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THIENOPYRIMIDINES AS MKNK1 AND MKNK2 INHIBITORS

The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2122NO – PubChem

 

Final Thoughts on Chemistry for (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one

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Total Syntheses of Amphidinolide T1, T3, T4, and T5

A concise, flexible, and high yielding entry into the family of amphidinolide T macrolides, a series of cytotoxic natural products of marine origin, has been developed. All individual members, except amphidinolide T3 (3), derive from compound 39 as a common synthetic intermediate which is formed from three building blocks of similar size and complexity. The fragment coupling steps involve a highly diastereoselective SnCl4 mediated reaction of the furanosyl sulfone derivative 11 with the silyl enol ether 18 and a palladium-catalyzed Negishi type coupling reaction between the polyfunctional organozinc reagent derived from iodide 32a and the enantiopure acid chloride 24b. The 19-membered macrocyclic ring is then formed by a high yielding ring closing metathesis (RCM) reaction of diene 33 catalyzed by the “second generation” ruthenium carbene complex 34. The efficiency of the RCM transformation stems, to a large extent, from the conformational bias introduced by the syn-syn-configured stereotriad at C12-C14 of the substrate which constitutes a key design element of the synthesis plan. The use of Nysted’s reagent 38 in combination with TiCl4 was required for the olefination of the sterically hindered ketone group in 36, whereas more conventional alkene formations were unsuccessful for this elaboration. Finally, it is shown that the inversion of a single and seemingly remote stereocenter (C12) in one of the building blocks not only affects the efficiency and stereochemical outcome of the RCM step but also exerts a significant influence on the course of the acyl-Negishi reaction, allowing a radical manifold to compete with productive cross coupling.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2136NO – PubChem

 

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16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, belongs to oxazolidine compound, is a common compound. Computed Properties of C10H11NO2In an article, once mentioned the new application about 16251-45-9.

Asymmetric tandem Michael-Aldol reactions between 3-cinnamoyloxazolidine-2- thiones and aldehydes

Reactions between chiral 3-cinnamoyl-4-methyl-5-phenyl-1,3-oxazolidine-2- thiones and aromatic aldehydes in the presence of BF3¡¤Et 2O diastereoselectively produced tricyclic compounds incorporating a bridgehead carbon bound to four heteroatoms in high yields. Four stereocenters were induced during the reaction. The tricyclic products were transformed into propane-1,3-diols bearing three consecutive stereocenters by acid hydrolysis, S-methylation, and reductive removal of the chiral auxiliary.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2177NO – PubChem

 

More research is needed about (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one

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Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP

3,5-Diaryl-4,5-dihydropyrazoles were discovered to be potent KSP inhibitors with excellent in vivo potency. These enzyme inhibitors possess desirable physical properties that can be readily modified by incorporation of a weakly basic amine. Careful adjustment of amine basicity was essential for preserving cellular potency in a multidrug resistant cell line while maintaining good aqueous solubility.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2152NO – PubChem

 

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Stereoselective synthesis of pamamycin-607

A macrodiolide antibiotic pamamycin-607 was synthesized by joining two hydroxy acid components. Three cis-2, 5-disubstituted tetrahydrofuran rings in the molecule were stereoselectively prepared by radical cyclization reactions of beta-alkoxyvinyl ketone intermediates and a beta-alkoxymethacrylate substrate. The key step of the synthesis is characterized by the predominant threo product formation in the radical cyclization reaction of a beta-alkoxymethacrylate intermediate.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2168NO – PubChem

 

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Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: Synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6- [(5-phenylpyridin-2-yl)methoxy]-4,5-dihydro-1H-thiopyrano[2,3,4-cd]indol-2- yl]ethoxy]butanoic acid

Leukotriene biosynthesis inhibitors have potential as new therapies for asthma and inflammatory diseases. The recently disclosed thiopyrano[2,3,4- cd]indole class of 5-lipoxygenase (5-LO) inhibitors has been investigated with particular emphasis on the side chain bearing the acidic functionality. The SAR studies have shown that the inclusion of a heteroatom (O or S) in conjunction with an alpha-ethyl substituted acid leads to inhibitors of improved potency. The most potent inhibitor prepared contains a 2-ethoxybutanoic acid side chain. This compound, 14d (2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5- phenylpyridin-2-yl)methoxy]-4,5-dihydro-1H-thiopyrano[2,3,4-cd]indol-2- yl]ethoxy]butanoic acid, L-699,333), inhibits 5-HPETE production by human 5- LO and LTB4 biosynthesis by human PMN leukocytes and human whole blood (IC50s of 22 nM, 7 nM and 3.8 muM, respectively). The racemic acid 14d has been shown to be functionally active in a rat pleurisy model (inhibition of LTB4, ED50 = 0.65 mg/kg, 6 h pretreatment) and in the hyperreactive rat model of antigen-induced dyspnea (50% inhibition at 2 and 4 h pretreatment; 0.5 mg/kg po). In addition, 14d shows excellent functional activity against antigen-induced bronchoconstriction in the conscious squirrel monkey [89% inhibition of the increase in R(L) and 68% inhibition in the decrease in C(dyn) (0.1 mg/kg, n = 3)] and in the conscious sheep models of asthma (iv infusion at 2.5 mug/kg/min). Acid 14d is highly selective as an inhibitor of 5-LO activity when compared to the inhibition of human 15-LO, porcine 12-LO and ram seminal vesicle cyclooxygenase (IC50 > 5 muM) or competition in a FLAP binding assay (IC50 > 10 muM). Resolution of 14d affords 14g, the most potent diastereomer, which inhibits the 5-HPETE production of human 5-LO and LTB4 biosynthesis of human PMN leukocytes and human whole blood with IC50s of 8 nM, 4 nM, and 1 muM respectively. The in vitro and in vivo profile of 14d is comparable to that of MK-0591, which has showed biochemical efficacy in inhibiting ex vivo LTB4 biosynthesis and urinary LTE4 excretion in clinical trials.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2165NO – PubChem

 

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Formula: C10H11NO2, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 16251-45-9, name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one. In an article£¬Which mentioned a new discovery about 16251-45-9

A refined synthesis of enantiomerically pure 2-aminocyclobutanecarboxylic acids

The synthesis of enantiomerically pure 2-aminocyclobutanecarboxylic acids has been refined to improve both the efficiency and the simplicity. These improvements provide a shorter and easier access to the racemic cis-cyclobutane beta-amino acid core. Derivatization of this material with a chiral non-racemic oxazolidin-2-one allows easy diastereoisomeric separation and presents the advantage of allowing the non-destructive cleavage of the chiral auxiliary either by hydrolysis or by ammonolysis, thus providing an efficacious access to N-protected derivatives of all four stereoisomers of Boc-2-aminocyclobutanecarboxylic acid.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2156NO – PubChem

 

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Heteroaromatic side-chain analogs of pregabalin

A series of heteroaromatic analogs of pregabalin has been identified that possess anticonvulsant activity in the DBA/2 mouse model. The methods of synthesis and preliminary pharmacology are discussed herein.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2185NO – PubChem

 

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USE OF THIA OXO COMPOUNDS FOR LOWERING APO C3

Methods are disclosed to reduce apolipoprotein C-III (apoC-III) mRNA or protein in a subject in need thereof, comprising administering a pharmaceutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C1-C6 alkyl groups, with the proviso that R1 and R2 are not both hydrogen.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2113NO – PubChem

 

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 16251-45-9, molcular formula is C10H11NO2, introducing its new discovery. 16251-45-9

SUBSTITUTED PYRAZOLO-PYRIDINAMINES

The present invention relates to substituted pyrazolopyridine compounds of general formula I as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2121NO – PubChem