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PE20020332A1 - Derivados de 4-fenil-piridina como antagonistas de receptores de neuroquinina nk-1 - Google Patents

Derivados de 4-fenil-piridina como antagonistas de receptores de neuroquinina nk-1

Info

Publication number
PE20020332A1
PE20020332A1 PE2001000779A PE2001000779A PE20020332A1 PE 20020332 A1 PE20020332 A1 PE 20020332A1 PE 2001000779 A PE2001000779 A PE 2001000779A PE 2001000779 A PE2001000779 A PE 2001000779A PE 20020332 A1 PE20020332 A1 PE 20020332A1
Authority
PE
Peru
Prior art keywords
halogen
alkyl
trifluoromethyl
alcoxy
neuroquinin
Prior art date
Application number
PE2001000779A
Other languages
English (en)
Inventor
Thierry Godel
Torsten Hoffmann
Patrick Schnider
Heinz Stadler
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20020332A1 publication Critical patent/PE20020332A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • A—HUMAN NECESSITIES
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

SE REFIERE A DERIVADOS DE 4-FENIL PIRIDINA DE FORMULA I DONDE R ES H, HALOGENO, R1 ES (C=C)mR1', (CR'=CR")mR1'; R1 ES HALOGENO, CIANO, (C)mR'R"R5; CONR'R", COO(CH2)mR5, ENTRE OTROS; R' Y R" SON H, OH, ALQUILO, CICLOALQUILO, ARILO; R5 ES H, CIANO, OH, HALOGENO, TRIFLUOROMETILO, ENTRE OTROS; R6 ES H, ALQUILO, TRIFLUOROMETILO, ARILO, ENTRE OTROS; R7 ES CO(CH2)mOH, OXO; R2 ES H, ALQUILO, ALCOXI, HALOGENO, CF3; R3 Y R3' SON H, ALQUILO O FORMAN JUNTOS CICLOALQUILO; R4 Y R4' SON H, HALOGENO, CF3, ALQUILO, ALCOXI; R Y R2, R4 Y R4' SON HC=CH-CH=CH OPCIONALMENTE SUSTITUIDO POR ALQUILO HALOGENO, ALCOXI; X ES CONR8, (CH2)pO, NR8CO, ENTRE OTROS; n ES 1-2; m ES 0-4; o Y p SON 1-2. SON COMPUESTOS PREFERIDOS N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-(4-HIDROXIACETIL-PIPERACIN-1-ILO)-N-METIL-4-o-TOLIL-NICOTINAMIDA, N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-CLORO-N-METIL-4-o-TOLIL-NICOTINAMIDA, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON ANTAGONISTAS DE RECEPTORES DE NEUROQUININA NK-1 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE ARTRITIS REUMATOIDE, ASMA, ENFERMEDAD INFLAMATORIA DEL INTESTINO, MODULACION DEL SISTEMA NERVIOSO CENTRAL
PE2001000779A 2000-08-08 2001-08-06 Derivados de 4-fenil-piridina como antagonistas de receptores de neuroquinina nk-1 PE20020332A1 (es)

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EP00117003 2000-08-08

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PE20020332A1 true PE20020332A1 (es) 2002-05-10

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