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AR039192A1 - Derivados de diazabicicloalcano con actividad antagonista de nk1 - Google Patents

Derivados de diazabicicloalcano con actividad antagonista de nk1

Info

Publication number
AR039192A1
AR039192A1 ARP030101105A ARP030101105A AR039192A1 AR 039192 A1 AR039192 A1 AR 039192A1 AR P030101105 A ARP030101105 A AR P030101105A AR P030101105 A ARP030101105 A AR P030101105A AR 039192 A1 AR039192 A1 AR 039192A1
Authority
AR
Argentina
Prior art keywords
morpholin
group
alkyl
indolyl
substituted
Prior art date
Application number
ARP030101105A
Other languages
English (en)
Inventor
Scharrenburg Guustaaf J M Van
Boer Dirk De
Hein K A C Coolen
Mayke B Hesselink
Bakker Wouter I Iwema
Maarseveen Jan H Van
Andrew C Mccreary
Gijsbert D Kuil
Original Assignee
Solvay Pharm Bv
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 Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of AR039192A1 publication Critical patent/AR039192A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61P1/08Drugs 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/06Antimigraine agents
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P27/16Otologicals
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P37/00Drugs for immunological or allergic disorders
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    • 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Un grupo de singulares derivados de diazabicicloalcano que tienen interesante actividad antagonista del receptor NK1 de neuroquinina, representados por la fórmula general (1) en donde: R1 representa fenilo, 2-indolilo, 3-indolilo, 3-indazolilo o benzo[b]tiofen-3-ilo, cuyos grupos pueden estar sustituidos con halógeno o alquilo C1-3; R2 y R3 representan independientemente halógeno, H, OCH3, CH3 y CF3, R4, R5 y R6 independientemente representan H, OH, O-alquilo C1-4, CH2OH, NH2, dialquil (C1-3)N, pirrolidin-1-ilo, piperidin-1-ilo, morfolin-4-ilo o morfolin-4-ilo sustituido con uno o dos grupos metilo o metoximetilo, morfolin-4-ilamino, morfolin-4-ilmetilo, imidazol-1-ilo, tiomorfolin-4-ilo, 1,1-dioxotiomorfolin-4-ilo o 3-oxa-8-azabiciclo[3.2.1]oct-8-ilo; R4 y R5 juntos pueden representar un grupo ceto, un grupo 1,3-dioxan-2-ilo o un grupo 1,3-dioxolan-2-ilo, X representa O ó S; n tiene el valor de 1, 2 o 3; a es el átomo de C asimétrico 8a, 9a o 10a cuando n es igual a 1, 2 o 3 respectivamente. También se refiere a un método para la preparación de los compuestos, y a composiciones farmacéuticas que contienen al menos uno de estos compuestos como un ingrediente activo.
ARP030101105A 2002-04-04 2003-03-28 Derivados de diazabicicloalcano con actividad antagonista de nk1 AR039192A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02076405 2002-04-04

Publications (1)

Publication Number Publication Date
AR039192A1 true AR039192A1 (es) 2005-02-09

Family

ID=28685940

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101105A AR039192A1 (es) 2002-04-04 2003-03-28 Derivados de diazabicicloalcano con actividad antagonista de nk1

Country Status (20)

Country Link
US (1) US7202238B2 (es)
EP (1) EP1495022B1 (es)
JP (1) JP2005525395A (es)
KR (1) KR20040095361A (es)
CN (1) CN1279041C (es)
AR (1) AR039192A1 (es)
AT (1) ATE435863T1 (es)
AU (1) AU2003224162B2 (es)
BR (1) BR0306148A (es)
CA (1) CA2462708A1 (es)
DE (1) DE60328272D1 (es)
HR (1) HRP20040273A2 (es)
IL (2) IL160943A0 (es)
MX (1) MXPA04004812A (es)
NO (1) NO20044775L (es)
PL (1) PL371378A1 (es)
RU (1) RU2310656C2 (es)
UA (1) UA77515C2 (es)
WO (1) WO2003084955A1 (es)
ZA (1) ZA200404744B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1556054A4 (en) * 2002-05-29 2007-09-05 Univ California ANTAGONIZING NK1 RECEPTORS RESTRICT DRUG ABUSE
AR045796A1 (es) * 2003-09-26 2005-11-16 Solvay Pharm Bv Derivados de hexa y octahidro - pirido (1,2-a) pirazina con actividad antagonista de nk1. composiciones farmaceuticas.
WO2006013205A1 (en) * 2004-08-04 2006-02-09 Solvay Pharmaceuticals B.V. Neurokinin-1 receptor antagonists for the treatment of conditions responsive to testosterone elevation
DE102006049452A1 (de) 2006-10-17 2008-05-08 Grünenthal GmbH Substituierte Tetrahydropyrolopiperazin-Verbindungen und deren Verwendung in Arzneimitteln
WO2010011912A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Trpv4 antagonists
WO2010011914A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Trpv4 antagonists
WO2013049164A1 (en) * 2011-09-29 2013-04-04 Abbvie Inc. SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS
US8648074B2 (en) 2011-09-29 2014-02-11 Abbvie Inc. Substituted octahydropyrrolo[1,2-a]pyrazine sulfonamides as calcium channel blockers
US9181259B2 (en) * 2012-02-22 2015-11-10 Leo Pharma A/S Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists
BR112015013948A2 (pt) 2012-12-12 2017-07-11 Abbvie Inc derivados diazepínicos úteis como bloqueadores do canal de cálcio no tratamento de dor
LT3024463T (lt) * 2013-07-25 2020-07-10 Neuren Pharmaceuticals Limited Neuroapsauginiai bicikliniai junginiai ir jų panaudojimo būdai autizmo spektro sutrikimų ir neuroliginių vystymosi sutrikimų gydymui
WO2015024203A1 (en) * 2013-08-20 2015-02-26 Leo Pharma A/S Novel neurokinin 1 receptor antagonist compounds ii
WO2018175385A1 (en) 2017-03-20 2018-09-27 The Broad Institute, Inc. Compounds and methods for the treatment of parasitic diseases

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1125112A (en) * 1966-01-07 1968-08-28 Science Union & Cie New derivatives of diazabicyclo-decane and process for preparing them
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
ES2167563T3 (es) * 1995-05-23 2002-05-16 Janssen Pharmaceutica Nv Derivados de (2-morfolinilmetil)benzamida.
GB9510600D0 (en) * 1995-05-25 1995-07-19 Fujisawa Pharmaceutical Co Piperazine derivatives
JP3071829B2 (ja) 1995-05-25 2000-07-31 藤沢薬品工業株式会社 ニューロキニン受容体拮抗剤としての1−ベンゾイル−2−(インドリル−3−アルキル)−ピペラジン誘導体
DE69621831T2 (de) 1995-12-18 2003-01-02 Fujisawa Pharmaceutical Co., Ltd. Piperazinderivative als tachykinin antagonisten
AUPO735997A0 (en) 1997-06-17 1997-07-10 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
EP0899270B1 (de) 1997-08-27 2008-05-21 Solvay Pharmaceuticals GmbH Indolmethyl-N,N'-bisacylpiperazine als Neurokininrezeptorantagonisten
DE19824865A1 (de) * 1997-08-27 1999-03-04 Solvay Pharm Gmbh Neue Harnstoffderivate
EP0982030A3 (en) * 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
KR20010086104A (ko) * 1998-12-14 2001-09-07 후지야마 아키라 피페라진 유도체
DE10036818A1 (de) * 2000-07-28 2002-02-07 Solvay Pharm Gmbh Neue N-Triazolylmethyl-Piperazinderivate als Neurokininrezeptor-Antagonisten

Also Published As

Publication number Publication date
NO20044775L (no) 2004-12-16
CA2462708A1 (en) 2003-10-16
US7202238B2 (en) 2007-04-10
IL160943A (en) 2008-11-03
AU2003224162B2 (en) 2008-06-12
AU2003224162A1 (en) 2003-10-20
MXPA04004812A (es) 2004-08-11
CN1279041C (zh) 2006-10-11
HRP20040273A2 (en) 2005-02-28
RU2004112415A (ru) 2005-03-27
IL160943A0 (en) 2004-08-31
DE60328272D1 (de) 2009-08-20
BR0306148A (pt) 2004-10-19
ATE435863T1 (de) 2009-07-15
CN1592747A (zh) 2005-03-09
RU2310656C2 (ru) 2007-11-20
KR20040095361A (ko) 2004-11-12
JP2005525395A (ja) 2005-08-25
EP1495022A1 (en) 2005-01-12
HK1070356A1 (en) 2005-06-17
US20050119267A1 (en) 2005-06-02
WO2003084955A1 (en) 2003-10-16
UA77515C2 (en) 2006-12-15
ZA200404744B (en) 2005-09-21
EP1495022B1 (en) 2009-07-08
PL371378A1 (en) 2005-06-13

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