EA201890769A1 - Производные 2,3,4,5-тетрагидропиридин-6-амина - Google Patents

Производные 2,3,4,5-тетрагидропиридин-6-амина

Info

Publication number
EA201890769A1
EA201890769A1 EA201890769A EA201890769A EA201890769A1 EA 201890769 A1 EA201890769 A1 EA 201890769A1 EA 201890769 A EA201890769 A EA 201890769A EA 201890769 A EA201890769 A EA 201890769A EA 201890769 A1 EA201890769 A1 EA 201890769A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
dementia
beta
tetrahydropyridin
disease
Prior art date
Application number
EA201890769A
Other languages
English (en)
Other versions
EA035026B1 (ru
Inventor
Фредерик Ян Рита Ромбаутс
Хенрикус Якобус Мария Гейсен
Свен Францискус Анна Ван Брандт
Андрес Авелино Трабанко-Суарес
Original Assignee
Янссен Фармацевтика Н.В.
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 Янссен Фармацевтика Н.В. filed Critical Янссен Фармацевтика Н.В.
Publication of EA201890769A1 publication Critical patent/EA201890769A1/ru
Publication of EA035026B1 publication Critical patent/EA035026B1/ru

Links

Classifications

    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • 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

Landscapes

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

Abstract

Настоящее изобретение относится к ингибиторам бета-секретазы, представляющим собой соединения 2,3,4,5-тетрагидропиридин-6-амина, имеющие структуру, представленную в формуле (I)где радикалы определены в описании изобретения. Настоящее изобретение также направлено на фармацевтические композиции, содержащие такие соединения, на способы получения таких соединений и композиций и на применение таких соединений и композиций для предупреждения и лечения расстройств, в которые вовлечена бета-секретаза, таких как болезнь Альцгеймера (AD), умеренное когнитивное нарушение, угасание, деменция, деменция с тельцами Леви, синдром Дауна, деменция, ассоциированная с инсультом, деменция, ассоциированная с болезнью Паркинсона, или деменция, ассоциированная с бета-амилоидом.
EA201890769A 2015-09-23 2016-09-23 Производные 2,3,4,5-тетрагидропиридин-6-амина EA035026B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15186394 2015-09-23
EP16172005 2016-05-30
PCT/EP2016/072710 WO2017050978A1 (en) 2015-09-23 2016-09-23 2,3,4,5-tetrahydropyridin-6-amine derivatives

Publications (2)

Publication Number Publication Date
EA201890769A1 true EA201890769A1 (ru) 2018-09-28
EA035026B1 EA035026B1 (ru) 2020-04-20

Family

ID=56985626

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201890769A EA035026B1 (ru) 2015-09-23 2016-09-23 Производные 2,3,4,5-тетрагидропиридин-6-амина

Country Status (14)

Country Link
US (1) US20180334447A1 (ru)
EP (1) EP3353163B1 (ru)
JP (1) JP2018527387A (ru)
KR (1) KR20180053357A (ru)
CN (1) CN108026069A (ru)
AU (1) AU2016328589A1 (ru)
BR (1) BR112018005591A2 (ru)
CA (1) CA2995161A1 (ru)
EA (1) EA035026B1 (ru)
HK (1) HK1254800A1 (ru)
IL (1) IL258217A (ru)
MX (1) MX2018003565A (ru)
TW (1) TW201726651A (ru)
WO (1) WO2017050978A1 (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20210261561A1 (en) * 2018-04-23 2021-08-26 Shionogi & Co., Ltd. Bicyclic heterocycle derivatives having selective bace1 inhibitory activity
US11629154B2 (en) 2018-04-27 2023-04-18 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
CN114380736B (zh) * 2020-10-21 2023-10-03 复旦大学 一种2,3,4,5-四氢吡啶类化合物的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077328A1 (es) * 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US9556135B2 (en) * 2012-10-12 2017-01-31 Amgen, Inc. Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
EP2961749B1 (en) 2013-03-01 2019-10-09 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
AU2015220873A1 (en) * 2014-02-19 2016-08-11 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as BACE1 inhibitors for treatment of Alzheimer's disease

Also Published As

Publication number Publication date
WO2017050978A1 (en) 2017-03-30
EP3353163A1 (en) 2018-08-01
IL258217A (en) 2018-05-31
JP2018527387A (ja) 2018-09-20
BR112018005591A2 (pt) 2018-10-09
HK1254800A1 (zh) 2019-07-26
TW201726651A (zh) 2017-08-01
EA035026B1 (ru) 2020-04-20
AU2016328589A1 (en) 2018-03-01
KR20180053357A (ko) 2018-05-21
CN108026069A (zh) 2018-05-11
EP3353163B1 (en) 2020-02-05
MX2018003565A (es) 2018-06-18
US20180334447A1 (en) 2018-11-22
CA2995161A1 (en) 2017-03-30

Similar Documents

Publication Publication Date Title
EA201891494A1 (ru) Гетероциклические соединения в качестве иммуномодуляторов
EA201992878A1 (ru) Соединения для лечения болезни хантингтона
BR112018076534A2 (pt) compostos heterocíclicos como imunomoduladores
CY1120846T1 (el) 2-αμινο-6-(διφθορομεθυλ)-5,5-διφθορο-6-φαινυλ-3,4,5,6-τετραϋδροπυριδινες ως αναστολεις bace1
EA201891203A1 (ru) Гетероциклические соединения в качестве иммуномодуляторов
EA202091709A1 (ru) Ингибиторы днк-пк
EA201791367A1 (ru) Соединения 2,3,4,5-тетрагидропиридин-6-амин и 3,4-дигидро-2h-пиррол-5-амин - ингибиторы бета-секретазы
PH12017500829A1 (en) 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer's disease
EA201691447A1 (ru) 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
EA201691134A1 (ru) Новые ингибиторы глутаминазы
EA201291435A1 (ru) Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)
EA201791030A1 (ru) 2-амино-5,5-дифтор-6-(фторметил)-6-фенил-3,4,5,6-тетрагидпропиридины в качестве ингибиторов bace1
EA201391296A1 (ru) ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE)
EA201391251A1 (ru) ПРОИЗВОДНЫЕ 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE)
EA201990400A1 (ru) Соединения и композиции и их применение
EA201491116A1 (ru) Производные 6-дифторметил-5,6-дигидро-2h-[1,4]оксазин-3-амина
EA201890449A1 (ru) Фумагиллиновые гетероциклические соединения и способы их получения и применения
EA202090414A1 (ru) Соединения и их применение
EA201791804A1 (ru) Соединения 1-гетероциклил изохроманила и аналоги для лечения расстройств цнс
PH12019500198A1 (en) Compounds and compositions and uses thereof
EA201890460A1 (ru) Композиции и способы лечения и предотвращения нейродегенеративных расстройств
EA201890769A1 (ru) Производные 2,3,4,5-тетрагидропиридин-6-амина
EA201991898A1 (ru) Двойные ингибиторы magl и faah
EA201992055A1 (ru) Ингибиторы бета-секретазы

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