Heteroaryl substituted derivatives of 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one, process and intermediates for their preparation and pharmaceutical preparations containing thereof

In the present invention there are disclosed 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one heteroaryl substituted derivatives of the general formula I, in which A and B together represent a bivalent radical of the general formula -N=CH- (a), -CH=N- (b)...

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Hauptverfasser: BACKX LEO JACOBUS JOZEF, HEERES JAN, HENDRICKX ROBERT JOZEF MARIA, DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L, VAN DER EYCKEN LUC ALFONS LEO
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creator BACKX LEO JACOBUS JOZEF
HEERES JAN
HENDRICKX ROBERT JOZEF MARIA
DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L
VAN DER EYCKEN LUC ALFONS LEO
description In the present invention there are disclosed 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one heteroaryl substituted derivatives of the general formula I, in which A and B together represent a bivalent radical of the general formula -N=CH- (a), -CH=N- (b), -CHi2-CHi2- (c), -CH=CH- (d), -C(=O)-CHi2- (e) or -CHi2-C(=O)- (f), whereby in the bivalent radical of the formula (a) or (b) the hydrogen atom can be optionally substituted with an alkyl group containing 1 to 6 carbon atoms and in the bivalent radical of the formulas (c), (d), (e) or (f) one or two hydrogen atoms can be optionally substituted with alkyl groups containing 1 to 6 carbon atoms, Re1 represents a hydrogen atom, an alkyl group containing 1 to 6 carbon atoms or a halogen, Re2 represents a hydrogen atom or a halogen atom, Re3 represents a hydrogen atom, an alkyl group containing 1 to 8 carbon atoms, a cycloalkyl group containing 3 to 6 carbon atoms or an alkyl group containing 1 to 8 carbon atoms being substituted with hydroxyl, an oxo group a cycloalkyl containing 3 to 6 carbon atoms or an aryl group, Het represents a heterocyclic radical being defined in the Claims and the aryl group is represented by phenyl being optionally substituted with alkyl containing 1 to 6 carbon atoms or with a halogen, further their N-oxides, stereochemically isomeric forms and pharmaceutically acceptable acid addition salts, intermediates of the general formula III in which Re1, Re2 and Het are as specified above and W represents a leaving group such as halogen or sulfonyloxy and their acid addition salts or stereochemically isomeric forms, further process for preparing the compounds of the general formula I as well as pharmaceutical preparations based thereon. The compounds of the general formula are suitable for treating hyperlipemia.
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The compounds of the general formula are suitable for treating hyperlipemia.</description><edition>7</edition><language>eng</language><subject>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</subject><creationdate>2000</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20000412&amp;DB=EPODOC&amp;CC=CZ&amp;NR=286476B6$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20000412&amp;DB=EPODOC&amp;CC=CZ&amp;NR=286476B6$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>BACKX LEO JACOBUS JOZEF</creatorcontrib><creatorcontrib>HEERES JAN</creatorcontrib><creatorcontrib>HENDRICKX ROBERT JOZEF MARIA</creatorcontrib><creatorcontrib>DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L</creatorcontrib><creatorcontrib>VAN DER EYCKEN LUC ALFONS LEO</creatorcontrib><title>Heteroaryl substituted derivatives of 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one, process and intermediates for their preparation and pharmaceutical preparations containing thereof</title><description>In the present invention there are disclosed 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one heteroaryl substituted derivatives of the general formula I, in which A and B together represent a bivalent radical of the general formula -N=CH- (a), -CH=N- (b), -CHi2-CHi2- (c), -CH=CH- (d), -C(=O)-CHi2- (e) or -CHi2-C(=O)- (f), whereby in the bivalent radical of the formula (a) or (b) the hydrogen atom can be optionally substituted with an alkyl group containing 1 to 6 carbon atoms and in the bivalent radical of the formulas (c), (d), (e) or (f) one or two hydrogen atoms can be optionally substituted with alkyl groups containing 1 to 6 carbon atoms, Re1 represents a hydrogen atom, an alkyl group containing 1 to 6 carbon atoms or a halogen, Re2 represents a hydrogen atom or a halogen atom, Re3 represents a hydrogen atom, an alkyl group containing 1 to 8 carbon atoms, a cycloalkyl group containing 3 to 6 carbon atoms or an alkyl group containing 1 to 8 carbon atoms being substituted with hydroxyl, an oxo group a cycloalkyl containing 3 to 6 carbon atoms or an aryl group, Het represents a heterocyclic radical being defined in the Claims and the aryl group is represented by phenyl being optionally substituted with alkyl containing 1 to 6 carbon atoms or with a halogen, further their N-oxides, stereochemically isomeric forms and pharmaceutically acceptable acid addition salts, intermediates of the general formula III in which Re1, Re2 and Het are as specified above and W represents a leaving group such as halogen or sulfonyloxy and their acid addition salts or stereochemically isomeric forms, further process for preparing the compounds of the general formula I as well as pharmaceutical preparations based thereon. The compounds of the general formula are suitable for treating hyperlipemia.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2000</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFjk1OxDAMhbthgYAzkAM0i_6osGYE6gFYsRmZxp1apHHkuKPJXJhrkEGzYMfK8nvfs99t9T2iojBI9iZtn0lJN0VnHAodQemIyfBsmrqzjvjEHoLtbfYr6sKnHBcM2dvGRooocKayXbW27ktkyU7Ythb8V9G60Tb1xVAhOHMRLAesTRSeMCUDwRkKpdCKjkDL75nF6IIkhcEIUipx-OXiArLChJvSBP6vnczEQYEChcMlLMjzfXUzg0_4cJ131ePb6_tutBh5jymWQwF1v_ton4f-aXgZuv-JH6I5brA</recordid><startdate>20000412</startdate><enddate>20000412</enddate><creator>BACKX LEO JACOBUS JOZEF</creator><creator>HEERES JAN</creator><creator>HENDRICKX ROBERT JOZEF MARIA</creator><creator>DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L</creator><creator>VAN DER EYCKEN LUC ALFONS LEO</creator><scope>EVB</scope></search><sort><creationdate>20000412</creationdate><title>Heteroaryl substituted derivatives of 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one, process and intermediates for their preparation and pharmaceutical preparations containing thereof</title><author>BACKX LEO JACOBUS JOZEF ; HEERES JAN ; HENDRICKX ROBERT JOZEF MARIA ; DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L ; VAN DER EYCKEN LUC ALFONS LEO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CZ286476B63</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2000</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>BACKX LEO JACOBUS JOZEF</creatorcontrib><creatorcontrib>HEERES JAN</creatorcontrib><creatorcontrib>HENDRICKX ROBERT JOZEF MARIA</creatorcontrib><creatorcontrib>DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L</creatorcontrib><creatorcontrib>VAN DER EYCKEN LUC ALFONS LEO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>BACKX LEO JACOBUS JOZEF</au><au>HEERES JAN</au><au>HENDRICKX ROBERT JOZEF MARIA</au><au>DE CHAFFOY DE COURCELLES DIDIER ROBERT GUY GABRI™L</au><au>VAN DER EYCKEN LUC ALFONS LEO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Heteroaryl substituted derivatives of 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one, process and intermediates for their preparation and pharmaceutical preparations containing thereof</title><date>2000-04-12</date><risdate>2000</risdate><abstract>In the present invention there are disclosed 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one heteroaryl substituted derivatives of the general formula I, in which A and B together represent a bivalent radical of the general formula -N=CH- (a), -CH=N- (b), -CHi2-CHi2- (c), -CH=CH- (d), -C(=O)-CHi2- (e) or -CHi2-C(=O)- (f), whereby in the bivalent radical of the formula (a) or (b) the hydrogen atom can be optionally substituted with an alkyl group containing 1 to 6 carbon atoms and in the bivalent radical of the formulas (c), (d), (e) or (f) one or two hydrogen atoms can be optionally substituted with alkyl groups containing 1 to 6 carbon atoms, Re1 represents a hydrogen atom, an alkyl group containing 1 to 6 carbon atoms or a halogen, Re2 represents a hydrogen atom or a halogen atom, Re3 represents a hydrogen atom, an alkyl group containing 1 to 8 carbon atoms, a cycloalkyl group containing 3 to 6 carbon atoms or an alkyl group containing 1 to 8 carbon atoms being substituted with hydroxyl, an oxo group a cycloalkyl containing 3 to 6 carbon atoms or an aryl group, Het represents a heterocyclic radical being defined in the Claims and the aryl group is represented by phenyl being optionally substituted with alkyl containing 1 to 6 carbon atoms or with a halogen, further their N-oxides, stereochemically isomeric forms and pharmaceutically acceptable acid addition salts, intermediates of the general formula III in which Re1, Re2 and Het are as specified above and W represents a leaving group such as halogen or sulfonyloxy and their acid addition salts or stereochemically isomeric forms, further process for preparing the compounds of the general formula I as well as pharmaceutical preparations based thereon. The compounds of the general formula are suitable for treating hyperlipemia.</abstract><edition>7</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 Heteroaryl substituted derivatives of 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one, process and intermediates for their preparation and pharmaceutical preparations containing thereof
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