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Pharmaceutical Substances Syntheses, Patents, Applications - Part 77. 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 | Eprosartan 761 xin 1. NaOH CHjOH H2O 2. MnOj toluene CH2CI2 XIV COOH O 0 2- H3cA CH3 . DMAP -------------------xv XV 1. D8U 2. NaOH k Eprosartan D8U ethyl acetate 2-butyl-4- methyl acrylate XVI formylimidazole XVI X piperidine 65 C -----------k XVII xvn iv 1. toluene 1OO C 2. NoOH Eprosartan 0 1. piperidine toluene 2. NaOH XIV 4- X Eprosartan or bisulfite addition compound f j alternative synthesis of VI valeronitrile HCI H3C OH O C ----------- H C Ti CH3 HCI NH methyl volerimidote hydrochloride XVIII 762 E Eprosartan xvin TEA DMF ----------- methyl 4- N- 1 -iminopen tyl amino -methyl benzoate XIX XIX OHCk.Br T 0 h3c ch3 2-bromo-3- 1 -methylethoxy -2-propenal K2CO3r chci3 h2o ----------- Reference s . a Wittenberger S.J. et al. Synth. Commun. SYNCAV 23 3231 1993 . Keenan R.M. et al. J. Med. Chem. JMCMAR 36 1880 1993 . EP 403 159 SmithKline Beecham appl. 7.6.1990 USA-prior. 14.6.1989 . b Weinstock J. et al. J. Med. Chem. JMCMAR 34 1514 1991 . c US 5 185 351 SmithKline Beecham 9.2.1993 USA-prior. 14.6.1989 6.4.1990 14.12.1990 . d WO 9 835 962 SmithKline Beecham appl. 13.2.1998 USA-prior. 14.2.1997 e WO 9 835 963 SmithKline Beecham appl. 13.2.1998 USA-prior. 14.2.1997 . f Shilera S.C. et al. J. Org. Chem. JOCEAH 62 8449 1997 . Eprosartan dihydrate WO9 736 874 SmithKline Beecham appl. 26.3.1997 USA-prior. 29.3.1996 . combination with ACE inhibitors EP 629 408 MS Dohme-Chibret appl. 14.12.1993 EP-prior. 16.6.1993 . WO 9 702 032 Merck Co. appl. 26.6.1996 USA-prior. 30.6.1995 . pharmaceutical compositions and use in the treatment of macular degeneration infarction left ventricular hypertrophy WO 9 210 179 SmithKline Beecham appl. 12.12.1991 GB-prior. 14.12.1990 . WO 9 210 180 SmithKline Beecham appl. 12.12 1991 GB-prior. 14.12.1990 . WO 9 210 181 SmithKline Beecham appl. 12.12.1991 GB-prior. 14.12.1990 . use in the treatment of diabetic nephropathy retinopathy atheroma angina pectoris stroke or prevention of restenosis or improving cognitive function WO 92 101 82-88 .
