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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P1/08—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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P11/16—Central respiratory analeptics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/06—Antimigraine agents
    • 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
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    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (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 (21)

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)
HK (1) HK1070356A1 (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
AU2003243353A1 (en) * 2002-05-29 2003-12-19 The Regents Of The University Of California Antagonizing nk1 receptors inhibits consumption of substances of abuse
SA04250304B1 (ar) 2003-09-26 2009-03-11 سولفاي فارماسوتيكالز بي . في مشتقات هكسا - واوكتاهيدرو - بيريدو {1،2-a} بيرازين ذات نشاط مضاد لـ nk1
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
AR088064A1 (es) 2011-09-29 2014-05-07 Abbvie Inc Octahidropirrolo[1,2-a]pirazina sulfonamidas sustituidas como bloqueadores de canales de calcio
WO2013049164A1 (en) * 2011-09-29 2013-04-04 Abbvie Inc. SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS
RU2631319C2 (ru) * 2012-02-22 2017-09-21 Лео Фарма А/С Новые соединения - антагонисты рецептора нейрокинина 1
EP2931727A1 (en) 2012-12-12 2015-10-21 Abbvie Inc. Diazepine derivatives useful as calcium channel blockers in the treatment of pain
RS60679B1 (sr) * 2013-07-25 2020-09-30 Neuren Pharmaceuticals Ltd Neurozaštitna biciklična jedinjenja i postupci za njihovu upotrebu u lečenju poremećaja iz spektra autizma i neurorazvojnih poremećaja
WO2015024203A1 (en) * 2013-08-20 2015-02-26 Leo Pharma A/S Novel neurokinin 1 receptor antagonist compounds ii
IL269390B (en) 2017-03-20 2022-08-01 Broad Inst Inc Preparations and methods for the treatment of parasitic diseases

Family Cites Families (11)

* 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 their preparation and pharmaceutical preparations containing them
JPH11505815A (ja) * 1995-05-23 1999-05-25 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 （２−モルホリニルメチル）ベンズアミン誘導体
KR19990021857A (ko) 1995-05-25 1999-03-25 후지야마 아키라 뉴로키닌 수용체 길항물질로서 1-벤조일-2-(인돌일-3-알킬)-피페라진 유도체
GB9510600D0 (en) 1995-05-25 1995-07-19 Fujisawa Pharmaceutical Co Piperazine derivatives
CA2240835A1 (en) 1995-12-18 1997-06-26 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives as tachykinin antagonists
AUPO735997A0 (en) 1997-06-17 1997-07-10 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
DE59814233D1 (de) 1997-08-27 2008-07-03 Solvay Pharm Gmbh Indolmethyl-N,N'-bisacylpiperazine als Neurokininrezeptorantagonisten
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
AU768652B2 (en) * 1998-12-14 2003-12-18 Astellas Pharma Inc. Piperazine derivatives
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
PL371378A1 (en) 2005-06-13
NO20044775L (no) 2004-12-16
HRP20040273A2 (en) 2005-02-28
EP1495022B1 (en) 2009-07-08
DE60328272D1 (de) 2009-08-20
US7202238B2 (en) 2007-04-10
MXPA04004812A (es) 2004-08-11
RU2310656C2 (ru) 2007-11-20
CN1279041C (zh) 2006-10-11
CA2462708A1 (en) 2003-10-16
RU2004112415A (ru) 2005-03-27
UA77515C2 (en) 2006-12-15
AU2003224162B2 (en) 2008-06-12
EP1495022A1 (en) 2005-01-12
IL160943A0 (en) 2004-08-31
KR20040095361A (ko) 2004-11-12
CN1592747A (zh) 2005-03-09
IL160943A (en) 2008-11-03
AU2003224162A1 (en) 2003-10-20
ZA200404744B (en) 2005-09-21
BR0306148A (pt) 2004-10-19
JP2005525395A (ja) 2005-08-25
HK1070356A1 (en) 2005-06-17
WO2003084955A1 (en) 2003-10-16
US20050119267A1 (en) 2005-06-02
ATE435863T1 (de) 2009-07-15

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