EA201691447A1 - 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера - Google Patents

2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера

Info

Publication number
EA201691447A1
EA201691447A1 EA201691447A EA201691447A EA201691447A1 EA 201691447 A1 EA201691447 A1 EA 201691447A1 EA 201691447 A EA201691447 A EA 201691447A EA 201691447 A EA201691447 A EA 201691447A EA 201691447 A1 EA201691447 A1 EA 201691447A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alzheimer
disease
treatment
triftor
tetragidropyridines
Prior art date
Application number
EA201691447A
Other languages
English (en)
Other versions
EA031132B1 (ru
Inventor
Карстен Джухл
Мауро Мариго
Лена Тагмозе
Томас Дженсен
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 EA201691447A1 publication Critical patent/EA201691447A1/ru
Publication of EA031132B1 publication Critical patent/EA031132B1/ru

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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

Landscapes

  • 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)

Abstract

Изобретение направлено на новые ингибиторы фермента ВАСЕ1. Отдельные аспекты изобретения направлены на фармацевтические композиции, содержащие указанные соединения, и применения этих соединений для лечения нарушений, на которые уменьшение скоплений Аβ оказывает благоприятное действие, например, болезни Альцгеймера.
EA201691447A 2014-02-19 2015-02-17 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера EA031132B1 (ru)

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 (2)

Publication Number Publication Date
EA201691447A1 true EA201691447A1 (ru) 2016-12-30
EA031132B1 EA031132B1 (ru) 2018-11-30

Family

ID=59009438

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201691447A EA031132B1 (ru) 2014-02-19 2015-02-17 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера

Country Status (25)

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

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA117695C2 (uk) 2014-02-19 2018-09-10 Х. Луннбек А/С 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби 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
AU2016305275A1 (en) * 2015-08-12 2018-02-08 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
WO2017044807A2 (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
TW201726651A (zh) 2015-09-23 2017-08-01 健生藥品公司 2,3,4,5-四氫吡啶-6-胺衍生物
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
PL3532064T3 (pl) 2016-10-28 2020-11-16 H. Lundbeck A/S Terapie skojarzone obejmujące imidazopirazynony do leczenia zaburzeń psychiatrycznych i/lub poznawczych
BR112018013084A2 (pt) 2016-10-28 2018-12-11 H Lundbeck As tratamentos de combinação compreendendo a administração de imidazopirazinonas
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
AU2018346709A1 (en) 2017-10-05 2020-04-16 Fulcrum Therapeutics, Inc. Use of p38 inhibitors to reduce expression of DUX4
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
AU2018385453B2 (en) 2017-12-14 2024-02-08 H. Lundbeck A/S Combination treatments comprising administration of 1H-pyrazolo(4,3-b)pyridines
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
CN117447475A (zh) 2017-12-20 2024-01-26 H.隆德贝克有限公司 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶
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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1395257A1 (en) * 2001-06-12 2004-03-10 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
GB0124928D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
BRPI0307351B8 (pt) * 2002-02-12 2021-05-25 Smithkline Beecham Corp composto, composição farmacêutica, uso de um composto, e, processo para preparar um composto
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
DK2580200T3 (en) 2010-06-09 2017-01-09 Janssen Pharmaceutica Nv 5,6-dihydro-2H- [1,4] oxazin-3-YLAMINDERIVATER THAT COULD BE USED AS INHIBITORS OF BETA-secretase (BACE)
CA2816285A1 (en) * 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
EP2663559B1 (en) 2011-01-12 2015-07-01 Novartis AG Oxazine derivatives and their use in the treatment of neurological disorders
HUE029226T2 (en) 2011-01-13 2017-02-28 Novartis Ag New heterocyclic derivatives and their use in the treatment of neurological diseases
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
MX2013013692A (es) * 2011-06-07 2014-03-05 Siena Biotech Spa Halogenoalquil-1,3-oxazinas como inhibidores de beta secretasa 1 (bace1) y/o beta secretasa 2 (bace2).
UY34278A (es) * 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
US8338413B1 (en) * 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
WO2013142613A1 (en) 2012-03-20 2013-09-26 Elan Pharmaceuticals, Inc. Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
UA117695C2 (uk) 2014-02-19 2018-09-10 Х. Луннбек А/С 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера
TW201623295A (zh) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 具有bace1抑制活性之二氫噻及二氫衍生物

Also Published As

Publication number Publication date
US20170066741A1 (en) 2017-03-09
RU2016133626A3 (ru) 2018-09-25
CL2016002072A1 (es) 2017-01-20
EP3107897A1 (en) 2016-12-28
MX2016010777A (es) 2016-10-26
SG11201606812WA (en) 2016-09-29
TW201609700A (zh) 2016-03-16
UA117695C2 (uk) 2018-09-10
ECSP16072941A (es) 2017-02-24
AP2016009370A0 (en) 2016-08-31
PH12016501600A1 (en) 2017-02-06
MA39225A1 (fr) 2017-04-28
WO2015124576A1 (en) 2015-08-27
PE20161225A1 (es) 2016-12-04
US20150232449A1 (en) 2015-08-20
US9353084B2 (en) 2016-05-31
AU2015220873A1 (en) 2016-08-11
JP6483146B2 (ja) 2019-03-13
CR20160352A (es) 2016-10-20
EA031132B1 (ru) 2018-11-30
IL246875A0 (en) 2016-08-31
CA2940028A1 (en) 2015-08-27
KR20160115936A (ko) 2016-10-06
RU2016133626A (ru) 2018-03-20
CN106029639B (zh) 2019-01-08
GEP20186892B (en) 2018-09-10
JP2017506237A (ja) 2017-03-02
AR099489A1 (es) 2016-07-27
CN106029639A (zh) 2016-10-12
DOP2016000194A (es) 2016-09-30

Similar Documents

Publication Publication Date Title
EA201691447A1 (ru) 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
EA201790817A1 (ru) 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 для лечения болезни альцгеймера
PH12017500841B1 (en) 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
EA201791030A1 (ru) 2-амино-5,5-дифтор-6-(фторметил)-6-фенил-3,4,5,6-тетрагидпропиридины в качестве ингибиторов bace1
EA201790806A1 (ru) Иммунорегулирующие средства
EA201691582A1 (ru) Новые фармацевтические препараты
EA201790764A1 (ru) Новые соединения карбоновых кислот, подходящие для ингибирования микросомальной простагландин-e2-синтазы 1
EA201791874A1 (ru) Фторированные ингибиторы лизилоксидазоподобного фермента-2 и их применение
EA201600589A1 (ru) Ингибиторы диацилглицеринацилтрансферазы 2 для применения в лечении метаболических и связанных с метаболизмом расстройств
EA201791259A1 (ru) Производные пиперидина в качестве ингибиторов hdac1/2
EA201890449A1 (ru) Фумагиллиновые гетероциклические соединения и способы их получения и применения
EA201990400A1 (ru) Соединения и композиции и их применение
MY174747A (en) Bace1 inhibitors
MX2019006863A (es) Inhibidores de heparanasa y uso de los mismos.
EA201790315A1 (ru) Модуляторы x-рецепторов печени
PH12017501668A1 (en) Bace1 inhibitors
MX2016016061A (es) 2,2,2-trifluoroetil-tiadiazinas.

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU