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Barbituric acid derivatives as inhibitors of TNF-alpha converting enzyme (TACE) and/or matrix metalloproteinases

The present application describes novel barbituric acid derivatives of formula I: 1or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-alpha converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

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

 

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Design, Synthesis, Safener Activity, and Molecular Docking of Novel N-Substituted Thiazide/Thiazole Derivatives

A series of novel substituted thiazide/thiazole compounds were designed by splicing active groups and bioisosterism. The title compounds were synthesized via the cyclization, acylation, and carbamylation. All the compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS. The single crystal of compound 3f was determined by X-ray crystallography. The biological activity tests indicated that all the compounds showed potential safener activity to the herbicide chlorsulfuron, in which compound 3e showed almost the same level as the commercialized safener AD-67. The molecular docking results were in good agreement with the bioassay results, which demonstrated that compound 3e might compete with chlorsulfuron in the acetolactate synthase active site, causing the herbicide ineffective in maize.

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

 

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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

 

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The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research.Keep reading other articles of 3,4-Dihydro-2H-benzo[b][1,4]thiazine!Electric Literature of 3080-99-7

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An odorless, one-pot synthesis of nitroaryl thioethers via SNAr reactions through the in situ generation of S-alkylisothiouronium salts

A newly developed C-S bond formation nucleophilic aromatic substitution (SNAr) reaction in aqueous Triton X-100 (TX100) micelles has been disclosed. This chemistry, in which odorless, cheap and stable thiourea in place of thiols is used as the sulfur reagent, provides an efficient approach for the generation of nitroaryl thioethers, which are useful structural units of many bioactive molecules, rendering this methodology attractive to both synthetic and medicinal chemistry.

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

 

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COMPOUND HAVING 11 beta HSD1 INHIBITORY ACTIVITY

The present invention provides compounds having excellent 11-HSD1 inhibitory activity. A compound represented by the following formula (I): [wherein X 1 represents an oxygen atom, or the formula -(CR 11 R 12 ) p -, etc., Y 1 represents a hydrogen atom, a hydroxyl group, etc., Z 1 represents an oxygen atom or the formula -(NR 14 )-, R 1 represents a hydrogen atom, a halogen atom, a cyano group, a C 1-4 alkyl group, a C 1-4 alkyl group substituted with 1 to 3 halogen atoms, a C 1-4 alkoxy group, a C 1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R 2 represents a hydrogen atom or a C 1-4 alkyl group, and n represents an integer of 1 or 2]

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

 

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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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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? , category: thiazines, 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

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

 

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Synthesis and Reactivity of 4-Substituted-2,3-dihydrobenzo-1,4-thiazines

A series of derivatives of 4H-2,3-dihydrobenzo-1,4-thiazine has been prepared. 4-Acetyl-2,3-dihydrobenzo-1,4-thiazine undergoes self-condensation by n-butylmagnesium bromide affording the corresponding 4-acetoacetyl-2,3-dihydrobenzo-1,4-thiazine, which, is converted to 5H-1,4-thiazino<2,3,4-ij>quinolin-5-one.Halogenation of the acetyl derivative takes place at the position 2 of the heterocyclic ring and oxidation leads to 1-oxides and 1,1-dioxides.

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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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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