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The present application relates to novel substituted indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H84NO – PubChem

 

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The alkenyldiarylmethanes (ADAMs) are a class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) targeting HIV-1. Four chemically and metabolically stabilized ADAMs incorporating N-methoxyimidoyl halide replacements of the methyl esters of the lead compound were previously reported. In this study, twenty-five new ADAMs were synthesized in order to investigate the biological consequences of installing nine different methyl ester bioisosteres at three different locations. Attempts to define a universal rank order of methyl ester bioisosteres and discover the ‘best’ one in terms of inhibitory activity versus HIV-1 reverse transcriptase (RT) led to the realization that the potencies are critically dependent on the surrounding structure at each location, and therefore the definition of universal rank order is impossible. This investigation produced several new non-nucleoside reverse transcriptase inhibitors in which all three of the three methyl esters of the lead compound were replaced by methyl ester bioisosteres, resulting in compounds that are more potent as HIV-1 RT inhibitors and antiviral agents than the lead compound itself and are expected to also be more metabolically stable than the lead compound.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H616NO – PubChem

 

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The (chitosan-Schiff base)cobalt(II) complex was found to be an efficient catalyst for the oxidative carbonylation (CO/O2) of 2-aminoalkan-1-ols 1 to give oxazolidin-2-ones 2, in the presence of NaI. The effects of promoters, temperature, solvents, and other reaction conditions were investigated in this study.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H758NO – PubChem

 

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An improved one-pot procedure for the three-component coupling reaction of aldehydes, amides and dienophiles (AAD reaction) has been developed. Compared to known protocols for this type of reaction, the use of aromatic solvents in the presence of dehydrating reagents allows an efficient synthesis of previously not accessible products. Condensation of ubiquitous available aldehydes and amides and subsequent Diels-Alder reactions with dienophiles furnishes endo-selective amino-functionalized hexahydroisoindole-1,3-dione and tetrahydrophthalic acid derivatives in good yield.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H695NO – PubChem

 

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A recently developed GC-MS analytical method for the quantitative determination of oxazaphosphorines and their metabolites in blood plasma, using stable trifluoroacetyl derivatives and electron capture negative chemical ionization detection, was applied to measure the partitioning of the antitumor drug ifosfamide and its metabolites between plasma and red blood cells for four cancer patients. The separation of a constant volume of red blood cells was performed using a special instrument, MESED, through centrifugation of blood samples. The measured compounds were ifosfamide, 2- and 3-dechloroethylifosfamide, 4-ketoifosfamide, carboxyifosfamide, ifosfamide mustard, 2-chloroethylamine and 1,3-oxazolidin-2-one. Concentration-time profiles for the metabolites in the two blood fractions and partitioning factors between erythrocytes and plasma were obtained. For ifosfamide itself, and metabolites with an intact ring system, a partitioning factor between 1 and 2 was observed for the concentration ratio between red blood cells and plasma in the patients studied. However, for the compounds with an open structure, carboxyifosfamide and ifosfamide mustard, partitioning factors higher than 3 were obtained. The active antitumor metabolite ifosfamide mustard showed a strong preference for the red blood cells in the measured patient samples. This means that erythrocytes may play an important role in the transport and the subsequent release of the active alkylating agent to the tumor cells.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H831NO – PubChem

 

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The enantioselective alpha-arylation of both lactones and acyl oxazolidones has been accomplished using a combination of diaryliodonium salts and copper catalysis. These mild catalytic conditions provide a new strategy for the enantioselective construction and retention of enolizable alpha-carbonyl benzylic stereocenters, a valuable synthon for the production of medicinal agents.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H594NO – PubChem

 

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A new method of arylating N-H and O-H containing compounds at room temperature with phenylboronic acids and cupric acetate in the presence of a tertiary amine promoter is described. Substrates include phenols, amines, anilines, amides, imides, ureas, carbamates, and sulfonamides.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H412NO – PubChem

 

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The He(I) photoelectron spectra of some heterocyclic penta-atomic rings containing carboamido, thiocarbamido or selenocarbamido groups are reported.Ab initio and CNDO/2 computational methods have been used to assign the first four ionized molecular orbitals, by comparison with previously studied related molecules.Structural effects in homologous series of compounds, particularly conjugation between N and C=Y (Y=O, S, Se) moiety, and the through-space interaction between ring heteroatoms are analyzed.

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Oxazolidine – Wikipedia,
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PROBLEM TO BE SOLVED: To provide a production method capable of obtaining an ethylenically unsaturated group-containing isocyanate compound with high yield, which is excellent in safety to human bodies or environments without using phosgene and in which the production processes and production facilities are simplified.SOLUTION: There is a method for producing an ethylenically unsaturated group-containing isocyanate compound which produces a compound having an ethylenically unsaturated bond and an isocyanate group in the molecule using an amino alcohol as a raw material, wherein the method has a step of producing a cyclic compound having a urethane bond in the molecule as an intermediate.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H141NO – PubChem

 

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An efficient and practical protocol for the protection of various structurally and electronically divergent aryl and aliphatic amines using (Boc)2O in the presence of a catalytic amount of molecular iodine (10 mol%) under solvent-free conditions at ambient temperature is presented.

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Reference:
Oxazolidine – Wikipedia,
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