59057-83-9

Upstream product

• 29266-68-0 1,2-benzisothiazole-3-acetic acid 
• 6187-89-9 3-methyl-1,2-benzisothiazole 

Relevant academic research and scientific papers

Amino sulfonyl compound, preparation method and uses thereof

The present invention relates to a new amino sulfonyl compound represented by a general formula I, or a tautomer, an enantiomer, a racemate or a pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and uses thereof, wherein the compound can be used for treatment of epilepsy, convulsion, obesity, and the like. The general formula I is defined in the specification.

Complete 1H and 13C NMR spectral assignment of benzo[d]isothiazole derivatives and of an isoindole isoster

The complete 1H and 13C NMR assignments of the novel compoundmethyl 2-amino-3-(benzo[d]isothiazol-3-yl)propanoate (1), of 3-amino-5-methylbenzo[d]isothiazole (2) and N-(t-butyloxycarbonyl)-2- aminobenzo[d]isothiazol-3(2H)-one (3) and

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.

Certain 1,2-benzisoxazole derivatives

Disclosed are 1,2-benzisoxazole and 1,2-benzisothiazole derivatives represented by formula I STR1 wherein X represents oxygen or sulfur; Z rep;esents carbon (CH) so as to complete the imidazol-1-yl ring radical or Z represents nitrogen (N) so as to complete the 1,2,4-triazol-1-yl ring radical; R1 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; R2 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; or R1 and R2 combined represent lower alkylene; or R1 combined with R5 located on the Z-carbon atom of the imidazolyl radical represents C2 -C4 -alkylene; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, halogen, trifluoromethyl, cyano, nitro, amino, hydroxy, lower alkanoyloxy, carbocyclic aroyloxy, lower alkoxy, or carbocyclic aryl; or R3 and R4, together when located on adjacent carbon atoms, represent lower alkylenedioxy; or R3 and R4, together when located on the carbon atoms to which attached a benzo-fused or C5 -C7 -cycloalka-fused ring, respectively; R5 located on carbon represents hydrogen, lower alkyl or hydroxy-lower alkyl; R6 located on carbon represents hydrogen or lower alkyl; or when Z represents carbon, R5 located on the Z-carbon atom combined with R6 located on the adjacent carbon atom represents C3 -C5 -alkylene; and pharmaceutically acceptable salts thereof; which are active in mammals as anticonvulsant agents.