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PE20142450A1 - Difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos como inhibidores de bace1 - Google Patents

Difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos como inhibidores de bace1

Info

Publication number
PE20142450A1
PE20142450A1 PE2014002406A PE2014002406A PE20142450A1 PE 20142450 A1 PE20142450 A1 PE 20142450A1 PE 2014002406 A PE2014002406 A PE 2014002406A PE 2014002406 A PE2014002406 A PE 2014002406A PE 20142450 A1 PE20142450 A1 PE 20142450A1
Authority
PE
Peru
Prior art keywords
difluoro
hexahydro
cyclopentaoxacinyls
benzooxacinyls
bace1 inhibitors
Prior art date
Application number
PE2014002406A
Other languages
English (en)
Inventor
Hans Hilpert
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20142450A1 publication Critical patent/PE20142450A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/041,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/121,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • 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
    • C07D413/10Heterocyclic 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 carbon chain containing aromatic rings

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE DIFLUORO-CICLOPENTAOXACINILOS Y DIFLUOROENZOOXACINILOS DE FORMULA (I) DONDE R1, R2, R3, R4, R5 Y n SON COMO SE DESCRIBEN EN EL PRESENTE. SON COMPUESTOS PREFERIDOS: [3-((4S,4aR,7aR)-2-AMINO-5,5-DIFLUORO-4-METIL-4,4a,5,6,7,7a-HEXAHIDRO-CICLOPENTA[e][1,3]OXAZIN-4-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-BUT-2-INILOXI-PIRAZINA-2-CARBOXILICO; [3-((4S,4aR,7aR)-2-AMINO-5,5-DIFLUORO-4-METIL-4,4a,5,6,7,7a-HEXAHIDRO-CICLOPENTA[e][1,3]OXAZIN-4-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-FLUOROMETIL-PIRAZINA-2-CARBOXILICO; ENTRE OTROS. TAMBIEN SE REFIERE A COMPOSICIONES FARMACEUTICAS. DICHOS COMPUESTOS TIENEN ACTIVIDAD INHIBIDORA BACE1 SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER
PE2014002406A 2012-06-26 2013-06-24 Difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos como inhibidores de bace1 PE20142450A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12173690 2012-06-26

Publications (1)

Publication Number Publication Date
PE20142450A1 true PE20142450A1 (es) 2015-01-28

Family

ID=48672630

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014002406A PE20142450A1 (es) 2012-06-26 2013-06-24 Difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos como inhibidores de bace1

Country Status (22)

Country Link
US (1) US9181232B2 (es)
EP (1) EP2864324B1 (es)
JP (1) JP6251257B2 (es)
KR (1) KR20150023450A (es)
CN (1) CN104470915B (es)
AU (1) AU2013283524B2 (es)
BR (1) BR112014029742A2 (es)
CA (1) CA2872181A1 (es)
CL (1) CL2014003325A1 (es)
CO (1) CO7151509A2 (es)
CR (1) CR20140528A (es)
EA (1) EA025273B1 (es)
HK (1) HK1206344A1 (es)
IL (1) IL236138A (es)
MA (1) MA37763B1 (es)
MX (1) MX2014014937A (es)
NZ (1) NZ702253A (es)
PE (1) PE20142450A1 (es)
PH (1) PH12014502623B1 (es)
SG (1) SG11201407576YA (es)
UA (1) UA113309C2 (es)
WO (1) WO2014001228A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
PH12012501081A1 (en) 2009-12-11 2012-10-29 Shionogi & Co Oxazine derivatives
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9296734B2 (en) 2013-03-01 2016-03-29 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EA201591614A1 (ru) 2013-03-08 2015-12-30 Эмджен Инк. Соединения 1,3-оксазин-2-амина, конденсированные с перфторированным циклопропилом, в качестве ингибиторов бета-секретазы и способы их применения
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
CA2957544C (en) 2014-08-08 2023-01-24 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
RU2712272C2 (ru) 2015-03-20 2020-01-28 Ф. Хоффманн-Ля Рош Аг Ингибиторы бета-секретазы
JP7353708B2 (ja) * 2018-04-27 2023-10-02 塩野義製薬株式会社 選択的bace1阻害活性を有するテトラヒドロピラノオキサジン誘導体

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
GB0912778D0 (en) * 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
PH12012501081A1 (en) * 2009-12-11 2012-10-29 Shionogi & Co Oxazine derivatives
UA103272C2 (uk) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2

Also Published As

Publication number Publication date
US9181232B2 (en) 2015-11-10
PH12014502623A1 (en) 2015-01-21
NZ702253A (en) 2016-06-24
MA37763B1 (fr) 2017-05-31
EP2864324B1 (en) 2018-03-28
CO7151509A2 (es) 2014-12-29
CR20140528A (es) 2015-01-12
PH12014502623B1 (en) 2015-01-21
HK1206344A1 (en) 2016-01-08
MX2014014937A (es) 2015-03-09
US20150133440A1 (en) 2015-05-14
UA113309C2 (xx) 2017-01-10
JP2015521640A (ja) 2015-07-30
AU2013283524A1 (en) 2014-11-13
WO2014001228A1 (en) 2014-01-03
SG11201407576YA (en) 2015-03-30
AU2013283524B2 (en) 2017-03-30
EA201590066A1 (ru) 2015-04-30
JP6251257B2 (ja) 2017-12-20
EA025273B1 (ru) 2016-12-30
CA2872181A1 (en) 2014-01-03
IL236138A (en) 2016-10-31
KR20150023450A (ko) 2015-03-05
CL2014003325A1 (es) 2015-04-24
IL236138A0 (en) 2015-02-01
MA37763A1 (fr) 2016-08-31
EP2864324A1 (en) 2015-04-29
BR112014029742A2 (pt) 2017-06-27
CN104470915B (zh) 2019-07-26
CN104470915A (zh) 2015-03-25

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