JO3458B1 - 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 - Google Patents

2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1

Info

Publication number
JO3458B1
JO3458B1 JOP/2015/0260A JOP20150260A JO3458B1 JO 3458 B1 JO3458 B1 JO 3458B1 JO P20150260 A JOP20150260 A JO P20150260A JO 3458 B1 JO3458 B1 JO 3458B1
Authority
JO
Jordan
Prior art keywords
tetrahydropyridines
difluoromethyl
difluoro
phenyl
amino
Prior art date
Application number
JOP/2015/0260A
Other languages
English (en)
Inventor
Marigo Mauro
Tagmose Lena
Juhl Karsten
Original Assignee
H Lundbeck As
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 As filed Critical H Lundbeck As
Application granted granted Critical
Publication of JO3458B1 publication Critical patent/JO3458B1/ar

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Classifications

    • 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
    • A61K31/4439—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
    • 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

Abstract

يتم توجيه الاختراع الحالي إلى مثبطات جديدة لإنزيم <span dir="LTR"> BACE 1</span>. يتم توجيه السمات المنفصلة من الاختراع إلى تركيبات صيدلانية تشمل المركبات المذكورة و استخدامات المركبات لعلاج اضطربات يكون من المفيد لها خفص رواسب <span dir="LTR">A</span><span dir="LTR">β</span> مثل مرض الزهايمر.
JOP/2015/0260A 2014-11-10 2015-10-25 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 JO3458B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201400648 2014-11-10
DKPA201500447 2015-08-07

Publications (1)

Publication Number Publication Date
JO3458B1 true JO3458B1 (ar) 2020-07-05

Family

ID=54783558

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2015/0260A JO3458B1 (ar) 2014-11-10 2015-10-25 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1

Country Status (43)

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

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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
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
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
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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
US11634416B2 (en) 2017-12-14 2023-04-25 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
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 (ar) 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
CY1120846T1 (el) 2020-05-29
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
SI3218365T1 (sl) 2018-12-31
MA40955A (fr) 2017-09-20
CR20170186A (es) 2017-07-27
ZA201702797B (en) 2019-05-29

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