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EA200501041A1 - Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина и их применение в качестве антагонистов нейрокининов - Google Patents

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

Info

Publication number
EA200501041A1
EA200501041A1 EA200501041A EA200501041A EA200501041A1 EA 200501041 A1 EA200501041 A1 EA 200501041A1 EA 200501041 A EA200501041 A EA 200501041A EA 200501041 A EA200501041 A EA 200501041A EA 200501041 A1 EA200501041 A1 EA 200501041A1
Authority
EA
Eurasian Patent Office
Prior art keywords
antagonistic activity
neurokinins
pyrrolidin
piperidin
substituted derivatives
Prior art date
Application number
EA200501041A
Other languages
English (en)
Other versions
EA009078B1 (ru
Inventor
Франс Эдуард Янссенс
Франсуа Мария Соммен
Бенуа Кристиан Альберт Гилейн Де Бук
Йозеф Элизабет Ленартс
Original Assignee
Янссен Фармацевтика Н. В.
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 Янссен Фармацевтика Н. В. filed Critical Янссен Фармацевтика Н. В.
Publication of EA200501041A1 publication Critical patent/EA200501041A1/ru
Publication of EA009078B1 publication Critical patent/EA009078B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Данное изобретение относится к замещенным производным 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина, обладающим антагонистической активностью по отношению к нейрокининам, в частности антагонистической активностью в отношении NK, комбинированной антагонистической активностью в отношении NK/NKи комбинированной антагонистической активностью в отношении NK/NK/NK, их получению, композициям, содержащим их, и к их применению в качестве лекарственного средства, в частности, для лечения шизофрении, тревоги, депрессии, рвоты и IBS. Соединения по изобретению могут быть представлены общей формулой (I), где все заместители имеют значения, указанные в п.1, и к ним также относятся фармацевтически приемлемые соли присоединения кислот или оснований, стереохимически изомерные формы, N-оксиды и пролекарства таких соединений.Отчет о международном поиске был опубликован 2004.08.12.
EA200501041A 2002-12-23 2003-12-17 Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина и их применение в качестве антагонистов нейрокининов EA009078B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0214831 2002-12-23
PCT/EP2003/051041 WO2004056799A2 (en) 2002-12-23 2003-12-17 Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists

Publications (2)

Publication Number Publication Date
EA200501041A1 true EA200501041A1 (ru) 2005-12-29
EA009078B1 EA009078B1 (ru) 2007-10-26

Family

ID=32668698

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200501041A EA009078B1 (ru) 2002-12-23 2003-12-17 Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина и их применение в качестве антагонистов нейрокининов

Country Status (31)

Country Link
US (1) US7795261B2 (ru)
EP (1) EP1581518B1 (ru)
JP (1) JP4746878B2 (ru)
KR (1) KR101049073B1 (ru)
CN (1) CN100586945C (ru)
AR (1) AR042651A1 (ru)
AT (1) ATE500242T1 (ru)
AU (1) AU2003302488B2 (ru)
BR (1) BR0317658A (ru)
CA (1) CA2508657C (ru)
CL (1) CL2003002725A1 (ru)
CY (1) CY1112601T1 (ru)
DE (1) DE60336266D1 (ru)
DK (1) DK1581518T3 (ru)
EA (1) EA009078B1 (ru)
ES (1) ES2361161T3 (ru)
HK (1) HK1087703A1 (ru)
HR (1) HRP20050556B1 (ru)
IL (1) IL169336A (ru)
JO (1) JO2696B1 (ru)
MX (1) MXPA05006887A (ru)
MY (1) MY145135A (ru)
NO (1) NO331174B1 (ru)
NZ (1) NZ541035A (ru)
PA (1) PA8593301A1 (ru)
PL (1) PL376048A1 (ru)
PT (1) PT1581518E (ru)
SI (1) SI1581518T1 (ru)
TW (1) TWI329109B (ru)
UA (1) UA80584C2 (ru)
WO (1) WO2004056799A2 (ru)

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ES2431524T3 (es) 2004-04-13 2013-11-26 Incyte Corporation Derivados de piperazinilpiperidina como antagonistas de los receptores de quimiocinas
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WO2006071875A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
US7635698B2 (en) * 2004-12-29 2009-12-22 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
EP1858896B1 (en) * 2005-03-08 2010-08-18 Janssen Pharmaceutica NV Diaza-spiro-[4.4]-nonane derivatives as neurokinin (nk1) antagonists
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EP2099454A4 (en) * 2006-11-17 2010-11-10 Abbott Lab AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS
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CN105037275B (zh) * 2007-03-31 2019-05-10 英特威国际有限公司 制备齐帕特罗及其盐的方法
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ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
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JP2016514670A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド 他の薬物と組み合わせたグアニル酸シクラーゼ受容体アゴニスト
JP2016514671A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼのアゴニストおよびその使用
SI3297631T1 (sl) 2015-05-18 2019-12-31 Nerre Therapeutics Limited Antagonist NK-1/NK-3 receptorja za zdravljenje oblivov vročine
HUE065300T2 (hu) 2018-03-14 2024-05-28 Kandy Therapeutics Ltd Kettõs NK-1/NK-3 receptor antagonistákat tartalmazó új gyógyászati kiszerelés
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Also Published As

Publication number Publication date
EP1581518B1 (en) 2011-03-02
CN1726207A (zh) 2006-01-25
KR101049073B1 (ko) 2011-07-15
IL169336A (en) 2013-01-31
IL169336A0 (en) 2007-07-04
NO20053569L (no) 2005-09-15
SI1581518T1 (sl) 2011-06-30
HRP20050556A2 (en) 2006-07-31
NZ541035A (en) 2008-05-30
EA009078B1 (ru) 2007-10-26
WO2004056799A3 (en) 2004-08-12
BR0317658A (pt) 2005-12-06
TW200500359A (en) 2005-01-01
WO2004056799A2 (en) 2004-07-08
US20060040950A1 (en) 2006-02-23
MXPA05006887A (es) 2005-08-16
JP2006514027A (ja) 2006-04-27
UA80584C2 (ru) 2007-10-10
EP1581518A2 (en) 2005-10-05
NO331174B1 (no) 2011-10-24
CN100586945C (zh) 2010-02-03
US7795261B2 (en) 2010-09-14
CA2508657C (en) 2013-02-19
KR20050085098A (ko) 2005-08-29
HRP20050556B1 (hr) 2014-03-28
JO2696B1 (en) 2013-03-03
HK1087703A1 (en) 2006-10-20
AU2003302488A1 (en) 2004-07-14
CY1112601T1 (el) 2016-02-10
CL2003002725A1 (es) 2005-04-08
DK1581518T3 (da) 2011-06-06
AU2003302488B2 (en) 2009-10-08
AR042651A1 (es) 2005-06-29
ES2361161T3 (es) 2011-06-14
ATE500242T1 (de) 2011-03-15
NO20053569D0 (no) 2005-07-21
JP4746878B2 (ja) 2011-08-10
CA2508657A1 (en) 2004-07-08
TWI329109B (en) 2010-08-21
PA8593301A1 (es) 2004-08-31
PL376048A1 (en) 2005-12-12
PT1581518E (pt) 2011-05-12
DE60336266D1 (de) 2011-04-14
MY145135A (en) 2011-12-30

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