EA201790817A1 - 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 для лечения болезни альцгеймера - Google Patents

2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 для лечения болезни альцгеймера

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Publication number
EA201790817A1
EA201790817A1 EA201790817A EA201790817A EA201790817A1 EA 201790817 A1 EA201790817 A1 EA 201790817A1 EA 201790817 A EA201790817 A EA 201790817A EA 201790817 A EA201790817 A EA 201790817A EA 201790817 A1 EA201790817 A1 EA 201790817A1
Authority
EA
Eurasian Patent Office
Prior art keywords
disease
diftor
allzheimer
tetrahydropyridines
dimethyl
Prior art date
Application number
EA201790817A
Other languages
English (en)
Inventor
Карстен Джул
Лена Тэгмоуз
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 EA201790817A1 publication Critical patent/EA201790817A1/ru

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    • 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
    • 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
    • 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

Abstract

Настоящее изобретение относится к соединениям формулы Iпри этом соединения являются ингибиторами фермента ВАСЕ1. Отдельные аспекты настоящего изобретения относятся к фармацевтическим композициям, содержащим указанные соединения, и к применениям соединений для лечения нарушений, при которых полезно снижение отложений Аβ, таких как болезнь Альцгеймера.
EA201790817A 2014-11-10 2015-11-09 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 для лечения болезни альцгеймера EA201790817A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201400649 2014-11-10
DKPA201500450 2015-08-07
PCT/EP2015/076014 WO2016075062A1 (en) 2014-11-10 2015-11-09 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer's disease

Publications (1)

Publication Number Publication Date
EA201790817A1 true EA201790817A1 (ru) 2017-09-29

Family

ID=54476983

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201790817A EA201790817A1 (ru) 2014-11-10 2015-11-09 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 для лечения болезни альцгеймера

Country Status (26)

Country Link
US (1) US10059669B2 (ru)
EP (1) EP3218362B1 (ru)
JP (1) JP2017533253A (ru)
KR (1) KR20170082529A (ru)
CN (1) CN107074809A (ru)
AU (1) AU2015345257A1 (ru)
BR (1) BR112017009647A2 (ru)
CA (1) CA2964305A1 (ru)
CL (1) CL2017001113A1 (ru)
CO (1) CO2017004530A2 (ru)
CR (1) CR20170187A (ru)
DO (1) DOP2017000118A (ru)
EA (1) EA201790817A1 (ru)
EC (1) ECSP17028463A (ru)
ES (1) ES2710602T3 (ru)
IL (1) IL252091A0 (ru)
MX (1) MX2017006048A (ru)
NI (1) NI201700056A (ru)
PE (1) PE20170947A1 (ru)
PH (1) PH12017500829A1 (ru)
RU (1) RU2017116197A (ru)
SG (1) SG11201703177WA (ru)
SV (1) SV2017005434A (ru)
TN (1) TN2017000134A1 (ru)
WO (1) WO2016075062A1 (ru)
ZA (1) ZA201702799B (ru)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
MX2018001699A (es) * 2015-08-12 2018-05-07 H Lundbeck As 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1.
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
CN106366073B (zh) * 2016-10-24 2018-11-30 扬子江药业集团南京海陵药业有限公司 一种盐酸替吡嘧啶的制备方法
DK3532064T3 (da) 2016-10-28 2020-08-24 H Lundbeck As Kombinationsbehandlinger omfattende imidazopyrazinoner til behandlingen af psykiatriske og/eller kognitive lidelser
CN109803653A (zh) 2016-10-28 2019-05-24 H.隆德贝克有限公司 包括给予咪唑并吡嗪酮的组合治疗
TW201829394A (zh) * 2016-12-21 2018-08-16 丹麥商Ｈ 朗德貝克公司 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物
SI3723807T1 (sl) 2017-12-14 2022-01-31 H. Lundbeck A/S Kombinirana zdravljenja, ki obsegajo dajanje 1H-pirazolo(4,3-b)piridinov
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
CN109970681A (zh) * 2019-04-19 2019-07-05 安徽海康药业有限责任公司 一种瑞格列奈的合成方法
CN113720930A (zh) * 2021-07-26 2021-11-30 南京一诺医药科技有限公司 一种hplc-ms/ms联用检测人血浆中奥美拉唑的方法
CN114235985A (zh) * 2021-11-25 2022-03-25 南京海纳医药科技股份有限公司 一种hplc-ms/ms联用检测人血浆中胍法辛的方法

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002100399A1 (en) 2001-06-12 2002-12-19 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
EP2258687B1 (en) 2002-02-12 2012-12-26 Glaxosmithkline LLC Nicotinamide derivates useful as P38 inhibitors
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
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)
CN103429589A (zh) 2011-01-12 2013-12-04 诺瓦提斯公司 噁嗪衍生物及其在治疗神经障碍中的用途
PL2663561T3 (pl) 2011-01-13 2016-10-31 Nowe pochodne heterocykliczne i ich zastosowanie w leczeniu zaburzeń neurologicznych
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
BR112013031098A2 (pt) 2011-06-07 2016-12-06 Hoffmann La Roche halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou 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
CA2867851A1 (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
TWI639607B (zh) 2013-06-18 2018-11-01 美國禮來大藥廠 Ｂａｃｅ抑制劑
EP3107897A1 (en) 2014-02-19 2016-12-28 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease
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
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
MX2018001699A (es) 2015-08-12 2018-05-07 H Lundbeck As 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1.

Also Published As

Publication number Publication date
RU2017116197A (ru) 2018-12-13
ES2710602T3 (es) 2019-04-26
US10059669B2 (en) 2018-08-28
BR112017009647A2 (pt) 2017-12-19
CL2017001113A1 (es) 2017-12-01
EP3218362B1 (en) 2019-01-09
EP3218362A1 (en) 2017-09-20
ECSP17028463A (es) 2017-08-31
SG11201703177WA (en) 2017-05-30
CA2964305A1 (en) 2016-05-19
PH12017500829A1 (en) 2017-10-09
AU2015345257A1 (en) 2017-05-04
CN107074809A (zh) 2017-08-18
KR20170082529A (ko) 2017-07-14
DOP2017000118A (es) 2017-07-15
JP2017533253A (ja) 2017-11-09
SV2017005434A (es) 2017-07-19
WO2016075062A1 (en) 2016-05-19
ZA201702799B (en) 2018-08-29
CO2017004530A2 (es) 2017-07-28
CR20170187A (es) 2018-02-01
TN2017000134A1 (en) 2018-10-19
IL252091A0 (en) 2017-07-31
MX2017006048A (es) 2017-06-19
NI201700056A (es) 2017-09-22
US20170313658A1 (en) 2017-11-02
PE20170947A1 (es) 2017-07-13

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