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QUINOXALINE AND PYRIDOPYRAZINE DERIVATIVES AS PI3KBETA INHIBITORS

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kbeta inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

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

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PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Theoretical and experimental studies of cycloconjugation involving second-row elements

In a method proposed to investigate conjugative interactions between second-row elements (S, P) amd a pi-electron system, barriers to amide rotation have been measured using NMR line-shape methods, for N-acetyl-4-X(hetero)-1,4-dihydropyridines (X = SO2,7; P(O)OCH3,13; C(CH3)2, 6 (reference)) as well as the dihydro (8a) and tetrahydro (9) derivatives, respectively, of 7. It is suggested that such interactions would stabilize the transition states for amide rotation by cycloconjugation but not the planar equilibrium states, compressing the barriers relative to reference 6. In fact, amide barriers in 7,13, and N-acetylpyrrole are substantially (>6 kcal) less than in 6, 8ab, and 9, all ca. 17 kcal, in all of which saturated centers interrupt possible cycloconjugation. These conclusions are supported by the results of ab initio calculations at the Hartree-Fock level with the 3-21G(*) basis set.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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BENZENE-FUSED 6-MEMBERED OXYGEN-CONTAINING HETEROCYCLIC DERIVATIVES OF BICYCLIC HETEROARYLS

The invention relates to new derivatives of formula 1, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Substituted Imidazopyridinyl-Aminopyridine Compounds

The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. SDS of cas: 39093-93-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 39093-93-1, in my other articles.

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TETRAHYDROPYRAN-BASED THIODISACCHARIDE MIMICS AS GALECTIN-3 INHIBITORS

The present disclosure relates to compounds of Formula (1), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods making and using such compounds and compositions.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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AhR MODULATORS

Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae: (I) wherein the letters and symbols X1, X2, Z, R1b, R1c, R1d, R1e, R2a, R2b, R2c and R2d have the meanings provided in the specification.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Synthetic Route of 39093-93-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 39093-93-1, molcular formula is C4H9NO2S, introducing its new discovery.

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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SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES

There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Tetrahydroquinoline Derivatives And Their Pharmaceutical Use

Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem