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Pharmaceutical Substances Syntheses, Patents, Applications - Part 60

Pharmaceutical Substances Syntheses, Patents, Applications - Part 60. 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 | Desiprami ne D 591 Desipramine ATC N06AA01 Use antidepressant RN 50-47-5 MF C18H22N2 MW 266.39 EINECS 200-040-0 LD5 22 mg kg M i.v. 448 mg kg M p.o. 29 mg kg R Í.V. 375 mg kg R p.o. CN 10 1 l-dihydro-7V-methyl-5 -dibenz h azepine-5-propanamine monohydrochloride RN. 58-28-6 MF CI8H22N2 HC1 MW 302.85 EINECS 200-373-1 LDS 37 mg kg M Í.V. 315 mg kg M p.o. 19 mg kg R Í.V. 871 mg kg R p.o. 25 mg kg dog i.v. 10 11 -dihydra-5H-dib nz b f ozepine 1 1. NaNH2 2. Br x Cl 1. sodium amide 2. 1 -bromo-3-chloro-propane 5- 3-chloropropyl -10.11-dihydro-5H-dibenz b f azepine H3C NH2 --------Í------- methylamine 3- benzylmethyl- amino propyl chloride from 1-bromo-3-chloro-propane and benzylmethylamine Desipramine 0 Cl 0 ch3 Desipramine ethyl chloroformate Reference s a FR-M 796 Geigy appl. 3.9.1960 CH-prior. 4.9.1959 . GB 908 788 Geigy appl. 1960 CH-pnor. 1959 . DE 1 189 550 Geigy appl. 1960 CH-prior. 1959 . b US 3 454 698 Colgate-Palmolive 8.7.1969 prior. 25.5.1960 . US 3 454 554 Colgate-Palmolive 8.7.1969 prior. 25.5.1960 . c DE 1 288 599 Geigy appl. 13.3.1962 CH-prior. 14.3.1961 . DE 1 445 800 Geigy appl. 2.3.1962 CH-prior. 3.3.1961 . Formulationfs drg. 25 mg tabl. 25 mg 592 D Desloratadine Trade Nameịs D Pertofran Novartis F Pertofran Novartis as J Pertofran Fujisawa Pharma hydrochloride USA Norpramin Hoechst Petylyl ASTA Medica GB Pertofran Geigy wfm Marion Roussel as AWD ĩ Nortimil Chiesi hydrochloride Desloratadine Sch-34117 Use non-sedating antihistamine metabolite of loratadine RN 100643-71-8 MF C19H19C1N2 MW 310.83 CN 8-Chloro-6 l 1 -dihydro-1 l- 4-piperidinylidene -5H-benz 5 6 cyclohepta l 2-blpyridine loratadine q. V. NaOH C2H5OH ---- -------- 8-chloroazatadine cf. loratadine BrCN ------ cyanogen bromide Desloratadine Reference s a b wo 8 503 707 Schering Corp. appl. 8.2.1985 USA-prior. 15.2.1984 . polymorphs WO 9 901 450 Schering Corp. appl. 1.7.1998 USA-prior. 2.7.1997 . eye drops containing loratadine metabolites WO 9 848 803 Schering-Plough K.K. WO-prior. 25.4.1997 .