Simple exploration of Tetrahydropyran-4-carbaldehyde

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Solid dispersions containing an apoptosis-inducing agent

A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

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Modular synthesis of 3,6-disubstituted-1,2,4-triazines via the cyclodehydration of beta-keto- N -acylsulfonamides with hydrazine salts

A straightforward method for preparing 3,6-disubstituted-1,2,4-triazines through a redox-efficient cyclodehydration of beta-keto-N-acylsulfonamides with hydrazine salts is described. Two approaches for synthesizing the requisite beta-keto-N-acylsulfonamides are presented, which allow for the late stage incorporation of either the C3 or C6 substituent in a flexible manner from acid chlorides or alpha-bromoketones, respectively. The scope of this methodology includes primary and secondary sp3-linked substituents at both the C3 and C6 positions, and the mild reaction conditions tolerate a variety of sensitive functionalities.

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Final Thoughts on Chemistry for (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal

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Towards selective ethylene tetramerization

And the magic number is… . A large amount of oligomer-free 1-octene (99.9%) was produced from ethylene by a catalytic system based on chromium during the formation of polyethylene wax [see GC-MS chromatogram; the other three significant peaks are methanol (quenching agent), ethyl acetate (needle-rinsing agent), and toluene (solvent)]. Copyright

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Half-sandwich Ru(II) halogenido, valproato and 4-phenylbutyrato complexes containing 2,2?-dipyridylamine: Synthesis, characterization, solution chemistry and in vitro cytotoxicity

Halogenido and carboxylato Ru(II) half-sandwich complexes of the general composition [Ru(eta6-p-cym)(dpa)X]PF6 (1-5) were prepared and thoroughly characterized with various techniques (e.g., mass spectrometry, NMR spectroscopy and X-ray analysis); dpa = 2,2?-dipyridylamine; p-cym = p-cymene; X = Cl- (for 1), Br- (for 2), I- (for 3), valproate(1-) (for 4) or 4-phenylbutyrate(1-) (for 5). A single-crystal X-ray analysis showed a pseudo-octahedral piano-stool geometry of [Ru(eta6-p-cym)(dpa)I]PF6 (3), with a eta6-coordinated p-cymene, bidentate N-donor dpa ligand and iodido ligand coordinated to the Ru(II) atom. The results of the 1H-NMR solution behaviour studies proved that the complexes 1-5 hydrolyse were in the mixture of solvents used (10% MeOD-d4/90% D2O). Complexes 1-5 were in vitro inactive against the A2780 human ovarian carcinoma cell line, up to the highest tested concentration (IC50 > 100 muM).

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Brief introduction of Tetrahydro-2H-pyran-4-ol

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Phenylalanine enamide derivatives

Phenylalanine enamide derivatives of formula (1) are described: 1wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain ?CH2?CH(R)13 , ?CH=C(R)? or 2?in which R is a carboxylic acid (?CO2H) or a derivative or biostere thereof; X is an ?O? or ?S? atom or ?N(R2)? group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

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Extracurricular laboratory:new discovery of 50675-18-8

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.50675-18-8, Name is Tetrahydropyran-4-carbaldehyde, molecular formula is C6H10O2. In a Patent£¬once mentioned of 50675-18-8, name: Tetrahydropyran-4-carbaldehyde

Novel Tricyclic Compounds

The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

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CRYSTAL STRUCTURE OF BIS(2-AMINOETHYL)AMINE(DI-2-PYRIDYLAMINE)ZINC(II)NITRATE AND THE ELECTRONIC PROPERTIES OF THE COPPER(II)-DOPED SYSTEM

The crystal structure of the title compound 2 has been determined by X-ray crystallographic analysis using photographic data.The complex crystallises in the monoclinic space group P21/c, with a=12.34(5), b=16.26(5), c=9.92(5) Angstroem, beta=92.0(5)o, and Z=4.The zinc(II) ion is five-co-ordinate with a distorted trigonal-bipyramidal stereochemistry, the mean out-of-plane and in-plane Zn-N bond distances being 2.20 and 2.09 Angstroem respectively.The e.s.r. and electronic spectra of 1percent copper-doped 2 have been determined using polycrystalline samples and single-crystal techniques and the results interpreted to suggest that the stereochemistry of the doped CuN5 chromophore corresponds closely to that observed in the isomorphous 2 complex, rather than to the stereochemistry of the ZnN5 chromophore of the host lattice.Caution is expressed over the use of the Zn-N distances and N-Zn-N angles to describe the stereochemistry of the CuNx chromophore when doped into isomorphous zinc(II) complexes as host lattices and the use of the electronic reflectance spectra of copper(II)-doped zinc(II) complexes as a criterion for comparable stereochemistries is advocated.A comparison of the g and A factors and one-electron orbital energies is made with other very distorted copper(II) systems.

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Simple exploration of Tetrahydro-2H-pyran-4-ol

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TETRASUBSTITUTED CYCLOHEXYL COMPOUNDS AS KINASE INHIBITORS

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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Tetrahydropyran – Wikipedia,
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Luminescence and electroluminescence of Al(III), B(III), Be(II) and Zn(II) complexes with nitrogen donors

Blue luminescent complexes of aluminum(III), boron(III), beryllium(II) and zinc(II) using ligands that contain only nitrogen donor atoms are presented. The ligands in these complexes are based on di-2-pyridylamine and 7-azaindole. Complexes containing derivatives of 7-azaindole and di-2-pyridylamine are described. Electroluminescent properties for some of the promising compounds are also discussed.

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Design, synthesis, and structure – Activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors

Phosphodiesterase 4 catalyzes the hydrolysis of cyclic AMP and is a target for the development of anti-inflammatory agents. We have designed and synthesized a series of phenyl alkyl ketones as PDE4 inhibitors. Among them, 13 compounds were identified as having submicromolar IC50 values. The most potent compounds have IC50 values of in the mid- to low-nanomolar range. Compound 5v also showed preference for PDE4 with selectivity of >2000-fold over PDE7, PDE9, PDE2, and PDE5. Docking of 5v, 5zf, and 5za into the binding pocket of the PDE4 catalytic domain revealed a similar binding profile to PDE4 with rolipram except that the fluorine atoms of the difluoromethyl groups of 5v, 5za, and 5zf are within a reasonable range for hydrogen bond formation with the amide hydrogen of Thr 333 and the long alkyl chain bears additional van der Waals interactions with His 160, Asp 318, and Tyr 159.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics