Tag: M.W:100-200

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Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target

The discovery of the activating mutation V617F in the JH2 domain of Jak2 and the modulation of oncogenic Stat3 by Jak2 inhibitors have spurred a great interest in the inhibition of the Jak2/Stat pathway in oncology. In this Letter, we communicate the discovery of novel inhibitors of the Jak2/Stat5 axis, the N-(1H-pyrazol-3-yl)pyrimidin-2-amino derivatives. The rationale, synthesis and biological evaluation of these derivatives are reported. Two lead analogs from this series, 6 and 9, displayed prolonged residence time on Jak2, at enzymatic level. Although 6 and 9 exhibited moderate selectivity in a selected kinase panel, we chose to test these inhibitors in vivo as a consequence to their long residence time. However, extended inhibition of Jak2 due to the long residence time, in the form of inhibiting phosphorylation of downstream Stat5, was not recapitulated in an in vivo setting.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents

A series of linezolid analogues containing a hydrazone moiety were designed, synthesized and evaluated for their antibacterial activity. Most compounds exhibited more potent antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens as compared with linezolid and radezolid. Compounds 9a, 9c, 9f, 9g, 10m and 10t were more potent against tested clinical isolates of MRSA, MSSA, VRE and LREF as compared to linezolid. Compound 9a exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9a showed remarkable antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.0675 mg/mL, respectively, which was 15- to 30-fold more potent than linezolid.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. category: Thiomorpholine, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 39093-93-1, name is Thiomorpholine 1,1-dioxide. In an article£¬Which mentioned a new discovery about 39093-93-1

Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an alpha-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere

Overexpression of the antiapoptotic protein Mcl-1 provides a survival advantage to some cancer cells, making inhibition of this protein an attractive therapeutic target for the treatment of certain types of tumors. Herein, we report our efforts toward the identification of a novel series of macrocyclic Mcl-1 inhibitors featuring an alpha-hydroxy phenylacetic acid pharmacophore or bioisostere. This work led to the discovery of 1, a potent Mcl-1 inhibitor (IC50 = 19 nM in an OPM-2 cell viability assay) with good pharmacokinetic properties and excellent in vivo efficacy in an OPM-2 multiple myeloma xenograft model.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. COA of Formula: C4H9NO2S, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 39093-93-1, name is Thiomorpholine 1,1-dioxide. In an article£¬Which mentioned a new discovery about 39093-93-1

NITROGENOUS HETEROCYCLIC COMPOUND, PREPARATION METHOD, INTERMEDIATE, COMPOSITION AND USE

Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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ANTI-MALARIAL AGENTS

The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.C4H9NO2S, introducing its new discovery. , Recommanded Product: 39093-93-1

EXTENDED BETULINIC ACID ANALOGS

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II:. These compounds are useful for the treatment of HIV and AIDS.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Product Details of 39093-93-1, 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

Homogeneous Aqueous Oxidation of Organic Molecules by OxoneR and Catalysis by a Water-Soluble Manganese Porphyrin Complex

Peroxymonosulfate (KHSO5) oxidizes a wide variety of water-soluble organic molecules in aqueous solutions, and the reactions are generally more rapid in phosphate buffer (pH 6-7) than in pure water.A water-soluble porphyrin complex, meso-tetrakis(4-N-methylpyridyl)porphyrinatomanganese(III) chloride, catalyzes epoxidation and hydroxylation under neutral pH conditions.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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CRYSTALLINE FILGOTINIB SULFONIC ACID ADDITION SALTS

The present invention relates to filgotinib sulfonic acid addition salts, their polymorphs, a method of preparing the same as well as a pharmaceutical composition comprising the same.

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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, Quality Control of Thiomorpholine 1,1-dioxide, 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

5H-PYRIDO[3,2-B]INDOLE COMPOUNDS AS ANTICANCER AGENTS

The present invention is directed to tricyclic compounds of formula (I), pharmaceutically acceptable compositions comprising compounds of the invention and said compositions for use in methods for the treatment of various disorders in particular cancer.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem