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PE20161225A1 - 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer - Google Patents

2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer

Info

Publication number
PE20161225A1
PE20161225A1 PE2016001299A PE2016001299A PE20161225A1 PE 20161225 A1 PE20161225 A1 PE 20161225A1 PE 2016001299 A PE2016001299 A PE 2016001299A PE 2016001299 A PE2016001299 A PE 2016001299A PE 20161225 A1 PE20161225 A1 PE 20161225A1
Authority
PE
Peru
Prior art keywords
trifluoro
amino
alzheimer
treatment
tetrahydropyridines
Prior art date
Application number
PE2016001299A
Other languages
English (en)
Inventor
Thomas Jensen
Lena Tagmose
Mauro Marigo
Karsten Juhl
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 PE20161225A1 publication Critical patent/PE20161225A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic 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
    • C07D211/72Heterocyclic 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
    • 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
    • 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
    • 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
    • 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
    • C07D227/00Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
    • C07D227/02Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D227/06Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D227/10Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invencion se refiere a un compuesto de formula (I) o una sal de la misma farmaceuticamente aceptable donde: Ar es fenilo, piridilo, entre otros; R1 es alquilo C1-C3 o fluoroalquilo C1-C3; R2 es H, halogeno, entre otros; R3 es alquilo C1-C3 o una sal de este. Son compuestos preferidos N-(3-((2R,5R)-6-amino-3,3,5-trifluoro-2,5-dimetil-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-fluoropicolinamida; N-(3-((2R,5R)-6-amino-3,3,5-trifluoro-2,5-dimetil-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-cloropicolinamida, entre otros. Dichos compuestos inhiben la enzima BACE1 y son utiles en el tratamiento del Alzheimer
PE2016001299A 2014-02-19 2015-02-17 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer PE20161225A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201400086 2014-02-19
DKPA201400349 2014-07-01

Publications (1)

Publication Number Publication Date
PE20161225A1 true PE20161225A1 (es) 2016-12-04

Family

ID=59009438

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001299A PE20161225A1 (es) 2014-02-19 2015-02-17 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer

Country Status (25)

Country Link
US (2) US20170066741A1 (es)
EP (1) EP3107897A1 (es)
JP (1) JP6483146B2 (es)
KR (1) KR20160115936A (es)
CN (1) CN106029639B (es)
AP (1) AP2016009370A0 (es)
AR (1) AR099489A1 (es)
AU (1) AU2015220873A1 (es)
CA (1) CA2940028A1 (es)
CL (1) CL2016002072A1 (es)
CR (1) CR20160352A (es)
DO (1) DOP2016000194A (es)
EA (1) EA031132B1 (es)
EC (1) ECSP16072941A (es)
GE (1) GEP20186892B (es)
IL (1) IL246875A0 (es)
MA (1) MA39225A1 (es)
MX (1) MX2016010777A (es)
PE (1) PE20161225A1 (es)
PH (1) PH12016501600A1 (es)
RU (1) RU2016133626A (es)
SG (1) SG11201606812WA (es)
TW (1) TW201609700A (es)
UA (1) UA117695C2 (es)
WO (1) WO2015124576A1 (es)

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CR20160352A (es) 2014-02-19 2016-10-20 H Lundbeck As 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como 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
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
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EP3347486A4 (en) * 2015-09-09 2019-06-19 The Trustees of Columbia University in the City of New York REDUCTION OF ER-MAM-LOCALIZED APP-C99 AND METHOD FOR THE TREATMENT OF ALZHEIMER DISEASE
TW201726651A (zh) * 2015-09-23 2017-08-01 健生藥品公司 2,3,4,5-四氫吡啶-6-胺衍生物
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
SG11201903770UA (en) 2016-10-28 2019-05-30 H Lundbeck As Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders
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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
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CN111601593B (zh) 2017-10-05 2022-04-15 弗尔康医疗公司 P38激酶抑制剂降低dux4和下游基因表达以用于治疗fshd
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
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
KR102507861B1 (ko) 2018-04-19 2023-03-09 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법
KR102510077B1 (ko) 2018-04-24 2023-03-14 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법
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Also Published As

Publication number Publication date
TW201609700A (zh) 2016-03-16
CN106029639A (zh) 2016-10-12
CN106029639B (zh) 2019-01-08
EA031132B1 (ru) 2018-11-30
PH12016501600A1 (en) 2017-02-06
US20150232449A1 (en) 2015-08-20
ECSP16072941A (es) 2017-02-24
EA201691447A1 (ru) 2016-12-30
CL2016002072A1 (es) 2017-01-20
CA2940028A1 (en) 2015-08-27
UA117695C2 (uk) 2018-09-10
US9353084B2 (en) 2016-05-31
WO2015124576A1 (en) 2015-08-27
JP2017506237A (ja) 2017-03-02
AR099489A1 (es) 2016-07-27
RU2016133626A3 (es) 2018-09-25
IL246875A0 (en) 2016-08-31
DOP2016000194A (es) 2016-09-30
CR20160352A (es) 2016-10-20
MX2016010777A (es) 2016-10-26
EP3107897A1 (en) 2016-12-28
RU2016133626A (ru) 2018-03-20
KR20160115936A (ko) 2016-10-06
JP6483146B2 (ja) 2019-03-13
AU2015220873A1 (en) 2016-08-11
GEP20186892B (en) 2018-09-10
MA39225A1 (fr) 2017-04-28
SG11201606812WA (en) 2016-09-29
US20170066741A1 (en) 2017-03-09
AP2016009370A0 (en) 2016-08-31

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