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Novell IL-8 compounds and methods of using them are provided.

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Oxazolidine – Wikipedia,
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A novel approach for the umpolung alpha-arylation of amides is presented. By the nucleophilic phenylation of O-silyl N,O-ketene acetals, generated in situ from N-alkoxy amides, a phenyl group can be introduced onto the alpha-carbon atom of amides through N?O bond cleavage in a two-step, one-pot process. The asymmetric synthesis of alpha-aryl amides through the diastereoselective arylation of a chiral N,O-ketene acetal is also described.

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Oxazolidine – Wikipedia,
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Iminium ions, generated by decarbonylation of N-benzyl-5-[1-(methoxycarbonyl)-4-oxopentyl]prolines, undergo intramolecular cyclization to afford 2,4-disubstituted tropanes in good yields. This transformation is also shown to be a stereospecific reaction. The value of these substituted tropanes has been demonstrated by functional group manipulation, leading to the enantiospecific synthesis of (±)-ferruginine, an alkaloid isolated from Darlinga ferruginea, and its unnatural enantiomer, (-)-ferruginine.

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Oxazolidine – Wikipedia,
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We have carried out the optimization of substituents at the C-3 or the C-5 position on the pyrrolidine ring of VLA-4 antagonist 3 with 2-(phenylamino)-7- fluorobenzoxazolyl moiety for the purpose of improving in vivo efficacy while maintaining good aqueous solubility. As a result, we successfully increased in vitro activity in the presence of 3% human serum albumin and achieved an exquisite lipophilic and hydrophilic balance of compounds suitable for oral administrative regimen. The modification resulted in the identification of zwitterionic compound 7n with (5S)-[methoxy(methyl)amino]methylpyrrolidine, which significantly alleviated bronchial hyper-responsiveness to acetylcholine chloride at 12.5 mg/kg, p.o. in a murine asthma model and showed favorable aqueous solubility (JP1, 89 mug/mL; JP2, 462 mug/mL). Furthermore, this compound showed good oral bioavailability (F = 54%) in monkeys.

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Oxazolidine – Wikipedia,
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Described herein are 1,4-substituted piperidine compounds according to Formula (I) that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

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Oxazolidine – Wikipedia,
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New 2-(substituted-phenoxy)propionic acid derivatives are provided, which have the structure of the general formula: STR1 and R2 is a hydrogen atom or a lower alkyl group. They have a high herbicidal activity to weeds, particularly graminaceous weeds, while they have little or no phytotoxicity to broad leaved crop plants and are therefore useful as selective herbicide.

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Equilibrium constants for iminium-ion formation in the reaction of acetone in aqueous solution at 35 deg C with pyrazolidinium, isoxazolidinium, O,N-dimethylhydroxylammonium, and N,N’-dimethylhydrazinium ions were found to be 9.33, 8.96, 0.117, and 0.057 M-1, respectively.The kinetics of hydrolysis of the iminium ions were studied in every case except that of the N-isopropylidene-O,N-dimethylhydroxylammonium ion, whose hydrolysis is too fast to follow by the techniques used with the other iminium ions.The rate of hydrolysis of the N-isopropylidenepyrazolium ion is independent of the pH from about pH 3 to 6; it is hydrogen ion catalyzed at lower pHs and hydroxide ion catalyzed at higher pHs.The rate of hydrolysis of N-isopropylideneisoxazolidinium ions is pH independent from pH 0.5 to about 2, increases until about pH 4, remains pH independent until pH 6.5, and has become too fast to measure above pH 8.Both reactions are general base catalyzed in all the buffers studied.A mechanism is described to fit the kinetics of each of these reactions.The dedeuteration of acetone-d6 was studied in pyridine buffers in the presence of each of the four hydrazine and hydroxylamine derivatives and also in the presence of the dimethylammonium and pyrrolidinium ion (which was also studied in 3-dimethylaminopropionitrile buffers).All six of these secondary ammonium ions catalyze the dedeuteration by transforming the acetone-d6 to an iminium ion that is dedeuterated by pyridine more rapidly than the ketone is.The iminium-ion formation is a relatively rapid eqiuilibrium in all cases except that of pyrrolidinium ions, where the intermediate iminum ion loses deuterium and hydrolyzes at comparable rates, and possibly the case of dimethylammonium ions, where the amount of catalysis via iminium-ion formation is too small to reveal mechanistic details.The effect of structure on the efficiency of catalysis of dedeuteration via iminium-ion formation is discussed.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1287NO – PubChem

 

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The nucleophilic gamma-phenylation and gamma-alkylation of alpha,beta-unsaturated amides have been developed. This umpolung reaction allows the regioselective introduction of phenyl and alkyl groups to a vinylketene N,O-acetal, which is generated in situ from an alpha,beta-unsaturated N-alkoxyamide, followed by N-O bond cleavage in a two-step, one-pot process.

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Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: Novel analogs of linezolid

The synthesis and antibacterial activity of oxazolidinones containing dihydro-1,2-oxazine and 2-pyrazoline ring systems are described. Linezolid analogs utilizing dihydro-1,2-oxazines as morpholine mimics were prepared utilizing a nitrosoamine/diene 4+2 cycloaddition strategy. Pyrazolidine, hexahydro-pyridazine, and 2-pyrazoline analogs more closely related to eperezolid were also prepared. The most active of these new oxazolidinones were the dihydro-1,2-oxazine 6 and the 2-pyrazoline 20 both of which had potency similar to linezolid against a panel of Gram-positive bacteria.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1283NO – PubChem

 

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PYRAZOLE DERIVATIVES AS SGC STIMULATORS

There are described imidazole and pyrazole derivatives which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.

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Oxazolidine – Wikipedia,
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