- Benzisoxazole heterocyclic compound as well as preparation method and application thereof
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The invention relates to a benzisoxazole heterocyclic compound and a preparation method and application thereof, and the structural formula comprises the formula (I). (II), (III), and particularly provides a specific preparation method of the compound. The derivative has good anticonvulsant activity and can be used as an anti-epileptic drug.
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- Amino sulfonyl compound, preparation method and uses thereof
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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.
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Paragraph 0161; 0163
(2016/12/01)
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- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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- Resistance-repellent retroviral protease inhibitors
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Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
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Page/Page column 26; 45
(2008/06/13)
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- A new method for the preparation of 1,2-benzisoxazole-3-carboxaldehyde
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Synthesis of 1,2-benzisoxazole-3-carboxaldehyde is achieved from 3-methyl 1,2-benzisoxazole via 3-ethoxymethyl-1,2-benzisoxazole (4).
- Kalkote, Uttam R.,Panchgalle, Sharad P.,Mahakal, Kumodini K.,Choudhary, Suman M.,Chavan, Subhash P.
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- Optimization of 3-(1H-Indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists
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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.
- Henke, Brad R.,Aquino, Christopher J.,Birkemo, Larry S.,Croom, Dallas K.,Dougherty Jr., Robert W.,Ervin, Gregory N.,Grizzle, Mary K.,Hirst, Gavin C.,James, Michael K.,Johnson, Michael F.,Queen, Kennedy L.,Sherrill, Ronald G.,Sugg, Elizabeth E.,Suh, Edward M.,Szewczyk, Jerzy W.,Unwalla, Rayomand J.,Yingling, Jeff,Willson, Timothy M.
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p. 2706 - 2725
(2007/10/03)
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- α-Bromoacetophenones in Heterocyclic Synthesis: A Convenient One-Pot Synthesis and the Chemical Behaviour of 3-Bromomethylbenzoisoxazole
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A novel one-pot synthesis of 3-bromomethylbenzoisoxazole (3) utilizing o-hydroxy-α-bromoacetophenone is reported.Coupling of 3 with benzenediazonium chloride afforded, the first reported, C-(3-benzoisoxazolyl)-N-(phenyl)formohydrazidoyl bromide (13).The chemical behaviour of 3 and 13 towards a variety of chemical reagents has been investigated.
- Mohareb, Rafat Milad,Sherif, Sherif Mourad,Shams, Hoda Zaki,El-Torgoman, Abdel Moneim
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p. 1067 - 1071
(2007/10/02)
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- Certain 1,2-benzisoxazole derivatives
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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.
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- Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
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Methane-sulfonamide derivatives of the formula: STR1 wherein R1 is hydrogen or a halogen atom, R2 and R3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group: --CH2 SO2 NR2 R3 is bonded to the carbon atom of either of X and Y, and an alkali metal salt thereof, and a process for the preparation of said methane-sulfonamide derivatives. Said compounds have an excellent anticonvulsant activity and are useful as anticonvulsants for controlling convulsions and seizures in patients with epilepsy.
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