Dihydro-as-triazino(5,6-c)quinoline derivatives, process for their preparation and pharmaceutical compositions containing these compounds

• Main Authors: BERENYI GEB. POLDERMANN, EDIT, KOSOCZKY, IBOLYA, GRASSER, KATALIN, KOVACS GEB. PALOTAI, AGNES, GOROG, PETER, PETOCZ, LUJZA
• Format: Patent
• Language: English; French; German
• Published: 28.10.1981
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Die Anmeldung betrifft Dihydro-as-triazino-[5, 6-c]chinolinderivate der allgemeinen Formel worin R für ein Wasserstoffatom, einen Alkylrest mit 1 bis 12 Kohlenstoffatom(en), einen, gegebenenfalls am Arylkern durch 1 oder mehr Alkylrest(e) mit 1 bis 4 Kohlenstoffatom(en), Alkoxyrest(e) mit 1 bis 4 Kohlenstoffatom(en), Halogenatom(e), Trifluormethylrest(e), Nitrogruppe(n) und/oder Hydroxygruppe(n), identisch oder verschieden substituierten, Aralkylrest mit 1 bis 4 Kohlenstoffatom(en) im Alkylteil oder einen, gegebenenfalls durch 1 oder mehr Alkylrest(e) mit 1 bis 4 Kohlenstoffatom(en), Alkoxyrest(e) mit 1 bis 4 Kohlenstoffatom(en), Halogenatom(e), Trifluormethylrest(e), Nitrogruppe(n) und/oder Hydroxygruppe(n), identisch oder verschieden substituierten, Phenylrest steht und X1 ein Wasserstoffatom oder einen, gegebenenfalls durch 1 oder mehr Halogenatom(e) substituierten, Formylrest oder Alkylcarbonylrest mit 2 bis 6 Kohlenstoffatomen bedeutet und entweder X2 oder X3 Wasserstoff oder einen, gegebenenfalls durch 1 oder mehr Halogenatom(e) substituierten, Formylrest oderAlkylcarbonylrest mit 2 bis 6 Kohlenstoffatomen darstellt und entweder X2 und Z zusammen oder X3 und Z zusammen eine chemische Bindung darstellen, wobei dasjenige von X2 und X3, welches an dieser Bindung beteiligt ist, keine der obigen Bedeutungen haben kann, 1. Claims for the Contracting states : BE, CH/LI, DE, FR, GB, IT, NL, SE Dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula see diagramm : EP0038528,P16,F1 wherein R represents an alkyl radical having 4, 5 or 8 carbon atoms or a phenyl radical and X1 means a hydrogen atom or an acetyl radical and either X2 or X3 represents hydrogen or an acetyl radical and the other of X2 and X3 has no meaning and the dotted lines mean 1 chemical bond each only either the one or the other being present with the further definition that in case X1 represents hydrogen none of X2 and X3 means hydrogen as well as their acid addition salts. 1. Claims for the Contracting state : AT A process for preparing dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula see diagramm : EP0038528,P17,F2 wherein R represents an alkyl radical having 4, 5 or 8 carbon atoms or a phenyl radical and X1 means a hydrogen atom or an acetyl radical and either X2 or X3 represents hydrogen or an acetyl radical and the other of X2 and X3 has no meaning and the dotted lines mean 1 chemical bond each only either the one or the other being present with the further definition that in case X1 represents hydrogen none of X2 and X3 means hydrogen as well as their acid addition salts, characterized in that in a manner known per se one acetylizes acid addition salts of dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula see diagramm : EP0038528,P18,F1 wherein R is as above defined and Z1 represents hydrogen and either Z2 or Z3 means hydrogen and the other of Z2 and Z3 has no meaning and the dotted lines mean 1 chemical bond each only either the one or the other being present with acetic acid and/or derivatives of it active regarding acetylation as acetylating agents and optionally one converts possibly obtained monoacetyl-dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula I or acid addition salts thereof, respectively, optionally after liberating the former from the latter or converting the latter into the former, respectively, by further acetylation with acetic acid and/or derivatives of it active regarding acetylation as acetylating agents into diacetyldihydro-as-triazino[5,6-c]quinoline derivatives having the general formula I or acid addition salts thereof, respectively, whereafter in a manner known per se optionally one converts the obtained dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula I with inorganic or organic acids into acid addition salts or optionally one converts the obtained acid addition salts of the dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula I with bases into the free dihydro-as-triazino[5,6-c]quinoline derivatives having the general formula I or in other acid addition salts, respectively.