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Imidazolothiazole compounds for the treatment of disease

Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Decarboxylative aldol-type reaction of 2-(trifluoroacetyl)-1,3-diazoles with activated acetic acids

The highly electrophilic ketones 2-(trifluoroacetyl)-1,3-diazoles easily undergo a decarboxylative aldol-type reaction with activated acetic acids to afford heterocyclic trifluoromethyl-substituted alcohols bearing various functionalities. Georg Thieme Verlag Stuttgart.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Chemistry, like all the natural sciences, SDS of cas: 4865-84-3, begins with the direct observation of nature¡ª in this case, of matter. In a Patent£¬Which mentioned a new discovery about 4865-84-3.

ARYL SUBSTITUTED OLEFINIC COMPOUNDS AS PDE10A INHIBITORS

The present invention provicles aryl substituted olefinic compounds as Phosphodiesterase 10A (PDE 10A) in- hibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders by inhibiting Phosphodiesterase 10A enzyme. Also provided herein are processes for preparing compounds described herein, inter- mediates used in their synthesis, pharmaceutical compositions thereof.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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1,2-BENZISOXAZOLE-3-METHANE-SULFONIC ACID AMMONIUM SALT

The present invention provides substantially isolated ammonium salt of 1,2- benzisoxazole-3-methane sulfonic acid (BOS-NH4), which can be crystalline. The present invention also provides substantially chemically pure BOS-NH4, which is non- hygroscopic or slightly hygroscopic. Another aspect of the present invention is directed to processes of preparing the BOS-NH4. The present invention also provides processes for preparing l,2-benzisoxazole-3-methane-sulfonyl chloride (BOS-Cl) using the BOS-NH4. The present invention also provides processes for preparing zonisamide using the BOS-NH4 or BOS-Cl.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Condensation reactions of various nucleophiles with 3-formylchromone

3-Formylchromones 1 are condensed with 1-(2,4-difluorophenyl-2-[1,2,4] tnazol-4-yl)ethanone in acetic anhydride to afford 3-[3-(2,4-difluoro-phenyl)-3- oxo-2-[1,2,4]triazol-4-yl)propenyl]chromon-4-ones 2. 3-Formylchromone 1 when heated with benzo[d]isoxazol-3-yl-acetic acid in dry pyridine yield 3-(2-benzo[d]isoxazol-3-yl-vinyl)chromon-4-ones 3. Further, 3-formylchromone 1 on heating with N-methylpiperizine in ethanol give 1-(2-hydroxyphenyl)-3-(4- methyl-piperazin-1-yl)propenones 4.

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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,
Benzisoxazole – an overview | ScienceDirect Topics

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IMPROVED AND SIMPLIFIED PROCESS FOR THE PREPARATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACID

A process for preparation of 1,2-benzisoxazole-3-acetic acid reacting 4-hydroxy coumarin and hydroxylamine in water according to the following scheme of reaction. Formula (I).

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Enantioselective nickel-catalyzed Michael additions of azaarylacetates and acetamides to nitroalkenes

Put a nickel in it: Azaarylacetates and acetamides, which have been neglected as substrates in catalytic asymmetric synthesis, undergo highly enantioselective Michael additions to nitroalkenes in the presence of a chiral nickel(II)-bis(diamine) complex (see scheme; Bn=benzyl, MS=molecular sieves). This process is tolerant of a wide variety of azaarenes in the pronucleophile. Copyright

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

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Recent advances in 4-hydroxycoumarin chemistry. Part 2: Scaffolds for heterocycle molecular diversity

The present paper aims to review the synthetic applicability of 4-hydroxycoumarin in heterocyclic synthesis during the period from 1996 up to now. This compound can be used as building blocks for five, six, and seven-membered heterocycles as well as fused rings.

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Benzisoxazole – Wikipedia,
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1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS

The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), O Y R5 R6 N R2 R3 R4 X Z R1 R7 R7 R10 n (I) 5 wherein X, Y,Z,n,R1, R2, R3, R4, R5, R6, R7 and R10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D 2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.10

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