http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-348550-A1

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d202e9e866984fe229f6facc38f1d740
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-495
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-44
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-44
filingDate 1967-12-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1969-06-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-348550-A1
titleOfInvention A PROCEDURE FOR THE PREPARATION OF QUINOXALINE COMPOUNDS.
abstract Novel 5- and 6-carbamoyl-2,3-dichloroquinoxaline derivatives of the general formula wherein X is a hydrogen or halogen atom or a C 1-6 alkyl or C 1-6 alkoxy radical each of R and R 1 is a hydrogen atom or a C 1-6 alkyl (straight, branched or cyclic), C 1-6 haloalkyl (phenylhydroxy)-C 1-6 alkyl, di(C 1-6 alkyl)amino-C 1-6 alkyl, acylamino-C 1-6 alkyl, mono hydroxy C 1-6 alkyl, di-hydroxy-C 1-6 alkyl, C 1-6 alkoxy-C 1-6 alkyl, acyloxy-C 1-6 alkyl, C 1-6 alkyl substituted by a 5- or 6-membered heterocyclic radical containing one or more oxygen, sulphur or nitrogen hetero atoms, di(C 1-6 alkyl)aminophenyl, mono- or dihalophenyl, mono- or di- (C 1-6 alkoxy)phenyl, mono- or di-(C 1-6 alkyl)- phenyl, (hydroxy - C 1-6 - alkyl) - phenyl, (C 1-6 alkyl)halophenyl, C 1-6 alkyl-(C 1-6 alkoxy)-phenyl, (C 1-6 alkoxy)halophenyl, alkenyl or alkynyl radical, or a 5- or 6-membered heterocyclic radical containing one or more oxygen, sulphur or nitrogen hetero atoms, with the proviso that R and R 1 are not both hydrogen atoms, or R and R 1 are joined together to form a heterocyclic group which optionally contains an oxygen, sulphur or nitrogen hetero atom in addition to the nitrogen atom attached to the carbonyl function, and which may be substituted by a hydroxy or C 1-6 alkyl group and acid addition salts of said derivatives having a basic substituent on the carbamoyl radical are prepared by reaction of a 5- or 6-chlorocarbonyl- 2,3-dichloroquinoxaline derivative of the general formula with an amine of the general formula RR 1 NH, and when R and/or R 1 is a basic substituent, optional treatment of the hydrochloride salt formed with a base and optional conversion of the resulting free base to another acid addition salt thereof. 6 - Chlorocarbonyl - 2,3,7 - trichloroquinozaline and 6 - chlorocarbonyl - 7 - methoxy - 2,3 - dichloroquinoxaline are prepared by reaction of 2-chloro-4,5-diaminobenzoic acid and 4,5-diamino - 2 - methoxybenzoic acid, respectively, with diethyl oxalate, followed by treatment of the resulting 2,3-dihydroxy-7-chloroquinoxaline- 6 - carboxylic acid and 2,3 - dihydroxy - 7- methoxyquinoxaline - 6 - carboxylic acid, respectively, with phosphorus oxychloride. 4,5- Diamino - 2 - methoxybenzoic acid is prepared by catalytic hydrogenation of 4,5-dinitro-2- methoxybenzoic acid. Pharmaceutical compositions having gastric secretion-inhibiting properties comprise as active ingredient a 5- or 6-carbamoyl-2,3-dichloroquinoxaline derivative of the first or second general formula above or an acid addition salt of such a derivative having a basic substituent on the carbamoyl radical, together with an inert carrier diluent or coating, and may be administered orally or parenterally.
priorityDate 1966-12-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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