DK2443105T3 - Nyt phenylimidazolderivat som pde10a-enzyminhibitor - Google Patents

Nyt phenylimidazolderivat som pde10a-enzyminhibitor Download PDF

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Publication number
DK2443105T3
DK2443105T3 DK10725373.4T DK10725373T DK2443105T3 DK 2443105 T3 DK2443105 T3 DK 2443105T3 DK 10725373 T DK10725373 T DK 10725373T DK 2443105 T3 DK2443105 T3 DK 2443105T3
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disorder
type
dementia
disease
compound
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DK10725373.4T
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English (en)
Inventor
Morten Langgård
Jacob Nielsen
John Paul Kilburn
Mohamed M Farah
Andreas Ritzen
Jan Kehler
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Lundbeck & Co As H
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Priority claimed from PCT/DK2009/050134 external-priority patent/WO2009152825A1/en
Application filed by Lundbeck & Co As H filed Critical Lundbeck & Co As H
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Publication of DK2443105T3 publication Critical patent/DK2443105T3/da

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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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • 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
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (8)

1. Forbindelse 5,8-Dimethyl-2-[2-(l-methyl-4-phenyl-lH-imidazol-2-yl)-ethyl]-[l,2,4]triazolo[l,5-a]pyrazin
og farmaceutisk acceptable syreadditionssalte deraf.
2. Forbindelse ifølge krav 1 til anvendelse som et lægemiddel.
3. Forbindelse ifølge krav 1 til anvendelse i behandlingen afen neurodegenerativ eller psykisk lidelse, alene eller i kombination med et eller flere neuroleptiske midler valgt fra gruppen bestående afsertindol, olanzapin, risperidon, quetiapin, aripiprazol, haloperidol, clozapin, ziprasidon og osanetant, hvor den neurodegenerative lidelse er valgt fra gruppen bestående af Alzheimers sygdom, multiinfarkt demens, alkoholisk demens eller anden stof-relate ret demens, demens associeret med intrakranielle tumorer eller cerebral trauma, demens associeret med Huntingtons sygdom eller Parkinsons sygdom, eller AIDS; delirium; amnestisk lidelse; post-traumatisk stresssyndrom; mental retardering; et indlæringsproblem, for eksempel ordblindhed, talblind hed, eller en lidelse af skriftlig udtryk; ADHD; og aldersrelateret kognitiv svækkelse, og den psykiske lidelse er valgt fra gruppen bestående af skizofreni, for eksempel af den paranoide, desorganiserede, katatoniske, udifferentierede, eller residuale type; skizofreniform lidelse; skizoaffektiv lidelse, foreksempel af vrangforestillingstypen eller den depressive type; vrangforestillinger; bipolar lidelse, for eksempel bipolar lidelse type 1, bipolar lidelse type 2, og cyklotymi; stoffremkaldt psykotisk lidelse, for eksempel psykose fremkaldt af alkohol, amfetamin, cannabis, kokain, hallucinogener, inhalanter, opioider, eller phencyclidin; personlighedsforstyrrelse af den paranoide type; og personlighedsforstyrrelse af den skizoide type.
4. Anvendelse af forbindelse ifølge krav 1 til fremstillingen af et lægemiddel til behandlingen af en neurodegenerativ eller psykisk lidelse, hvor den neurodegenerative lidelse er valgt fra gruppen bestående af Alzheimers sygdom, multiinfarkt demens, alkoholisk demens eller anden stof-relate ret demens, demens associeret med intrakranielle tumorer eller cerebral trauma, demens associeret med Huntingtons sygdom eller Parkinsons sygdom, eller AIDS-relateret demens; delirium; amnestisk lidelse; post-traumatisk stresssyndrom; mental retardering; et indlæringsproblem, for eksempel ordblindhed, talblindhed, eller en lidelse afskriftlig udtryk; ADHD; og aldersrelateret kognitiv svækkelse, og den psykiske lidelse er valgt fra gruppen bestående af skizofreni, for eksempel af den paranoide, desorganiserede, katatoniske, udifferentierede, eller residuale type; skizofreniform lidelse; skizoaffektiv lidelse, foreksempel af vrangforestillingstypen eller den depressive type; vrangforestillinger; bipolar lidelse, for eksempel bipolar lidelse type 1, bipolar lidelse type 2, og cyklotymi; stoffremkaldt psykotisk lidelse, for eksempel psykose fremkaldt af alkohol, amfetamin, cannabis, kokain, hallucinogener, inhalanter, opioider, eller phencyclidin; personlighedsforstyrrelse af den paranoide type; og personlighedsforstyrrelse af den skizoide type.
5. Farmaceutisk sammensætning omfattende forbindelsen ifølge krav 1, og en eller flere farmaceutisk acceptable bærere, diluenter og excipienser.
6. Anvendelse af forbindelse ifølge krav 1 og endvidere en forbindelse valgt fra gruppen bestående af sertindol, olanzapin, risperidon, quetiapin, aripiprazol, haloperidol, clozapin, ziprasidon og osanetant til fremstillingen af et lægemiddel til behandlingen af en neurodegenerativ eller psykisk lidelse, hvor den neurodegenerative lidelse er valgt fra gruppen bestående af Alzheimers sygdom, multiinfarkt demens, alkoholisk demens eller anden stof-relate ret demens, demens associeret med intrakranielle tumorer eller cerebral trauma, demens associeret med Huntingtons sygdom eller Parkinsons sygdom, eller AIDS-relateret dementia; delirium; amnestisk lidelse; post-traumatisk stresssyndrom; mental retardering; et indlæringsproblem, for eksempel ordblindhed, talblindhed, eller en lidelse afskriftlig udtryk; ADHD; og aldersrelateret kognitiv svækkelse, og den psykiske lidelse er valgt fra gruppen bestående af skizofreni, for eksempel af den paranoide, desorganiserede, katatoniske, udifferentierede, eller residuale type; skizofreniform lidelse; skizoaffektiv lidelse, foreksempel af vrangforestillingstypen eller den depressive type; vrangforestillinger; bipolar lidelse, for eksempel bipolar lidelse type 1, bipolar lidelse type 2, og cyklotymi; stoffremkaldt psykotisk lidelse, for eksempel psykose fremkaldt af alkohol, amfetamin, cannabis, kokain, hallucinogener, inhalanter, opioider, eller phencyclidin; personlighedsforstyrrelse af den paranoide type; og personlighedsforstyrrelse af den skizoide type.
7. Forbindelse ifølge krav 1 og endvidere en forbindelse valgt fra gruppen bestående af sertindol, olanzapin, risperidon, quetiapin, aripiprazol, haloperidol, clozapin, ziprasidon og osanetant som et kombineret præparat for simultan, separat eller sekventiel anvendelse i behandlingen af en neurodegenerativ eller psykisk lidelse, hvor den neurodegenerative lidelse er valgt fra gruppen bestående af Alzheimers sygdom, multiinfarkt demens, alkoholisk demens eller anden stofrelateret demens, demens associeret med intrakranielle tumorer eller cerebral trauma, demens associeret med Huntingtons sygdom eller Parkinsons sygdom, eller AIDS-relateret demens; delirium; amnestisk lidelse; post-traumatisk stresssyndrom; mental retardering; et indlæringsproblem, foreksempel ordblindhed, talblindhed, eller en lidelse afskriftlig udtryk; ADHD; og aldersrelateret kognitiv svækkelse, og den psykiske lidelse er valgt fra gruppen bestående af skizofreni, for eksempel af den paranoide, desorganiserede, katatoniske, udifferentierede, eller residuale type; skizofreniform lidelse; skizoaffektiv lidelse, for eksempel af vrangforestillingstypen eller den depressive type; vrangforestillinger; bipolar lidelse, for eksempel bipolar lidelse type 1, bipolar lidelse type 2, og cyklotymi; stoffremkaldt psykotisk lidelse, for eksempel psykose fremkaldt af alkohol, amfetamin, cannabis, kokain, hallucinogener, inhalanter, opioider, eller phencyclidin; personlighedsforstyrrelse af den paranoide type; og personlighedsforstyrrelse af den skizoide type.
8. Forbindelse ifølge krav 1 til anvendelse i behandlingen af en neurodegenerativ eller psykisk lidelse, hvor den neurodegenerative lidelse er valgt fra gruppen bestående af Alzheimers sygdom, multiinfarkt demens, alkoholisk demens eller anden stof-relateret demens, demens associeret med intrakranielle tumorer eller cerebral trauma, demens associeret med Huntingtons sygdom eller Parkinsons sygdom, eller AIDS-relateret demens; delirium; amnestisk lidelse; posttraumatisk stresssyndrom; mental retardering; et indlæringsproblem, for eksempel ordblindhed, talblindhed, eller en lidelse afskriftlig udtryk; ADHD; og aldersrelateret kognitiv svækkelse, og den psykiske lidelse er valgt fra gruppen bestående af skizofreni, foreksempel af den paranoide, desorganiserede, katatoniske, udifferentierede, eller residuale type; skizofreniform lidelse; skizoaffektiv lidelse, for eksempel af vrangforestillingstypen eller den depressive type; vrangforestillinger; bipolar lidelse, for eksempel bipolar lidelse type 1, bipolar lidelse type 2, og cyklotymi; stoffremkaldt psykotisk lidelse, for eksempel psykose fremkaldt af alkohol, amfetamin, cannabis, kokain, hallucinogener, inhalanter, opioider, eller phencyclidin; personlighedsforstyrrelse af den paranoide type; og personlighedsforstyrrelse af den skizoide type.
DK10725373.4T 2009-06-19 2010-06-17 Nyt phenylimidazolderivat som pde10a-enzyminhibitor DK2443105T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/DK2009/050134 WO2009152825A1 (en) 2008-06-20 2009-06-19 Novel phenylimidazole derivatives as pde10a enzyme inhibitors
PCT/DK2010/050147 WO2010145668A1 (en) 2009-06-19 2010-06-17 Novel phenylimidazole derivative as pde10a enzyme inhibitor

Publications (1)

Publication Number Publication Date
DK2443105T3 true DK2443105T3 (da) 2015-01-12

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DK10725373.4T DK2443105T3 (da) 2009-06-19 2010-06-17 Nyt phenylimidazolderivat som pde10a-enzyminhibitor

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EP (1) EP2443105B1 (da)
JP (1) JP5768044B2 (da)
AR (1) AR077144A1 (da)
AU (1) AU2010262190B2 (da)
CA (1) CA2765750A1 (da)
CR (1) CR20110654A (da)
CY (1) CY1115971T1 (da)
DK (1) DK2443105T3 (da)
DO (1) DOP2011000397A (da)
ES (1) ES2527216T3 (da)
GE (1) GEP20146100B (da)
GT (1) GT201100322A (da)
HR (1) HRP20141222T1 (da)
IL (1) IL216684A (da)
MA (1) MA33367B1 (da)
MX (1) MX2011013400A (da)
MY (1) MY156785A (da)
NZ (1) NZ597203A (da)
PL (1) PL2443105T3 (da)
PT (1) PT2443105E (da)
SG (1) SG176680A1 (da)
SI (1) SI2443105T1 (da)
SM (1) SMT201500003B (da)
TW (1) TW201100430A (da)
UA (2) UA102693C2 (da)
WO (1) WO2010145668A1 (da)
ZA (1) ZA201109271B (da)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8133897B2 (en) 2008-06-20 2012-03-13 H. Lundbeck A/S Phenylimidazole derivatives as PDE10A enzyme inhibitors
TWI501965B (zh) 2008-06-20 2015-10-01 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之新穎苯基咪唑衍生物
TWI485151B (zh) 2009-12-17 2015-05-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族苯基咪唑衍生物
JO3089B1 (ar) * 2010-11-19 2017-03-15 H Lundbeck As مشتقات ايميدازول كمثبطات لانزيمات pde10a
US8552045B2 (en) 2010-11-19 2013-10-08 H. Lundbeck A/S Tricyclic imidazole compounds as PDE10 inhibitors
KR20140009372A (ko) 2011-02-18 2014-01-22 알러간, 인코포레이티드 포스포다이에스테라제 10(pde10a)의 억제제로서의 치환된 6,7-다이알콕시-3-아이소퀴놀리놀 유도체
CN103874701A (zh) * 2011-09-09 2014-06-18 H.隆德贝克有限公司 吡啶化合物和其用途
EP2763989A1 (en) * 2011-09-09 2014-08-13 H. Lundbeck A/S Pyridine compounds and uses thereof
WO2013034755A1 (en) * 2011-09-09 2013-03-14 H. Lundbeck A/S Triazolopyrazine derivatives and their use for treating neurological and psychiatric disorders
WO2013034758A1 (en) * 2011-09-09 2013-03-14 H. Lundbeck A/S Substituted triazolopyrazines and uses thereof
TWI570124B (zh) 2011-12-21 2017-02-11 Ｈ 朗德貝克公司 作為ｐｄｅ１０ａ酵素抑制劑的喹啉衍生物
WO2013107856A1 (en) * 2012-01-20 2013-07-25 H. Lundbeck A/S Imidazole derivatives as pde10a enzyme inhibitors
WO2013127817A1 (en) 2012-02-27 2013-09-06 H. Lundbeck A/S Imidazole derivatives as pde10a enzyme inhibitors
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
BR112020013743A2 (pt) * 2018-11-06 2020-12-01 H. Lundbeck A/S hemiadipato de 5,8-dimetil-2-[2-(1-metil-4-fenil-1h-imidazol-2-il)-etil]-[1,2,4]triazolo[1,5-a]pirazina
WO2020094592A1 (en) * 2018-11-06 2020-05-14 H. Lundbeck A/S Compounds for treating negative symptoms and cognitive impairments

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CR20110654A (es) 2012-03-09
JP2012530086A (ja) 2012-11-29
DOP2011000397A (es) 2012-07-15
CA2765750A1 (en) 2010-12-23
WO2010145668A1 (en) 2010-12-23
JP5768044B2 (ja) 2015-08-26
GT201100322A (es) 2014-02-06
EP2443105A1 (en) 2012-04-25
TW201100430A (en) 2011-01-01
AU2010262190A1 (en) 2012-01-19
IL216684A (en) 2016-03-31
MX2011013400A (es) 2012-02-21
ZA201109271B (en) 2013-02-27
PL2443105T3 (pl) 2015-03-31
SI2443105T1 (sl) 2015-02-27
SMT201500003B (it) 2015-03-05
NZ597203A (en) 2013-03-28
MY156785A (en) 2016-03-31
UA106378C2 (ru) 2014-08-26
CY1115971T1 (el) 2017-01-25
AR077144A1 (es) 2011-08-03
ES2527216T3 (es) 2015-01-21
IL216684A0 (en) 2012-02-29
UA102693C2 (ru) 2013-08-12
PT2443105E (pt) 2015-01-14
EP2443105B1 (en) 2014-10-29
AU2010262190B2 (en) 2013-01-31
HRP20141222T1 (hr) 2015-02-27
SG176680A1 (en) 2012-01-30
MA33367B1 (fr) 2012-06-01
GEP20146100B (en) 2014-05-27

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