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BENZISOXAZOLE COMPOUND AND USE THEREOF

A benzisoxazole compound represented by general formula (I) or a pharmaceutically acceptable salt thereof wherein, when the bond (a) between the 2- and 3-positions represents a single bond, Rarepresents the group (II) (wherein R represents hydrogen, alkyl, alkenyl, cycloalkylalkyl, cycloalkylalkenyl, phenylalkenyl, naphthylalkyl or naphthylalkenyl; A represents linear or branched alkylene; and n represents 1, 2 or 3) and Rbrepresents oxygen, or alternatively when the bond (a) between the 2- and 3-positions represents a double bond, Rais absent; Rbrepresents either the group (III), wherein each symbol is as defined above, or the group (IV), wherein E represents oxygen or sulfur, and R, A and n are each as defined above; and R1, R2, R3 and R4 are each as defined in the specification. This compound has a centroselective acetylcholine esterase inhibiting activity and/or a potent affinity for sigma receptor.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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ACRYLATED URETHANES, PROCESSES FOR MAKING THE SAME AND CURABLE COMPOSITIONS INCLUDING THE SAME

The present invention is directed to acrylated urethanes including the reaction product of: (1)(a) at least one urethane having at least two isocyanate groups and at least one acrylate group; and (b) at least one alcohol compound having at least two hydroxyl groups; or (2) (a) at least one isocyanate functional urethane which is the reaction product of at least one alcohol compound selected from the group consisting of amino alcohols, thioether alcohols, phosphino alcohols and mixtures thereof and at least one polyisocyanate; and (b) at least one hydroxy-functional material having at least one acrylate group; curable compositions including the same and processes for making the same.

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A Novel Synthesis of 3-Amino-1,2-benzisoxazoles – an Entry into the Isoxazolo<3,4,5-ef><1,4>benzoxazepine Ring System

A novel synthesis of 3-amino-1,2-benzisoxazole (3) from 2-<(isopropylideneamino)oxy>benzonitrile (2) is described.This methodology was used to synthesize 3-amino-4-hydroxy-1,2-benzisoxazole (10), which served as an intermediate for a number of isoxazolo<3,4,5-ef><1,4>benzoxazepines.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Isoxazole derivatives

An isoxazole compound having the following formula: wherein R1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson’s disease, depression and Alzheimer’s disease.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Pyrazolopyridine derivatives useful in treating inflammation and allergic conditions

A compound of formula (I) or a salt thereof: STR1 wherein: R1 is hydrogen, C1-6 alkyl or phenyl optionally substituted by halogen, CF3, C1-4 alkoxy or C1-4 alkyl; R2 is hydrogen or C1-6 alkyl; R3 is C2-10 alkenyl or C1-10 alkyl substituted by hydroxy, C1-4 alkoxy, thiol, C1-4 alkylthio or NR7 R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl or together are C3-6 polymethylene; R4 and R5 are independently hydrogen or C1-4 alkyl; and R6 is hydrogen; or C1-4 alkyl or benzyl attached at nitrogen atom 1 or 2; having anti-inflammatory and/or anti-allergy activity.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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A compilation of two decades of mutagenicity test results with the ames Salmonella typhimurium and L5178Y mouse lymphoma cell mutation assays

As previously reported [Cameron, T. P., Rogers-Back, A. M., Lawlor, T. E., Harbell, J. W., Seifried, H. E., and Dunkel, V. C. (1991) Gentoxicity of multifunctional acrylates in the Salmonella/mammalian-microsome assay and mouse lymphoma TK+/- assay. Environ. Mol. Mutagen. 17, 264-271], the National Cancer Institute (NCI) shares the responsibility of selecting the most significant chemicals for carcinogenicity testing by the National Toxicology Program (NTP) and has used data from Salmonella and mouse lymphoma mutagenicity assays to aid in the selection and prioritization of chemicals to be further evaluated in chronic 2 year rodent studies. In addition, a number of antineoplastic and anti-AIDS drugs in preclinical evaluation were tested for the NCI’s Division of Cancer Treatment Toxicology Branch. In the NCI/NTP chemical selection process, it is no longer necessary to test chemicals prior to sending them to the NTP so the NCI program has ceased performing mutagenicity tests. Some of the testing data has been made available in summary form in the Chemical Carcinogenisis Research Information System (CCRIS), which is searchable on the NLM TOXNET system. The limitations in using this source are that only summary results are available and many negative test results are not included. A summary table that presents the results for each compound is provided in the Appendix with raw data provided in the Supporting Information. The Appendix table contains the compound name, CAS number, and a summary of the data from the Ames test and the mouse lymphoma assay.

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Benzisoxazole – Wikipedia,
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Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria

The discovery and development of new antibiotics capable of curing infections due to multidrug-resistant and pandrug-resistant Gram-negative bacteria are a major challenge with fundamental importance to our global healthcare system. Part of our broad program at Novartis to address this urgent, unmet need includes the search for new agents that inhibit novel bacterial targets. Here we report the discovery and hit-to-lead optimization of new inhibitors of phosphopantetheine adenylyltransferase (PPAT) from Gram-negative bacteria. Utilizing a fragment-based screening approach, we discovered a number of unique scaffolds capable of interacting with the pantetheine site of E. coli PPAT and inhibiting enzymatic activity, including triazolopyrimidinone 6. Structure-based optimization resulted in the identification of two lead compounds as selective, small molecule inhibitors of bacterial PPAT: triazolopyrimidinone 53 and azabenzimidazole 54 efficiently inhibited E. coli and P. aeruginosa PPAT and displayed modest cellular potency against the efflux-deficient E. coli DeltatolC mutant strain.

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Benzisoxazole – Wikipedia,
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Discovery of Benzo[d]isoxazol-6-ol

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CLEANING COMPOSITIONS WITH POLYALKANOLAMINES

The invention relates to cleaning compositions comprising polyalkanolamine polymers. The present invention further relates to methods of cleaning dishware and hard surfaces using such cleaning compositions.

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Benzisoxazole – Wikipedia,
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Simple exploration of Benzo[d]isoxazol-3-amine

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Preparation of 2-hydroxybenzamidines from 3-aminobenzisoxazoles

2-Hydroxybenzamidines have been prepared from 3-aminobenzisoxazoles by reductive cleavage of the nitrogen-oxygen bond using catalytic hydrogenation, Zn/AcOH or NiCl2/NaBH4. This ring-opening reaction can be accomplished chemoselectively in the presence of a variety of hydrogenation-sensitive functional groups including an aryl bromide, benzyl carbamate, and olefin.

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Benzisoxazole – Wikipedia,
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Photochemistry of matrix-isolated 3-chloro-1,2-benzisoxazole: Generation and characterization of 2-cyanophenoxyl radical and other reactive intermediates

Photochemistry of 3-chloro-1,2-benzisoxazole 1 in N2 and Ar matrices at 10 K leads to N-chloro-ketenimine 3 and 2-cyanophenyl-hypochlorite 4. The reaction kinetics and the observed photoisomerization of 3 to 4 indicate that ketenimine 3, possibly formed via an elusive vinylnitrene VN, is an intermediate in the formation of hypochlorite 4. A new pathway involving the formation of 2-cyanophenoxyl radical 5, which was captured only in Ar matrix, was also observed. Radical 5 is possibly formed via photodetachment of Cl atom from 1 (or VN) and might explain the formation of 3-chloro-6-oxocyclohexa-1,4-dienecarbonitrile 2 in N2 and Ar matrices. All the species were characterized by IR spectroscopy and theoretical calculations. The computed geometric and electronic structure of radical 5 is discussed. Overall, the results provided further insight into the mechanism of the photochemistry of 1,2-benzisoxazoles and allowed characterization of new interesting reactive intermediates.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics