N-acyl-2-substituted-4-(benzimidazolyl-or imidazopyridinyl-substituted pesidues)-piperidines as tachykinin antagonists

N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted...

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Hauptverfasser: F. E. JANSSENS, F. M. SOMMEN, D. L. N. G. SURLERAUX
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F. M. SOMMEN
D. L. N. G. SURLERAUX
description N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted by OH, TO, oxo or a ketalised oxo substituent of formula OCH2CH2O or OCH2CH2CH2O; R2 = Ar2, Ar2(1-6C alkyl), Het or Het(1-6C alkyl); L = a group of formula (i) or (ii); p = 0, 1 or 2; Y, depending on whether the optional second bond is present or not, is (i) a bivalent radical of formula CH2, CH(OH), C(O), O, S, SO, SO2, NR3, CH2NR3 or CONR3, or (ii) a trivalent radical of formula CH; A=B is a bivalent radical of formula CH=CH, N=CH or CH=N; R3 = H or R; R4 = H, R, 3-7C cycloalkyl, Alk-R7 or Alk-Z-R8; Alk = 1-6C alkanediyl; Z = O, S or NR3; R7 = Ph (optionally substituted by 1-2 halo, R or RO); furanyl (optionally substituted by 1-2 R or hydroxy(1-6C alkyl)); thienyl (optionally substituted by 1-2 halo or R); oxazolyl, thiazolyl or pyridinyl (all optionally substituted by 1-2 R); R8 = R (optionally substituted by OH, COOH or COOR); R5 = H, halo, OH or RO; R6 = H, R or Ar1(1-6 alkyl); Ar1 = Ph (optionally substituted by 1-3 halo, T, T', CN, CONH2, TO or T'O); Ar2 = naphthalenyl, or Ph (optionally substituted by 1-3 OH, halo, CN, NO2, NH2, NHT, N(T)2, T, T', TO, T'O, COOH, COOT, CONH2, CONHT or CON(T)2); Het = pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl or benzothienyl (all optionally substituted on carbon by 1-2 halo, T or mono-, di- or tri(halo)methyl); T, T', R, = 1-4C alkyl, halo(1-4C alkyl), 1-6C alkyl respectively.
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SURLERAUX</creatorcontrib><description>N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted by OH, TO, oxo or a ketalised oxo substituent of formula OCH2CH2O or OCH2CH2CH2O; R2 = Ar2, Ar2(1-6C alkyl), Het or Het(1-6C alkyl); L = a group of formula (i) or (ii); p = 0, 1 or 2; Y, depending on whether the optional second bond is present or not, is (i) a bivalent radical of formula CH2, CH(OH), C(O), O, S, SO, SO2, NR3, CH2NR3 or CONR3, or (ii) a trivalent radical of formula CH; A=B is a bivalent radical of formula CH=CH, N=CH or CH=N; R3 = H or R; R4 = H, R, 3-7C cycloalkyl, Alk-R7 or Alk-Z-R8; Alk = 1-6C alkanediyl; Z = O, S or NR3; R7 = Ph (optionally substituted by 1-2 halo, R or RO); furanyl (optionally substituted by 1-2 R or hydroxy(1-6C alkyl)); thienyl (optionally substituted by 1-2 halo or R); oxazolyl, thiazolyl or pyridinyl (all optionally substituted by 1-2 R); R8 = R (optionally substituted by OH, COOH or COOR); R5 = H, halo, OH or RO; R6 = H, R or Ar1(1-6 alkyl); Ar1 = Ph (optionally substituted by 1-3 halo, T, T', CN, CONH2, TO or T'O); Ar2 = naphthalenyl, or Ph (optionally substituted by 1-3 OH, halo, CN, NO2, NH2, NHT, N(T)2, T, T', TO, T'O, COOH, COOT, CONH2, CONHT or CON(T)2); Het = pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl or benzothienyl (all optionally substituted on carbon by 1-2 halo, T or mono-, di- or tri(halo)methyl); T, T', R, = 1-4C alkyl, halo(1-4C alkyl), 1-6C alkyl respectively.</description><edition>6</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>1999</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=19990127&amp;DB=EPODOC&amp;CC=CN&amp;NR=1206414A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25544,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19990127&amp;DB=EPODOC&amp;CC=CN&amp;NR=1206414A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>F. E. JANSSENS</creatorcontrib><creatorcontrib>F. M. SOMMEN</creatorcontrib><creatorcontrib>D. L. N. G. SURLERAUX</creatorcontrib><title>N-acyl-2-substituted-4-(benzimidazolyl-or imidazopyridinyl-substituted pesidues)-piperidines as tachykinin antagonists</title><description>N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted by OH, TO, oxo or a ketalised oxo substituent of formula OCH2CH2O or OCH2CH2CH2O; R2 = Ar2, Ar2(1-6C alkyl), Het or Het(1-6C alkyl); L = a group of formula (i) or (ii); p = 0, 1 or 2; Y, depending on whether the optional second bond is present or not, is (i) a bivalent radical of formula CH2, CH(OH), C(O), O, S, SO, SO2, NR3, CH2NR3 or CONR3, or (ii) a trivalent radical of formula CH; A=B is a bivalent radical of formula CH=CH, N=CH or CH=N; R3 = H or R; R4 = H, R, 3-7C cycloalkyl, Alk-R7 or Alk-Z-R8; Alk = 1-6C alkanediyl; Z = O, S or NR3; R7 = Ph (optionally substituted by 1-2 halo, R or RO); furanyl (optionally substituted by 1-2 R or hydroxy(1-6C alkyl)); thienyl (optionally substituted by 1-2 halo or R); oxazolyl, thiazolyl or pyridinyl (all optionally substituted by 1-2 R); R8 = R (optionally substituted by OH, COOH or COOR); R5 = H, halo, OH or RO; R6 = H, R or Ar1(1-6 alkyl); Ar1 = Ph (optionally substituted by 1-3 halo, T, T', CN, CONH2, TO or T'O); Ar2 = naphthalenyl, or Ph (optionally substituted by 1-3 OH, halo, CN, NO2, NH2, NHT, N(T)2, T, T', TO, T'O, COOH, COOT, CONH2, CONHT or CON(T)2); Het = pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl or benzothienyl (all optionally substituted on carbon by 1-2 halo, T or mono-, di- or tri(halo)methyl); T, T', R, = 1-4C alkyl, halo(1-4C alkyl), 1-6C alkyl respectively.</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>1999</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFi7EKwkAQRNNYiPoNXqnFgYnBXoJilco-bHKrLp57R3YjJF9vkBR2VsPMezNP3qWFpvc2s9LVoqSdorO53dTIA73IwRD8yENrphb7lhzxuP08TEQh16FsbaSIXwPFgBiF5tE_iYkNsMI9MInKMpndwAuuplwk6_PpWlwsxlChRGiQUauiTLPdIU_z4_6_8QGcZEYB</recordid><startdate>19990127</startdate><enddate>19990127</enddate><creator>F. E. JANSSENS</creator><creator>F. M. SOMMEN</creator><creator>D. L. N. G. SURLERAUX</creator><scope>EVB</scope></search><sort><creationdate>19990127</creationdate><title>N-acyl-2-substituted-4-(benzimidazolyl-or imidazopyridinyl-substituted pesidues)-piperidines as tachykinin antagonists</title><author>F. E. JANSSENS ; F. M. SOMMEN ; D. L. N. G. SURLERAUX</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CN1206414A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1999</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>F. E. JANSSENS</creatorcontrib><creatorcontrib>F. M. SOMMEN</creatorcontrib><creatorcontrib>D. L. N. G. SURLERAUX</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>F. E. JANSSENS</au><au>F. M. SOMMEN</au><au>D. L. N. G. SURLERAUX</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>N-acyl-2-substituted-4-(benzimidazolyl-or imidazopyridinyl-substituted pesidues)-piperidines as tachykinin antagonists</title><date>1999-01-27</date><risdate>1999</risdate><abstract>N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted by OH, TO, oxo or a ketalised oxo substituent of formula OCH2CH2O or OCH2CH2CH2O; R2 = Ar2, Ar2(1-6C alkyl), Het or Het(1-6C alkyl); L = a group of formula (i) or (ii); p = 0, 1 or 2; Y, depending on whether the optional second bond is present or not, is (i) a bivalent radical of formula CH2, CH(OH), C(O), O, S, SO, SO2, NR3, CH2NR3 or CONR3, or (ii) a trivalent radical of formula CH; A=B is a bivalent radical of formula CH=CH, N=CH or CH=N; R3 = H or R; R4 = H, R, 3-7C cycloalkyl, Alk-R7 or Alk-Z-R8; Alk = 1-6C alkanediyl; Z = O, S or NR3; R7 = Ph (optionally substituted by 1-2 halo, R or RO); furanyl (optionally substituted by 1-2 R or hydroxy(1-6C alkyl)); thienyl (optionally substituted by 1-2 halo or R); oxazolyl, thiazolyl or pyridinyl (all optionally substituted by 1-2 R); R8 = R (optionally substituted by OH, COOH or COOR); R5 = H, halo, OH or RO; R6 = H, R or Ar1(1-6 alkyl); Ar1 = Ph (optionally substituted by 1-3 halo, T, T', CN, CONH2, TO or T'O); Ar2 = naphthalenyl, or Ph (optionally substituted by 1-3 OH, halo, CN, NO2, NH2, NHT, N(T)2, T, T', TO, T'O, COOH, COOT, CONH2, CONHT or CON(T)2); Het = pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl or benzothienyl (all optionally substituted on carbon by 1-2 halo, T or mono-, di- or tri(halo)methyl); T, T', R, = 1-4C alkyl, halo(1-4C alkyl), 1-6C alkyl respectively.</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 N-acyl-2-substituted-4-(benzimidazolyl-or imidazopyridinyl-substituted pesidues)-piperidines as tachykinin antagonists
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