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CO2017004530A2 - 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1 - Google Patents

2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1

Info

Publication number
CO2017004530A2
CO2017004530A2 CONC2017/0004530A CO2017004530A CO2017004530A2 CO 2017004530 A2 CO2017004530 A2 CO 2017004530A2 CO 2017004530 A CO2017004530 A CO 2017004530A CO 2017004530 A2 CO2017004530 A2 CO 2017004530A2
Authority
CO
Colombia
Prior art keywords
tetrahydropyridines
difluoro
phenyl
amino
methyl
Prior art date
Application number
CONC2017/0004530A
Other languages
English (en)
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 CO2017004530A2 publication Critical patent/CO2017004530A2/es

Links

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
    • A61K31/444—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

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

Abstract

La presente invención se dirige a compuestos de acuerdo con la Fórmula I, compuestos que son inhibidores de la enzima BACE1. Aspectos separados de la invención se dirigen a composiciones farmacéuticas que comprenden dichos compuestos y a usos de los compuestos para tratar trastornos para los cuales la reducción de depósitos de Aβ es beneficiosa tal como la enfermedad de Alzheimer.
CONC2017/0004530A 2014-11-10 2017-05-05 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1 CO2017004530A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201400649 2014-11-10
DKPA201500450 2015-08-07
PCT/EP2015/076014 WO2016075062A1 (en) 2014-11-10 2015-11-09 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer's disease

Publications (1)

Publication Number Publication Date
CO2017004530A2 true CO2017004530A2 (es) 2017-07-28

Family

ID=54476983

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0004530A CO2017004530A2 (es) 2014-11-10 2017-05-05 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1

Country Status (26)

Country Link
US (1) US10059669B2 (es)
EP (1) EP3218362B1 (es)
JP (1) JP2017533253A (es)
KR (1) KR20170082529A (es)
CN (1) CN107074809A (es)
AU (1) AU2015345257A1 (es)
BR (1) BR112017009647A2 (es)
CA (1) CA2964305A1 (es)
CL (1) CL2017001113A1 (es)
CO (1) CO2017004530A2 (es)
CR (1) CR20170187A (es)
DO (1) DOP2017000118A (es)
EA (1) EA201790817A1 (es)
EC (1) ECSP17028463A (es)
ES (1) ES2710602T3 (es)
IL (1) IL252091A0 (es)
MX (1) MX2017006048A (es)
NI (1) NI201700056A (es)
PE (1) PE20170947A1 (es)
PH (1) PH12017500829A1 (es)
RU (1) RU2017116197A (es)
SG (1) SG11201703177WA (es)
SV (1) SV2017005434A (es)
TN (1) TN2017000134A1 (es)
WO (1) WO2016075062A1 (es)
ZA (1) ZA201702799B (es)

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* Cited by examiner, † Cited by third party
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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
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
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
CA2993630A1 (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-tetrahydropyridines as bace1 inhibitors
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
CN106366073B (zh) * 2016-10-24 2018-11-30 扬子江药业集团南京海陵药业有限公司 一种盐酸替吡嘧啶的制备方法
HUE050403T2 (hu) 2016-10-28 2020-12-28 H Lundbeck As Imidazopirazinonokkal végzett kombinációs kezelések pszichiátriai és/vagy kognitív betegségek kezelésére
WO2018078042A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising administration of imidazopyrazinones
TW201829394A (zh) * 2016-12-21 2018-08-16 丹麥商Ｈ 朗德貝克公司 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
HRP20211784T1 (hr) 2017-12-14 2022-02-18 H. Lundbeck A/S Kombinacijski tretmani koji se sastoje od primjene 1h-pirazolo[4,3-b]piridina
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
CN109970681A (zh) * 2019-04-19 2019-07-05 安徽海康药业有限责任公司 一种瑞格列奈的合成方法
CN113720930A (zh) * 2021-07-26 2021-11-30 南京一诺医药科技有限公司 一种hplc-ms/ms联用检测人血浆中奥美拉唑的方法
CN114235985A (zh) * 2021-11-25 2022-03-25 南京海纳医药科技股份有限公司 一种hplc-ms/ms联用检测人血浆中胍法辛的方法

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GB0124928D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
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AP2016009370A0 (en) 2014-02-19 2016-08-31 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
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
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
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
CA2993630A1 (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-tetrahydropyridines as bace1 inhibitors

Also Published As

Publication number Publication date
CR20170187A (es) 2018-02-01
KR20170082529A (ko) 2017-07-14
WO2016075062A1 (en) 2016-05-19
MX2017006048A (es) 2017-06-19
NI201700056A (es) 2017-09-22
JP2017533253A (ja) 2017-11-09
ES2710602T3 (es) 2019-04-26
US10059669B2 (en) 2018-08-28
ECSP17028463A (es) 2017-08-31
PE20170947A1 (es) 2017-07-13
SG11201703177WA (en) 2017-05-30
IL252091A0 (en) 2017-07-31
PH12017500829A1 (en) 2017-10-09
TN2017000134A1 (en) 2018-10-19
RU2017116197A (ru) 2018-12-13
CN107074809A (zh) 2017-08-18
EA201790817A1 (ru) 2017-09-29
DOP2017000118A (es) 2017-07-15
CA2964305A1 (en) 2016-05-19
US20170313658A1 (en) 2017-11-02
BR112017009647A2 (pt) 2017-12-19
AU2015345257A1 (en) 2017-05-04
EP3218362B1 (en) 2019-01-09
ZA201702799B (en) 2018-08-29
EP3218362A1 (en) 2017-09-20
SV2017005434A (es) 2017-07-19
CL2017001113A1 (es) 2017-12-01

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