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Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)

The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Substituted quinazolines and analogs and use thereof

The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer’s disease, amyotrophic lateral sclerosis, Huntington’s disease, Parkinson’s disease and Down’s syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus. Alzheimer’s disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome and Easy Science Experiments about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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High-throughput synthesis of azide libraries suitable for direct “click” chemistry and in situ screening

A key challenge in current drug discovery is the development of high-throughput (HT) amenable chemical reactions that allow rapid synthesis of diverse chemical libraries of enzyme inhibitors. The Cu(I)-catalyzed, 1,3-dipolar cycloaddition between an azide and an alkyne, better known as “click chemistry”, is one such method that has received the most attention in recent years. Despite its popularity, there is still a lack of robust and efficient chemical strategies that give access to diverse libraries of azide-containing building blocks (key components in click chemistry). We report herein a highly robust and efficient strategy for high-throughput synthesis of a 325-member azide library. The method is highlighted by its simplicity and product purity. The utility of the library is demonstrated with the subsequent “click” synthesis of the corresponding bidentate inhibitors against PTP1B.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Some scientific research about (S)-1,4-Benzodioxane-2-carboxylic acid

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CLEANING COMPOSITION AND METHOD OF MANUFACTURING METAL WIRING USING THE SAME

A cleaning composition includes about 0.01 to about 5 wt % of a chelating agent; about 0.01 to about 0.5 wt % of an organic acid; about 0.01 to about 1.0 wt % of an inorganic acid; about 0.01 to about 5 wt % of an alkali compound; and deionized water.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for 2879-20-1

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Synthesis of chiral alpha-amino tertiary boronic esters by enantioselective hydroboration of alpha-arylenamides

The rhodium-catalyzed asymmetric hydroboration of alpha-arylenamides with BI-DIME as the chiral ligand and (Bpin)2 as the reagent yields for the first time a series of alpha-amino tertiary boronic esters in good yields and excellent enantioselectivities (up to 99% ee).

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome Chemistry Experiments For Methyl 1,4-Benzodioxane-2-carboxylate

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Enantioselective Access to Chiral 2-Substituted 2,3-Dihydrobenzo[1,4]dioxane Derivatives through Rh-Catalyzed Asymmetric Hydrogenation

Rh-catalyzed asymmetric hydrogenation of various benzo[b][1,4]dioxine derivatives was successfully developed to prepare chiral 2-substituted 2,3-dihydrobenzo[1,4]dioxane derivatives using ZhaoPhos and N-methylation of ZhaoPhos ligands with high yields and excellent enantioselectivities (up to 99% yield, >99% enantiomeric excess (ee), turnover number (TON) = 24 000). Moreover, this asymmetric hydrogenation methodology, as the key step with up to 10 000 TON, was successfully applied to develop highly efficient synthetic routes for the construction of some important biologically active molecules, such as MKC-242, WB4101, BSF-190555, and (R)-doxazosin¡¤HCl.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Archives for Chemistry Experiments of 2879-20-1

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HETEROCYCLIC INHIBITORS OF MCT4

Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Application of 22013-33-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a article£¬once mentioned of 22013-33-8

TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX

Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3- diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Properties and Exciting Facts About (2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)methanol

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Synthesis, in vitro antimycobacterial and antibacterial evaluation of IMB-070593 derivatives containing a substituted benzyloxime moiety

A series of novel IMB-070593 derivatives containing a substituted benzyloxime moiety and displaying a remarkable improvement in lipophilicity were synthesized and evaluated for their in vitro antimycobacterial and antibacterial activity. Our results reveal that the target compounds 19a-m have considerable Gram-positive activity (MIC: <0.008-32 mug/mL), although they are generally less active than the reference drugs against the Gram-negative strains. In particular, compounds 19h, 19j, 19k and 19m show good activity (MICs: <0.008-4 mug/mL) against all of the tested Gram-positive strains, including ciprofloxacin (CPFX)- and/or levofloxacin (LVFX)-resistant MSSA, MRSA and MSSE. Moreover, compound 19l (MIC: 0.125 mug/mL) is found to be 2-4 fold more active than the parent IMB070593, CPFX and LVFX against M. tuberculosis H37Rv ATCC 27294. Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 39270-39-8. In my other articles, you can also check out more blogs about 39270-39-8

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for (2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)methanol

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Piperid-4-yl ureas and thio ureas used as antidepressant agents

The invention concerns the preparation of compounds of formula STR1 and acid addition and quaternary ammoniun salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula STR2 in which Q is O, S, –CR7 =CR8 –, –N=CR8 — and –N=N–; R4, R5 and R6, and R7 and R8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO2, NH2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH2 and hydroxy; and additionally either R4 and R5 when adjacent or R6 and R8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocylic or heterocyclic ring optionally carrying one or more substituents as defined above; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R1, R2, R3 and R9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is =O, =S or =NH; Y is –O– or a direct bond and Z is — CO– or –CH2 –, with the proviso that when Ar is unsubstituted phenyl and R9 is hydrogen then Y is –O–. The compounds of formula I exhibit psychotropic activity and are useful as antidepressants.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem