20503-39-3

Upstream product

• 19983-44-9 stattic 
• 76006-87-6 6-azido-2,3-dihydrobenzothiophen 1,1-dioxide 
• 20503-40-6 1,1-dioxo-1H-1λ6-benzo[b]thiophen-6-ylamine 
• 14315-13-0 2,3-dihydrobenzo[b]thiophene 1,1-dioxide 
• 51956-01-5 5-aminobenzo[b]thiophene 1,1-dioxide 
• 95-15-8 Benzo[b]thiophene 
• 825-44-5 benzothiophene-1,1-dioxide 
• 850855-54-8 N-(6-nitro-1,1-dioxo-1λ⁶-benzo[b]thiophen-5-yl)-acetamide 
• 858819-40-6 6-nitro-1,1-dioxo-1λ⁶-benzo[b]thiophen-5-ylamine 
• 857473-99-5 N-(1,1-dioxo-1λ⁶-benzo[b]thiophen-5-yl)-acetamide 
• 6577-74-8 1,1-dioxo-1λ⁶-benzo[b]thiophen-3-one-hydrazone 
• 20503-38-2 6-nitro-2,3-dihydro-benzo[b]thiophene-1,1-dioxide 

Downstream Products

• 117081-10-4 8-Ethyl-5,8-dihydro-5-oxo-thieno<3,2-g>chinolin-6-carbonsaeure 
• 1520073-15-7 4-[(1R)-2-((6-[4-(1,1-dioxido-2,3-dihydrobenzothiophen-6-yl)butoxy]hexyl)amino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol acetate salt 

Relevant academic research and scientific papers

Carbonic anhydrase inhibitors: Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides

A series of selected benzo[b]thiophene-5- and 6-sulfonamide derivatives previously reported to show cytotoxic activity and some others newly synthesized has been tested for the interactions with several CA isozymes, some of which are known to be involved

Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues

The interaction between Lymphocyte function-associated antigen 1 (LFA-1) and intercellular-adhesion molecule-1 (ICAM-1) plays important roles in the cell-mediated immune response and inflammation associated with dry eye disease. LFA-1/ICAM-1 antagonists can be used for the treatment of dry eye disease, such as Lifitegrast which has been approved by the FDA in 2016 as a new drug for the treatment of dry eye disease. In this study, we designed and synthesized some new structure compounds that are analogues to Lifitegrast, and their biological activities were evaluated by in vitro cell-based assay and also by in vivo mouse dry eye model. Our results demonstrated that one of these analogues of Lifitegrast (compound 1b) showed good LFA-1/ICAM-1 antagonist activity in in vitro assay; meanwhile, it also significantly reduced ocular surface epithelial cells damage, increased goblet cell density in dry eye mouse and highly improved the symptoms of dry eye mouse. [Figure not available: see fulltext.]

Proton pump inhibitors

A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R 1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R 2 , R 3 and R 4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R 5 and R 6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

Discovery of a rapidly metabolized, long-acting β2 adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing

A series of novel, potent, and selective human β2 adrenoceptor agonists incorporating a sulfone moiety on the terminal right-hand-side phenyl ring of (R)-salmeterol is presented. Sulfone 10b had salmeterol-like potency and selectivity profile, long duration of action on guinea pig trachea, and longer than salmeterol duration of action in vivo, suitable for once-daily dosing. It had lower than salmeterol oral absorption in rat, lower bioavailability in rat and dog, and a high turnover in human hepatocytes. It was metabolized in human hepatocytes by hydroxylation, oxidation, cleavage, and conjugation; most of the metabolites would be expected to have reduced or no β2 activity. The 4-biphenylsulfonic acid was identified as a crystalline, non-hygroscopic salt of 10b, suitable for inhaled delivery. Furthermore, it was free of any genetic toxicity issues and was considered as a backup to vilanterol.

PROTON PUMP INHIBITORS

A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

PROTON PUMP INHIBITORS

Proton pump inhibitors which have excellent proton pumping activity and which can be converted in vivo into proton pump inhibitors to exhibit antiulcer effect and so on, containing compounds represented by the general formula (I) or salts thereof or prodrugs of the same: (I) wherein X and Y are each independently a free valency or a spacer whose main chain has 1 to 20 carbon atoms; R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently hydrogen, an optionally substituted hydrocarbon group, optionally substituted thienyl, optionally substituted benzo[b]thienyl, optionally substituted furyl, optionally substituted pyridyl, optionally substituted pyrazolyl, optionally substituted pyrimidinyl, acyl, halogeno, cyano, or nitro; and R5 and R6 are each independently hydrogen or an optionally substituted hydrocarbon group.

BENZOTHIOPHENE-AND BENZOTHIOCHROMENE-COMPRISING DERIVATIVES OF PHENETHANOLAMINE FOR THE TREATMENT

Compounds of formula (I) and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma o

Synthesis and Photolysis of Azido-benzothiophens, -benzothiazoles, -benzimidazoles, and -indazoles: Novel 6,7-diamino-benzothiazoles, -benzimidazoles, and -indazoles and 6-Diethylamino-8H-thiazoloazepines

Irradiation of the 6-azidobenzothiazoles (4)-(9) (see Scheme) in the presence of an excess of a secondary amine gave either the corresponding 6,7-diaminobenzothiazole (14)-(20), a 6-amino-8H-thiazoloazepine (21)-(24), a mixture of both, or intractable material .Irradiation of 7-azido-3-methylbenzothiophen in an excess of diethylamine gave 7-amino-3-methylbenzothiophen and a trace of 3,3'-dimethyl-7,7'-azobenzothiophen. 6-Azidoindazole gave 7-amino-6-diethylaminoindazole (32) and 5(6)-azidobenzimidazole gave a mixture of 4(7)-amino- 5(6)-diethylaminobenzimidazole (33) and 5(6)-amino-4(7)-diethylaminobenzimidazole (34).Photolysis of either 6-azidobenzothiazole or its 2-methyl derivative in a methoxide-methanol-dioxan mixture gave the corresponding 6-methoxy-8H-thiazoloazepine, (30) or (31), respectively.