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BR0111538A - Derivados de 1,3,8-triaza-espiro 4,5!decan-4-ona como antogonistas de receptor de neurocinina - Google Patents

Derivados de 1,3,8-triaza-espiro 4,5!decan-4-ona como antogonistas de receptor de neurocinina

Info

Publication number
BR0111538A
BR0111538A BR0111538-3A BR0111538A BR0111538A BR 0111538 A BR0111538 A BR 0111538A BR 0111538 A BR0111538 A BR 0111538A BR 0111538 A BR0111538 A BR 0111538A
Authority
BR
Brazil
Prior art keywords
lower alkyl
hydrogen
halogen
phenyl
triaza
Prior art date
Application number
BR0111538-3A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR0111538A publication Critical patent/BR0111538A/pt

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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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D487/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P25/24—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P27/02—Ophthalmic agents
    • 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
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    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"DERIVADOS DE 1,3,8-TRIAZA-ESPIRO'4,5!DECAN-4-ONA COMO ANTAGONISTAS DE RECEPTOR DE NEUROCININA". A invenção refere-se a compostos da fórmula (I) em que R^ 1^ é hidrogênio, alquila inferior, alquenila inferior, fenila ou os seguintes grupos -(CH~ 2~)~ m~,-heterocíclicos não aromáticos, que estão opcionalmente substituídos por alquila inferior, ou é -(CH~ 2~)~ m~-heteroarila, que está opcionalmente substituída por um ou dois substituintes selecionados do grupo que consiste de alquila inferior, alcóxi inferior, halogênio, CF~ 3~, benzila ou ciano, ou é -(CH~ 2~)~ m~-C(O)-NRR', -(CH~ 2~)~ m~-C(O)-alquila inferior, -(CH~ 2~)~ m~-C(O)-O-alquila inferior, -(CH~ 2~)~ m~-O-alquila inferior, -(CH~ 2~)~ m~-CH[C(O)-O-alquila inforior]~ 2~, -(CH~ 2~)~ m~-CH(OH)-CH~ 2~-O-fenila, -(CH~ 2~)~ m~-CH(CF~ 3~)OH, -(CH~ 2~)~ m~-OH, -(CH~ 2~)~ m~-CN, -(CH~ 2~)~ m~-NRR', -(CH~ 2~)~ m~-cicloalquila ou -(CH~ 2~)~ m~-CHF~ 2~; R^ 2^ é hidrogênio, alquila inferior, halogênio ou alcóxi inferior; R^ 3^ é alquila inferior, alcóxi inferior, halogênio ou CF~ 3~ R,R' são iguais ou diferentes e são hidrogênio ou alquila inferior; x é >N-, >C= ou >CH-; X^ 1^/X^ 2^ são independentemente entre si hidrogênio, hidróxi ou alcóxi inferior ou podem ser juntos um grupo oxo; Y^ 1^/Y^ 2^ são independentemente entre si hidrogênio, alquila inferior, -(CH~ 2~)~ m~-fenila ou podem ser juntos um grupo oxo; Z é uma ligação, -CH~ 2~- ou -C(O)-; m é 0, 1, 2, 3 ou 4; n é 2 ou 3; n^ 1^ é 0, 1 ou 2; e a seus sais de adição ácidos farmaceuticamente aceitáveis. Os compostos descritos têm uma boa afinidade para o receptor de NK1.
BR0111538-3A 2000-06-08 2001-06-01 Derivados de 1,3,8-triaza-espiro 4,5!decan-4-ona como antogonistas de receptor de neurocinina BR0111538A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00112285 2000-06-08
PCT/EP2001/006305 WO2001094346A1 (en) 2000-06-08 2001-06-01 1,3,8-TRIAZA-SPIRO'4,5!DECAN-4-ONE DERIVATIVES AS NEUROKININ RECEPTOR ANTAGONISTS

Publications (1)

Publication Number Publication Date
BR0111538A true BR0111538A (pt) 2003-07-01

Family

ID=8168940

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0111538-3A BR0111538A (pt) 2000-06-08 2001-06-01 Derivados de 1,3,8-triaza-espiro 4,5!decan-4-ona como antogonistas de receptor de neurocinina

Country Status (17)

Country Link
US (1) US6482829B2 (pt)
EP (1) EP1292596B1 (pt)
JP (1) JP4245348B2 (pt)
KR (1) KR100518198B1 (pt)
CN (1) CN1261433C (pt)
AR (1) AR028683A1 (pt)
AT (1) ATE381565T1 (pt)
AU (2) AU2001267513B2 (pt)
BR (1) BR0111538A (pt)
CA (1) CA2411716C (pt)
DE (1) DE60131971T2 (pt)
ES (1) ES2296761T3 (pt)
MX (1) MXPA02012001A (pt)
PE (1) PE20020298A1 (pt)
UY (1) UY26754A1 (pt)
WO (1) WO2001094346A1 (pt)
ZA (1) ZA200209488B (pt)

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Also Published As

Publication number Publication date
ZA200209488B (en) 2004-02-23
MXPA02012001A (es) 2003-04-22
EP1292596A1 (en) 2003-03-19
DE60131971D1 (de) 2008-01-31
CA2411716C (en) 2010-06-22
DE60131971T2 (de) 2008-12-04
AR028683A1 (es) 2003-05-21
CA2411716A1 (en) 2001-12-13
WO2001094346A1 (en) 2001-12-13
CN1261433C (zh) 2006-06-28
AU2001267513B2 (en) 2006-03-16
JP2003535863A (ja) 2003-12-02
CN1436188A (zh) 2003-08-13
ES2296761T3 (es) 2008-05-01
UY26754A1 (es) 2001-12-28
PE20020298A1 (es) 2002-04-17
ATE381565T1 (de) 2008-01-15
JP4245348B2 (ja) 2009-03-25
AU6751301A (en) 2001-12-17
KR20030016283A (ko) 2003-02-26
KR100518198B1 (ko) 2005-10-04
US6482829B2 (en) 2002-11-19
US20020006932A1 (en) 2002-01-17
EP1292596B1 (en) 2007-12-19

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