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The present invention provides compounds represented by the formula (Ie) and the formula (If) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Compounds and methods which modulate feeding behavior and related diseases

There are provided compounds, compositions and methods of use thereof in the modulation of feeding behavior, obesity, diabetes, cancer (tumor), inflammatory disorders, depression, stress related disorders, Alzheimer’s disease and other disease conditions.

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Tetrahydropyran – Wikipedia,
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Palladium-catalyzed N-monoarylation of amidines and a one-pot synthesis of quinazoline derivatives

A method for the Pd-catalyzed N-arylation of both aryl and alkyl amidines with a wide range of aryl bromides, chlorides, and triflates is described. The reactions proceed in short reaction times and with excellent selectivity for monoarylation. A one-pot synthesis of quinazoline derivatives, via addition of an aldehyde to the crude reaction mixture following Pd-catalyzed N-arylation, is also demonstrated.

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Tetrahydropyran – Wikipedia,
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The Synthesis and Properties of 2-Substituted Dihydropyrimidines

Various 2-substituted 1,4-dihydro-4,4,6-trimethyl-1-phenylpyrimidines and 1,6-dihydro-4,6,6-trimethylpyrimidines were synthesized independently.For these dihydropyrimidines, the physical data such as the uv, ir, and nmr spectra and the oxidation potential were compared. 2-Dimethylamino substituted dihydropyrimidine showed the lowest oxidation potential, which expected the similar reducing ability as dihydropyridines.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS

The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORgamma modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORgamma receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

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Tetrahydropyran – Wikipedia,
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Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation

Phosphatidylinositol-3-kinase alpha (PI3Kalpha) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kalpha, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of 2H-Pyran-3,5(4H,6H)-dione

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Bicyclic Heterocycles with Nitrogen at the Ring Junction. Part 2. Application of the Dakin-West Reaction to the Synthesis of Imidazo<5,1-f>-1,2,4-triazin-4(3H)-ones

A series of novel acylamino alpha-keto-esters (4) have been prepared via a Dakin-West reaction of acylated alpha-amino-acids and ethyl oxalyl chloride.Their use in a general synthesis of imidazo<5,1-f>-1,2,4-triazin-4(3H)-ones (7) is described.The conversion of the imidazotriazinones into the corresponding imidazo<5,1-f>-1,2,4-triazines (20) and their 3,4-dehydro-derivatives (19) are also reported.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Green’ synthesis of 2-substituted 6-hydroxy-[3H]-pyrimidin-4-ones and 4,6-dichloropyrimidines: Improved strategies and mechanistic study

An improved route to 2-substituted 6-hydroxy-[3H]-pyrimidin-4-ones 4 and to 2-substituted 4,6-dichloropyrimidines 5 is reported. Without using highly toxic reactants, compounds 4 can be prepared conveniently in a one pot synthesis on a one mol scale with average yields up to 80%. 4,6-Dichloropyrimidines 5, which are usually prepared in small quantities, are synthesized with average yields of 80%, using up to 80g of starting material. The mechanism of the chlorination of 4 is investigated computationally for the first time. The results suggest that the chlorination with phosphoryl chloride occurs in an alternating phosphorylation-chlorination manner (pathway 1) which is preferred over a sequence which starts with two phosphorylations. The investigated 4,6-dichloropyrimidines described herein form strong complexes with dichlorophosphoric acid but weak complexes with hydrochloric acid (generated during workup). These latter complexes explain the necessity of using aqueous sodium carbonate during the working up. In order to prevent possible formation of pyrimidinium salts between intermediates or the final dichloropyrimidines and unreacted hydroxypyrimidone, the latter could be deactivated with a strong acid such as dichlorophosphoric acid, thus allowing chlorination but prohibiting salt formation. Because of its general applicability to all nitrogen heterocycle chlorinations with phosphoryl chloride, the proposed route to dichloropyrimidines without solvent or side products, using less toxic reactants, is of general synthetic interest.

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Tetrahydropyran – Wikipedia,
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Pyrimidine derivatives and new pyridine derivatives

Achirai pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains and various diseases associated with the N-type calcium channels.

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Tetrahydropyran – Wikipedia,
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Eco-friendly Synthesis of 3-(Aryl)-2,6-diphenylpyrimidin-4(3H)-ones, Ethyl-1-(aryl)-1,6-dihydro-2-(aryl)-6-oxopyrimidine-4-carboxylates and 6-(4-Arylphenyl)-2-isopropylpyrimidin-4(3H)-one

In present communication, we report the synthesis of pyrimidin-4(3H)-one derivatives by microwave irradiation in good yields and less reaction time. All titled compounds were characterized by IR, NMR and Mass spectral analyses.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics