BRPI0608074A2 - derivados de oxa-diaza-espiro-[5.5]-undecanona substituìdos e uso como antagonistas da neurocinina do mesmo - Google Patents

derivados de oxa-diaza-espiro-[5.5]-undecanona substituìdos e uso como antagonistas da neurocinina do mesmo

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Publication number
BRPI0608074A2
BRPI0608074A2 BRPI0608074-0A BRPI0608074A BRPI0608074A2 BR PI0608074 A2 BRPI0608074 A2 BR PI0608074A2 BR PI0608074 A BRPI0608074 A BR PI0608074A BR PI0608074 A2 BRPI0608074 A2 BR PI0608074A2
Authority
BR
Brazil
Prior art keywords
antagonistic activity
diaza
spiro
combined
substituted oxa
Prior art date
Application number
BRPI0608074-0A
Other languages
English (en)
Inventor
Sophie Coupa
Alain Philippe Poncelet
Bruno Schoent Jes
Frans Eduard Janssens
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 BRPI0608074A2 publication Critical patent/BRPI0608074A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nanotechnology (AREA)
  • Pulmonology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Molecular Biology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

DERIVADOS DE OXA-DIAZA-ESPIRO-[5.5]-UNDECANONA SUBSTITUIDOS E USO COMO ANTAGONISTAS DA NEUROCININA DO MESMO. A presente invenção refere-se a derivados de oxa-diaza-espiro[5.5]-undecanona substituidos tendo atividade antagonista de neurocinina, em particular uma atividade antagonista de NK~ 1~, uma atividade antagonista de NK~ 3~, uma atividade antagonista de NK~ 1~/NK~ 2~ combinada e uma atividade antagonista de NK~ 1~/NK~ 2~/NK~ 3~ combinada, sua preparação, composições compreendendo os mesmos e seu uso como um medicamento, em particular para o tratamento e/ou profilaxia de esquizofrenia, êmese, ansiedade e depressão, síndrome do intestino irritável (IBS), distúrbios do ritmo circadiano, pré-eclãmpsia, nonicepçáo, dor, em particular dor visceral e neuropática, pancreatite, inflamação neurogênica, asma, doença pulmonar obstrutiva crónica (COPD) e distúrbios da micção tais como incontinência urinária. Os compostos de acordo com a invenção podem ser representados pela Fórmula geral (1) e compreendem os sais de adição de ácido ou base farmaceuticamente aceitáveis dos mesmos, as formas estereoquimicamente isoméricas dos mesmos, a forma N-óxido dos mesmos e pró-fármacos dos mesmos, em que todos os substituintes são definidos como na reivindicação 1.
BRPI0608074-0A 2005-03-03 2006-03-03 derivados de oxa-diaza-espiro-[5.5]-undecanona substituìdos e uso como antagonistas da neurocinina do mesmo BRPI0608074A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05101657 2005-03-03
PCT/EP2006/060419 WO2006094934A1 (en) 2005-03-03 2006-03-03 Substituted oxa-diaza-spiro-[5.5]-undecanone derivatives and their use as neurokinin antagonists

Publications (1)

Publication Number Publication Date
BRPI0608074A2 true BRPI0608074A2 (pt) 2009-11-03

Family

ID=34938877

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0608074-0A BRPI0608074A2 (pt) 2005-03-03 2006-03-03 derivados de oxa-diaza-espiro-[5.5]-undecanona substituìdos e uso como antagonistas da neurocinina do mesmo

Country Status (15)

Country Link
US (1) US8138334B2 (pt)
EP (1) EP1874783B1 (pt)
JP (1) JP5094422B2 (pt)
KR (1) KR101355064B1 (pt)
CN (1) CN101133064B (pt)
AT (1) ATE469159T1 (pt)
AU (1) AU2006222061B2 (pt)
BR (1) BRPI0608074A2 (pt)
CA (1) CA2598530C (pt)
DE (1) DE602006014531D1 (pt)
EA (1) EA012421B1 (pt)
ES (1) ES2346147T3 (pt)
MX (1) MX2007010728A (pt)
NZ (1) NZ556629A (pt)
WO (1) WO2006094934A1 (pt)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー CRF−1受容体アンタゴニストとしてのピラゾロ[5,1b]オキサゾール誘導体
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
US10314835B2 (en) 2014-06-25 2019-06-11 Emory University Methods of managing conditioned fear with neurokinin receptor antagonists
KR101579688B1 (ko) 2014-07-08 2015-12-24 재단법인 전남생물산업진흥원 좁쌀풀 추출물을 유효성분으로 함유하는 과민성 대장증후군에 의한 내장 통증 억제예방 또는 치료용 약학 조성물
EP3704271A4 (en) 2017-11-02 2021-09-08 California Institute of Technology NEUROKININ ANTAGONISTS AND RELATED USES
WO2020048827A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 1, 3, 9-triazaspiro[5.5] undecan-2-one compounds
WO2020048828A1 (en) 2018-09-03 2020-03-12 Bayer Pharma Aktiengesellschaft 5-heteroaryl-3,9-diazaspiro[5.5]undecane compounds
WO2020048826A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds

Family Cites Families (13)

* Cited by examiner, † Cited by third party
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US5403593A (en) 1991-03-04 1995-04-04 Sandoz Ltd. Melt granulated compositions for preparing sustained release dosage forms
GB9109862D0 (en) 1991-05-08 1991-07-03 Beecham Lab Sa Pharmaceutical formulations
TW382017B (en) 1995-12-27 2000-02-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives
TW531537B (en) * 1995-12-27 2003-05-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-substituted piperidine derivatives
TW429256B (en) 1995-12-27 2001-04-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-(benzimidazolyl- and imidazopyridinyl)-piperidine derivatives
AU9540898A (en) 1997-08-29 1999-03-22 Dsm N.V. Granules free of excipients
US6482829B2 (en) * 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
ATE450504T1 (de) 2000-08-10 2009-12-15 Mitsubishi Tanabe Pharma Corp Prolinderivative und deren verwendung als medikamente
CA2447329C (en) * 2001-05-14 2009-07-28 F.Hoffmann-La Roche Ag 1-oxa-3,9-diaza-spiro[5,5]undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor
NZ571695A (en) 2001-12-28 2010-02-26 Acadia Pharm Inc Spiroazacyclic compounds as monoamine receptor for modulating 5-HT2A receptor-mediated events
MY141736A (en) * 2002-10-08 2010-06-15 Elanco Animal Health Ireland Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists
EP1635811A2 (en) * 2003-06-10 2006-03-22 Janssen Pharmaceutica N.V. Substituted 1, 4-di-piperidin-4-yl-piperazine derivative combined with an opioid analgesic and their use for the treatment of pain and side-effects associated with opioid-based treatments
KR100863854B1 (ko) * 2004-02-10 2008-10-15 에프. 호프만-라 로슈 아게 케모카인 ccr5 수용체 조절제

Also Published As

Publication number Publication date
US20100292228A1 (en) 2010-11-18
EA012421B1 (ru) 2009-10-30
ES2346147T3 (es) 2010-10-11
CN101133064A (zh) 2008-02-27
WO2006094934A8 (en) 2006-12-07
CN101133064B (zh) 2011-02-23
WO2006094934A1 (en) 2006-09-14
EP1874783A1 (en) 2008-01-09
ATE469159T1 (de) 2010-06-15
US8138334B2 (en) 2012-03-20
MX2007010728A (es) 2007-10-12
AU2006222061A1 (en) 2006-09-14
CA2598530A1 (en) 2006-09-14
JP2008531659A (ja) 2008-08-14
NZ556629A (en) 2010-04-30
DE602006014531D1 (de) 2010-07-08
EP1874783B1 (en) 2010-05-26
JP5094422B2 (ja) 2012-12-12
CA2598530C (en) 2014-12-16
AU2006222061B2 (en) 2011-04-28
KR20070113224A (ko) 2007-11-28
KR101355064B1 (ko) 2014-01-24
EA200701879A1 (ru) 2008-02-28

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 11A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]