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Pyrrolo-triazine derivative, its preparation process and its use in medicine (by machine translation)

The invention relates to a pyrrolotriazines derivative, a preparation method and an application of the pyrrolotriazines derivative on medicine. Concretely, the disclosed pyrrolotriazines derivative has obvious tyrosine kinase inhibition activity, and is an effective tyrosine kinase inhibitor, the pyrrolotriazines derivative provides a new research direction and an approach for developing novel tyrosine kinases inhibition medicines having low drug resistance or capable of alleviating drug resistance to inhibitors at early stage, and has wide application prospect and medicinal value.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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39093-93-1, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. 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

An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

Background: The carboxylesterase Notum has been shown to act as a key negative regulator of the Wnt signalling pathway by mediating the depalmitoleoylation of Wnt proteins. LP-922056 (1) is an orally active inhibitor of Notum. We are investigating the role of Notum in modulating Wnt signalling in the central nervous system and wished to establish if 1 would serve as a peripherally restricted control. An accessible and improved synthetic route would allow 1 to become more readily available as a chemical tool to explore the fundamental biology of Notum and build target validation to underpin new drug discovery programs. Results: An improved, scalable synthesis of 1 is reported. Key modifications include: (1) the introduction of the C7-cyclopropyl group was most effectively achieved with a Suzuki?Miyaura cross-coupling reaction with MIDA-boronate 11 (5 ? 6), and (2) C6 chlorination was performed with 1-chloro-1,2-benziodoxol-3-one (12) (6 ? 7) as a mild and selective electrophilic chlorination agent. This 7-step route from 16 has been reliably performed on large scale to produce multigram quantities of 1 in good efficiency and high purity. Pharmacokinetic studies in mouse showed CNS penetration of 1 is very low with a brain/plasma concentration ratio of just 0.01. A small library of amides 17 were prepared from acid 1 to explore if 1 could be modified to deliver a CNS penetrant tool by capping off the acid as an amide. Although significant Notum inhibition activity could be achieved, none of these amides demonstrated the required combination of metabolic stability along with cell permeability without evidence of P-gp mediated efflux. Conclusion: Mouse pharmacokinetic studies demonstrate that 1 is unsuitable for use in models of disease where brain penetration is an essential requirement of the compound but would be an ideal peripherally restricted control. These data will contribute to the understanding of drug levels of 1 to overlay with appropriate in vivo efficacy endpoints, i.e., the PK-PD relationship. The identification of a suitable analogue of 1 (or 17) which combines Notum inhibition with CNS penetration would be a valuable chemical probe for investigating the role of Notum in disease models.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 39093-93-1, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 39093-93-1

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.

2-METHYL-AZA-QUINAZOLINES

The present invention covers 2-methyl-aza-quinazoline compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Antiviral Compounds

Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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PYRROLO-AROMATIC HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF

The present invention relates to pyrrolo-aromatic heterocyclic compounds, a preparation method therefor and medical use thereof. Particularly, the present invention relates to a compound represented by formula I, a preparation method therefor, a pharmaceutical composition comprising the compound, and use of the compound as a BTK kinase inhibitor. The compound and the pharmaceutical composition comprising same can be used for the treating diseases associated with BTK kinase activity, such as inflammations, autoimmune disorders, and cancers. The definition of each substituent in formula I is the same as that in the description.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS

The present invention is directed to tricyclic compounds of the formula (I), wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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39093-93-1, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S. In a Article, authors is Nagarajan, K.£¬once mentioned of 39093-93-1

Nitroimidazoles: Part VII – 1-(1-Alkyl-5-nitroimidazol-2-yl)-aza(diaza,oxaza)cycloalkanes

Reaction of 1-methyl-2-methylsulphonyl-5-nitroimidazole (2) with pyrrolidine, piperidine and morpholine affords the amines (3a-c)(=9a-c) respectively in low yields, the reaction failing with other bases tried.Analogues (9d-t) have been obtained more readily by nitrating imidazoles (8), which are synthesized from thioureas (5) of cyclic secondary amines through the S-methylisothioureas (6) and the guanidinoacetals (7).

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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39093-93-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S. In a Article, authors is Shainyan£¬once mentioned of 39093-93-1

Triflamides and triflates of six-membered heterocyclic amines

Reactions of secondary cyclic amines (piperidine, morpholine, thiomorpholine, 1lambda6,4-thiazinane-1,1-dione) with trifluoromethanesulfonic anhydride or with N-phenyltriflimide both in the presence and in the absence of a base (Et3N) result in formation of corresponding triflamides and triflates of the initial amines. The triflates and triflamides can be distinguished by their 19F and 15N NMR spectra and the presence in the IR spectra of salts of absorption bands in the region 3270-3000 cm-1 lacking in the spectra of triflamides.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 39093-93-1, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 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. 39093-93-1

LYSYL OXIDASE INHIBITORS

This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 39093-93-1, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 39093-93-1

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

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 39093-93-1 is helpful to your research. 39093-93-1

39093-93-1, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. 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

Amphiphilic Indole Derivatives as Antimycobacterial Agents: Structure-Activity Relationships and Membrane Targeting Properties

Antibacterials that disrupt cell membrane function have the potential to eradicate ?persister? organisms and delay the emergence of resistance. Here we report the antimycobacterial activities of 4-fluoro and 6-methoxyindoles bearing a cationic amphiphilic motif represented by a lipophilic n-octyl side chain at position 1 and a positively charged azepanyl or 1,4-dioxa-8-azaspiro[4.5]decane moiety at position 3. These analogues exhibited balanced profiles of potency (Mycobacterium bovis BCG, M tuberculosis H37Rv), selective activity, solubility, and metabolic stability. Bacteriological mechanism of action investigations on a representative analogue revealed cell membrane permeabilization and depolarization in M bovis BCG. These membrane-related changes preceded cell death indicating that the loss in membrane integrity was not an epiphenomenon. Bactericidal activity was observed against both growing and nongrowing mycobacterial cultures. The analogue also upregulated cell envelope stress-inducible promoters piniBAC and pclgR, implicating the involvement of envelope-related targets in its mode of action.

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