PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(-O) or CH2 provided that at least one of Y and...
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creator | COESEMANS, ERWIN VAN LOMMEN, GUY, ROSALIA, EUGEEN BUNTINX, MIEKE BONGARTZ, JEAN-PIERRE, ANDRE, MARC VAN WAUWE, JEAN, PIERRE, FRANS |
description | The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(-O) or CH2 provided that at least one of Y and Z represents C(-O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1; provided that when Y and Z each represent C(-O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(-O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definition of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them. |
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The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.</description><language>eng ; fre ; ger</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>2008</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&date=20081029&DB=EPODOC&CC=EP&NR=1984349A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20081029&DB=EPODOC&CC=EP&NR=1984349A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>COESEMANS, ERWIN</creatorcontrib><creatorcontrib>VAN LOMMEN, GUY, ROSALIA, EUGEEN</creatorcontrib><creatorcontrib>BUNTINX, MIEKE</creatorcontrib><creatorcontrib>BONGARTZ, JEAN-PIERRE, ANDRE, MARC</creatorcontrib><creatorcontrib>VAN WAUWE, JEAN, PIERRE, FRANS</creatorcontrib><title>PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS</title><description>The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(-O) or CH2 provided that at least one of Y and Z represents C(-O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1; provided that when Y and Z each represent C(-O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(-O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definition of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.</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>2008</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZDAJ8AxwDfJ08fRzVXABMsIcQzzDXIMVHIMVnCOcg4wVglydXQNC_IMUHP1CHN39_TyDQ4J5GFjTEnOKU3mhNDeDgptriLOHbmpBfnxqcUFicmpeakm8a4ChpYWJsYmlo6ExEUoAkbMnRA</recordid><startdate>20081029</startdate><enddate>20081029</enddate><creator>COESEMANS, ERWIN</creator><creator>VAN LOMMEN, GUY, ROSALIA, EUGEEN</creator><creator>BUNTINX, MIEKE</creator><creator>BONGARTZ, JEAN-PIERRE, ANDRE, MARC</creator><creator>VAN WAUWE, JEAN, PIERRE, FRANS</creator><scope>EVB</scope></search><sort><creationdate>20081029</creationdate><title>PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS</title><author>COESEMANS, ERWIN ; VAN LOMMEN, GUY, ROSALIA, EUGEEN ; BUNTINX, MIEKE ; BONGARTZ, JEAN-PIERRE, ANDRE, MARC ; VAN WAUWE, JEAN, PIERRE, FRANS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_EP1984349A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; ger</language><creationdate>2008</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>COESEMANS, ERWIN</creatorcontrib><creatorcontrib>VAN LOMMEN, GUY, ROSALIA, EUGEEN</creatorcontrib><creatorcontrib>BUNTINX, MIEKE</creatorcontrib><creatorcontrib>BONGARTZ, JEAN-PIERRE, ANDRE, MARC</creatorcontrib><creatorcontrib>VAN WAUWE, JEAN, PIERRE, FRANS</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>COESEMANS, ERWIN</au><au>VAN LOMMEN, GUY, ROSALIA, EUGEEN</au><au>BUNTINX, MIEKE</au><au>BONGARTZ, JEAN-PIERRE, ANDRE, MARC</au><au>VAN WAUWE, JEAN, PIERRE, FRANS</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS</title><date>2008-10-29</date><risdate>2008</risdate><abstract>The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(-O) or CH2 provided that at least one of Y and Z represents C(-O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1; provided that when Y and Z each represent C(-O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(-O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definition of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.</abstract><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 | PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS |
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