CY1120846T1 - 2-αμινο-6-(διφθορομεθυλ)-5,5-διφθορο-6-φαινυλ-3,4,5,6-τετραϋδροπυριδινες ως αναστολεις bace1 - Google Patents

2-αμινο-6-(διφθορομεθυλ)-5,5-διφθορο-6-φαινυλ-3,4,5,6-τετραϋδροπυριδινες ως αναστολεις bace1

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Publication number
CY1120846T1
CY1120846T1 CY20181101200T CY181101200T CY1120846T1 CY 1120846 T1 CY1120846 T1 CY 1120846T1 CY 20181101200 T CY20181101200 T CY 20181101200T CY 181101200 T CY181101200 T CY 181101200T CY 1120846 T1 CY1120846 T1 CY 1120846T1
Authority
CY
Cyprus
Prior art keywords
inhibitors
bace1
difthoromethyl
difforro
tetrahydropyridine
Prior art date
Application number
CY20181101200T
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 CY1120846T1 publication Critical patent/CY1120846T1/el

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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
    • 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
    • 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

Abstract

Η παρούσα εφεύρεση απευθύνεται σε ενώσεις του χημικού τύπου (I) οι οποίες είναι αναστολείς του ενζύμου BACE1. Ξεχωριστές απόψεις του θέματος της εφεύρεσης απευθύνονται σε φαρμακευτικές συνθέσεις περιλαμβάνοντας τις εν λόγω ενώσεις και χρήσεις των ενώσεων για αγωγή διαταραχών για τις οποίες η μείωση των εναποθέσεων Αβ είναι ευεργετική όπως είναι η νόσος του Αλτσχάιμερ.
CY20181101200T 2014-11-10 2018-11-13 2-αμινο-6-(διφθορομεθυλ)-5,5-διφθορο-6-φαινυλ-3,4,5,6-τετραϋδροπυριδινες ως αναστολεις bace1 CY1120846T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201400648 2014-11-10
DKPA201500447 2015-08-07
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
CY1120846T1 true CY1120846T1 (el) 2020-05-29

Family

ID=54783558

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20181101200T CY1120846T1 (el) 2014-11-10 2018-11-13 2-αμινο-6-(διφθορομεθυλ)-5,5-διφθορο-6-φαινυλ-3,4,5,6-τετραϋδροπυριδινες ως αναστολεις bace1

Country Status (43)

Country Link
US (3) US9346797B1 (el)
EP (2) EP3218365B1 (el)
JP (1) JP6629320B2 (el)
KR (1) KR20170081184A (el)
CN (1) CN107074836B (el)
AU (1) AU2015345258B2 (el)
BR (1) BR112017009583A2 (el)
CA (1) CA2965563A1 (el)
CL (1) CL2017001112A1 (el)
CO (1) CO2017004465A2 (el)
CR (1) CR20170186A (el)
CY (1) CY1120846T1 (el)
DK (1) DK3218365T3 (el)
DO (1) DOP2017000117A (el)
EA (1) EA032339B1 (el)
EC (1) ECSP17028459A (el)
ES (1) ES2694860T3 (el)
GE (1) GEP20196949B (el)
GT (1) GT201700099A (el)
HR (1) HRP20181698T1 (el)
HU (1) HUE040304T2 (el)
IL (1) IL252089B (el)
JO (1) JO3458B1 (el)
LT (1) LT3218365T (el)
MA (1) MA40955B1 (el)
ME (1) ME03723B (el)
MX (1) MX2017006049A (el)
NI (1) NI201700055A (el)
PE (1) PE20170946A1 (el)
PH (1) PH12017500841B1 (el)
PL (1) PL3218365T3 (el)
PT (1) PT3218365T (el)
RS (1) RS57946B1 (el)
RU (1) RU2017116196A (el)
SG (1) SG11201703547XA (el)
SI (1) SI3218365T1 (el)
SV (1) SV2017005435A (el)
TN (1) TN2017000144A1 (el)
TR (1) TR201816427T4 (el)
TW (1) TWI690318B (el)
UA (1) UA119576C2 (el)
WO (1) WO2016075063A1 (el)
ZA (1) ZA201702797B (el)

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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
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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MA46621A (fr) 2016-10-28 2021-06-02 H Lundbeck As Traitements combinés comprenant l'administration d'imidazopyrazinones
PL3532064T3 (pl) 2016-10-28 2020-11-16 H. Lundbeck A/S Terapie skojarzone obejmujące imidazopirazynony do leczenia zaburzeń psychiatrycznych i/lub poznawczych
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
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AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
CN111511742B (zh) 2017-12-20 2023-10-27 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

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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
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
EP3334720A1 (en) 2015-08-12 2018-06-20 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins 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

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LT3218365T (lt) 2018-12-10
ME03723B (me) 2021-04-20
DK3218365T3 (en) 2018-11-26
CA2965563A1 (en) 2016-05-19
TR201816427T4 (tr) 2018-11-21
RU2017116196A3 (el) 2019-05-14
ES2694860T3 (es) 2018-12-27
EP3218365B1 (en) 2018-10-10
CO2017004465A2 (es) 2017-07-19
PH12017500841A1 (en) 2017-10-30
MA40955B1 (fr) 2018-11-30
US20160130267A1 (en) 2016-05-12
GT201700099A (es) 2019-07-29
RS57946B1 (sr) 2019-01-31
TN2017000144A1 (en) 2018-10-19
CL2017001112A1 (es) 2017-12-01
PT3218365T (pt) 2018-11-22
EA032339B1 (ru) 2019-05-31
GEP20196949B (en) 2019-02-25
JP2017533245A (ja) 2017-11-09
ECSP17028459A (es) 2017-08-31
WO2016075063A1 (en) 2016-05-19
EP3461483A1 (en) 2019-04-03
AU2015345258B2 (en) 2020-05-21
CN107074836A (zh) 2017-08-18
CN107074836B (zh) 2020-03-27
PL3218365T3 (pl) 2019-02-28
US10603310B2 (en) 2020-03-31
RU2017116196A (ru) 2018-12-14
TW201628616A (zh) 2016-08-16
US20170319564A1 (en) 2017-11-09
JP6629320B2 (ja) 2020-01-15
IL252089A0 (en) 2017-07-31
UA119576C2 (uk) 2019-07-10
US10045974B2 (en) 2018-08-14
MX2017006049A (es) 2017-06-19
KR20170081184A (ko) 2017-07-11
BR112017009583A2 (pt) 2017-12-26
PH12017500841B1 (en) 2017-10-30
NI201700055A (es) 2017-09-22
PE20170946A1 (es) 2017-07-13
AU2015345258A1 (en) 2017-05-04
US20190000823A1 (en) 2019-01-03
US9346797B1 (en) 2016-05-24
EP3218365A1 (en) 2017-09-20
HUE040304T2 (hu) 2019-02-28
TWI690318B (zh) 2020-04-11
SG11201703547XA (en) 2017-05-30
HRP20181698T1 (hr) 2018-12-28
EA201790818A1 (ru) 2017-09-29
IL252089B (en) 2020-03-31
SV2017005435A (es) 2017-07-19
DOP2017000117A (es) 2017-07-31
JO3458B1 (ar) 2020-07-05
SI3218365T1 (sl) 2018-12-31
MA40955A (fr) 2017-09-20
CR20170186A (es) 2017-07-27
ZA201702797B (en) 2019-05-29

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