UA117695C2 - 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера - Google Patents

2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера Download PDF

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Publication number
UA117695C2
UA117695C2 UAA201608414A UAA201608414A UA117695C2 UA 117695 C2 UA117695 C2 UA 117695C2 UA A201608414 A UAA201608414 A UA A201608414A UA A201608414 A UAA201608414 A UA A201608414A UA 117695 C2 UA117695 C2 UA 117695C2
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Ukraine
Prior art keywords
trifluoro
fluorophenyl
amino
dimethyl
tetrahydropyridin
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UAA201608414A
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English (en)
Ukrainian (uk)
Inventor
Карстен Юхль
Мауро Маріґо
Лєна Таґмос
Томас Єнсен
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Х. Луннбек А/С
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Publication of UA117695C2 publication Critical patent/UA117695C2/uk

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    • 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
    • C07D401/12Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic 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
    • C07D211/72Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D227/00Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
    • C07D227/02Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D227/06Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D227/10Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12Heterocyclic 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
    • 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
    • C07D417/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
UAA201608414A 2014-02-19 2015-02-17 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера UA117695C2 (uk)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201400086 2014-02-19
DKPA201400349 2014-07-01
PCT/EP2015/053327 WO2015124576A1 (en) 2014-02-19 2015-02-17 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Publications (1)

Publication Number Publication Date
UA117695C2 true UA117695C2 (uk) 2018-09-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201608414A UA117695C2 (uk) 2014-02-19 2015-02-17 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера

Country Status (25)

Country Link
US (2) US20170066741A1 (OSRAM)
EP (1) EP3107897A1 (OSRAM)
JP (1) JP6483146B2 (OSRAM)
KR (1) KR20160115936A (OSRAM)
CN (1) CN106029639B (OSRAM)
AP (1) AP2016009370A0 (OSRAM)
AR (1) AR099489A1 (OSRAM)
AU (1) AU2015220873A1 (OSRAM)
CA (1) CA2940028A1 (OSRAM)
CL (1) CL2016002072A1 (OSRAM)
CR (1) CR20160352A (OSRAM)
DO (1) DOP2016000194A (OSRAM)
EA (1) EA031132B1 (OSRAM)
EC (1) ECSP16072941A (OSRAM)
GE (1) GEP20186892B (OSRAM)
IL (1) IL246875A0 (OSRAM)
MA (1) MA39225A1 (OSRAM)
MX (1) MX2016010777A (OSRAM)
PE (1) PE20161225A1 (OSRAM)
PH (1) PH12016501600A1 (OSRAM)
RU (1) RU2016133626A (OSRAM)
SG (1) SG11201606812WA (OSRAM)
TW (1) TW201609700A (OSRAM)
UA (1) UA117695C2 (OSRAM)
WO (1) WO2015124576A1 (OSRAM)

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EA031132B1 (ru) 2014-02-19 2018-11-30 Х. Лундбекк А/С 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
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
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
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
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CA2997947A1 (en) 2015-09-09 2017-03-16 The Trustees Of Columbia University In The City Of New York Reduction of er-mam-localized app-c99 and methods of treating alzheimer's disease
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BR112018013084A2 (pt) 2016-10-28 2018-12-11 H Lundbeck As tratamentos de combinação compreendendo a administração de imidazopirazinonas
HUE050403T2 (hu) 2016-10-28 2020-12-28 H Lundbeck As Imidazopirazinonokkal végzett kombinációs kezelések pszichiátriai és/vagy kognitív betegségek kezelésére
BR112018017058A2 (pt) 2016-12-21 2019-07-02 H Lundbeck As 6-amino-5-fluoro-5-(fluorometil)-2,3,4,5-tetra-hidropiridin-2-il-fenil-5-(metóxi-d3)-pirazina-2-carboxamidas e derivados fluorados do mesmo como inibidores de bace1
PT3691620T (pt) 2017-10-05 2022-10-06 Fulcrum Therapeutics Inc Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CN111465410B (zh) 2017-12-14 2022-10-25 H.隆德贝克有限公司 包括施用1h-吡唑并[4,3-b]吡啶的组合治疗
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
KR102507861B1 (ko) 2018-04-19 2023-03-09 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법
KR102510077B1 (ko) 2018-04-24 2023-03-14 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법
US12042492B2 (en) 2020-10-09 2024-07-23 Texas Tech University System BACE1 inhibitory ligand molecules against amyloid beta-induced synaptic and mitochondrial toxicities

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Publication number Publication date
CL2016002072A1 (es) 2017-01-20
JP2017506237A (ja) 2017-03-02
TW201609700A (zh) 2016-03-16
PH12016501600A1 (en) 2017-02-06
CN106029639A (zh) 2016-10-12
US20170066741A1 (en) 2017-03-09
PE20161225A1 (es) 2016-12-04
JP6483146B2 (ja) 2019-03-13
EA031132B1 (ru) 2018-11-30
MX2016010777A (es) 2016-10-26
ECSP16072941A (es) 2017-02-24
KR20160115936A (ko) 2016-10-06
CR20160352A (es) 2016-10-20
AU2015220873A1 (en) 2016-08-11
SG11201606812WA (en) 2016-09-29
CN106029639B (zh) 2019-01-08
RU2016133626A (ru) 2018-03-20
MA39225A1 (fr) 2017-04-28
EP3107897A1 (en) 2016-12-28
US20150232449A1 (en) 2015-08-20
EA201691447A1 (ru) 2016-12-30
DOP2016000194A (es) 2016-09-30
IL246875A0 (en) 2016-08-31
AP2016009370A0 (en) 2016-08-31
CA2940028A1 (en) 2015-08-27
WO2015124576A1 (en) 2015-08-27
RU2016133626A3 (OSRAM) 2018-09-25
US9353084B2 (en) 2016-05-31
AR099489A1 (es) 2016-07-27
GEP20186892B (en) 2018-09-10

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