EA199800604A1 - Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперидинина как антагонисты рецепторов тахикинина - Google Patents

Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперидинина как антагонисты рецепторов тахикинина

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EA199800604A1
EA199800604A1 EA199800604A EA199800604A EA199800604A1 EA 199800604 A1 EA199800604 A1 EA 199800604A1 EA 199800604 A EA199800604 A EA 199800604A EA 199800604 A EA199800604 A EA 199800604A EA 199800604 A1 EA199800604 A1 EA 199800604A1
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alkyl
hydrogen
formula
substituted
hydroxyl
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EA199800604A
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EA001559B1 (ru
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Франс Эдуард Жансенс
Франсуа Мария Соммен
Доминик Луи Нестор Гилейн Сюрлеро
Ив Эмиль Мария Ван Росбрук
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Жансен Фармасетика Н.В.
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Application filed by Жансен Фармасетика Н.В. filed Critical Жансен Фармасетика Н.В.
Publication of EA199800604A1 publication Critical patent/EA199800604A1/ru
Publication of EA001559B1 publication Critical patent/EA001559B1/ru

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    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/40—Oxygen atoms
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Hydrogenated Pyridines (AREA)

Abstract

Настоящее изобретение касается соединений формулы (I), их N-оксидных форм, фармацевтически приемлемых солей присоединения и стереохимически изомерных форм, где n равно 0, 1 или 2; m равно 1 или 2, при условии, что если m равно 2, то n равно 1; р равно 0, 1 или 2; =Q является =O или =NR; X является ковалентной связью или бивалентным радикалом формулы -O-, -S-, -NR-; Rявляется Ar, ArCалкилом или ди(Ar)Cалкилом, где каждая Cалкильная группа произвольно замещена гидроксилом, Cалкилоксизаместителем, оксозаместителем или кетализованным оксозаместителем формулы -O-CH-CH-O- или -O-CH-CH-CH-O-; Rявляется Ar, ArCалкилом; Het или HetCалкилом; Rявляется водородом или Cалкилом; Rявляется водородом; Cалкилом; Cалкилокси-Cалкилом; гидрокси-Cалкилом; карбоксилом; Cалкилоксикарбонилом или Ar; Rявляется водородом; гидроксилом; Ar; ArCалкилоксигруппой; ди(Ar)Cалкилоксигруппой; ди(Ar)Cалкилтиогруппой; ArCалкилсульфоксигруппой; ди(Ar)Cалкилсульфоксигруппой; ArCалкилсульфонилом; ди(Ar)Cалкилсульфонилом; -NRR; Cалкилом, замещенным –NRR; или радикалом формулы (a-1) или (a-2); Rи Rмогут быть соединены; Rявляется водородом; гидроксилом; Cалкилоксигруппой; Cалкилом или ArCалкилом; Ar, Arи Arявляются фенилом или замещенным фенилом; Arтакже является нафталинилом; и Het является необязательно замещенным моноциклическим или бициклическим гетероциклом; в качестве антагонистов вещества P; их получения, содержащих их композиций и их применения в качестве лекарственных препаратов.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199800604A 1995-12-27 1996-12-20 Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперидина как антагонисты рецепторов тахикинина EA001559B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP95203651 1995-12-27
PCT/EP1996/005883 WO1997024324A1 (en) 1995-12-27 1996-12-20 1-(1,2-disubstituted piperidinyl)-4-substituted piperidine derivatives as tachykinin receptor antagonists

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EA199800604A1 true EA199800604A1 (ru) 1998-12-24
EA001559B1 EA001559B1 (ru) 2001-04-23

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US (2) US6169097B1 (ru)
EP (1) EP0855999B1 (ru)
JP (1) JP4039691B2 (ru)
KR (1) KR100493574B1 (ru)
CN (1) CN1131854C (ru)
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BR (1) BR9612334A (ru)
CA (1) CA2238818C (ru)
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SI (1) SI0855999T1 (ru)
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