91360-95-1Relevant academic research and scientific papers
Regiospecific synthesis of 6-halouridine derivatives: An effective method for coupling sterically hindered pyrimidine bases to ribose
Blackburn, Daniel J.,Kent, Greggory T.,Wu, Weiming
, p. 1348 - 1350 (2017/03/10)
6-Halouridine derivatives were synthesized regiospecifically through the coupling of N3-protected 6-halouracil to a ribose derivative. The combination of the silylating reagent N,O-bis(trimethylsilyl)acetamide and Lewis acid catalyst trimethylsilyl triflu
Heterocyclic derivative and pharmaceutical composition comprising the same
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Page/Page column 223; 224, (2016/01/10)
The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun
Concise synthesis of substituted quinolizin-4-ones by ring-closing metathesis
Alanine, Thomas A.,Galloway, Warren R. J. D.,McGuire, Thomas M.,Spring, David R.
supporting information, p. 5767 - 5776 (2014/10/15)
The 4H-quinolizin-4-one scaffold is of significant pharmaceutical interest. This heterocyclic structure is predicted to have attractive physico-chemical properties and is present in a variety of biologically active molecules. Despite these interesting characteristics, 4H-quinolizin-4-ones are largely under-represented in current small molecule screening libraries, and, therefore, this scaffold has been poorly investigated. Herein, a new strategy is reported for the syntheses of these rare and biologically interesting 4H-quinolizin-4-ones. This modular route involves the regioselective N-alkylation of 6-halo-2-pyridones followed by a Stille cross-coupling, ring-closing metathesis, and palladium-catalyzed dehydrogenation reaction sequence. This method furnishes the target compounds in good yields and allows for access to unusual substitution patterns that are difficult to achieve by using other synthetic strategies.
Cyplecksins are covalent inhibitors of the pleckstrin homology domain of cytohesin
Hussein, Mohamed,Bettio, Martina,Schmitz, Anton,Hannam, Jeffrey S.,Theis, Julian,Mayer, Günter,Dosa, Stefan,Gütschow, Michael,Famulok, Michael
supporting information, p. 9529 - 9533 (2013/09/23)
The covalent grip: A new class of 5-bromobarbiturates (Cyplecksins; see structure) act by a covalent mechanism to inhibit the biological function of the pleckstrin homology domain of cytohesins, small guanine nucleotide exchange factors for the Ras-like ARF-GTPases. In cells, Cyplecksins interfere with the phosphoinositol-dependent membrane recruitment of cytohesins. Cyplecksins may be useful in validating cytohesins as potential drug targets. Copyright
NOVEL HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Paragraph 0341; 0342, (2013/06/28)
The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun
PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
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Page/Page column 28, (2012/01/13)
Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, L2, and Q are defined herein.
Planar chiral flavinium salts - Prospective catalysts for enantioselective sulfoxidation reactions
Jurok, Radek,Cibulka, Radek,Dvorakova, Hana,Hampl, Frantisek,Hodacova, Jana
supporting information; experimental part, p. 5217 - 5224 (2010/11/02)
A novel planar chiral flavinium salt, 3-benzyl-5-ethyl-10-(8- phenylnaphthalen-1-yl)isoalloxazinium perchlorate (2b), which bears a phenyl cap that covers one side of the isoalloxazinium skeleton plane, has been prepared as a potential catalyst for the enantioselective H2O2 oxidation of sulfides. The rate of H2O2 oxidation of sulfides in the presence of racemic 2b is comparable to that of the reaction catalysed by 5-ethyl-3,10-dimethylisoalloxazinium perchlorate, which indicates that the bulky shielding substituent does not influence the catalytic activity of the flavinium unit. The turnover frequency for the oxidation of thioanisole with hydrogen peroxide with 2b is 870 h-1. The enantiomerically pure salts (+)-2b and (-)-2b were prepared from the pure enantiomers (+)-3b and (-)-3b of 3-benzyl-10-(8-phenylnaphthalen-1-yl)isoalloxazine (3b) obtained by HPLC separation of racemic 3b on a chiral stationary phase. The enantiomerically pure salts (+)-2b and (-)-2b catalyse the H2O2 oxidation of para-substituted thioanisoles with enantiomeric excesses of 34-44%. The highest enantioselectivity (54% ee) was observed in the oxidation of methyl naphthyl sulfide.
PYRIMIDINDIONE DERIVATIVES AS PROKINETICIN 2 RECEPTOR ANTAGONISTS
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Page/Page column 78, (2010/11/24)
The present invention relates to certain novel compounds of Formula (I), which are suitable for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.
PROKINETICIN 1 RECEPTOR
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Page/Page column 66, (2008/06/13)
The present invention relates to methods of monitoring the biological activity of the PK1 receptor.
A facile synthesis of 5-acylbarbituric acids under microwave irradiations
Singh, Palwinder,Paul, Kamaldeep
, p. 1105 - 1108 (2007/10/03)
N-Monosubstituted and N,N'-disubstituted barbituric acids on treatment with benzoic anhydride/acetic anhydride under microwave irradiations without using any solvent provide a convenient methodology for the synthesis of 5-benzoyl/ acylbarbituric acids in moderate to high yields.
