4-PHENYL-PYRIDINE DERIVATIVES

Jedinjenja opšte formuleu kojoj označavajuR vodonik, C1-7-alkil, C1-7-alkoksi, halogen ili trifluormetil;R1 vodonik ili halogen; iliR i R1 mogu zajedno formirati -CH=CH-CH=CH-;R2 i R2' a nezavisno jedan od drugog označavaju vodonik, halogen, trifluormetil, C1-7-alkoksi ili cijano-grupu;iliR2 i...

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Hauptverfasser: BOES, MICHAEL, GALLEY, GUIDO, HUNKELER, WALTER, BRANCA, QUIRICO, GODEL, THIERRY, STADLER, HEINZ, SCHNIDER, PATRICK, HOFFMANN, TORSTEN
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creator BOES, MICHAEL
GALLEY, GUIDO
HUNKELER, WALTER
BRANCA, QUIRICO
GODEL, THIERRY
STADLER, HEINZ
SCHNIDER, PATRICK
HOFFMANN, TORSTEN
description Jedinjenja opšte formuleu kojoj označavajuR vodonik, C1-7-alkil, C1-7-alkoksi, halogen ili trifluormetil;R1 vodonik ili halogen; iliR i R1 mogu zajedno formirati -CH=CH-CH=CH-;R2 i R2' a nezavisno jedan od drugog označavaju vodonik, halogen, trifluormetil, C1-7-alkoksi ili cijano-grupu;iliR2 i R2' mogu zajedno formirati grupu -CH=CH-CH=CH-, koja je opciono supstituisana sa jednim ili dva supstituenta odabrana između C1-7-alkila ili C1-7-alkoksi-grupe;R3 vodonik, C1-7-alkil ili formira C3-6-cikloalkil-grupu;R4 -N(R5)2, -N (R5) (CH2)nOH, -N(R5)S(O)2- C1-7-alkil, -N (R5) S (O)2-fenil,-N=CH-N (R5)2, -N(R5)C(O)R5 ili ciklični tercijarni amin grupeili grupe pri čemu je ciklični tercijarni amin grupe odabran od grupe koja uključujepirol-1-il, imidazol-1-il, piperidin-1-il, piperazin-1-il, morfolin-4-il, tiomorfolin-4-il, 1-okso-tiomorfolin-4-il ili 1,1-diokso-tiomorfolin-4-il;R5 nezavisno jedan od drugog označava vodonik, C3-6-cikloalkil, benzil ili C1-7-alkil;R6 vodonik, hidroksi, C1-7-alkil, -(CH2)nCOO- C1-7-alkil, -N(R5)CO- C1-7-alkil, hidroksi- C1-7-alkil, cijan, -(CH2)nO (CH2)nOH, -CHO ili petočlanu ili šestočlanu heterocikličnu grupu koja uključuje piridinil, pirimidinil, oksadiazolil, triazolil, tetrazolil, tiazolil, tienil, furil, piranil, pirolil, imidazolil, pirazolil, izotiazolil, piperazinil ili piperidil, koja je opciono vezana preko alkilenske grupe;X -C(O)N(R5)-;N 0 - 4; im 1 ili 2;i njihove farmaceutski prihvatljive kiselinske adicione soli.Prijava sadrži još 6 patentnih zahteva. The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R    is hydrogen or halogen; or R and R    may be together -CH=CH-CH=CH-; R and R   may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R    is hydrogen, lower alkyl or form a cycloalkyl group; R    is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R    is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R    is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group,
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fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_RS53869B1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>RS53869B1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_RS53869B13</originalsourceid><addsrcrecordid>eNrjZJA10Q3wcPWL9NENiAzydPH0c1VwcQ3yDHMM8QxzDeZhYE1LzClO5YXS3Axybq4hzh66qQX58anFBYnJqXmpJfFBwabGFmaWTobGBBUAAOUkIDA</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>4-PHENYL-PYRIDINE DERIVATIVES</title><source>esp@cenet</source><creator>BOES, MICHAEL ; GALLEY, GUIDO ; HUNKELER, WALTER ; BRANCA, QUIRICO ; GODEL, THIERRY ; STADLER, HEINZ ; SCHNIDER, PATRICK ; HOFFMANN, TORSTEN</creator><creatorcontrib>BOES, MICHAEL ; GALLEY, GUIDO ; HUNKELER, WALTER ; BRANCA, QUIRICO ; GODEL, THIERRY ; STADLER, HEINZ ; SCHNIDER, PATRICK ; HOFFMANN, TORSTEN</creatorcontrib><description>Jedinjenja opšte formuleu kojoj označavajuR vodonik, C1-7-alkil, C1-7-alkoksi, halogen ili trifluormetil;R1 vodonik ili halogen; iliR i R1 mogu zajedno formirati -CH=CH-CH=CH-;R2 i R2' a nezavisno jedan od drugog označavaju vodonik, halogen, trifluormetil, C1-7-alkoksi ili cijano-grupu;iliR2 i R2' mogu zajedno formirati grupu -CH=CH-CH=CH-, koja je opciono supstituisana sa jednim ili dva supstituenta odabrana između C1-7-alkila ili C1-7-alkoksi-grupe;R3 vodonik, C1-7-alkil ili formira C3-6-cikloalkil-grupu;R4 -N(R5)2, -N (R5) (CH2)nOH, -N(R5)S(O)2- C1-7-alkil, -N (R5) S (O)2-fenil,-N=CH-N (R5)2, -N(R5)C(O)R5 ili ciklični tercijarni amin grupeili grupe pri čemu je ciklični tercijarni amin grupe odabran od grupe koja uključujepirol-1-il, imidazol-1-il, piperidin-1-il, piperazin-1-il, morfolin-4-il, tiomorfolin-4-il, 1-okso-tiomorfolin-4-il ili 1,1-diokso-tiomorfolin-4-il;R5 nezavisno jedan od drugog označava vodonik, C3-6-cikloalkil, benzil ili C1-7-alkil;R6 vodonik, hidroksi, C1-7-alkil, -(CH2)nCOO- C1-7-alkil, -N(R5)CO- C1-7-alkil, hidroksi- C1-7-alkil, cijan, -(CH2)nO (CH2)nOH, -CHO ili petočlanu ili šestočlanu heterocikličnu grupu koja uključuje piridinil, pirimidinil, oksadiazolil, triazolil, tetrazolil, tiazolil, tienil, furil, piranil, pirolil, imidazolil, pirazolil, izotiazolil, piperazinil ili piperidil, koja je opciono vezana preko alkilenske grupe;X -C(O)N(R5)-;N 0 - 4; im 1 ili 2;i njihove farmaceutski prihvatljive kiselinske adicione soli.Prijava sadrži još 6 patentnih zahteva. The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R    is hydrogen or halogen; or R and R    may be together -CH=CH-CH=CH-; R and R&lt;2'&gt;   are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R&lt;2'&gt;   may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R    is hydrogen, lower alkyl or form a cycloalkyl group; R    is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R    is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R    is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.</description><language>eng ; srp</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>2015</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=20150831&amp;DB=EPODOC&amp;CC=RS&amp;NR=53869B1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20150831&amp;DB=EPODOC&amp;CC=RS&amp;NR=53869B1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>BOES, MICHAEL</creatorcontrib><creatorcontrib>GALLEY, GUIDO</creatorcontrib><creatorcontrib>HUNKELER, WALTER</creatorcontrib><creatorcontrib>BRANCA, QUIRICO</creatorcontrib><creatorcontrib>GODEL, THIERRY</creatorcontrib><creatorcontrib>STADLER, HEINZ</creatorcontrib><creatorcontrib>SCHNIDER, PATRICK</creatorcontrib><creatorcontrib>HOFFMANN, TORSTEN</creatorcontrib><title>4-PHENYL-PYRIDINE DERIVATIVES</title><description>Jedinjenja opšte formuleu kojoj označavajuR vodonik, C1-7-alkil, C1-7-alkoksi, halogen ili trifluormetil;R1 vodonik ili halogen; iliR i R1 mogu zajedno formirati -CH=CH-CH=CH-;R2 i R2' a nezavisno jedan od drugog označavaju vodonik, halogen, trifluormetil, C1-7-alkoksi ili cijano-grupu;iliR2 i R2' mogu zajedno formirati grupu -CH=CH-CH=CH-, koja je opciono supstituisana sa jednim ili dva supstituenta odabrana između C1-7-alkila ili C1-7-alkoksi-grupe;R3 vodonik, C1-7-alkil ili formira C3-6-cikloalkil-grupu;R4 -N(R5)2, -N (R5) (CH2)nOH, -N(R5)S(O)2- C1-7-alkil, -N (R5) S (O)2-fenil,-N=CH-N (R5)2, -N(R5)C(O)R5 ili ciklični tercijarni amin grupeili grupe pri čemu je ciklični tercijarni amin grupe odabran od grupe koja uključujepirol-1-il, imidazol-1-il, piperidin-1-il, piperazin-1-il, morfolin-4-il, tiomorfolin-4-il, 1-okso-tiomorfolin-4-il ili 1,1-diokso-tiomorfolin-4-il;R5 nezavisno jedan od drugog označava vodonik, C3-6-cikloalkil, benzil ili C1-7-alkil;R6 vodonik, hidroksi, C1-7-alkil, -(CH2)nCOO- C1-7-alkil, -N(R5)CO- C1-7-alkil, hidroksi- C1-7-alkil, cijan, -(CH2)nO (CH2)nOH, -CHO ili petočlanu ili šestočlanu heterocikličnu grupu koja uključuje piridinil, pirimidinil, oksadiazolil, triazolil, tetrazolil, tiazolil, tienil, furil, piranil, pirolil, imidazolil, pirazolil, izotiazolil, piperazinil ili piperidil, koja je opciono vezana preko alkilenske grupe;X -C(O)N(R5)-;N 0 - 4; im 1 ili 2;i njihove farmaceutski prihvatljive kiselinske adicione soli.Prijava sadrži još 6 patentnih zahteva. The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R    is hydrogen or halogen; or R and R    may be together -CH=CH-CH=CH-; R and R&lt;2'&gt;   are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R&lt;2'&gt;   may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R    is hydrogen, lower alkyl or form a cycloalkyl group; R    is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R    is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R    is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.</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>2015</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZJA10Q3wcPWL9NENiAzydPH0c1VwcQ3yDHMM8QxzDeZhYE1LzClO5YXS3Axybq4hzh66qQX58anFBYnJqXmpJfFBwabGFmaWTobGBBUAAOUkIDA</recordid><startdate>20150831</startdate><enddate>20150831</enddate><creator>BOES, MICHAEL</creator><creator>GALLEY, GUIDO</creator><creator>HUNKELER, WALTER</creator><creator>BRANCA, QUIRICO</creator><creator>GODEL, THIERRY</creator><creator>STADLER, HEINZ</creator><creator>SCHNIDER, PATRICK</creator><creator>HOFFMANN, TORSTEN</creator><scope>EVB</scope></search><sort><creationdate>20150831</creationdate><title>4-PHENYL-PYRIDINE DERIVATIVES</title><author>BOES, MICHAEL ; GALLEY, GUIDO ; HUNKELER, WALTER ; BRANCA, QUIRICO ; GODEL, THIERRY ; STADLER, HEINZ ; SCHNIDER, PATRICK ; HOFFMANN, TORSTEN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RS53869B13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; srp</language><creationdate>2015</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>BOES, MICHAEL</creatorcontrib><creatorcontrib>GALLEY, GUIDO</creatorcontrib><creatorcontrib>HUNKELER, WALTER</creatorcontrib><creatorcontrib>BRANCA, QUIRICO</creatorcontrib><creatorcontrib>GODEL, THIERRY</creatorcontrib><creatorcontrib>STADLER, HEINZ</creatorcontrib><creatorcontrib>SCHNIDER, PATRICK</creatorcontrib><creatorcontrib>HOFFMANN, TORSTEN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>BOES, MICHAEL</au><au>GALLEY, GUIDO</au><au>HUNKELER, WALTER</au><au>BRANCA, QUIRICO</au><au>GODEL, THIERRY</au><au>STADLER, HEINZ</au><au>SCHNIDER, PATRICK</au><au>HOFFMANN, TORSTEN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>4-PHENYL-PYRIDINE DERIVATIVES</title><date>2015-08-31</date><risdate>2015</risdate><abstract>Jedinjenja opšte formuleu kojoj označavajuR vodonik, C1-7-alkil, C1-7-alkoksi, halogen ili trifluormetil;R1 vodonik ili halogen; iliR i R1 mogu zajedno formirati -CH=CH-CH=CH-;R2 i R2' a nezavisno jedan od drugog označavaju vodonik, halogen, trifluormetil, C1-7-alkoksi ili cijano-grupu;iliR2 i R2' mogu zajedno formirati grupu -CH=CH-CH=CH-, koja je opciono supstituisana sa jednim ili dva supstituenta odabrana između C1-7-alkila ili C1-7-alkoksi-grupe;R3 vodonik, C1-7-alkil ili formira C3-6-cikloalkil-grupu;R4 -N(R5)2, -N (R5) (CH2)nOH, -N(R5)S(O)2- C1-7-alkil, -N (R5) S (O)2-fenil,-N=CH-N (R5)2, -N(R5)C(O)R5 ili ciklični tercijarni amin grupeili grupe pri čemu je ciklični tercijarni amin grupe odabran od grupe koja uključujepirol-1-il, imidazol-1-il, piperidin-1-il, piperazin-1-il, morfolin-4-il, tiomorfolin-4-il, 1-okso-tiomorfolin-4-il ili 1,1-diokso-tiomorfolin-4-il;R5 nezavisno jedan od drugog označava vodonik, C3-6-cikloalkil, benzil ili C1-7-alkil;R6 vodonik, hidroksi, C1-7-alkil, -(CH2)nCOO- C1-7-alkil, -N(R5)CO- C1-7-alkil, hidroksi- C1-7-alkil, cijan, -(CH2)nO (CH2)nOH, -CHO ili petočlanu ili šestočlanu heterocikličnu grupu koja uključuje piridinil, pirimidinil, oksadiazolil, triazolil, tetrazolil, tiazolil, tienil, furil, piranil, pirolil, imidazolil, pirazolil, izotiazolil, piperazinil ili piperidil, koja je opciono vezana preko alkilenske grupe;X -C(O)N(R5)-;N 0 - 4; im 1 ili 2;i njihove farmaceutski prihvatljive kiselinske adicione soli.Prijava sadrži još 6 patentnih zahteva. The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R    is hydrogen or halogen; or R and R    may be together -CH=CH-CH=CH-; R and R&lt;2'&gt;   are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R&lt;2'&gt;   may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R    is hydrogen, lower alkyl or form a cycloalkyl group; R    is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R    is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R    is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.</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 4-PHENYL-PYRIDINE DERIVATIVES
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