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The reaction of beta- and gamma-haloamines with carbon dioxide to give pharmaceutically relevant 2-oxazolidinones and 1,3-dioxazin-2-ones, was found to proceed efficiently in the presence of a base and in the absence of catalyst. After optimization of reaction conditions, the system was successfully expanded to a variety of haloamines, even at multigram scale. The reaction was further studied in silico by DFT calculations. The reaction of beta- and gamma-haloamines with carbon dioxide to give pharmaceutically relevant cyclic urethanes was found to proceed efficiently in the presence of a base and in the absence of catalyst (see figure). After optimization of reaction conditions, the system was expanded to a variety of haloamines, even at a multigram scale. The reaction was further studied in silico by DFT calculations.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1447NO – PubChem

 

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The solubility-driven structural modification of (pyridin-3-yl) benzoxazinyl-oxazolidinones is described, which resulted in the development of a new series of benzoxazinyl-oxazolidinone analogues with high antibacterial activity against Gram-positive pathogens, including that against linezolid-resistant strains and low hERG inhibition. With regard to structure-activity relationship (SAR) trends among the various substituents on the pyridyl ring, relatively small and nonbasic substituents were preferable to sterically demanding or basic substituents. Oxazolidinone ring substitution on the pyridyl ring generated analogues with antibacterial activity superior to imidazolidinone ring. Solubility was enhanced by the incorporation of polar groups, especially when compounds were converted to their prodrugs. Among the prodrugs, compound 85 exhibited excellent solubility and a good pharmacokinetic profile. In a MRSA systemic infection model, compound 85 displayed an ED 50 = 5.00 mg/kg, a potency that is 2-fold better than that of linezolid.

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Oxazolidine – Wikipedia,
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A method of treating allergic disorders and pharmaceutical compositions therefore are disclosed for a series of 5-[(4-aryl-1-piperazinyl)alkyl]-2-oxazolidinone derivatives of Formula I. These compounds are useful in inhibiting Type I allergic STR1 responses in a living animal and thus can be used to treat allergic phenomena such as asthma, rhinitis, atopic dermatitis, chronic hives, allergic conjunctivitis and the like.

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Oxazolidine – Wikipedia,
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The preparation of a series of 24 N-benzhydrylpiperazine derivatives is described. Their efficacy as calcium antagonists was examined with reference to changes in the permeability of the cell membrane to extracellular and intracellular calcium. Compounds 14, 15, 17 and 19 were the most powerful when compared with known calcium antagonists such as cinnarizine, flunarizine, and aligeron ([1-diphenylmethyl)-4-(2-propenyl)]-piperazine), and were selected for further study.

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Oxazolidine – Wikipedia,
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The present invention provides compounds, compositions thereof, and methods of using the same.

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Oxazolidine – Wikipedia,
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The development of 2-phenylbenzoxazoles as inhibitors of cholesteryl ester transfer protein (CETP) is described. Efforts focused on finding suitable replacements for the central piperidine with the aim of reducing hERG binding: a main liability of our benchmark benzoxazole (1a). Replacement of the piperidine with a cyclohexyl group successfully attenuated hERG binding, but was accompanied by reduced in vivo efficacy. The approach of substituting a piperidine moiety with an oxazolidinone also attenuated hERG binding. Further refinement of this latter scaffold via SAR at the pyridine terminus and methyl branching on the oxazolidinone led to compounds 7e and 7f, which raised HDLc by 33 and 27 mg/dl, respectively, in our transgenic mouse PD model and without the hERG liability of previous series.

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Oxazolidine – Wikipedia,
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Three different protocols for the syntheses of hydroxyalkylnitramines are presented and compared. Safety issues regarding the synthesis of nitramines are also discussed.

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Oxazolidine – Wikipedia,
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The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes. [image]

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Oxazolidine – Wikipedia,
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Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit.

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The present invention comprises a new class of compounds useful for the prophylaxis and treatment of p38 kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, B1, B2, C1-4, L1, R1, R2, R5, m and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of kinase mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and intermediates and processes useful for the preparation of compounds of Formula I

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