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HRP20181698T1 - 2-amino-6-(difluormetil)-5,5-difluor-6-fenil-3,4,5,6-tetrahidropiridini kao inhibitori bace1 - Google Patents

2-amino-6-(difluormetil)-5,5-difluor-6-fenil-3,4,5,6-tetrahidropiridini kao inhibitori bace1

Info

Publication number
HRP20181698T1
HRP20181698T1 HRP20181698TT HRP20181698T HRP20181698T1 HR P20181698 T1 HRP20181698 T1 HR P20181698T1 HR P20181698T T HRP20181698T T HR P20181698TT HR P20181698 T HRP20181698 T HR P20181698T HR P20181698 T1 HRP20181698 T1 HR P20181698T1
Authority
HR
Croatia
Prior art keywords
tetrahydropyridines
difluoromethyl
difluoro
phenyl
amino
Prior art date
Application number
HRP20181698TT
Other languages
English (en)
Inventor
Karsten Juhl
Lena TAGMOSE
Mauro Marigo
Original Assignee
H. Lundbeck A/S
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 H. Lundbeck A/S filed Critical H. Lundbeck A/S
Publication of HRP20181698T1 publication Critical patent/HRP20181698T1/hr

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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
HRP20181698TT 2014-11-10 2018-10-17 2-amino-6-(difluormetil)-5,5-difluor-6-fenil-3,4,5,6-tetrahidropiridini kao inhibitori bace1 HRP20181698T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DKPA201400648 2014-11-10
DKPA201500447 2015-08-07
EP15805109.4A EP3218365B1 (en) 2014-11-10 2015-11-09 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
PCT/EP2015/076015 WO2016075063A1 (en) 2014-11-10 2015-11-09 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors

Publications (1)

Publication Number Publication Date
HRP20181698T1 true HRP20181698T1 (hr) 2018-12-28

Family

ID=54783558

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20181698TT HRP20181698T1 (hr) 2014-11-10 2018-10-17 2-amino-6-(difluormetil)-5,5-difluor-6-fenil-3,4,5,6-tetrahidropiridini kao inhibitori bace1

Country Status (43)

Country Link
US (3) US9346797B1 (hr)
EP (2) EP3461483A1 (hr)
JP (1) JP6629320B2 (hr)
KR (1) KR20170081184A (hr)
CN (1) CN107074836B (hr)
AU (1) AU2015345258B2 (hr)
BR (1) BR112017009583A2 (hr)
CA (1) CA2965563A1 (hr)
CL (1) CL2017001112A1 (hr)
CO (1) CO2017004465A2 (hr)
CR (1) CR20170186A (hr)
CY (1) CY1120846T1 (hr)
DK (1) DK3218365T3 (hr)
DO (1) DOP2017000117A (hr)
EA (1) EA032339B1 (hr)
EC (1) ECSP17028459A (hr)
ES (1) ES2694860T3 (hr)
GE (1) GEP20196949B (hr)
GT (1) GT201700099A (hr)
HR (1) HRP20181698T1 (hr)
HU (1) HUE040304T2 (hr)
IL (1) IL252089B (hr)
JO (1) JO3458B1 (hr)
LT (1) LT3218365T (hr)
MA (1) MA40955B1 (hr)
ME (1) ME03723B (hr)
MX (1) MX2017006049A (hr)
NI (1) NI201700055A (hr)
PE (1) PE20170946A1 (hr)
PH (1) PH12017500841B1 (hr)
PL (1) PL3218365T3 (hr)
PT (1) PT3218365T (hr)
RS (1) RS57946B1 (hr)
RU (1) RU2017116196A (hr)
SG (1) SG11201703547XA (hr)
SI (1) SI3218365T1 (hr)
SV (1) SV2017005435A (hr)
TN (1) TN2017000144A1 (hr)
TR (1) TR201816427T4 (hr)
TW (1) TWI690318B (hr)
UA (1) UA119576C2 (hr)
WO (1) WO2016075063A1 (hr)
ZA (1) ZA201702797B (hr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20180244645A1 (en) * 2015-08-12 2018-08-30 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
JOP20190081A1 (ar) 2016-10-13 2019-04-11 Novartis Ag مشتق أوكسازين للاستخدام في علاج أو الوقاية من اعتلال وعائي دماغي نشواني
CA3041607A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders
US10912773B2 (en) 2016-10-28 2021-02-09 H. Lundbeck A/S Combinations comprising substituted imidazo[1,5-a]pyrazinones as PDE1 inhibitors
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
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
PL3723807T3 (pl) 2017-12-14 2022-01-24 H. Lundbeck A/S Leczenie skojarzone obejmujące podawanie 1h-pirazolo­[4,3-b]pirydyn
WO2019121840A1 (en) 2017-12-20 2019-06-27 H. Lundbeck A/S Pyrazolo[3,4-b]pyridines and imidazo[1,5-b]pyridazines as pde1 inhibitors

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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
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
AU2011263797B2 (en) * 2010-06-09 2014-06-05 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
KR20140051822A (ko) 2011-01-12 2014-05-02 노파르티스 아게 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도
ES2576182T3 (es) 2011-01-13 2016-07-06 Novartis Ag Derivados de heterocíclicos novedosos y su uso en el tratamiento de trastornos neurológicos
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
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EA023261B1 (ru) * 2011-06-07 2016-05-31 Ф.Хоффманн-Ля Рош Аг Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и(или) bace2
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JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
WO2015124576A1 (en) 2014-02-19 2015-08-27 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
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
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
US20180244645A1 (en) 2015-08-12 2018-08-30 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
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

Also Published As

Publication number Publication date
ECSP17028459A (es) 2017-08-31
PT3218365T (pt) 2018-11-22
EA201790818A1 (ru) 2017-09-29
CO2017004465A2 (es) 2017-07-19
PH12017500841A1 (en) 2017-10-30
DOP2017000117A (es) 2017-07-31
IL252089B (en) 2020-03-31
IL252089A0 (en) 2017-07-31
ES2694860T3 (es) 2018-12-27
RU2017116196A (ru) 2018-12-14
JO3458B1 (ar) 2020-07-05
BR112017009583A2 (pt) 2017-12-26
DK3218365T3 (en) 2018-11-26
EP3218365A1 (en) 2017-09-20
US10603310B2 (en) 2020-03-31
CY1120846T1 (el) 2020-05-29
GEP20196949B (en) 2019-02-25
PE20170946A1 (es) 2017-07-13
UA119576C2 (uk) 2019-07-10
US9346797B1 (en) 2016-05-24
JP6629320B2 (ja) 2020-01-15
MA40955A (fr) 2017-09-20
US20190000823A1 (en) 2019-01-03
EP3461483A1 (en) 2019-04-03
US20160130267A1 (en) 2016-05-12
MX2017006049A (es) 2017-06-19
LT3218365T (lt) 2018-12-10
ZA201702797B (en) 2019-05-29
PL3218365T3 (pl) 2019-02-28
AU2015345258B2 (en) 2020-05-21
MA40955B1 (fr) 2018-11-30
SI3218365T1 (sl) 2018-12-31
NI201700055A (es) 2017-09-22
SV2017005435A (es) 2017-07-19
TWI690318B (zh) 2020-04-11
GT201700099A (es) 2019-07-29
PH12017500841B1 (en) 2017-10-30
AU2015345258A1 (en) 2017-05-04
CR20170186A (es) 2017-07-27
RS57946B1 (sr) 2019-01-31
EA032339B1 (ru) 2019-05-31
HUE040304T2 (hu) 2019-02-28
WO2016075063A1 (en) 2016-05-19
JP2017533245A (ja) 2017-11-09
CN107074836A (zh) 2017-08-18
CN107074836B (zh) 2020-03-27
KR20170081184A (ko) 2017-07-11
SG11201703547XA (en) 2017-05-30
CL2017001112A1 (es) 2017-12-01
TN2017000144A1 (en) 2018-10-19
TW201628616A (zh) 2016-08-16
EP3218365B1 (en) 2018-10-10
RU2017116196A3 (hr) 2019-05-14
ME03723B (me) 2021-04-20
TR201816427T4 (tr) 2018-11-21
US20170319564A1 (en) 2017-11-09
CA2965563A1 (en) 2016-05-19
US10045974B2 (en) 2018-08-14

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