TAILIEUCHUNG - Pharmaceutical Substances Syntheses, Patents, Applications - Part 77

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 T 0 h3c ch3 2-bromo-3- 1 -methylethoxy -2-propenal K2CO3r chci3 h2o ----------- Reference s . a Wittenberger . et al. Synth. Commun. SYNCAV 23 3231 1993 . Keenan . et al. J. Med. Chem. JMCMAR 36 1880 1993 . EP 403 159 SmithKline Beecham appl. USA-prior. . b Weinstock J. et al. J. Med. Chem. JMCMAR 34 1514 1991 . c US 5 185 351 SmithKline Beecham USA-prior. . d WO 9 835 962 SmithKline Beecham appl. USA-prior. e WO 9 835 963 SmithKline Beecham appl. USA-prior. . f Shilera . et al. J. Org. Chem. JOCEAH 62 8449 1997 . Eprosartan dihydrate WO9 736 874 SmithKline Beecham appl. USA-prior. . combination with ACE inhibitors EP 629 408 MS Dohme-Chibret appl. EP-prior. . WO 9 702 032 Merck Co. appl. USA-prior. . pharmaceutical compositions and use in the treatment of macular degeneration infarction left ventricular hypertrophy WO 9 210 179 SmithKline Beecham appl. GB-prior. . WO 9 210 180 SmithKline Beecham appl. 1991 GB-prior. . WO 9 210 181 SmithKline Beecham appl. GB-prior. . 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 .

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