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Pharmaceutical Substances Syntheses, Patents, Applications - Part 180

Pharmaceutical Substances Syntheses, Patents, Applications - Part 180. 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. | Rebamipide R 1791 Formulations tabl. 125 mg Trade Name s GB Razoxin ICI wfm Rebamipide Proamipide ATC A02BX Use ulcer therapeutic RN 90098-04-7 MF C19H15C1N2O4 MW 370.79 LD50 572 mg kg M i.v. 700 mg kg R i.v. 2g kg dog p.o. CN a- 4-chlorobenzoyl amino -l 2-dihydro-2-oxo-4-quinolinepropanoic acid aniline CH3 acetoocetyl chloride O O H3C 0 UY CH3 HN CH n J O NaOC2H5 . 2 - 3------- I 1. N-bromo-succinimide 4- bromomethyl - diethyl acetamido- 2 1H -quinolinone 1 malonote 3- 2-oxo-1 2-dihydro-quinalin-4-yl alanine ci r r Vci . k7co o z J --------------------- 4-chlorobenzoyl chloride ethyl 2-acetamîdo-2- ethoxycarbony -3- 2-oxo-1.2-dihydroquinolin-4-yl -propionate II Reference s DOS 3 324 034 Otsuka appl. 7.4.1983 J-prior. 7.5.1982 . GB 2 123 825 Otsuka appl. 7.5.1983 J-prior. 7.5.1982 . Uchida M. et al. Chem. Pharm. Bull. CPBTAL 33 3775 1985 . ora and parenteral formulations JP 60 019 767 Otsuka appl. 7.11.1983 . Formulation s tabl. 100 mg 1792 R Reboxetine Trade Name s I Mucosta Otsuka 1990 Reboxetine FCE-20124 ATC N06AX18 Use antidepressant selective norepinephrine reuptake inhibitor RN 98769-81-4 MF C19H23NO3 MW 313.40 CN R R -2- 2-Ethoxyphenoxy phenylmethyl morpholine mesilate RN 98769-82-5 MF C19H23NO3 CH4O3S MW 409.50 trans- cinnomyl alcohol NaOH H2O dioxane I -------------------------- h3 1. KO I CH3 ch3 2. Red Al --------------------- 1. potassium tert-butoxide 2. sodium bis- 2-methoxyethoxy -aluminum hydride 1. gaseous NHj 0 2- Cl kc --------------- . 2. chloroacetyl chloride Reference s racemic synthesis DE 2 901 032 Farmitalia Carlo Erba appl. 12.1.1979 I-prior. 20.1.1978 . synthesis of stereoisomers of reboxetine DE 3 540 093 Farmitalia Carlo Erba appl. 12.11.1985 GB-prior. 22.11.1984 . configurational studies on 2- a- 2-ethoxyphenoxy benzyl morpholine Melloni. P. Della Torre A. Lazzari E. Mazzini G. Meroni M. Tetrahedron TETRAB 41 7 1393 1985 . Remifentanil R 1793 Formulation s tabl. 2 mg 4 mg Trade Name s D Edronax Pharmacia Upjohn GB Edronax Pharmacia .