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EA201890256A1 - 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 - Google Patents

2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1

Info

Publication number
EA201890256A1
EA201890256A1 EA201890256A EA201890256A EA201890256A1 EA 201890256 A1 EA201890256 A1 EA 201890256A1 EA 201890256 A EA201890256 A EA 201890256A EA 201890256 A EA201890256 A EA 201890256A EA 201890256 A1 EA201890256 A1 EA 201890256A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tetrahydropyridine
fluoromethyl
fluoro
phenyl
amino
Prior art date
Application number
EA201890256A
Other languages
English (en)
Inventor
Карстен Джухл
Лена Тагмоуз
Мауро Мариго
Original Assignee
Х. Лундбекк А/С
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 Х. Лундбекк А/С filed Critical Х. Лундбекк А/С
Publication of EA201890256A1 publication Critical patent/EA201890256A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Настоящее изобретение предусматривает соединения формулы Iдля лечения нейродегенеративных или когнитивных заболеваний. Способ дополнительно включает промежуточные соединения на основе пиперидин-2-она и пиперидин-2-тиона для соединений формулы I.
EA201890256A 2015-08-12 2016-08-10 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 EA201890256A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201500465 2015-08-12
PCT/EP2016/069029 WO2017025559A1 (en) 2015-08-12 2016-08-10 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors

Publications (1)

Publication Number Publication Date
EA201890256A1 true EA201890256A1 (ru) 2018-06-29

Family

ID=56615973

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201890256A EA201890256A1 (ru) 2015-08-12 2016-08-10 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1

Country Status (26)

Country Link
US (2) US20180244645A1 (ru)
EP (1) EP3334720A1 (ru)
JP (1) JP2018531889A (ru)
KR (1) KR20180033524A (ru)
CN (1) CN107849011A (ru)
AR (1) AR105668A1 (ru)
AU (1) AU2016305275A1 (ru)
BR (1) BR112017007472A2 (ru)
CA (1) CA2993630A1 (ru)
CL (1) CL2018000375A1 (ru)
CO (1) CO2018000798A2 (ru)
CR (1) CR20180077A (ru)
DO (1) DOP2018000040A (ru)
EA (1) EA201890256A1 (ru)
EC (1) ECSP18010535A (ru)
HK (1) HK1253372A1 (ru)
IL (1) IL257007A (ru)
MA (1) MA42597A (ru)
MX (1) MX2018001699A (ru)
NI (1) NI201800020A (ru)
PE (1) PE20181015A1 (ru)
PH (1) PH12018500268A1 (ru)
RU (1) RU2018104868A (ru)
TN (1) TN2018000035A1 (ru)
TW (1) TW201718543A (ru)
WO (1) WO2017025559A1 (ru)

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JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3627B1 (ar) 2015-04-30 2020-08-27 H Lundbeck As إيميدازو بيرازينونات على هيئة مثبطات pde1
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
US10912773B2 (en) 2016-10-28 2021-02-09 H. Lundbeck A/S Combinations comprising substituted imidazo[1,5-a]pyrazinones as PDE1 inhibitors
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SMT202100655T1 (it) 2017-12-14 2022-01-10 H Lundbeck As Trattamenti combinati che comprendono la somministrazione di 1h-pirazolo[4,3-b]piridina
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
JP7194738B2 (ja) 2017-12-20 2022-12-22 ハー・ルンドベック・アクチエゼルスカベット ＰＤＥ１阻害剤としてのピラゾロ［３，４－ｂ］ピリジン及びイミダゾ［１，５－ｂ］ピリダジン
KR20210112968A (ko) 2020-03-07 2021-09-15 장성환 양면 인쇄가 가능한 라벨 제조방법
KR20230012296A (ko) 2021-07-15 2023-01-26 장성환 양면 인쇄가 가능한 라벨 제조방법

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MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) * 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療

Also Published As

Publication number Publication date
CL2018000375A1 (es) 2018-07-06
US10011596B2 (en) 2018-07-03
AU2016305275A1 (en) 2018-02-08
US20170044151A1 (en) 2017-02-16
CO2018000798A2 (es) 2018-05-10
EP3334720A1 (en) 2018-06-20
IL257007A (en) 2018-03-29
PH12018500268A1 (en) 2018-08-13
ECSP18010535A (es) 2018-04-30
NI201800020A (es) 2018-06-29
DOP2018000040A (es) 2018-04-30
WO2017025559A1 (en) 2017-02-16
TW201718543A (zh) 2017-06-01
PE20181015A1 (es) 2018-06-26
HK1253372A1 (zh) 2019-06-14
MX2018001699A (es) 2018-05-07
CN107849011A (zh) 2018-03-27
MA42597A (fr) 2018-06-20
US20180244645A1 (en) 2018-08-30
KR20180033524A (ko) 2018-04-03
AR105668A1 (es) 2017-10-25
CR20180077A (es) 2018-04-09
BR112017007472A2 (pt) 2018-01-23
CA2993630A1 (en) 2017-02-16
JP2018531889A (ja) 2018-11-01
TN2018000035A1 (en) 2019-07-08
RU2018104868A (ru) 2019-09-13

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