EA201400183A1 - Фенил-3-азабицикло[3.1.0]гекс-3-илметаноны и их применение в качестве лекарственного средства - Google Patents

Фенил-3-азабицикло[3.1.0]гекс-3-илметаноны и их применение в качестве лекарственного средства

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Publication number
EA201400183A1
EA201400183A1 EA201400183A EA201400183A EA201400183A1 EA 201400183 A1 EA201400183 A1 EA 201400183A1 EA 201400183 A EA201400183 A EA 201400183A EA 201400183 A EA201400183 A EA 201400183A EA 201400183 A1 EA201400183 A1 EA 201400183A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
application
azabicyclo
hex
phenyl
Prior art date
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EA201400183A
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English (en)
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EA024933B1 (ru
Inventor
Рикардо Джованнини
Барбара Бертани
Марко Феррара
Айан Лингард
Рокко Маццаферро
Хольгер Розенброк
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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Application filed by Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of EA201400183A1 publication Critical patent/EA201400183A1/ru
Publication of EA024933B1 publication Critical patent/EA024933B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P25/18Antipsychotics, 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
    • A61P25/28Drugs 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)

Abstract

В заявке описаны замещенные фенил-3-азабицикло[3,1,0]гекс-3-илметаноны общей формулы (I)в которой R, R, R, R, Rи Rявляются такими, как описано в настоящем изобретении, и их соли, предпочтительно их фармацевтически приемлемые соли. В заявке также описаны получение указанных соединений, фармацевтические композиции, содержащие соединения общей формулы (I), и применение указанных соединений для лечения различных патологических состояний, таких как патологические состояния, связанные с позитивными и негативными симптомами шизофрении, а также нарушений познавательной способности, связанных с шизофренией, болезнью Альцгеймера и другими неврологическими и психическими нарушениями. Соединения, предлагаемые в настоящем изобретении, обладают способностью ингибировать переносчик-1 глицина (GlyT1).
EA201400183A 2011-08-03 2012-08-02 Фенил-3-азабицикло[3.1.0]гекс-3-илметаноны и их применение в качестве лекарственного средства EA024933B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11176468 2011-08-03
PCT/EP2012/065140 WO2013017657A1 (en) 2011-08-03 2012-08-02 Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament

Publications (2)

Publication Number Publication Date
EA201400183A1 true EA201400183A1 (ru) 2014-06-30
EA024933B1 EA024933B1 (ru) 2016-11-30

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US (1) US9012489B2 (ru)
EP (1) EP2739615B1 (ru)
JP (1) JP5850589B2 (ru)
KR (1) KR101944686B1 (ru)
CN (2) CN105837562B (ru)
AP (1) AP2014007399A0 (ru)
AR (1) AR087436A1 (ru)
AU (1) AU2012292036C1 (ru)
BR (1) BR112014001642B1 (ru)
CA (1) CA2843805C (ru)
CL (1) CL2014000246A1 (ru)
CO (1) CO6870037A2 (ru)
CY (1) CY1119326T1 (ru)
DK (1) DK2739615T3 (ru)
EA (1) EA024933B1 (ru)
EC (1) ECSP14013221A (ru)
ES (1) ES2623006T3 (ru)
GE (1) GEP20166483B (ru)
HR (1) HRP20170695T1 (ru)
HU (1) HUE033134T2 (ru)
IL (1) IL229962A (ru)
LT (1) LT2739615T (ru)
MA (1) MA35286B1 (ru)
ME (1) ME02672B (ru)
MX (1) MX347828B (ru)
MY (1) MY167396A (ru)
PE (1) PE20141352A1 (ru)
PH (1) PH12014500276A1 (ru)
PL (1) PL2739615T3 (ru)
PT (1) PT2739615T (ru)
RS (1) RS55927B1 (ru)
SI (1) SI2739615T1 (ru)
TN (1) TN2014000044A1 (ru)
TW (1) TWI543974B (ru)
UA (1) UA114405C2 (ru)
UY (1) UY34239A (ru)
WO (1) WO2013017657A1 (ru)

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AR106679A1 (es) 2015-11-13 2018-02-07 Basf Se Oxadiazoles sustituidos para combatir hongos fitopatógenos
EP3373735A1 (en) 2015-11-13 2018-09-19 Basf Se Substituted oxadiazoles for combating phytopathogenic fungi
EA201891146A1 (ru) 2015-11-19 2018-12-28 Басф Се Замещенные оксадиазолы для борьбы с фитопатогенными грибами
AU2017250397A1 (en) 2016-04-11 2018-10-11 Basf Se Substituted oxadiazoles for combating phytopathogenic fungi
WO2018224455A1 (en) 2017-06-07 2018-12-13 Basf Se Substituted cyclopropyl derivatives
CN113784966B (zh) 2019-05-01 2024-07-19 勃林格殷格翰国际有限公司 Glyt1抑制剂的固体形式
KR20220125326A (ko) 2020-01-09 2022-09-14 디스크 메디슨, 인크. 적혈구형성 프로토포르피린증, x-연계된 프로토포르피린증, 또는 선천성 적혈구 조혈포르피린증을 글리신 운반 억제제로 치료하는 방법
CA3188340A1 (en) * 2020-08-13 2022-02-17 Boehringer Ingelheim International Gmbh Treatment of cognitive impairement associated with schizophrenia
CA3195702A1 (en) 2020-10-13 2022-04-21 Boehringer Ingelheim International Gmbh Process of reworking
MX2024006371A (es) * 2021-11-24 2024-07-15 Maplight Therapeutics Inc Métodos para tratar trastornos neurológicos.
CN114957087A (zh) * 2022-04-13 2022-08-30 湖南复瑞生物医药技术有限责任公司 一种帕罗韦德中间体制备方法
TW202348602A (zh) * 2022-06-10 2023-12-16 大陸商成都百裕製藥股份有限公司 吡咯烷衍生物、藥物组合物及其製藥用途
WO2024042043A1 (en) 2022-08-24 2024-02-29 Boehringer Ingelheim International Gmbh A scalable process for the preparation of a glyt-1 inhibitor
CN121443286A (zh) * 2023-05-25 2026-01-30 地图之光治疗股份有限公司 用于治疗神经障碍的组合物
WO2025140479A1 (zh) * 2023-12-29 2025-07-03 苏州科睿思制药有限公司 Iclepertin的晶型及其制备方法和用途

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MA35286B1 (fr) 2014-07-03
AU2012292036A1 (en) 2014-01-16
AR087436A1 (es) 2014-03-26
EA024933B1 (ru) 2016-11-30
NZ619258A (en) 2015-12-24
JP2014524414A (ja) 2014-09-22
UY34239A (es) 2013-02-28
AU2012292036C1 (en) 2017-03-23
CA2843805C (en) 2021-03-23
CN103797005B (zh) 2016-05-11
KR101944686B1 (ko) 2019-02-01
ECSP14013221A (es) 2014-03-31
JP5850589B2 (ja) 2016-02-03
MX2014001252A (es) 2014-05-13
DK2739615T3 (en) 2017-05-08
LT2739615T (lt) 2017-04-10
MY167396A (en) 2018-08-16
KR20140051922A (ko) 2014-05-02
EP2739615A1 (en) 2014-06-11
AP2014007399A0 (en) 2014-01-31
CL2014000246A1 (es) 2014-08-08
EP2739615B1 (en) 2017-03-15
TWI543974B (zh) 2016-08-01
IL229962A (en) 2016-09-29
US9012489B2 (en) 2015-04-21
CN103797005A (zh) 2014-05-14
WO2013017657A1 (en) 2013-02-07
MX347828B (es) 2017-05-15
PH12014500276A1 (en) 2017-02-01
TN2014000044A1 (en) 2015-07-01
PL2739615T3 (pl) 2017-08-31
CY1119326T1 (el) 2018-02-14
SI2739615T1 (sl) 2017-07-31
CN105837562A (zh) 2016-08-10
CN105837562B (zh) 2020-01-17
PE20141352A1 (es) 2014-10-12
UA114405C2 (uk) 2017-06-12
BR112014001642A2 (pt) 2017-02-14
HRP20170695T1 (hr) 2017-07-28
US20130197011A1 (en) 2013-08-01
PT2739615T (pt) 2017-06-09
AU2012292036B2 (en) 2016-10-06
ES2623006T3 (es) 2017-07-10
BR112014001642B1 (pt) 2022-03-22
CA2843805A1 (en) 2013-02-07
GEP20166483B (en) 2016-05-25
HK1193100A1 (zh) 2014-09-12
RS55927B1 (sr) 2017-09-29
CO6870037A2 (es) 2014-02-20
TW201321364A (zh) 2013-06-01
HUE033134T2 (en) 2017-11-28
ME02672B (me) 2017-06-20

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