Mercaptoimidazoles as CCR2 receptor antagonists
The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or h...
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creator | VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN |
description | The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; R4 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; or R3 and R4 taken together may form a bivalent radical of formula -C(-O)-NH-NH-C(-O)-; n is 1, 2, 3, 4 or 5; provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(-O)-OH, C(-O)-O-C1-6alkyl or C(-O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(-O)-NH-C1-4alkyl-NH2 and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents and R1 and R5 represents hydrogen, then R4 is other than hydrogen having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (1) and pharmaceutical compositions comprising them. |
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fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_CN1745069A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>CN1745069A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_CN1745069A3</originalsourceid><addsrcrecordid>eNrjZND3TS1KTiwoyc_MzUxJrMrPSS1WSCxWcHYOMlIoSk1OBcoUKSTmlSSm5-dlFpcU8zCwpiXmFKfyQmluBnk31xBnD93Ugvz41OKCxOTUvNSSeGc_Q3MTUwMzS0djwioAioIqKw</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Mercaptoimidazoles as CCR2 receptor antagonists</title><source>esp@cenet</source><creator>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</creator><creatorcontrib>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</creatorcontrib><description>The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; R4 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; or R3 and R4 taken together may form a bivalent radical of formula -C(-O)-NH-NH-C(-O)-; n is 1, 2, 3, 4 or 5; provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(-O)-OH, C(-O)-O-C1-6alkyl or C(-O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(-O)-NH-C1-4alkyl-NH2 and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents and R1 and R5 represents hydrogen, then R4 is other than hydrogen having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (1) and pharmaceutical compositions comprising them.</description><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>2006</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=20060308&DB=EPODOC&CC=CN&NR=1745069A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,778,883,25547,76298</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20060308&DB=EPODOC&CC=CN&NR=1745069A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</creatorcontrib><title>Mercaptoimidazoles as CCR2 receptor antagonists</title><description>The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; R4 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; or R3 and R4 taken together may form a bivalent radical of formula -C(-O)-NH-NH-C(-O)-; n is 1, 2, 3, 4 or 5; provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(-O)-OH, C(-O)-O-C1-6alkyl or C(-O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(-O)-NH-C1-4alkyl-NH2 and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents and R1 and R5 represents hydrogen, then R4 is other than hydrogen having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (1) 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>2006</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZND3TS1KTiwoyc_MzUxJrMrPSS1WSCxWcHYOMlIoSk1OBcoUKSTmlSSm5-dlFpcU8zCwpiXmFKfyQmluBnk31xBnD93Ugvz41OKCxOTUvNSSeGc_Q3MTUwMzS0djwioAioIqKw</recordid><startdate>20060308</startdate><enddate>20060308</enddate><creator>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</creator><scope>EVB</scope></search><sort><creationdate>20060308</creationdate><title>Mercaptoimidazoles as CCR2 receptor antagonists</title><author>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN1745069A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2006</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>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>VAN LOMMEN GUY ROSALIA EUGEEN,DOYON JULIEN GEORGES PIERRE-OL,VAN WAUWE JEAN PIERRE FRANS,COOLS MARINA LUCIE LOUISE,COESEMANS ERWIN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Mercaptoimidazoles as CCR2 receptor antagonists</title><date>2006-03-08</date><risdate>2006</risdate><abstract>The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; R4 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; or R3 and R4 taken together may form a bivalent radical of formula -C(-O)-NH-NH-C(-O)-; n is 1, 2, 3, 4 or 5; provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(-O)-OH, C(-O)-O-C1-6alkyl or C(-O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(-O)-NH-C1-4alkyl-NH2 and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents and R1 and R5 represents hydrogen, then R4 is other than hydrogen having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (1) 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 | Mercaptoimidazoles as CCR2 receptor antagonists |
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