Day: January 21, 2021

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Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants

The macrocyclic urea 2, a byproduct in the synthesis of benzoxaborole 1, was identified to be a novel and potent HCV protease inhibitor. We further explored this motif by synthesizing additional urea-based inhibitors and by characterizing them in replicase HCV protease-resistant mutants assay. Several compounds, exemplified by 12, were found to be more potent in HCV replicon assays than leading second generation inhibitors such as danoprevir and TMC-435350. Additionally, following oral administration, inhibitor 12 was found in rat liver in significantly higher concentrations than those reported for both danoprevir and TMC-435350, suggesting that inhibitor 12 has the combination of anti-HCV and pharmacokinetic properties that warrants further development of this series.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Computed Properties of C4H9NO2S, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 39093-93-1

Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists-Increasing selectivity over hERG

A direct correlation between hERG binding and QTc prolongation was established for a series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists. Compounds within this class with greater selectivity over hERG were developed. Compound 4h proved to have the best profile, with MCH-R1 Ki = 16 nm and hERG IC50 = 25 muM.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, COA of Formula: C4H9NO2S, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S

INDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS

The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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PROCESS FOR THE PREPARATION OF ISOXAZOLYL- METHOXY NICOTINIC ACIDS

The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors

The design, synthesis, and screening of dual PI3K/mTOR inhibitors that gave nanomolar enzymatic and cellular activities on both targets with an acceptable kinase selectivity profile are described. A docking study was performed to understand the binding mode of the compounds and to explain the differences in biological activity. In addition, cellular effects of the best dual inhibitors were determined on six cancer cell lines and compared to those on a healthy diploid cell line for cellular cytotoxicity. Two compounds are highly potent on cancer cells in the submicromolar range without any toxicity on healthy cells. A more detailed analysis of the cellular effect of these PI3K/mTOR dual inhibitors demonstrated that they induce G1-phase cell cycle arrest in breast cancer cells and trigger apoptosis. These compounds show an interesting kinase profile as dual PI3K/mTOR tool compounds or as a chemical series for further optimization to progress into in vivo experiments.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: Thiomorpholine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S

SOLID FORMS OF 1,L-DIOXO-4-THIOMORPHOLINYL)-[6-[[3(4-FLUOROPHENYL)-5-METHYL-4-ISOXAZOLYL]METHOXY]-3-PYRIDINYL]-METHANONE

The instant invention relates to novel solid forms of the compound of formula (I), as well as solvates, inclusion complexes with other suitable compounds, processes for their manufacture, pharmaceutical compositions containing these solid forms, and their use as medicaments.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Synthetic Route of 39093-93-1, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 39093-93-1, Thiomorpholine 1,1-dioxide, introducing its new discovery.

Anilinoquinazoline inhibitors of the RET kinase domain – Elaboration of the 7-position

We have previously reported a series of anilinoquinazoline derivatives as potent and selective biochemical inhibitors of the RET kinase domain. However, these derivatives displayed diminished cellular potency. Herein we describe further optimisation of the series through modification of their physicochemical properties, delivering improvements in cell potency. However, whilst cellular selectivity against key targets could be maintained, combining cell potency and acceptable pharmacokinetics proved challenging.

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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INDAZOLE-CARBOXAMIDE COMPOUNDS

The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

If you are interested in 39093-93-1, you can contact me at any time and look forward to more communication. Safety of Thiomorpholine 1,1-dioxide

Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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JAK kinase inhibitors and uses thereof (by machine translation)

The invention discloses a having the following general formula (I) compound. The invention also disclosed comprising this compound JAK kinase inhibitor and the compounds in the preparation of the treatment in the JAK related diseases of the application. JAK kinase inhibitors of the present invention, can inhibit the signal transduction of the involved in various JAK1, JAK2, JAK3 and TYK2 kinase biological activity, can effectively clinical treatment of various inflammatory diseases and JAK-mediated signal transduction by the driving of various diseases, very broad application prospects. . (by machine translation)

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Indole and indazole compounds as an inhibitor of cellular necrosis

The present invention refers to a formula (1) compounds of, pharmaceutically acceptable salts or isomers thereof thereof, and characterized by by containing as active ingredients-associated diseases, cell death and method for the prevention or treatment of relates and compositions. [Formula 1] In formula said R 1, R 2, R 3, R 4, R 5, R 6, A, X, n and m to equal the specification. (by machine translation)

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem