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Pharmaceutical Substances Syntheses, Patents, Applications - Part 72

Pharmaceutical Substances Syntheses, Patents, Applications - Part 72. 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 | Doxazosin D 711 1. NoNH 1. sodium amide 2. 1 -ethyl-3-chlora pyrrolidine h2so4 diphenylacetonitrile Reference s US 3 192 230 A. H. Robins 29.6.1965 prior. 9.2.1961 . Lunsford C.D. et al. J. Med. Chem. JMCMAR 7 302 1964 . Formulation s amp. 20 mg ml Trade Name s D Dopram Brenner wfm I F Dopram Martinet wfm GB Dopram Anpharm Doxapril Carlo Erba wfm Doxapril Farmalabor wfm J Dopram Kissei USA Dopram Robins as hydrochloride Doxazosin ATC C02CA04 Use arreceptor antagonist antihypertensive RN 74191-85-8 MF C23H25N5O5 MW 451.48 LD50 1000 mg kg M R p.o. CN l- 4-amino-6 7-dimethoxy-2-quinazolinyl -4- 2 3-dihydro-l 4-benzodioxin-2-yl carbonyl piperazine hydrochloride RN 70918-01-3 MF C23H25N5O5 HCl MW 487.94 mesylate RN 77883-43-3 MF C23H25N5O5 CH4O3S MW 547.59 LDS0 2935 mg kg M p.o. 5 g kg R p.o. 1 g kg dog p.o. 0 0 piperazine 1 4-benzodioxan-2-ylcarbonyl chloride N- 1 4-benzodioxan-2-ylcarbonyl piperazine I 712 D Doxefazepam 1 4-amino 2-chloro-6 7-dimethaxyquinazoline cf. prozasine synthesis Reference s DE 2 847 623 Pfizer appl. 2.11.1978 GB-prior. 5.11.1977 . US 4 188 390 Pfizer 12.2.1980 GB-prior. 5.11.1977 . EP 848 001 Alfa Chem. appl. 17.10.1997 I-prior. 13.12.1996 . WO 9 935 143 Knoll appl. 18.12.1998 D-pnor. 6.1.1998 medical use for treatment of atherosclerosis US 4 758 569 Pfizer 19.7.1988 appl. 26.8.1987 . osmotic device US 4 837 111 Alza 6.6.1989 appl. 21.3.1988 . Formulation s tabl. 1 mg 2 mg 4 mg Trade Name s D Cardular Pfizer 1989 as I Cardura Roerig 1989 as Normothen Fisons mesylate mesylate Italchimici 1989 as Diblocin Astra 1989 as Dedralen Lifepharma mesylate mesylate 1989 as mesylate J Cardenalin Pfizer GB Cardura Invicta 1989 as USA Cardura Pfizer 1990 as mesylate mesylate Doxefazepam ATC N05CD12 Use hypnotic RN 40762-15-0 MF C17H 4C1FN2O3 MW 348.76 LD50 74 mg kg M i.p. 1500 mg kg M p.o. 586 mg kg R i.p. 1500 mg kg M p.ơ. CN 7-chloro-5- 2-fluorophenyl -l 3-dihydro-3-hydroxy-l- 2-hydroxyethyl -2 7-l 4-benzodiazepin-2-one hci 0 0 . H-.C X - ---------- 1 .