Analogifremgangsmåte for fremstilling av antipicornavirale pyridazinaminer og mellomprodukt for fremstilling av slike

Piperidinyl, pyrrolldinyl, azepinyl og plperazlnyl pyridazlner med formel. der en eller to karbonatomer tildelen kan være substituert med C_-alkyl. C-C-alkyloksy eller to karbonatomer av CH-gruppene til nevnte del kan være koblet med en C-alkandlylrest; X betyr CH eller N; Rbetyr hydrogen, C_-alkyl,...

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Hauptverfasser: STOKBROEKX, RAYMOND ANTOINE, LUYCKX, MARCEL GEREBERNUS MARIA, GRAUWELS, GILBERT ARTHUR JULES, EYCKEN, CYRIEL ALPHONS MARIA VAN DER
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creator STOKBROEKX, RAYMOND ANTOINE
LUYCKX, MARCEL GEREBERNUS MARIA
GRAUWELS, GILBERT ARTHUR JULES
EYCKEN, CYRIEL ALPHONS MARIA VAN DER
description Piperidinyl, pyrrolldinyl, azepinyl og plperazlnyl pyridazlner med formel. der en eller to karbonatomer tildelen kan være substituert med C_-alkyl. C-C-alkyloksy eller to karbonatomer av CH-gruppene til nevnte del kan være koblet med en C-alkandlylrest; X betyr CH eller N; Rbetyr hydrogen, C_-alkyl, halo, hydroksy, trlfluormetyl, cyano, C^-alkyloksy, C_-alkyltlo, C_-alkylsulflnyl, Cj^-alkylsulfonyl, C_4-alkyloksykarbonyl, C_-alkylkar-bonyl eller aryl; Rog Rbetyr hver uavhengig hydrogen eller C_-alkyl; Alk betyr Cj^-alkandlyl;og Rbetyr hver uavhengig hydrogen, C_-alkyl eller halo; og Bet betyr. addisjonssalter og stereokjemiske isomerlske former derav, idet de nevnte forbindelsene har antlpicor-naviral aktivitet. Farmasaytlske sammensetninger som inneholder disse forbindelsene som aktiv ingrediens og en fremgangsmåte for fremstilling av nevnte forbindelser og farmasaytlske sammensetninger er beskrevet. Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula wherein X represents CH or N; R represents hydrogen, C1-4alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4alkyloxy, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyl or aryl; R and R represent hydrogen or C1-4alkyl; Alk represents C1-4alkanediyl; R and R represent hydrogen, C1-4alkyl or halo; and Het represents the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. Pharmaceutical compositions containing these compounds as active ingredient, and methods of preparing said compounds and pharmaceutical compositions.
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C-C-alkyloksy eller to karbonatomer av CH-gruppene til nevnte del kan være koblet med en C-alkandlylrest; X betyr CH eller N; Rbetyr hydrogen, C_-alkyl, halo, hydroksy, trlfluormetyl, cyano, C^-alkyloksy, C_-alkyltlo, C_-alkylsulflnyl, Cj^-alkylsulfonyl, C_4-alkyloksykarbonyl, C_-alkylkar-bonyl eller aryl; Rog Rbetyr hver uavhengig hydrogen eller C_-alkyl; Alk betyr Cj^-alkandlyl;og Rbetyr hver uavhengig hydrogen, C_-alkyl eller halo; og Bet betyr. addisjonssalter og stereokjemiske isomerlske former derav, idet de nevnte forbindelsene har antlpicor-naviral aktivitet. Farmasaytlske sammensetninger som inneholder disse forbindelsene som aktiv ingrediens og en fremgangsmåte for fremstilling av nevnte forbindelser og farmasaytlske sammensetninger er beskrevet. Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula wherein X represents CH or N; R represents hydrogen, C1-4alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4alkyloxy, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyl or aryl; R and R represent hydrogen or C1-4alkyl; Alk represents C1-4alkanediyl; R and R represent hydrogen, C1-4alkyl or halo; and Het represents the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. 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C-C-alkyloksy eller to karbonatomer av CH-gruppene til nevnte del kan være koblet med en C-alkandlylrest; X betyr CH eller N; Rbetyr hydrogen, C_-alkyl, halo, hydroksy, trlfluormetyl, cyano, C^-alkyloksy, C_-alkyltlo, C_-alkylsulflnyl, Cj^-alkylsulfonyl, C_4-alkyloksykarbonyl, C_-alkylkar-bonyl eller aryl; Rog Rbetyr hver uavhengig hydrogen eller C_-alkyl; Alk betyr Cj^-alkandlyl;og Rbetyr hver uavhengig hydrogen, C_-alkyl eller halo; og Bet betyr. addisjonssalter og stereokjemiske isomerlske former derav, idet de nevnte forbindelsene har antlpicor-naviral aktivitet. Farmasaytlske sammensetninger som inneholder disse forbindelsene som aktiv ingrediens og en fremgangsmåte for fremstilling av nevnte forbindelser og farmasaytlske sammensetninger er beskrevet. Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula wherein X represents CH or N; R represents hydrogen, C1-4alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4alkyloxy, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyl or aryl; R and R represent hydrogen or C1-4alkyl; Alk represents C1-4alkanediyl; R and R represent hydrogen, C1-4alkyl or halo; and Het represents the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. 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C-C-alkyloksy eller to karbonatomer av CH-gruppene til nevnte del kan være koblet med en C-alkandlylrest; X betyr CH eller N; Rbetyr hydrogen, C_-alkyl, halo, hydroksy, trlfluormetyl, cyano, C^-alkyloksy, C_-alkyltlo, C_-alkylsulflnyl, Cj^-alkylsulfonyl, C_4-alkyloksykarbonyl, C_-alkylkar-bonyl eller aryl; Rog Rbetyr hver uavhengig hydrogen eller C_-alkyl; Alk betyr Cj^-alkandlyl;og Rbetyr hver uavhengig hydrogen, C_-alkyl eller halo; og Bet betyr. addisjonssalter og stereokjemiske isomerlske former derav, idet de nevnte forbindelsene har antlpicor-naviral aktivitet. Farmasaytlske sammensetninger som inneholder disse forbindelsene som aktiv ingrediens og en fremgangsmåte for fremstilling av nevnte forbindelser og farmasaytlske sammensetninger er beskrevet. Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula wherein X represents CH or N; R represents hydrogen, C1-4alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4alkyloxy, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyl or aryl; R and R represent hydrogen or C1-4alkyl; Alk represents C1-4alkanediyl; R and R represent hydrogen, C1-4alkyl or halo; and Het represents the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. Pharmaceutical compositions containing these compounds as active ingredient, and methods of preparing said compounds and pharmaceutical compositions.</abstract><edition>6</edition><oa>free_for_read</oa></addata></record>
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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
title Analogifremgangsmåte for fremstilling av antipicornavirale pyridazinaminer og mellomprodukt for fremstilling av slike
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