EA200701879A1 - Замещённые производные оксадиазаспиро [5.5] ундеканона и их применение в качестве антагонистов нейрокинина - Google Patents

Замещённые производные оксадиазаспиро [5.5] ундеканона и их применение в качестве антагонистов нейрокинина

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Publication number
EA200701879A1
EA200701879A1 EA200701879A EA200701879A EA200701879A1 EA 200701879 A1 EA200701879 A1 EA 200701879A1 EA 200701879 A EA200701879 A EA 200701879A EA 200701879 A EA200701879 A EA 200701879A EA 200701879 A1 EA200701879 A1 EA 200701879A1
Authority
EA
Eurasian Patent Office
Prior art keywords
antagonistic activity
neurokinin
combined
undeacanon
oxadiazaspiro
Prior art date
Application number
EA200701879A
Other languages
English (en)
Other versions
EA012421B1 (ru
Inventor
Франс Эдуард Янссенс
Софи Купа
Алан Филипп Понселе
Брюно Схунтьес
Original Assignee
Янссен Фармацевтика Н. В.
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 Янссен Фармацевтика Н. В. filed Critical Янссен Фармацевтика Н. В.
Publication of EA200701879A1 publication Critical patent/EA200701879A1/ru
Publication of EA012421B1 publication Critical patent/EA012421B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/537—Heterocyclic 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Landscapes

  • 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nanotechnology (AREA)
  • Pulmonology (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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

Данное изобретение касается замещенных производных оксадиазаспиро[5.5]ундеканона, имеющих антагонистическую активность в отношении нейрокинина, в частности NK-антагонистическую активность, NK-антагонистическую активность, объединенную NK/NK-антагонистическую активность и объединенную NK/NK/NK-антагонистическую активность, их получения, композиций, их содержащих, и их применения в качестве лекарственного средства, в частности, для лечения и/или профилактики шизофрении, рвоты, тревожности и депрессии, синдрома раздраженного кишечника (IBS), нарушений циркадного ритма, преэклампсии, ноцицепции, боли, в частности висцеральной и невропатической боли, панкреатита, нейрогенного воспаления, астмы, хронического обструктивного заболевания легких (ХОЗЛ) и расстройств мочеиспускания, таких как недержание мочи. Соединения в соответствии с данным изобретением могут быть представлены общей формулой (I) и включают также их фармацевтически приемлемые кислотно-аддитивные соли или основно-аддитивные соли, их стереохимически изомерные формы, форму N-оксида и пролекарства, где все заместители являются такими, как определено в п.1.
EA200701879A 2005-03-03 2006-03-03 Замещённые производные оксадиазаспиро[5.5]ундеканона и их применение в качестве антагонистов нейрокинина EA012421B1 (ru)

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 (2)

Publication Number Publication Date
EA200701879A1 true EA200701879A1 (ru) 2008-02-28
EA012421B1 EA012421B1 (ru) 2009-10-30

Family

ID=34938877

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200701879A EA012421B1 (ru) 2005-03-03 2006-03-03 Замещённые производные оксадиазаспиро[5.5]ундеканона и их применение в качестве антагонистов нейрокинина

Country Status (15)

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

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US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid 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
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
WO2011095450A1 (en) 2010-02-02 2011-08-11 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
WO2015200594A2 (en) 2014-06-25 2015-12-30 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
US11458129B2 (en) 2017-11-02 2022-10-04 California Institute Of Technology Neurokinin antagonists and uses thereof
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

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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
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
TW382017B (en) 1995-12-27 2000-02-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives
TR200000529T2 (tr) 1997-08-29 2000-08-21 Dsm N.V. İçinde eksipiyan olmayan granüller
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
JP4101053B2 (ja) * 2000-08-10 2008-06-11 田辺三菱製薬株式会社 プロリン誘導体及びその医薬用途
DK1390372T3 (da) * 2001-05-14 2008-09-15 Hoffmann La Roche 1-oxa-3,9-diaza-spiro '5,5]undecan-2-on-derivater og anvendelse deraf som neurokininreceptorantagonist
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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
CA2527856A1 (en) * 2003-06-10 2004-12-23 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
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Also Published As

Publication number Publication date
MX2007010728A (es) 2007-10-12
NZ556629A (en) 2010-04-30
ES2346147T3 (es) 2010-10-11
KR101355064B1 (ko) 2014-01-24
KR20070113224A (ko) 2007-11-28
BRPI0608074A2 (pt) 2009-11-03
EP1874783B1 (en) 2010-05-26
US8138334B2 (en) 2012-03-20
AU2006222061A1 (en) 2006-09-14
WO2006094934A1 (en) 2006-09-14
CN101133064A (zh) 2008-02-27
JP2008531659A (ja) 2008-08-14
US20100292228A1 (en) 2010-11-18
DE602006014531D1 (de) 2010-07-08
CA2598530A1 (en) 2006-09-14
JP5094422B2 (ja) 2012-12-12
EA012421B1 (ru) 2009-10-30
CN101133064B (zh) 2011-02-23
WO2006094934A8 (en) 2006-12-07
AU2006222061B2 (en) 2011-04-28
ATE469159T1 (de) 2010-06-15
CA2598530C (en) 2014-12-16
EP1874783A1 (en) 2008-01-09

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU