINE

The present invention relates to a novel process for the preparation of a compound of the formula (I) and pharmaceutically acceptable acid addition salts thereof, which is useful for prophylaxis and treatment of respiratory syncytial virus (RSV) infection in mammal or human being.

COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE

The invention relates to the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and X are as defined in the description and claims, which are useful for the treatment or prophylaxis of RSV infection.

COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE

A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1, R2 and X are as defined in description and in claims, can be used as a medicament.