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Reference of 3080-99-7, 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 a type is Patent, 3080-99-7, molecular formula is C8H9NS, introducing its new discovery.

Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds

[Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.

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

 

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. Safety of 3,4-Dihydro-2H-benzo[b][1,4]thiazine, In a article, mentioned the application of 3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, molecular formula is C8H9NS

Synthesis and antitumor activity of some new substituted quinolin-4- one and 1,7-naphthyridin-4-one analogs

The synthesis of some new analogs of quinolin-4-one and 1,7- naphthyridin-4-one is described. The prepared compounds were tested for their in vitro antitumor and cdc2 kinase or cdc25 phosphatase inhibitory activity. Compound ethyl 7-oxo-2,3-dihydro-7H-pyrido [1,2,3-de][2,3- b]pyrido-1,4-thiazine-6-carboxylate (6b) showed antitumor activity against CNS SNB-75, breast T-47D, and lung NCI-H522 cancer cell lines with GI50 values of 8.3, 17.6, and 22.7 muM, respectively. Meanwhile, the compounds ethyl 4-oxo-8-phenylthio-1H,4H-quinoline-3-carboxylate (11a) and 4-oxo-8- phenylthio-1H,4H-1,7-naphthyridine-3-carboxylic acid (12b) have proved to be cdc25 phosphatase inhibitors at IC50 values of 11 and 5 muM, respectively.

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

 

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Chemistry can be defined as the study of matter and the changes it undergoes. Formula: C8H9NS. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, molecular formula is C8H9NS, introducing its new discovery.

Development of high-affinity 5-HT3 receptor antagonists. Structure- affinity relationships of novel 1,7-annelated indole derivatives. 1

On the basis of the structures of ondansetron and GR 65,630, its ring- opened C-linked methylimidazole analogue, novel 1,7-annelated indole derivatives were synthesized as potential 5-HT3 antagonists. Receptor binding studies show that all compounds display a high affinity for the 5- HT3 receptors. In both series annelation results in compounds being 7 and 4 times more potent than the references ondansetron and GR 65,630, respectively. Similar to ondansetron, the 1,7-annelated indoles show little stereoselectivity. The (-)-isomers are only slightly more potent than the (+)-isomers. The receptor binding profile of l-10-[(2-methyl-1H-imidazol-1- yl)methyl]-5,6,8,9,10,11-hexahydro-4H-pyrido[3,2,1-jk]carbazol-11-one hydrochloride (24b) (INN cilansetron) shows that the compound displays, besides a high affinity for 5-HT3 receptors (K(i) = 0.19 nM), a weak affinity for sigma-receptors (K(i) = 340 nM), muscarine M1 receptors (K(i) = 910 nM), and 5-HT4 receptors (K(i) = 960 nM) and no affinity (K(i) ? 5000 nM) for all the other receptor types tested (n = 37). The new compounds fit the proposed necessary chemical template for binding: a heteroaromatic ring system, a coplanar carbonyl group, and a nitrogen center at well-defined distances. The enhanced potency of the annelated 1,7-indole derivatives indicates that the extra ring provides a favorable hydrophobic area for interaction with the 5-HT3 receptor site. In vivo cilansetron is more potent and induces less central side effects than ondansetron. At present cilansetron is in clinical trials.

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

 

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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

 

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Iridium-catalyzed dehydrogenative alpha-Functionalization of (Hetero)aryl-Fused cyclic secondary amines with indoles

Herein, by employing dehydrogenation as a substrate-activating strategy, a new iridium-catalyzed direct alpha-functionalization of (hetero)aryl-fused cyclic secondary amines with indoles has been demonstrated, which proceeds with merits that include high step- and atom-efficiency, readily available feedstocks, a simple catalyst system, good functional group tolerance, and operational simplicity.

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

 

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Aromatic Ring Bromination in 1,4-Benzothiazines, 1,4-Benzoxathianes and 1,4-Benzodithianes: the Occurrence of Vicarious Nucleophilic Substitution of Hydrogen and Electrophilic Aromatic Substitution Mechanisms

1,4-benzodithianes, 1,4-benzothiazines and 1,4-benzoxathianes, when treated with bromine in anhydrous chloroform, undergo regiospecific monobromination at the aromatic ring.Based on semiempirical quantum mechanical calculations, the regiochemistry of the reaction in the case of 1,4-benzothiazines and 1,4-benzoxathianes was shown to be consistent with a charge-controlled electrophilic aromatic substitution reaction where the Br+ species comes from monobromosulfonium ions (as 2).On the contrary, in the case of 1,4-benzodithianes, the bromination is accomplished by Br- via an orbital-controlled vicarious nucleophilic substitution of hydrogen occurring on dibromodisulfonium ions (as 4).

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

 

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Eliminative Ring Fission of 4-Acyl-2,3-dihydro-4H-1,4-benzothiazines

The behavior of 4-acyl-2,3-dihydro-1,4-benzothiazines 1-11 upon treatment with lithium diisopropylamide (LDA) in THF at -78 deg C has been examined.Very marked differences have been observed.Whereas unsubstituted and monosubstituted derivatives (1-4) readily undergo “eliminative ring fission”, providing 2-(alkylthio)phenylenamides 12, 2-aminophenyl vinyl sulfides 16, and 3-acylbenzothiazolines 13, 2,3-disubstituted derivatives (5-7) do not react at all.The relationship between structural features of the above-mentioned dihydrobenzothiazines and their reactivity is considered.Lithium ion plays a fundamental role in providing activation for the ring-opening reaction.

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

 

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NON-SYSTEMIC TGR5 AGONISTS

Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, where in R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided

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

 

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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

 

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? , name: 3,4-Dihydro-2H-benzo[b][1,4]thiazine, The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, molecular formula is C8H9NS. In a article£¬once mentioned of 3080-99-7

The scandium rare earth catalyst in the alkylation reaction of the amine to the location in the application (by machine translation)

The present invention relates to rare earth catalyst in catalytic aromatic amine containing scandium para-selectivity of the alkylation reaction in the application, the structural formula of the scandium rare earth catalyst are as follows: Aromatic amine aromatic primary amine or aromatic secondary amine. The invention also discloses a method for alkylation of the amine of preparation method: formula (1) aromatic amines of the formula (2) of the olefin in the scandium rare earth under the action of catalyst, in organic solvent for 60 – 150 C lower reaction, to obtain the location of alkylated aromatic amine, the reaction route is as follows: Wherein R1 Hydrogen, aromatic itaconate C1 – C10 Alkyl; R2 Hydrogen, C1 – C4 Alkyl, C1 – C4 Alkoxy, aryl or halogen; and R2 Can not be substituted in the para position; X is methylene or sulfur atom, n1 for 0 – 4 in either a value; R3 For C1 – C20 Alkyl, aryl or R5 Through a number of methylene ring, the number of methylene n2 for 1 – 4 in either a value; R4 Hydrogen, C1 – C20 Alkyl, aryl, thienyl, benzofuranyl or substituted aryl group; R5 Hydrogen, methyl or methylene; R6 Is hydrogen. (by machine translation)

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