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3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF

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

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1419NO – PubChem

 

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DISUBSTITUTED OXAZOLIDIN-2-ONES 5-HYDROXYTRYPTAMINE RECEPTOR 2B ACTIVITY MODULATORS

Pharmaceutical compositions of the invention comprise disubstituted oxazolidin-2-ones derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 2b activity.

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Bioisosteric replacement and related analogs in the design, synthesis and evaluation of ligands for muscarinic acetylcholine receptors

Previous structure-activity relationship studies involving a series of lactone-based muscarinic ligands identified a lead compound containing a diphenylmethylpiperazine moiety (4; IC50 = 340 nM). The purpose of the present work is to investigate 1,3-benzodioxoles, 4,4-diethyl substituted tetrahydrofurans, 5-substituted oxazolidinones and chromones as bioisosteric replacements for the lactone ring in a novel series of muscarinic ligands. The approach provided compounds with improved % inhibition values and identified a non-selective muscarinic ligand with an IC50 value of 280 nM. The structure-activity relationship for this new series will be discussed. Selected compounds were evaluated in preliminary assays for subtype selectivity and were found to be non-selective.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1432NO – PubChem

 

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Copper-catalyzed oxidative cross-coupling of H-phosphonates and amides to N-acylphosphoramidates

A simple combination of copper(II) acetate (Cu(OAc)2) and an appropriate base could promote oxidative cross-coupling of H-phosphonates and amides using air as a terminal oxidant. The substrate scope was broad with respect to both dialkyl H-phosphonates and nitrogen nucleophiles (including oxazolidinone, lactam, pyrrolidinone, urea, indole, and sulfonamide derivatives), giving the corresponding P-N coupling products in moderate to high yields.

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Oxazolidine – Wikipedia,
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Solution and solid state studies of hydrogen bonding in substituted oxazolidinones by spectroscopic and quantum chemical methods

Structure and hydrogen bonding interactions of bioactive oxazolidinones have been studied by means of NMR and vibrational spectroscopies and quantum chemical calculations. We have demonstrated that oxazolidinone derivatives form hydrogen bonds in solution and solid state. Conformational space search has revealed predominant conformations in solution. In low polarity solvents, such as chloroform, dimers are formed presumably by intermolecular hydrogen bonds between two oxazolidinone molecules forming the most stable complexes, which has also been found in the solid state by IR spectroscopy and crystallography. In solvents of higher polarities, like methanol and dimethylsulfoxide, intermolecular interactions with solvent molecules and in dimers are present. As expected, raising the temperature broke hydrogen bonds, which was reflected in down-field chemical shifts of corresponding resonances. On the other hand, raising the solution concentration considerably affected oxazolidinone resonances only in chloroform, corroborating the formation of oxazolidinone dimers. These results may help in better understanding oxazolidinone structure, properties and interactions when designing new bioactive compounds and pharmaceutical products.

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Oxazolidine – Wikipedia,
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Silver-catalyzed hydroamination of siloxy alkynes

(Chemical Equation Presented) New catalytic process: The silver-catalyzed hydroamination of siloxy alkynes with secondary amides furnishes silyl ketene aminals with high efficiency and excellent diastereoselectivity (see scheme), including some that are unavailable by conventional silylation methods. The reaction comprises a fast and reversible silver-alkyne complexation, followed by a rate-determining C-N bond-forming step.

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Oxazolidine – Wikipedia,
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N-BENZYL OXAZOLIDINONES AND RELATED HETEROCYCLEIC COMPOUNDS AS POTENTIATORS OF GLUTAMATE RECEPTORS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compounds are active as potentiators of glutamate receptors, in particular mGluR2.

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PYRAZOLYL DERIVATIVES AS SYK INHIBITORS

The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer

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Antibiotic sulfonylaminocarbonyl activated beta-lactams

This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of the formula STR1 wherein R401 and R402 are the same or different and are (a) hydrogen, (b) (C1 -C12) alkyl (c) (C2 -C8) alkenyl, (d) (C2 -C8) alkynyl, (e) (C3 -C10) cycloalkyl, (f) phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1 -C4) alkyl, and (C1 -C4) alkoxy, (g) benzyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1 -C4) alkyl, and (C1 -C4) alkoxy, (h) –CH2 –O–CO–CH2 –NHR420, (i) –CH2 –O–CO2 –R430, (j) –CH2 F, or (k) –CHF2 ; wherein R420 is (a) hydrogen, (b) –COH, or (c) –CO–O–C(CH3)3 ; wherein R430 is (C1 -C8) alkyl, –(CH2) 2 OC(O)NH2, –(CH 2)2 Cl, –(CH2)2 OCH3 or –(CH2)2 NHCOH; wherein R300 is an acyl group derived from a carboxylic acid; wherein R100 is an optionally substituted heterocyclic moiety of Formula 2, 3, 4 or 5 STR2

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Oxazolidine – Wikipedia,
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5-ALKYLTHIO-7-[(4-ARYLBENZYL)AMINO]-1(2)H-PYRAZOLO[4,3-D]PYRIMIDINES FOR TREATMENT OF LYMPHOMA

The present invention relates to 5-alkylthio-7-[(4-arylbenzyl)amino]-1(2)H-pyrazolo[4,3-d]pyrimidine derivatives of formula I which are effective inhibitors of kinases and exhibit strong antiproliferative and proapoptotic properties on lymphoma cells. This invention further relates to use of said derivatives in the treatment of blood hyperproliferative diseases, such as Non-Hodgkin lymphomas.

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Oxazolidine – Wikipedia,
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