EA201290516A1 - Гетероароматические производные соединения фенилимидазола в качестве ингибиторов фермента pde10a - Google Patents

Гетероароматические производные соединения фенилимидазола в качестве ингибиторов фермента pde10a

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Publication number
EA201290516A1
EA201290516A1 EA201290516A EA201290516A EA201290516A1 EA 201290516 A1 EA201290516 A1 EA 201290516A1 EA 201290516 A EA201290516 A EA 201290516A EA 201290516 A EA201290516 A EA 201290516A EA 201290516 A1 EA201290516 A1 EA 201290516A1
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formula
effective amount
therapeutically effective
provides
patient
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EA201290516A
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English (en)
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EA023663B1 (ru
Inventor
Аск Пюшль
Якоб Нильсен
Ян Келер
Джон Пол Килберн
Мауро Мариго
Мортен Ланггор
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Х. Лундбекк А/С
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Publication of EA201290516A1 publication Critical patent/EA201290516A1/ru
Publication of EA023663B1 publication Critical patent/EA023663B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Valve Device For Special Equipments (AREA)

Abstract

Изобретение касается соединений, которые являются ингибиторами фермента PDE10A. В изобретении предлагается фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по настоящему изобретению и фармацевтически приемлемый носитель. В изобретении предлагается также способ получения соединений формулы I. Кроме того, в изобретении предлагается способ лечения пациента, страдающего от нейродегенеративного расстройства, который включает введение указанному пациенту терапевтически эффективного количества соединения формулы I. В изобретении предлагается также способ лечения пациента, страдающего от привыкания к чрезмерному употреблению лекарственных средств, который включает введение указанному пациенту терапевтически эффективного количества соединения формулы I. Кроме того, в изобретении предлагается способ лечения пациента, страдающего от психического расстройства, который включает введение указанному пациенту терапевтически эффективного количества соединения формулы I.
EA201290516A 2009-12-17 2010-12-15 Гетероароматические производные фенилимидазола в качестве ингибиторов фермента pde10a EA023663B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA200901339 2009-12-17
PCT/DK2010/050341 WO2011072694A1 (en) 2009-12-17 2010-12-15 Heteroaromatic phenylimidazole derivatives as pde10a enzyme inhibitors

Publications (2)

Publication Number Publication Date
EA201290516A1 true EA201290516A1 (ru) 2013-01-30
EA023663B1 EA023663B1 (ru) 2016-06-30

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EA201290516A EA023663B1 (ru) 2009-12-17 2010-12-15 Гетероароматические производные фенилимидазола в качестве ингибиторов фермента pde10a

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US (2) US9096589B2 (ru)
EP (1) EP2513107B1 (ru)
JP (1) JP5901535B2 (ru)
KR (1) KR101803984B1 (ru)
CN (1) CN102741250B (ru)
AR (1) AR079495A1 (ru)
AU (1) AU2010333435B2 (ru)
BR (1) BR112012017205A2 (ru)
CA (1) CA2783726A1 (ru)
CO (1) CO6612245A2 (ru)
CR (1) CR20120319A (ru)
CY (1) CY1115843T1 (ru)
DK (1) DK2513107T3 (ru)
DO (1) DOP2012000165A (ru)
EA (1) EA023663B1 (ru)
ES (1) ES2514647T3 (ru)
GE (1) GEP20156241B (ru)
GT (1) GT201200171A (ru)
HK (1) HK1177208A1 (ru)
HR (1) HRP20140898T1 (ru)
IL (1) IL220327A (ru)
MA (1) MA33922B1 (ru)
MX (1) MX2012006969A (ru)
MY (1) MY158197A (ru)
NZ (1) NZ600260A (ru)
PL (1) PL2513107T3 (ru)
PT (1) PT2513107E (ru)
RS (1) RS53579B1 (ru)
SG (1) SG181674A1 (ru)
SI (1) SI2513107T1 (ru)
SM (1) SMT201400158B (ru)
TN (1) TN2012000271A1 (ru)
TW (1) TWI485151B (ru)
UA (1) UA108487C2 (ru)
WO (1) WO2011072694A1 (ru)
ZA (1) ZA201204419B (ru)

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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
TWI487705B (zh) 2009-12-17 2015-06-11 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族芳基三唑衍生物
TWI481607B (zh) 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
WO2011150156A2 (en) * 2010-05-26 2011-12-01 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
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
WO2012096929A2 (en) 2011-01-11 2012-07-19 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
WO2012112946A1 (en) 2011-02-18 2012-08-23 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9938269B2 (en) * 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
AU2012311713A1 (en) * 2011-09-19 2014-03-13 F. Hoffmann-La Roche Ag Triazolopyridine compounds as PDE10A inhibitors
WO2013050527A1 (en) 2011-10-05 2013-04-11 H. Lundbeck A/S Quinazoline derivatives as pde10a enzyme inhibitors
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WO2013192273A1 (en) * 2012-06-19 2013-12-27 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9790203B2 (en) * 2012-11-26 2017-10-17 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)

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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
TWI487705B (zh) 2009-12-17 2015-06-11 Lundbeck & Co As H 作為pde10a酵素抑制劑之雜芳香族芳基三唑衍生物
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
TW201200516A (en) 2009-12-17 2012-01-01 Lundbeck & Co As H Phenylimidazole derivatives comprising an ethynylene linker as PDE10A enzyme inhibitors

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Publication number Publication date
HK1177208A1 (en) 2013-08-16
TN2012000271A1 (en) 2013-12-12
EP2513107A1 (en) 2012-10-24
HRP20140898T1 (hr) 2014-11-07
KR101803984B1 (ko) 2017-12-01
PL2513107T3 (pl) 2014-12-31
IL220327A0 (en) 2012-08-30
SMT201400158B (it) 2015-01-15
TWI485151B (zh) 2015-05-21
US20120309714A1 (en) 2012-12-06
AU2010333435A1 (en) 2012-06-21
GT201200171A (es) 2015-01-16
JP2013514284A (ja) 2013-04-25
IL220327A (en) 2014-12-31
KR20120112460A (ko) 2012-10-11
MX2012006969A (es) 2012-07-17
CA2783726A1 (en) 2011-06-23
US9669029B2 (en) 2017-06-06
GEP20156241B (en) 2015-02-10
CY1115843T1 (el) 2017-01-25
CN102741250A (zh) 2012-10-17
DOP2012000165A (es) 2012-12-15
MA33922B1 (fr) 2013-01-02
PT2513107E (pt) 2014-10-22
EP2513107B1 (en) 2014-07-30
ES2514647T3 (es) 2014-10-28
DK2513107T3 (da) 2014-10-13
SG181674A1 (en) 2012-07-30
SI2513107T1 (sl) 2014-11-28
CN102741250B (zh) 2015-10-14
UA108487C2 (en) 2015-05-12
WO2011072694A1 (en) 2011-06-23
CR20120319A (es) 2012-08-16
EA023663B1 (ru) 2016-06-30
TW201200515A (en) 2012-01-01
MY158197A (en) 2016-09-15
RS53579B1 (en) 2015-02-27
AU2010333435B2 (en) 2016-09-08
AR079495A1 (es) 2012-02-01
US9096589B2 (en) 2015-08-04
NZ600260A (en) 2014-08-29
JP5901535B2 (ja) 2016-04-13
US20150290191A1 (en) 2015-10-15
ZA201204419B (en) 2013-08-28
CO6612245A2 (es) 2013-02-01
BR112012017205A2 (pt) 2018-08-14

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