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Pharmaceutical Substances Syntheses, Patents, Applications - Part 15

Pharmaceutical Substances Syntheses, Patents, Applications - Part 15. Reference containing a collection of 2267 active pharmaceutical ingredients, including those launched recently. Listed alphabetically according to their INNs and established a link between INNs, structure, synthesis and production processes, patent and literature situation, medical use, and trade names. For pharmacists and researchers | Aspoxicillin A 141 with immovable E. coli ATCC 11303 Sato T. et al. Biotechnol. Bioeng. BIBIAU 17 1797 1975 . US 3 791 926 Tanabe 12.2.1974 J.-prior. 28.10.1971 . US 4 138 292 Tanabe 6.2.1979 J-prior. 2.7.1976 . Fusee M.C. et al. Appl. Environ. Microbiol. AEMIDF 42 672 1981 . US 4 436 813 Purification Engineering 13.3.1984 appl. 16.3.1982 . US 4 560 653 Grace 24.12.1985 appl. 6.6.1983 . EP 110 422 Tanabe appl. 2.12.1983 J.-prior. 3.12.1982 . Formulation s many different formulations Trade Name s D Eubiol Chephasaar F numerous combination preparations Mégamag Mayoly-Spindler as magnesium salt Sargenon ASTA Medica with arginine numerous combination preparations I Oral K Sclavo -comb. Polase Wyeth -comb. Aspoxicillin TA-058 ATC JOI Use semisynthetic penicillin for parenteral administration derivative of amoxicillin RN 63358-49-6 MF C21H27N5O7S MW 493.54 LD50 10g kg M i.v. CN 2S- 2a 5a 6ß -Ar-methyl-D-asparaginyl-A- 2-carboxy-3 3-dimethyl-7-oxo-4-thia-l- azabicyclo 3.2.0 hept-6-yl -D-2- 4-hydroxyphenyl glycinamide A A2 -HCI xr cooH 4-methyl D-ospcrtate Nps Cl K2C03 pH 8 ----------------------- o-nitrophenyl- sulfenyl chloride .Nps O HN ÏÏ Ï ö O TOOH I hydrochloride I HjC NH2 Nps O HN N COOH H N4-methyl-N2- o-nitrophenylsulfenyl -D-asparagine 0 0 DCC ------------ II N-hydroxy-succinimide 142 A Aspoxicillin n c2h5 3 dmf ------------------- III h2n .cooh 1 DMF NoOH Q ----------------------------- OH D-4-hydroxy-phenylglycine DMF THF N C2H5 3 25 C 1 N-methylmorpholine Aspoxicillin 2. isobutyl chloroformate 3. 6-aminopenicillanic acid 4. thiobenzamide Reference s Wagatsuma M. et al. J. Antibiot. JANTAJ 36 147 1983 . US 4 053 609 Tanabe Seiyaku 11.10.1977 UK-prior. 12.9.1975 J-prior. 27.12.1975 29.12.1975 . GB 1 533 413 Tanabe Seiyaku appl. 12.9.1975 and 16.8.1976 . GB 1 533 414 Tanabe Seiyaku appl. 3.12.1976 J-prior. 27.12.1975 . DOS 2 638 067 Tanabe Seiyaku appl. 24.8.1976 GB-prior. 12.9.1975 27.12.1975 29.12.1975 . purification US 4 313 875 Tanabe Seiyaku 2.2.1982 .