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

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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
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JO
Jordan
Prior art keywords
span
tetrahydropyridine
difluoromethyl
difluoro
phenyl
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JOP/2015/0260A
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English (en)
Inventor
Marigo Mauro
Tagmose Lena
Juhl Karsten
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H Lundbeck As
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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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    • 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

Landscapes

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

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

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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 (44)

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US (3) US9346797B1 (ar)
EP (2) EP3461483A1 (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 (2) 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)
SM (1) SMT201800570T1 (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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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
JP2018531889A (ja) * 2015-08-12 2018-11-01 ハー・ルンドベック・アクチエゼルスカベット Ｂａｃｅ１阻害剤としての２−アミノ−３−フルオロ−３−（フルオロメチル）−６−メチル−６−フェニル−３，４，５，６−テトラヒドロピリジン
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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KR20190077349A (ko) 2016-10-28 2019-07-03 하. 룬드벡 아크티에셀스카브 이미다조피라지논의 투여를 포함하는 병용 치료
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
RS62551B1 (sr) 2017-12-14 2021-12-31 H Lundbeck As Kombinovane terapije koje obuhvataju primenu 1h-pirazolo[4,3-b]piridina
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
EP3728250A1 (en) 2017-12-20 2020-10-28 H. Lundbeck A/S PYRAZOLO[3,4-beta]PYRIDINES AND IMIDAZO[1,5-beta]PYRIDAZINES AS PDE1 INHIBITORS

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JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
GEAP201814248A (en) 2014-02-19 2018-04-10 H Lundbeck As 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
JP2018531889A (ja) 2015-08-12 2018-11-01 ハー・ルンドベック・アクチエゼルスカベット Ｂａｃｅ１阻害剤としての２−アミノ−３−フルオロ−３−（フルオロメチル）−６−メチル−６−フェニル−３，４，５，６−テトラヒドロピリジン
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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EA201790818A1 (ru) 2017-09-29
IL252089B (en) 2020-03-31
RU2017116196A3 (ar) 2019-05-14
TN2017000144A1 (en) 2018-10-19
US20160130267A1 (en) 2016-05-12
ES2694860T3 (es) 2018-12-27
US20170319564A1 (en) 2017-11-09
DK3218365T3 (en) 2018-11-26
EP3218365A1 (en) 2017-09-20
RU2017116196A (ru) 2018-12-14
MA40955A (fr) 2017-09-20
GEAP201814485A (en) 2018-08-27
GT201700099A (es) 2019-07-29
US20190000823A1 (en) 2019-01-03
CO2017004465A2 (es) 2017-07-19
HUE040304T2 (hu) 2019-02-28
PH12017500841A1 (en) 2017-10-30
HRP20181698T1 (hr) 2018-12-28
PT3218365T (pt) 2018-11-22
ECSP17028459A (es) 2017-08-31
MX2017006049A (es) 2017-06-19
ZA201702797B (en) 2019-05-29
IL252089A0 (en) 2017-07-31
AU2015345258A1 (en) 2017-05-04
CL2017001112A1 (es) 2017-12-01
DOP2017000117A (es) 2017-07-31
SI3218365T1 (sl) 2018-12-31
SMT201800570T1 (it) 2019-01-11
SG11201703547XA (en) 2017-05-30
CY1120846T1 (el) 2020-05-29
EP3461483A1 (en) 2019-04-03
EA032339B1 (ru) 2019-05-31
UA119576C2 (uk) 2019-07-10
CN107074836A (zh) 2017-08-18
CN107074836B (zh) 2020-03-27
MA40955B1 (fr) 2018-11-30
JP6629320B2 (ja) 2020-01-15
ME03723B (me) 2021-04-20
PH12017500841B1 (en) 2017-10-30
BR112017009583A2 (pt) 2017-12-26
US9346797B1 (en) 2016-05-24
CA2965563A1 (en) 2016-05-19
TW201628616A (zh) 2016-08-16
EP3218365B1 (en) 2018-10-10
WO2016075063A1 (en) 2016-05-19
JP2017533245A (ja) 2017-11-09
AU2015345258B2 (en) 2020-05-21
TWI690318B (zh) 2020-04-11
GEP20196949B (en) 2019-02-25
PE20170946A1 (es) 2017-07-13
CR20170186A (es) 2017-07-27
TR201816427T4 (tr) 2018-11-21
SV2017005435A (es) 2017-07-19
KR20170081184A (ko) 2017-07-11
LT3218365T (lt) 2018-12-10
US10045974B2 (en) 2018-08-14
NI201700055A (es) 2017-09-22
PL3218365T3 (pl) 2019-02-28
US10603310B2 (en) 2020-03-31
RS57946B1 (sr) 2019-01-31

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