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A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C 1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group

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The rate of rearrangement of the 3-butanoyloxytetrahydropyran-2-yl radical (4) to give the product 5 of 1,2-migration of the acyloxy group has been determined by competition against the reaction of 4 with tributylstannane.The rate constant is larger than that for rearrangement of the acylic radical 18 but less than that for the substituted cholestanyl radical 19.Experiments with 17O- and 18O-labelled substrates indicate that the rearrangement of 4 proceeds with ca. 33percent transposition of the ether and carbonyl oxygen atoms, while there is also a small amount of scrambling in the product 12 formed by direct reduction of 4.The isotope labelling studies and the Arrhenius parameters (log = 12.7, Eact = 58 kJ mol-1) are consistent with the view that the reaction proceeds, at least in part, via dissociation into a tight anion radical-cation pair 22.A pathway via the three-membered transition sturcture 21 might also be involved.

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Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a tricyclic heteroaryl group substituted with R3a and zero to 2 R3b; and R1, R2, R3a, R3b, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

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You could be based in a university, combining chemical research with teaching; in a pharmaceutical company, working on developing and trialing new drugs; helping to ensure national healthcare provision keeps pace with new discoveries. 19752-84-2, Name is Tetrahydro-2H-pyran-3-ol, molecular formula is C5H10O2. In a Short Survey,once mentioned of 19752-84-2, Related Products of 19752-84-2

The non-haem Fe(II) and 2-oxoglutarate (2OG)-dependent oxygenases belong to a superfamily of structurally-related enzymes that play important biological roles in plants, microorganisms and animals. Structural, mechanistic and functional studies of 2OG oxygenases require efficient and effective biophysical tools. Nuclear magnetic resonance (NMR) spectroscopy is a useful tool to study this enzyme superfamily. It has been applied to obtain information about enzyme kinetics, identify and characterise 2OG oxygenase-catalysed oxidation products, elucidate the catalytic mechanism, monitor ligand binding and study protein dynamics. This review summarises the types of information that NMR spectroscopy can provide in the studies of 2OG oxygenases, highlights the advantages of the technique and describes its drawbacks.

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Human African trypanosomiasis (HAT) is a neglected tropical disease caused by infection with either of two subspecies of the parasite Trypanosoma brucei. Due to a lack of economic incentive to develop new drugs, current treatments have severe limitations in terms of safety, efficacy, and ease of administration. In an effort to develop new HAT therapeutics, we report the structure-activity relationships around T. brucei for a series of benzoxazepinoindazoles previously identified through a high-throughput screen of human kinase inhibitors, and the subsequent in vivo experiments for HAT. We identified compound 18, which showed an improved kinase selectivity profile and acceptable pharmacokinetic parameters, as a promising lead. Although treatment with 18 cured 60% of mice in a systemic model of HAT, the compound was unable to clear parasitemia in a CNS model of the disease. We also report the results of cross-screening these compounds against T. cruzi, L. donovani, and S. mansoni.

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Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme. Irreversible inhibitors are therefore the equivalent of poisons in heterogeneous catalysis. 19752-84-2, C5H10O2. A document type is Patent, introducing its new discovery., Electric Literature of 19752-84-2

The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.

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A catalyst don`t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. HPLC of Formula: C5H10O2HPLC of Formula: C5H10O2, , Name is Tetrahydro-2H-pyran-3-ol, molecular formula is C5H10O2. In a patent, introducing its new discovery.

The allylic epoxides (1)-(4) were transformed to the tetrahydrofurfuryl alcohols (17)-(20), respectively.The formation of (6) and (10) in the hydroboration-oxidation of (4) is interpreted.The monohydroboration-oxidation of (13) and (14) gave (15) and (16), respectively.

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The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 19752-84-2 is helpful to your research., Recommanded Product: Tetrahydro-2H-pyran-3-ol

In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction. 19752-84-2, Name is Tetrahydro-2H-pyran-3-ol, molecular formula is C5H10O2. In a Article,once mentioned of 19752-84-2, Recommanded Product: Tetrahydro-2H-pyran-3-ol

The regiochemical control of the ring opening of epoxides bearing polar remote functionalities, through chelation processes assisted by metal ions, was verified in the title compound (4).The use of metal assisted procedures in several ring opening reactions of 4 leads to a modification of the regiochemical outcome, and the attack of the nucleophile on the C-4 oxirane carbon is highly favored.

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Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In homogeneous catalysis, catalysts are in the same phase as the reactants.19752-84-2, C5H10O2. A document type is Article, introducing its new discovery., Reference of 19752-84-2

Multivariate curve resolution (MCR) methods are proposed to improve the analysis of volatile components of an Iranian rice sample (Domsiah) by headspace sampling coupled to gas chromatography-mass spectrometry. A total of 31 components was identified using similarity searches between mass spectra and mass spectrometry database. Then extended multivariate curve resolution-alternating least squares (MCR-ALS) by applying proper constraints is used to obtain pure elution and mass spectral profiles for the components present in each peak cluster. The resolved components were identified by similarity searches using the NIST mass database and their percentage were calculated for qualitative and quantitative analysis, respectively. The number of identified components was extended to 82 by applying the MCR-ALS techniques. The main identified volatile chemicals that were found in an Iranian rice sample (Domsiah) were; nonanal (18.22%), hexanal (14.33%), 2-benzoyl-6,7-dimethoxy-4-methylidene-2H-1,3-benzothiazine (7.81%), epilophodione (7.023%), and 1-methyl-4-(1-methylethenyl)cyclohexene (6.61%).

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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. In an article, published in an article, once mentioned the application of 19752-84-2, Name is Tetrahydro-2H-pyran-3-ol,molecular formula is C5H10O2, is a conventional compound. this article was the specific content is as follows.SDS of cas: 19752-84-2

tert-Butyl hydroperoxide (TBHP) stereoselectively oxidizes substituted 4-pentenols, when activated by (ethyl)[cis-(piperidine-2,6-diyl)dimethyl] vanadates. The reaction affords (tetrahydrofuran-2-yl)methanols in up to 89% yield, and in stereoselectivity ranging between moderate (cis:trans=32:68) to excellent (>99:1). Correlating structures of 4-pentenols, differing by substitution at tetragonal and trigonal stereocenters, to configuration of products obtained from oxidative cyclization provides a reaction model explaining the origin of stereoselectivity by (i) intramolecular oxygen atom transfer to (ii) a chair-like folded alkenol, being (iii) hydrogen-bonded to one of the two aminodiolate oxygens of the chelated vanadate, having (iv) substituents in the chair-like transition structure preferentially aligned equatorially. Substituents at trigonal stereocenters improve 2,5-cis- and 2,4-trans-selectivity for oxidative 4-pentenol cyclization in case of (Z)-configuration. An (E)-substituent does not alter selectivity exerted by a terminal (Z)-substituent of similar steric size. Larger (E)-groups increase the fraction of 2,5-trans-cyclized products. The reaction model additionally implements results from vanadium-51 NMR spectroscopy and density functional theory. According to theory, the (dialkoxy)(oxo)vanadium substituent exerts in the preferred end-on conformation almost no effect on structure and bonding of the peroxide group in tert-butylperoxy vanadates. Changing conformation to a higher in energy side-on arrangement puts the vanadate-bound tert-butylperoxy group into a position to serve in a concerted reaction as combined electron acceptor and oxygen atom donor.

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