50734-07-1Relevant articles and documents
PHARMACEUTICAL COMPOSITIONS COMPRISING ANTICOAGULANT N-(5-CHLOROPYRIDINE-2-YL)-2-({4-[ETHANIMIDOIL(METHYL)AMINO]BENZOYL}AMINO)-5-METHYLBENZAMIDE
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Page/Page column 7, (2018/01/20)
The invention relates to area of medicine, in particular to pharmacology, namely to novel pharmaceutical compositions for oral use for treatment of diseases associated with increased thrombus formation. The compositions comprise the anticoagulant N-(5-chloropyridine-2-yl)-2-({4-[ethanimidoil(methyl)amino]benzoyl}amino)-5-methylbenzamide or a pharmaceutically acceptable salt thereof, being a factor Xa inhibitor and polyprenol, and are protected from the contact with acidic gastric juice by an enteric coating or capsule. The compositions are of high efficacy and bioavailability and can be used to treat and prevent conditions characterized by undesirable thrombosis.
Synthesis and structure-activity relationships of 2- pyrazinylcarboxamidobenzoates and β-ionylideneacetamidobenzoates with retinoidal activity
Jones, Paul,Villeneuve, Gérald B.,Fei, Chengpei,DeMarte, Josie,Haggarty, Allison J.,Nwe, Khin Than,Martin, Deborah A.,Lebuis, Anne-Marie,Finkelstein, Joshua M.,Gour-Salin, Barbara J.,Chan, Tak Hang,Leyland-Jones, Brian R.
, p. 3062 - 3077 (2007/10/03)
The structure-activity relationships of two series of novel retinoids (2-pyrazinylcarboxamidobenzoates and β-ionylideneacetamidobenzoates) have been investigated by evaluating their ability to induce differentiation in both human promyelocytic leukemia (H
Synthesis of Monoamides of Methotrexate from L-Glutamic Acid Monoamide t-Butyl Esters
Antonjuk, David J.,Boadle, Deborah K.,Cheung, H.T.Andrew,Tran, Trung Q.
, p. 1989 - 2004 (2007/10/02)
Analoques of methotrexate (amethopterin) (1) with α- or γ-monoamide functions were synthesized starting with t-butyl L-isoglutamine (12a), t-butyl L-glutamine (22a), or the appropriate N'-alkyl or N'N'-dialkyl analoques (12b-k), (22d), (22k), (22l), and (22m).The corresponding N-benzyloxycarbonyl compounds (11) and/or (21) from which the above L-glutamic acid derivatives were obtained were generally synthesized by mixed-anhydride coupling of N-benzyloxycarbonyl-L-glutamic acid (9) with the appropriate amine, conversion into the t-butyl ester, and chromatographic separation.The resulting α-monoamide γ-t-butyl ester (11) and γ-monoamide α-t-butyl ester (21) are unambiguously distinguished by mass spectrometry and 13C n.m.r. spectroscopy.Factors which affect the γ-amide/α-amide product ratio are discussed.The N-deprotected L-glutamic acid monoamide t-butyl esters (12) or (22) were individually coupled to N-trifluoroacetyl-p-methylaminobenzoic acid, and the resulting α- or γ-monoamide t-butyl esters (13) or (23) of N-(p-methyl(trifluoroacetyl)aminobenzoyl)-L-glutamic acid was hydrolysed.The N-deprotected product, viz. t-butyl N-(p-methylaminobenzoyl)-L-glutamate α- or γ-monoamide (14) or (24) was converted into the appropriate methotrexate-monoamide t-butyl ester (15) or (25), and thence the desired methotrexate-monoamide (16) or (26), by reaction with 2,4-diamino-6-bromomethylpteridine (17) or by the Taylor procedure.Features of the mass and 13C n.m.r. spectra of the intermediates are discussed.