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ME03723B - 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori - Google Patents

2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori

Info

Publication number
ME03723B
ME03723B MEP-2018-267A MEP2018267A ME03723B ME 03723 B ME03723 B ME 03723B ME P2018267 A MEP2018267 A ME P2018267A ME 03723 B ME03723 B ME 03723B
Authority
ME
Montenegro
Prior art keywords
tetrahydropyridines
difluoromethyl
difluoro
phenyl
amino
Prior art date
Application number
MEP-2018-267A
Other languages
German (de)
English (en)
French (fr)
Inventor
Karsten Juhl
Lena Tagmose
Mauro Marigo
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 ME03723B publication Critical patent/ME03723B/me

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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

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)
MEP-2018-267A 2014-11-10 2015-11-09 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori ME03723B (me)

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
ME03723B true ME03723B (me) 2021-04-20

Family

ID=54783558

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2018-267A ME03723B (me) 2014-11-10 2015-11-09 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori

Country Status (44)

Country Link
US (3) US9346797B1 (me)
EP (2) EP3218365B1 (me)
JP (1) JP6629320B2 (me)
KR (1) KR20170081184A (me)
CN (1) CN107074836B (me)
AU (1) AU2015345258B2 (me)
BR (1) BR112017009583A2 (me)
CA (1) CA2965563A1 (me)
CL (1) CL2017001112A1 (me)
CO (1) CO2017004465A2 (me)
CR (1) CR20170186A (me)
CY (1) CY1120846T1 (me)
DK (1) DK3218365T3 (me)
DO (1) DOP2017000117A (me)
EA (1) EA032339B1 (me)
EC (1) ECSP17028459A (me)
ES (1) ES2694860T3 (me)
GE (1) GEP20196949B (me)
GT (1) GT201700099A (me)
HR (1) HRP20181698T1 (me)
HU (1) HUE040304T2 (me)
IL (1) IL252089B (me)
JO (1) JO3458B1 (me)
LT (1) LT3218365T (me)
MA (1) MA40955B1 (me)
ME (1) ME03723B (me)
MX (1) MX2017006049A (me)
NI (1) NI201700055A (me)
PE (1) PE20170946A1 (me)
PH (1) PH12017500841A1 (me)
PL (1) PL3218365T3 (me)
PT (1) PT3218365T (me)
RS (1) RS57946B1 (me)
RU (1) RU2017116196A (me)
SG (1) SG11201703547XA (me)
SI (1) SI3218365T1 (me)
SM (1) SMT201800570T1 (me)
SV (1) SV2017005435A (me)
TN (1) TN2017000144A1 (me)
TR (1) TR201816427T4 (me)
TW (1) TWI690318B (me)
UA (1) UA119576C2 (me)
WO (1) WO2016075063A1 (me)
ZA (1) ZA201702797B (me)

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
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
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
WO2017025559A1 (en) * 2015-08-12 2017-02-16 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
JOP20190081A1 (ar) * 2016-10-13 2019-04-11 Novartis Ag مشتق أوكسازين للاستخدام في علاج أو الوقاية من اعتلال وعائي دماغي نشواني
US10912773B2 (en) 2016-10-28 2021-02-09 H. Lundbeck A/S Combinations comprising substituted imidazo[1,5-a]pyrazinones as PDE1 inhibitors
US10905688B2 (en) 2016-10-28 2021-02-02 H. Lundbeck A/S Combinations comprising substituted imidazo[1,5-α]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
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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US7067507B2 (en) 2001-06-12 2006-06-27 Pharmacia & Upjohn Company Macrocycles useful in the treatment of Alzheimer's disease
GB0124928D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
DK1474395T3 (da) 2002-02-12 2008-02-11 Smithkline Beecham Corp Nicotinamidderivater, der er nyttige som p38-inhibitorer
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
TWI537263B (zh) 2010-06-09 2016-06-11 健生藥品公司 使用作為β-分泌酶抑制劑之5,6-二氫-2H-[1,4]-3-基-胺衍生物
AU2012206555A1 (en) 2011-01-12 2013-08-01 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
PH12013501480A1 (en) 2011-01-13 2022-10-26 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
CN103608345A (zh) 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
PE20140623A1 (es) 2011-06-07 2014-05-30 Hoffmann La Roche Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace2
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
WO2013142613A1 (en) 2012-03-20 2013-09-26 Elan Pharmaceuticals, Inc. Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof
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JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
TW201446758A (zh) 2013-03-01 2014-12-16 Amgen Inc 作爲β-分泌酶抑制劑的全氟化5,6-二氫-4H-1,3-□-2-胺化合物及其用途
TWI639607B (zh) 2013-06-18 2018-11-01 美國禮來大藥廠 Bace抑制劑
MA39225A1 (fr) 2014-02-19 2017-04-28 H Lundbeck As 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tétrahydropyridines utilisées en tant qu'inhibiteurs de bace1 dans le traitement de la maladie d'alzheimer
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
WO2017025559A1 (en) 2015-08-12 2017-02-16 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

Also Published As

Publication number Publication date
EP3218365B1 (en) 2018-10-10
MA40955B1 (fr) 2018-11-30
DK3218365T3 (en) 2018-11-26
PT3218365T (pt) 2018-11-22
MX2017006049A (es) 2017-06-19
EA201790818A1 (ru) 2017-09-29
TR201816427T4 (tr) 2018-11-21
PE20170946A1 (es) 2017-07-13
SI3218365T1 (sl) 2018-12-31
SMT201800570T1 (it) 2019-01-11
WO2016075063A1 (en) 2016-05-19
EA032339B1 (ru) 2019-05-31
IL252089B (en) 2020-03-31
GT201700099A (es) 2019-07-29
HRP20181698T1 (hr) 2018-12-28
GEP20196949B (en) 2019-02-25
CA2965563A1 (en) 2016-05-19
TW201628616A (zh) 2016-08-16
CN107074836A (zh) 2017-08-18
CN107074836B (zh) 2020-03-27
RS57946B1 (sr) 2019-01-31
KR20170081184A (ko) 2017-07-11
US9346797B1 (en) 2016-05-24
EP3461483A1 (en) 2019-04-03
JO3458B1 (ar) 2020-07-05
IL252089A0 (en) 2017-07-31
NI201700055A (es) 2017-09-22
MA40955A (fr) 2017-09-20
JP6629320B2 (ja) 2020-01-15
CR20170186A (es) 2017-07-27
ECSP17028459A (es) 2017-08-31
PH12017500841B1 (en) 2017-10-30
UA119576C2 (uk) 2019-07-10
JP2017533245A (ja) 2017-11-09
DOP2017000117A (es) 2017-07-31
TWI690318B (zh) 2020-04-11
LT3218365T (lt) 2018-12-10
EP3218365A1 (en) 2017-09-20
SV2017005435A (es) 2017-07-19
US20190000823A1 (en) 2019-01-03
US10045974B2 (en) 2018-08-14
BR112017009583A2 (pt) 2017-12-26
AU2015345258A1 (en) 2017-05-04
US20170319564A1 (en) 2017-11-09
ZA201702797B (en) 2019-05-29
HUE040304T2 (hu) 2019-02-28
ES2694860T3 (es) 2018-12-27
PL3218365T3 (pl) 2019-02-28
US10603310B2 (en) 2020-03-31
PH12017500841A1 (en) 2017-10-30
TN2017000144A1 (en) 2018-10-19
CL2017001112A1 (es) 2017-12-01
AU2015345258B2 (en) 2020-05-21
CO2017004465A2 (es) 2017-07-19
RU2017116196A (ru) 2018-12-14
RU2017116196A3 (me) 2019-05-14
SG11201703547XA (en) 2017-05-30
US20160130267A1 (en) 2016-05-12
CY1120846T1 (el) 2020-05-29

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