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NO331174B1 - Substituerte 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazinderivater og deres anvendelse som neurokininantagonister - Google Patents

Substituerte 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazinderivater og deres anvendelse som neurokininantagonister

Info

Publication number
NO331174B1
NO331174B1 NO20053569A NO20053569A NO331174B1 NO 331174 B1 NO331174 B1 NO 331174B1 NO 20053569 A NO20053569 A NO 20053569A NO 20053569 A NO20053569 A NO 20053569A NO 331174 B1 NO331174 B1 NO 331174B1
Authority
NO
Norway
Prior art keywords
pyrrolidin
piperidin
substituted
antagonistic activity
piperazine derivatives
Prior art date
Application number
NO20053569A
Other languages
English (en)
Other versions
NO20053569L (no
NO20053569D0 (no
Inventor
Frans Eduard Janssens
Joseph Elisabeth Leenaerts
Francois Maria Sommen
Benoit Christian Albert Ghislain De Boeck
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of NO20053569D0 publication Critical patent/NO20053569D0/no
Publication of NO20053569L publication Critical patent/NO20053569L/no
Publication of NO331174B1 publication Critical patent/NO331174B1/no

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

Landscapes

  • 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)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (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

Denne oppfinnelse vedrører substituerte 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazinderivater med neurokininantagonistisk aktivitet, spesielt NK1-antagonistisk aktivitet, en kombinert NK1/NK3-antagonistisk aktivitet og en kombinert NK1/NK2/NK3-antagonistisk aktivitet, deres fremstilling, sammensetninger omfattende dem og deres anvendelse som en medisin, spesielt for behandlingen av schizofreni, angst, depresjon, emese og IBS. Forbindelsene i henhold til oppfinnelsen kan representeres ved generell formel (I) og omfatter også de farmasøytisk akseptable syre- eller baseaddisjonssalter derav, de stereokjemisk isomere former derav, N-oksidformen derav og prodroger derav, hvori alle substituenter er definert som i krav 1.
NO20053569A 2002-12-23 2005-07-21 Substituerte 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazinderivater og deres anvendelse som neurokininantagonister NO331174B1 (no)

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 (3)

Publication Number Publication Date
NO20053569D0 NO20053569D0 (no) 2005-07-21
NO20053569L NO20053569L (no) 2005-09-15
NO331174B1 true NO331174B1 (no) 2011-10-24

Family

ID=32668698

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20053569A NO331174B1 (no) 2002-12-23 2005-07-21 Substituerte 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazinderivater og deres anvendelse som neurokininantagonister

Country Status (31)

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

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FR2847160A1 (fr) * 2002-11-20 2004-05-21 Oreal Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute
EA015517B1 (ru) 2004-04-13 2011-08-30 Инсайт Корпорейшн Производные пиперазинилпиперидина в качестве антагонистов хемокинового рецептора
WO2005123081A2 (en) * 2004-06-22 2005-12-29 Janssen Pharmaceutica N.V. (2-benzyl-4-{4-[1-(tetrahydrofuran-3-carbonyl)-pyrrolidin-3-yl]-piperazin-1-yl}-piperidin-1-yl)-(3,5-trifluoromethyl-phenyl))-methanone for the treatment of schizophrenia
WO2006071958A1 (en) * 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
WO2006071875A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
NZ556628A (en) 2005-03-08 2009-09-25 Janssen Pharmaceutica Nv Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists
DE102005038947A1 (de) * 2005-05-18 2006-11-30 Grünenthal GmbH Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln
US8754107B2 (en) * 2006-11-17 2014-06-17 Abbvie Inc. Aminopyrrolidines as chemokine receptor antagonists
MX2009010499A (es) * 2007-03-31 2009-10-19 Intervet Int Bv Procesos para elaborar zilpaterol y sales del mismo.
RU2442786C2 (ru) * 2007-03-31 2012-02-20 Интервет Интернэшнл Б.В. Способы получения зилпатерола и его солей
HUE029053T2 (en) * 2007-03-31 2017-01-30 Intervet Int Bv Process for the preparation of zilpaterol and its salts
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
JP5546451B2 (ja) 2007-06-04 2014-07-09 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 胃腸の障害、炎症、癌および他の障害の処置に有用なグアニル酸シクラーゼのアゴニスト
CA2689560A1 (en) * 2007-06-07 2008-12-11 F.Hoffmann-La Roche Ag Prolinamide derivatives as nk3 antagonists
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
US8507535B2 (en) * 2010-07-07 2013-08-13 Hoffmann-La Roche Inc. Methyl-pyrrolidine ether derivatives
KR20150046259A (ko) * 2012-08-23 2015-04-29 앨리오스 바이오파마 인크. 파라믹소바이러스 바이러스성 감염의 치료용 화합물
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
EP2968439A2 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
BR112017024852B1 (pt) 2015-05-18 2023-10-31 KaNDy Therapeutics Limited Usos de um composto antagonista do receptor nk-1/nk-3 duplo e de uma composição farmacêutica compreendendo dito composto para o tratamento de sintomas vasomotores associados com menopausa
EA202092131A1 (ru) 2018-03-14 2020-11-27 Кэнди Терапьютикс Лимитед Новый фармацевтический препарат, содержащий двойные антагонисты рецептора nk-1/nk-3
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof

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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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Also Published As

Publication number Publication date
DK1581518T3 (da) 2011-06-06
NZ541035A (en) 2008-05-30
TWI329109B (en) 2010-08-21
TW200500359A (en) 2005-01-01
EP1581518B1 (en) 2011-03-02
WO2004056799A3 (en) 2004-08-12
AU2003302488B2 (en) 2009-10-08
WO2004056799A2 (en) 2004-07-08
ES2361161T3 (es) 2011-06-14
JO2696B1 (en) 2013-03-03
KR101049073B1 (ko) 2011-07-15
DE60336266D1 (de) 2011-04-14
NO20053569L (no) 2005-09-15
EA200501041A1 (ru) 2005-12-29
EA009078B1 (ru) 2007-10-26
IL169336A (en) 2013-01-31
PT1581518E (pt) 2011-05-12
HRP20050556A2 (en) 2006-07-31
AU2003302488A1 (en) 2004-07-14
CY1112601T1 (el) 2016-02-10
CN1726207A (zh) 2006-01-25
EP1581518A2 (en) 2005-10-05
MXPA05006887A (es) 2005-08-16
BR0317658A (pt) 2005-12-06
JP4746878B2 (ja) 2011-08-10
HK1087703A1 (en) 2006-10-20
CA2508657A1 (en) 2004-07-08
AR042651A1 (es) 2005-06-29
IL169336A0 (en) 2007-07-04
NO20053569D0 (no) 2005-07-21
ATE500242T1 (de) 2011-03-15
PA8593301A1 (es) 2004-08-31
HRP20050556B1 (hr) 2014-03-28
CA2508657C (en) 2013-02-19
KR20050085098A (ko) 2005-08-29
CN100586945C (zh) 2010-02-03
MY145135A (en) 2011-12-30
US7795261B2 (en) 2010-09-14
US20060040950A1 (en) 2006-02-23
CL2003002725A1 (es) 2005-04-08
UA80584C2 (uk) 2007-10-10
PL376048A1 (en) 2005-12-12
SI1581518T1 (sl) 2011-06-30
JP2006514027A (ja) 2006-04-27

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