Sep-21 News Simple exploration of Tetrahydro-2H-pyran-4-carbonyl chloride

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The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

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Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein W, Y, Z, R1, R2, R3, R4 and R5 are described herein, and methods of using said compounds in the treatment of cancer.

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9/23/21 News Our Top Choice Compound: Tetrahydro-2H-pyran-4-carbonyl chloride

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A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a, 9b, 12a-12c, 14 and 15) were designed and synthesized. Their antitubercular activities were evaluated in vitro against M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 mug mL?1 and 6g was the most active compound (MIC = 0.625 mug mL?1). Compounds 6g and 7a also showed potent inhibitory activity against M. tuberculosis H37Rv (MIC = 0.39 mug mL?1) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.125 mug mL?1). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They exhibited low cytotoxicity against HepG2 and RAW264.7 cell lines. The results demonstrated m-amidophenol as an attractive scaffold for the development of new antitubercular agents.

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23-Sep-21 News Now Is The Time For You To Know The Truth About Tetrahydro-2H-pyran-4-carbonyl chloride

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The present invention relates to compounds of Formula I, wherein R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. In addition, the present invention relates to methods treating disorders related to matrix metalloproteases. More particularly, the compounds of the present invention are useful for treating stroke.

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Sep-21 News Awesome and Easy Science Experiments about Tetrahydro-2H-pyran-4-carbonyl chloride

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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

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22-Sep News Something interesting about Tetrahydro-2H-pyran-4-carbonyl chloride

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Compounds of formula (I) as described hereinprocesses for their production and their use as anti-cancer agents.

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Sep-21 News Why Are Children Getting Addicted To Tetrahydro-2H-pyran-4-carbonyl chloride

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We report our progress on the development of new synthetic anticancer lead compounds that modulate the splicing of mRNA. We also report the synthesis and evaluation of new biologically active ester and carbamate analogues. Further, we describe initial animal studies demonstrating the antitumor efficacy of compound 5 in vivo. Additionally, we report the enantioselective and diastereospecific synthesis of a new 1,3-dioxane series of active analogues. We confirm that compound 5 inhibits the splicing of mRNA in cell-free nuclear extracts and in a cell-based dual-reporter mRNA splicing assay. In summary, we have developed totally synthetic novel spliceosome modulators as therapeutic lead compounds for a number of highly aggressive cancers. Future efforts will be directed toward the more complete optimization of these compounds as potential human therapeutics. 2009 American Chemical Society.

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9/18 News Archives for Chemistry Experiments of Tetrahydro-2H-pyran-4-carbonyl chloride

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A simple method to convert readily available carboxylic acids into sulfinate salts by employing an interrupted Barton decarboxylation reaction is reported. A medicinally oriented panel of ten new sulfinate reagents was created using this method, including a key trifluoromethylcyclopropanation reagent, TFCS-Na. The reactivity of six of these salts towards C-H functionalization was field-tested using several different classes of heterocycles.

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9/18/21 News What Kind of Chemistry Facts Are We Going to Learn About Tetrahydro-2H-pyran-4-carbonyl chloride

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New drugs are urgently needed for the treatment of tropical parasitic diseases such as leishmaniasis and human African trypanosomiasis (HAT). This work involved a high-throughput screen of a focussed kinase set of ?3400 compounds to identify potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin6 complex. The aim of this study is to provide chemical validation that Leishmania CRK3-CYC6 is a drug target. Eight hit series were identified, of which four were followed up. The optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin dependent kinase CDK2. Selective at last: [1,2,4]Triazolo[1,5-a]pyridines, aminopyrazoles, and disubstituted ureas were explored as potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin6 complex. Optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin-dependent kinase CDK2.

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15-Sep News What I Wish Everyone Knew About Tetrahydro-2H-pyran-4-carbonyl chloride

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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer¿s disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer¿s Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I)

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Tetrahydropyran – Wikipedia,
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