The important role of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS

Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

A new application about 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)

The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Let¡¯s face it, organic chemistry can seem difficult to learn. 3080-99-7. Especially from a beginner¡¯s point of view. Like 3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine. In a document type is Article, introducing its new discovery.

Chemoselective Deprotection of Sulfonamides under Acidic Conditions: Scope, Sulfonyl Group Migration, and Synthetic Applications

Chemoselective acidic hydrolysis of sulfonamides with trifluoromethanesulfonic acid has been evaluated as a deprotection method and further extended to more complex synthetic applications. In contrast to conventional troublesome sulfonamide hydrolysis, a near-stoichiometric amount of acid was found to be sufficient to bring about efficient deprotection of various neutral or electron-deficient N-arylsulfonamides, whereas electron-rich substrates provided sulfonyl group migration products. The deprotection method developed is fully selective for N-arylsulfonamides, and the possibility to discriminate among various different sulfonamides is demonstrated.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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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, 3080-99-7, molcular formula is C8H9NS, introducing its new discovery. 3080-99-7

SPIRO-CYCLIC BETA-AMINO ACID DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEASES AND TNF-ALPHA CONVERTING ENZYME (TACE)

The present application describes novel spiro-cyclic beta-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-alpha converting enzyme (TACE), and/or aggrecanase inhibitors.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

A new application about 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists

4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (hTGR5 and mTGR5) with EC50 values in the low nanomolar range. Compound 23g, with an EC50 value of 0.72 nM on hTGR5 and an EC 50 value of 6.2 nM on mTGR5, was selected for further in vivo efficacy studies. This compound exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect. A single oral dose of 23g (50 mg/kg) significantly reduced blood glucose levels in db/db mice and caused a 49% reduction in the area under the blood glucose curve (AUC)0-120min following an oral glucose tolerance test (OGTT) in imprinting control region (ICR) mice. However, 23g stimulated gallbladder filling, which might result in side effects to the gallbladder.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Archives for Chemistry Experiments of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, belongs to thiazines compound, is a common compound. 3080-99-7In an article, authors is Babudri, Francesco, once mentioned the new application about 3080-99-7.

An Easy and Efficient Synthesis of 4H-Thiazolo<5,4,3-i,j>quinolin-4-ones and 5H-1,4-thiazino<2,3,4-i,j>quinolin-5-ones

The title heterocycles have been synthesized by a Claisen-type self condensation of acetylbenzothiazolines and acetyldihydrobenzothiazines and subsequent cyclization.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Awesome and Easy Science Experiments about 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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3080-99-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, molecular formula is C8H9NS. In a Article, authors is Satoh£¬once mentioned of 3080-99-7

Studies on a novel, potent and orally effective cholecystokinin A antagonist, FK-480. Synthesis and structure-activity relationships of FK-480 and related compounds

We prepared various novel tricyclic 1,4-benzodiazepine derivatives as cholecystokinin (CCK) A antagonists, which were evaluated preliminarily for inhibition of 125I-CCK-8 binding to rat pancreatic membranes in vitro and inhibiting effect on CCK-8-induced inhibition of charcoal meal gastric emptying in mice. On the basis of structure-activity relationship (SAR) studies, as well as the stability and availability of the starting materials of those compounds, (S)-N-[1-(2-fluorophenyl)-3,4,6,7-tetrahydro-4-oxo-pyrrolo[3,2,1-jk][1 ,4]benzodiazepin-3-yl]1 H-indole-2-carboxamide (9f, FK-480) was selected as a candidate compound for further evaluation. The absolute configuration of the precursor of FK-480, (3S)-amino-1,4-benzodiazepine derivative ((S)-8a, R1 = F) was determined by an X-ray crystallographic study of its ureido derivative with (S)-alpha-methylbenzyl isocyanate. FK-480 is now undergoing clinical studies for the treatment of chronic pancreatitis.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Archives for Chemistry Experiments of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, 3080-99-7, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, molecular formula is C8H9NS. In a Review, authors is Rajiv, Neethu£¬once mentioned of 3080-99-7

A review on synthesis of benzothiazine analogues

Scientific advances mainly involves the development of new and highly reactive compounds. Nitrogen and sulphur containing benzothiazines forms highly active heterocyclic agents. Benzothiazines are prominent class of heterocyclic compound. Many studies have been done in the development of benzothiazine analogues. Microwave assisted synthesis, regioselective techniques and other methods are also used for benzothiazine synthesis. Various methods have been developed for the synthesis of benzothiazine derivatives. Benzothiazines exhibits numerous therapeutic activities like anti-HIV, calcium antagonistic, anti-serotinin, analgesic, anti-mycobacterial anti-microbial, anti-oxidant, anti-rheumatic, anti-inflammatory, anti-hypertensive ,calcium channel blocker, anti-malarial, potassium channel opener, cardiovascular, anthelmintic, neuroprotective, aldose reductase inhibitor, herbicidal, pesticidal etc. This has raised the necessity to explore novel benzothiazine derivatives which can significantly contribute to the development of therapeutically active agents. And the newer development of novel benzothiazines derivatives also involves the same characteristic features and also contribute various activities.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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3080-99-7, 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, the author is Gigant, Nicolas and a compound is mentioned, 3080-99-7, 3,4-Dihydro-2H-benzo[b][1,4]thiazine, introducing its new discovery.

Construction of nitrogen-fused tetrahydroquinolines via a domino reaction

An efficient domino approach for the diastereoselective synthesis of polyfunctionalized nitrogen-fused tetrahydroquinoline frameworks under mild conditions has been developed. The scope and limitation of this transformation were investigated by using a range of readily accessible enamides and benzyl azides. This method is also applicable to the formation of 2,3-functionalized enamides.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes. The pharmacologic utility of TGR5 agonists has been limited by systemic target-related effects such as excessive gallbladder filling and blockade of gallbladder emptying. Gut-restricted TGR5 agonists, however, have the potential to avoid these side effects and consequently be developed into drugs with acceptable safety profiles. We describe the discovery and optimization of a series of gut-restricted TGR5 agonists that elicit a potent response in mice, with minimal gallbladder-related effects. The series includes 12 (TGR5 EC50: human, 143 nM; mouse, 1.2 nM), a compound with minimal systemic availability that may have therapeutic value to patients with type 2 diabetes mellitus, nonalcoholic steatohepatitis, or inflammatory bowel disease.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem