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NO20044775L - Diazabicykloalkanderivater med NK1 antagonistisk aktivitet - Google Patents

Diazabicykloalkanderivater med NK1 antagonistisk aktivitet

Info

Publication number
NO20044775L
NO20044775L NO20044775A NO20044775A NO20044775L NO 20044775 L NO20044775 L NO 20044775L NO 20044775 A NO20044775 A NO 20044775A NO 20044775 A NO20044775 A NO 20044775A NO 20044775 L NO20044775 L NO 20044775L
Authority
NO
Norway
Prior art keywords
morpholin
antagonistic activity
indolyl
halogen
substituted
Prior art date
Application number
NO20044775A
Other languages
English (en)
Inventor
Gustaaf Johan Mar Scharrenburg
Andrew C Mccreary
Jan H Van Maarseveen
Wouter I Iwema Bakker
Hein K A C Coolen
Dirk De Boer
Mayke B Hesselink
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 NO20044775L publication Critical patent/NO20044775L/no

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    • 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
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    • 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
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    • 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
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
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    • 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

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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

Den foreliggende oppfinnelsen vedrører en gruppe unike diazabicykloalkanderivater med intressant neurokinin-NKi reseptorantagonistisk aktivitet representert ved den generelle formelen (1): (1) der: R' står for fenyl, 2-indolyl, 3-indolyl, 3-indazolyl eller benzo[b]tiofen-3-yl, der gruppene kan være substituert med halogen eller alkyl (1-3C), R^ og B? står uavhengig av hverandre for halogen, H, OCH3, CH3 og CF3, R\ R' og R* står uavhengig av hverandre for H, OH, 0-alkyl(l-4C), CH2OH, NH2, dialkyl(l-3C)N, pyrrolidin-1-yl, piperidin-1-yl, morfolin-4-yl eller niorfolin-4-yl substituert med en eller to metyl- eller metoksymetylgmpper, morfolin-4-ylamino, morfolin-4-ylmetyl, imidazolyl-1-yl, tiomorfolin-4-yl, l,l-dioksotiomorfolin-4-yl eller 3-okBa-8-azabicyklo[3.2.I]okt-8-yl; R'* og R^ kan sammen stå for en keto-, en l,3-dioksan-2-yl- eller en l,3-dioksolan-2-yl gruppe, X står for enten O eller S, n har verdien 1,2 eller 3, a er et asymmetriske kaibonatomet 8a, 9a eller 1 Oa når n henholdsvis er lik 1,2 eller 3. Oppfinnelsen vedrører en fremgangsmåte til fiemstilling av de nye forbindelsene og føimasciytiske sairnnensetninger som inneholder minst en av disse forbindelsene som en aktiv ingrediens.
NO20044775A 2002-04-04 2004-11-03 Diazabicykloalkanderivater med NK1 antagonistisk aktivitet NO20044775L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02076405 2002-04-04
PCT/EP2003/050086 WO2003084955A1 (en) 2002-04-04 2003-04-02 Diazabicyclo alkane derivatives with nk1 antagonistic activity

Publications (1)

Publication Number Publication Date
NO20044775L true NO20044775L (no) 2004-12-16

Family

ID=28685940

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20044775A NO20044775L (no) 2002-04-04 2004-11-03 Diazabicykloalkanderivater med NK1 antagonistisk aktivitet

Country Status (20)

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

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
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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
CA2462708A1 (en) 2003-10-16
US7202238B2 (en) 2007-04-10
IL160943A (en) 2008-11-03
AR039192A1 (es) 2005-02-09
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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