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Pharmaceutical Substances Syntheses, Patents, Applications - Part 199

Pharmaceutical Substances Syntheses, Patents, Applications - Part 199. 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. | Temazepam T 1981 Temazepam Methyloxazepam ATC N05CD07 Use tranquilizer anticonvulsant sedative hypnotic RN 846-50-4 MF C16HI3C1N2O2 MW 300.75 EINECS 212-688-1 LD50 370 mg kg M p.o. 2g kg R p.o. 3620 mg kg dog p.o. CN 7-chloro-1 3-dihydro-3-hydroxy-1 -methyl-5-pheny I-2 7-1 4-benzodiazepin-2-one 7-chloro-5-phenyl- 2-oxo-1 3-dihydro- 2H-1 4-benzodiozepine 4-oxide cf. oxazepam synthesis dimethyl sulfote 3-acetoxy-7-chloro-1 -methyl-5-phenyl-2-oxo-1 3-dihydro-2H-1 4-benzodiozepine I 4n NaOH ------- Reference s GB 1 022 642 American Home appl. 28.8.1962 USA-prior. 29.8.1961 5.3.1962 . GB 1 022 645 American Home appl. 28.8.1962 USA-prior. 29.8.1961 5.3.1962 . Formulation s cps. 7.5 mg 10 mg 15 mg 20 mg 30 mg Trade Name s D Neodorm Knoll Remestan -mite Wyeth I Evipnos Pharmacia Norkotral Desitin . temazep ct-Arzneimittel Upjohn Planum -mite Pharmacia F Normison Wyeth Levanxol Carlo Erba Upjohn GB Euhypnos Montedison wfm Pronervon Produpharm Normison Wyeth Normison Wyeth-Lederle Lappe USA Restoril Novartis Temocapril RS-5142 CS 622 ATC C09AA Use antihypertensive ACE inhibitor RN 111902-57-9 MF C23H28N2O5S2 MW 476.62 CN 2S- 2a 6ß R -6- l- ethoxycarbonyl -3-phenylpropyl amino tetrahydro-5-oxo-2- 2-thienyl -l 4-thiazepinc-4 5 -acetic acid 1982 T Temocapril monohydrochloride RN 110221-44-8 MF. C23H28N2O5S2 HC1 MW 513.08 LD50 5 g kg M p.o. 5 g kg R p.o. 1. LiAIH4 2. Boc-0-Boc -----------------k 2. di-tert-butyl dicarbonote PCI5 a-hydroxy-2-thiopheneacetonitrile Boc 2-tert-butoxy-carbonylamino-1 - 2-thienyl -ethanol Boc 0 2-tert-butoxy-carbonylamino-1 -chlora-1 - 2- thienyl ethane I Na2C03 DMF 60 C --------------------- N-phtholoyl-L-cysteine benzhydryl ester S- 2-tert-butoxycorbonyl-amino-1 S - 2-thlenyl ethyl -N-phthaloyl-L-cysteine benzhydryl ester H 1. CFjCOOH 2. diphenylphosphoryl azide DMF 2S 6R -5-oxa-6-phthal- imido-2- 2-thienyl per- hydro-1 4-thiazepine 0 CH NaH DMF --------------------- IV tert-butyl bromoacetate III ch3nhnh2 ch3oh --------------------- methylhydrazine