MA40955A - 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 - Google Patents

2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1

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Publication number
MA40955A
MA40955A MA040955A MA40955A MA40955A MA 40955 A MA40955 A MA 40955A MA 040955 A MA040955 A MA 040955A MA 40955 A MA40955 A MA 40955A MA 40955 A MA40955 A MA 40955A
Authority
MA
Morocco
Prior art keywords
tetrahydropyridines
difluoromethyl
difluoro
phenyl
amino
Prior art date
Application number
MA040955A
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English (en)
Other versions
MA40955B1 (fr
Inventor
Karsten Juhl
Mauro Marigo
Lena Tagmose
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
Publication of MA40955A publication Critical patent/MA40955A/fr
Publication of MA40955B1 publication Critical patent/MA40955B1/fr

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    • 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
    • A61K31/435—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
    • A61K31/495—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

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

Abstract

<!--startfragment-->la présente invention concerne des composés de formule (i) qui sont des inhibiteurs de l'enzyme bace1. Différents aspects de l'invention concernent des compositions pharmaceutiques contenant lesdits composés, ainsi que les utilisations de ces composés dans le traitement de troubles dans lesquels la réduction de dépôts de bêta-amyloïdes est bénéfique, tels que la maladie d'alzheimer.<!--endfragment-->
MA40955A 2014-11-10 2015-11-09 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 MA40955B1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DKPA201400648 2014-11-10
DKPA201500447 2015-08-07
EP15805109.4A EP3218365B1 (fr) 2014-11-10 2015-11-09 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
PCT/EP2015/076015 WO2016075063A1 (fr) 2014-11-10 2015-11-09 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1

Publications (2)

Publication Number Publication Date
MA40955A true MA40955A (fr) 2017-09-20
MA40955B1 MA40955B1 (fr) 2018-11-30

Family

ID=54783558

Family Applications (1)

Application Number Title Priority Date Filing Date
MA40955A MA40955B1 (fr) 2014-11-10 2015-11-09 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1

Country Status (43)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
TW201718543A (zh) * 2015-08-12 2017-06-01 Ｈ 朗德貝克公司 作爲ｂａｃｅ１抑制劑之２－胺基－３－氟－３－（氟甲基）－６－甲基－６－苯基－３，４，５，６－四氫吡啶
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
JP2020500841A (ja) 2016-10-28 2020-01-16 ハー・ルンドベック・アクチエゼルスカベット イミダゾピラジノンの投与を含む併用療法
SI3532064T1 (sl) 2016-10-28 2020-10-30 H. Lundbeck A/S Kombinirana zdravljenja, ki obsegajo imidazopirazinone za zdravljenje psihiatričnih in/ali kognitivnih motenj
WO2018114910A1 (fr) 2016-12-21 2018-06-28 H. Lundbeck A/S 6-amino-5-fluoro-5-(fluorométhyl)-2,3,4,5-tétrahydropyridin-2-yl-phényl-5-(méthoxy-d3)-pyrazine-2-carboxamides et leurs dérivés fluorés en tant qu'inhibiteurs bace1
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
US11634416B2 (en) 2017-12-14 2023-04-25 H. Lundbeck A/S Combination treatments comprising administration of 1H-pyrazolo[4,3-b]pyridines
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

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CA2450167A1 (fr) 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles utiles dans le traitement de la maladie d'alzheimer
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EP2961749B1 (fr) 2013-03-01 2019-10-09 Amgen Inc. Composés perfluorés 5,6-dihydro-4h-1,3-oxazine-2-amine substitués en tant qu'inhibiteurs de la bêta-sécrétase et procédés d'utilisation correspondants
TWI639607B (zh) 2013-06-18 2018-11-01 美國禮來大藥廠 Ｂａｃｅ抑制劑
AU2015220873A1 (en) 2014-02-19 2016-08-11 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
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
TW201718543A (zh) 2015-08-12 2017-06-01 Ｈ 朗德貝克公司 作爲ｂａｃｅ１抑制劑之２－胺基－３－氟－３－（氟甲基）－６－甲基－６－苯基－３，４，５，６－四氫吡啶
WO2018114910A1 (fr) 2016-12-21 2018-06-28 H. Lundbeck A/S 6-amino-5-fluoro-5-(fluorométhyl)-2,3,4,5-tétrahydropyridin-2-yl-phényl-5-(méthoxy-d3)-pyrazine-2-carboxamides et leurs dérivés fluorés en tant qu'inhibiteurs bace1

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Publication number Publication date
IL252089B (en) 2020-03-31
ME03723B (fr) 2021-04-20
RU2017116196A3 (fr) 2019-05-14
EP3218365B1 (fr) 2018-10-10
PT3218365T (pt) 2018-11-22
CR20170186A (es) 2017-07-27
TWI690318B (zh) 2020-04-11
JO3458B1 (ar) 2020-07-05
CO2017004465A2 (es) 2017-07-19
IL252089A0 (en) 2017-07-31
LT3218365T (lt) 2018-12-10
ZA201702797B (en) 2019-05-29
US10603310B2 (en) 2020-03-31
NI201700055A (es) 2017-09-22
SG11201703547XA (en) 2017-05-30
RU2017116196A (ru) 2018-12-14
JP2017533245A (ja) 2017-11-09
DOP2017000117A (es) 2017-07-31
US20160130267A1 (en) 2016-05-12
AU2015345258B2 (en) 2020-05-21
US9346797B1 (en) 2016-05-24
HUE040304T2 (hu) 2019-02-28
PH12017500841A1 (en) 2017-10-30
CY1120846T1 (el) 2020-05-29
CL2017001112A1 (es) 2017-12-01
PE20170946A1 (es) 2017-07-13
BR112017009583A2 (pt) 2017-12-26
SI3218365T1 (sl) 2018-12-31
DK3218365T3 (en) 2018-11-26
GEP20196949B (en) 2019-02-25
HRP20181698T1 (hr) 2018-12-28
EP3218365A1 (fr) 2017-09-20
ES2694860T3 (es) 2018-12-27
KR20170081184A (ko) 2017-07-11
CA2965563A1 (fr) 2016-05-19
MX2017006049A (es) 2017-06-19
US20170319564A1 (en) 2017-11-09
US20190000823A1 (en) 2019-01-03
ECSP17028459A (es) 2017-08-31
EA201790818A1 (ru) 2017-09-29
EP3461483A1 (fr) 2019-04-03
US10045974B2 (en) 2018-08-14
WO2016075063A1 (fr) 2016-05-19
JP6629320B2 (ja) 2020-01-15
EA032339B1 (ru) 2019-05-31
MA40955B1 (fr) 2018-11-30
AU2015345258A1 (en) 2017-05-04
UA119576C2 (uk) 2019-07-10
TW201628616A (zh) 2016-08-16
RS57946B1 (sr) 2019-01-31
TN2017000144A1 (en) 2018-10-19
SV2017005435A (es) 2017-07-19
GT201700099A (es) 2019-07-29
PH12017500841B1 (en) 2017-10-30
PL3218365T3 (pl) 2019-02-28
TR201816427T4 (tr) 2018-11-21
CN107074836A (zh) 2017-08-18
CN107074836B (zh) 2020-03-27

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