EA200501040A1 - Замещенные производные 1-пиперидин-3-ил-4-пиперидин-4-илпиперазина и их применение в качестве антагонистов нейрокинина - Google Patents

Замещенные производные 1-пиперидин-3-ил-4-пиперидин-4-илпиперазина и их применение в качестве антагонистов нейрокинина

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Publication number
EA200501040A1
EA200501040A1 EA200501040A EA200501040A EA200501040A1 EA 200501040 A1 EA200501040 A1 EA 200501040A1 EA 200501040 A EA200501040 A EA 200501040A EA 200501040 A EA200501040 A EA 200501040A EA 200501040 A1 EA200501040 A1 EA 200501040A1
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EA
Eurasian Patent Office
Prior art keywords
disorders
neurokinin
piperidin
antagonistic activity
antagonize
Prior art date
Application number
EA200501040A
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English (en)
Other versions
EA008774B1 (ru
Inventor
Франс Эдуард Янссенс
Франсуа Мария Соммен
Бенуа Кристиан Альберт Гилейн Де Бук
Йозеф Элизабет Ленартс
Original Assignee
Янссен Фармацевтика Н. В.
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Application filed by Янссен Фармацевтика Н. В. filed Critical Янссен Фармацевтика Н. В.
Publication of EA200501040A1 publication Critical patent/EA200501040A1/ru
Publication of EA008774B1 publication Critical patent/EA008774B1/ru

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Abstract

Данное соединение относится к замещенным производным 1-пиперидин-3-ил-4-пиперидин-4-илпиперазина, обладающим антагонистической активностью против нейрокинина, в частности NK-антагонистической активностью, комбинированной NK/NK-антагонистической активностью и комбинированной NK/NK/NK-антагонистической активностью, их получению, содержащим их композициям и их применению в качестве лекарственного средства, в частности, для лечения шизофрении, рвоты, тревожности и депрессии, синдрома раздраженной толстой кишки (IBS), расстройств циркадного ритма, висцеральной боли, нейрогенного воспаления, астмы, нарушений мочеиспускания, таких как недержание мочи, и ноцицепции. Соединения по изобретению могут быть представлены общей формулой (I) и включают в себя также их фармацевтически приемлемые соли с кислотами или основаниями, их стереохимически изомерные формы, их N-оксидную форму и их пролекарства, где все заместители имеют значения, указанные в п.1. По причине их способности антагонизировать действиям нейрокининов блокированием рецепторов нейрокининов, в частности антагонизировать действия вещества P, нейрокинина A и нейрокинина B блокированием рецепторов NK, NKи NK, соединения по изобретению могут быть использованы в качестве лекарственного средства, в частности, при профилактике и терапевтическом лечении тахикининопосредованных состояний, таких как, например, нарушения ЦНС, в частности шизоаффективных нарушений, депрессии, нарушений типа тревожности, нарушений, относящихся к стрессу, нарушений сна, нарушений познавательной способности, изменения личности, нарушения аппетита, нейродегенеративных нарушений, нарушений типа аддикции, нарушений
EA200501040A 2002-12-23 2003-12-17 Замещенные производные 1-пиперидин-3-ил-4-пиперидин-4-илпиперазина и их применение в качестве антагонистов нейрокинина EA008774B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0214835 2002-12-23
PCT/EP2003/051035 WO2004056364A1 (en) 2002-12-23 2003-12-17 Substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists

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EA200501040A1 true EA200501040A1 (ru) 2005-12-29
EA008774B1 EA008774B1 (ru) 2007-08-31

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EA200501040A EA008774B1 (ru) 2002-12-23 2003-12-17 Замещенные производные 1-пиперидин-3-ил-4-пиперидин-4-илпиперазина и их применение в качестве антагонистов нейрокинина

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US (1) US7572786B2 (ru)
JP (1) JP4660198B2 (ru)
KR (1) KR101049075B1 (ru)
CN (1) CN100482229C (ru)
AR (1) AR042653A1 (ru)
AU (1) AU2003300578B2 (ru)
CA (1) CA2509088C (ru)
CL (1) CL2003002722A1 (ru)
DE (1) DE60317709T2 (ru)
EA (1) EA008774B1 (ru)
ES (1) ES2297275T3 (ru)
HK (1) HK1087924A1 (ru)
HR (1) HRP20050554B1 (ru)
IL (1) IL169337A (ru)
JO (1) JO2485B1 (ru)
MX (1) MXPA05006888A (ru)
MY (1) MY134383A (ru)
NO (1) NO331173B1 (ru)
NZ (1) NZ541036A (ru)
PA (1) PA8593201A1 (ru)
PL (1) PL214705B1 (ru)
TW (1) TWI327916B (ru)
UA (1) UA83474C2 (ru)
WO (1) WO2004056364A1 (ru)

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MY141736A (en) * 2002-10-08 2010-06-15 Elanco Animal Health Ireland Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists
EP1734966B1 (en) 2004-04-13 2013-07-31 Incyte Corporation Piperazinylpiperidine derivatives as chemokine receptor antagonists
GB0417702D0 (en) * 2004-08-09 2004-09-08 Merck Sharp & Dohme New uses
US8604200B2 (en) * 2005-03-08 2013-12-10 Janssen Pharmaceutica N.V. Diaza-spiro-{4,4}-nonane derivatives as neurokinin (NK1) antagonists
CN105209436B (zh) * 2013-03-15 2019-02-01 南洋理工大学 3-哌啶酮化合物及其作为神经激肽-1(nk1)受体拮抗剂的用途
ES2879375T3 (es) 2014-06-25 2021-11-22 Univ Emory Procedimientos de manejo del miedo condicionado con antagonistas del receptor de neuroquinina

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MY110227A (en) 1991-08-12 1998-03-31 Ciba Geigy Ag 1-acylpiperindine compounds.
NZ321575A (en) * 1995-10-30 1999-05-28 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives
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FR2791346B3 (fr) * 1999-03-25 2001-04-27 Sanofi Sa Nouveaux derives de morpholine, procede pour leur preparation et compositions pharmaceutiques les contenant
AU7788500A (en) * 1999-10-25 2001-05-08 Janssen Pharmaceutica N.V. Use of substance p antagonists for influencing the circadian timing system
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MY141736A (en) * 2002-10-08 2010-06-15 Elanco Animal Health Ireland Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists
AU2002368487A1 (en) * 2002-12-23 2004-07-14 Janssen Pharmaceutica N.V. Substituted 1,4-di-piperidin-4-yl-piperazine derivatives and their use as tachykinin antagonists
JP2006527236A (ja) * 2003-06-10 2006-11-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ オピオイド鎮痛薬と組合せた置換１，４−ジ−ピペリジン−４−イル−ピペラジン誘導体ならびに疼痛およびオピオイドに基づく処置に伴う副作用の処置のためのそれらの使用

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JP2006512348A (ja) 2006-04-13
US7572786B2 (en) 2009-08-11
CA2509088C (en) 2012-01-24
AU2003300578B2 (en) 2009-06-04
WO2004056364A1 (en) 2004-07-08
PA8593201A1 (es) 2004-07-26
IL169337A0 (en) 2007-07-04
HRP20050554B1 (hr) 2014-02-28
NO20053598D0 (no) 2005-07-22
CN100482229C (zh) 2009-04-29
JO2485B1 (en) 2009-01-20
HRP20050554A2 (en) 2006-06-30
KR20050085217A (ko) 2005-08-29
DE60317709D1 (de) 2008-01-03
JP4660198B2 (ja) 2011-03-30
NO20053598L (no) 2005-09-20
MXPA05006888A (es) 2005-08-16
CN1728999A (zh) 2006-02-01
DE60317709T2 (de) 2008-10-30
MY134383A (en) 2007-12-31
TWI327916B (en) 2010-08-01
IL169337A (en) 2011-07-31
TW200503715A (en) 2005-02-01
EA008774B1 (ru) 2007-08-31
CL2003002722A1 (es) 2005-04-08
CA2509088A1 (en) 2004-07-08
US20060252747A1 (en) 2006-11-09
AU2003300578A1 (en) 2004-07-14
AR042653A1 (es) 2005-06-29
ES2297275T3 (es) 2008-05-01
KR101049075B1 (ko) 2011-07-15
PL214705B1 (pl) 2013-09-30
HK1087924A1 (en) 2006-10-27
NZ541036A (en) 2007-07-27
NO331173B1 (no) 2011-10-24
UA83474C2 (ru) 2008-07-25
PL376075A1 (en) 2005-12-12

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