Category: 39093-93-1

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NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variablesHet, A, X, Y, Z, Rl, R2, R3, R4, R5 andQ are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, theinvention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP

Inspired by previous efforts in the pyrazolobenzoxazine class of KSP inhibitors, the design and synthesis of 1,4-diaryl-4,5-dihydropyrazole inhibitors of KSP are described. Crystallographic evidence of binding mode and in vivo potency data is also highlighted.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 39093-93-1, name is Thiomorpholine 1,1-dioxide, introducing its new discovery. Computed Properties of C4H9NO2S

INDOLEAMIDE COMPOUNDS AS AN IHNIBITOR OF CELLULAR NECROSIS

The present invention relates to a an indoleamide compound of chemical formula 1, pharmaceutically allowable salt thereof, or an isomer, to a composition for preventing or treating cellular necrosis and related diseases containing the same as an active ingredient, and to a method for manufacturing the composition. In the formula, R1, R2, R3, R4, and R5 are the same as defined in the specification.COPYRIGHT KIPO 2015

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 39093-93-1, name is Thiomorpholine 1,1-dioxide, introducing its new discovery. Recommanded Product: 39093-93-1

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu2/3 inhibition and a variety of CNS diseases and disorders. Though these tools typically have good selectivity for mGlu2/3 versus the remaining six members of the mGlu family, compounds that are selective for only one of the individual group II mGlus have proved elusive. Herein we report on the discovery of a potent and highly selective mGlu2 negative allosteric modulator 58 (VU6001192) from a series of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides. The concept for the design of this series centered on morphing a quinoline series recently disclosed in the patent literature into a chemotype previously used for the preparation of muscarinic acetylcholine receptor subtype 1 positive allosteric modulators. Compound 58 exhibits a favorable profile and will be a useful tool for understanding the biological implications of selective inhibition of mGlu2 in the CNS.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

39093-93-1, Name is Thiomorpholine 1,1-dioxide, belongs to Thiomorpholine compound, is a common compound. Formula: C4H9NO2SIn an article, once mentioned the new application about 39093-93-1.

Synthesis, Characterization and Catalytic Activity of a Tungsten(VI) Amino Triphenolate Complex

Abstract: Synthesis, characterization and catalytic activity of a novel tungsten(VI) amino triphenolate complex have been investigated. In particular, a tungsten(VI) amino triphenolate complex has been synthesized and tested in the oxidation of sulfides and cyclooctene, using hydrogen peroxide as terminal oxidant. The catalyst has proved to be air and water tolerant, also showing a good efficiency in terms of yields and selectivity. Moreover, an upgrade of our previous ligand synthesis is herein reported. The new developed procedure allows to obtain the triphenolamine in large scale without the use of chromatography for the intermediates purification. Graphical Abstract: [Figure not available: see fulltext.].

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 39093-93-1, name is Thiomorpholine 1,1-dioxide, introducing its new discovery. Recommanded Product: 39093-93-1

BENZOXAZINE ARYL SULFONAMIDE DERIVATIVES AS KV1.3 MODULATORS

Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, p, E, X, R1, R2, R3, R4R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology

FAAH inhibitors offer safety advantages by augmenting the anandamide levels ?on demand? to promote neuroprotective mechanisms without the adverse psychotropic effects usually seen with direct and chronic activation of the CB1 receptor. FAAH is an enzyme implicated in the hydrolysis of the endocannabinoid N-arachidonoylethanolamine (AEA), which is a partial agonist of the CB1 receptor. Herein, we report the discovery of a new series of highly potent and selective carbamate FAAH inhibitors and their evaluation for neuroprotection. The new inhibitors showed potent nanomolar inhibitory activity against human recombinant and purified rat FAAH, were selective (>1000-fold) against serine hydrolases MGL and ABHD6 and lacked any affinity for the cannabinoid receptors CB1 and CB2. Evaluation of FAAH inhibitors 9 and 31 using the in vitro competitive activity-based protein profiling (ABPP) assay confirmed that both inhibitors were highly selective for FAAH in the brain, since none of the other FP-reactive serine hydrolases in this tissue were inhibited by these agents. Our design strategy followed a traditional SAR approach and was supported by molecular modeling studies based on known FAAH cocrystal structures. To rationally design new molecules that are irreversibly bound to FAAH, we have constructed ?precovalent? FAAH-ligand complexes to identify good binding geometries of the ligands within the binding pocket of FAAH and then calculated covalent docking poses to select compounds for synthesis. FAAH inhibitors 9 and 31 were evaluated for neuroprotection in rat hippocampal slice cultures. In the brain tissue, both inhibitors displayed protection against synaptic deterioration produced by kainic acid-induced excitotoxicity. Thus, the resultant compounds produced through rational design are providing early leads for developing therapeutics against seizure-related damage associated with a variety of disorders.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS

The present invention provides Fused Tricyclic Compounds of the Formula (1) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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ANTIBACTERIAL QUINOLINE DERIVATIVES

The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. category: Thiomorpholine, 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

PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISORDERS

The present invention discloses pharmaceutical compositions comprising: a compound according to Formula I: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem