MA35748B1 - Fluorométhyl-5,6-dihydro-4h-[1,3]oxazines - Google Patents

Fluorométhyl-5,6-dihydro-4h-[1,3]oxazines

Info

Publication number
MA35748B1
MA35748B1 MA37156A MA37156A MA35748B1 MA 35748 B1 MA35748 B1 MA 35748B1 MA 37156 A MA37156 A MA 37156A MA 37156 A MA37156 A MA 37156A MA 35748 B1 MA35748 B1 MA 35748B1
Authority
MA
Morocco
Prior art keywords
oxazine
fluoromethyl
dihydro
present
compounds
Prior art date
Application number
MA37156A
Other languages
English (en)
Inventor
Hans Hilpert
Roland Humm
Thomas Woltering
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 MA35748B1 publication Critical patent/MA35748B1/fr

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La présente invention concerne des composés de formule (i) ayant une activité d'inhibition de la bace1, leur fabrication, des compositions pharmaceutiques les contenant et leur utilisation comme substances thérapeutiquement actives. Les composés actifs de la présente invention sont utiles dans le traitement thérapeutique et/ou prophylactique par exemple de la maladie d'alzheimer.
MA37156A 2012-01-26 2014-06-25 Fluorométhyl-5,6-dihydro-4h-[1,3]oxazines MA35748B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12152686 2012-01-26
PCT/EP2013/051166 WO2013110622A1 (fr) 2012-01-26 2013-01-23 Fluorométhyl-5,6-dihydro-4h-[1,3]oxazines

Publications (1)

Publication Number Publication Date
MA35748B1 true MA35748B1 (fr) 2014-12-01

Family

ID=47603713

Family Applications (1)

Application Number Title Priority Date Filing Date
MA37156A MA35748B1 (fr) 2012-01-26 2014-06-25 Fluorométhyl-5,6-dihydro-4h-[1,3]oxazines

Country Status (23)

Country Link
US (1) US9067926B2 (fr)
EP (1) EP2807155B1 (fr)
JP (1) JP5869151B2 (fr)
KR (1) KR101669349B1 (fr)
CN (1) CN104066727B (fr)
AR (1) AR089781A1 (fr)
AU (1) AU2013211646B2 (fr)
BR (1) BR112014015630B1 (fr)
CA (1) CA2856892C (fr)
CL (1) CL2014001838A1 (fr)
CO (1) CO6960553A2 (fr)
CR (1) CR20140306A (fr)
EA (1) EA027059B1 (fr)
IL (1) IL232764A (fr)
MA (1) MA35748B1 (fr)
MX (1) MX354173B (fr)
NZ (1) NZ625684A (fr)
PE (1) PE20142376A1 (fr)
PH (1) PH12014501334B1 (fr)
SG (1) SG11201403956VA (fr)
TW (1) TWI472528B (fr)
UA (1) UA113538C2 (fr)
WO (1) WO2013110622A1 (fr)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009151098A1 (fr) 2008-06-13 2009-12-17 塩野義製薬株式会社 DÉRIVÉ HÉTÉROCYCLIQUE CONTENANT DU SOUFRE AYANT UNE ACTIVITÉ INHIBANT LA β-SÉCRÉTASE
UA110467C2 (uk) † 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
EP2912035A4 (fr) 2012-10-24 2016-06-15 Shionogi & Co Dérivés de dihydrooxazine ou d'oxazépine ayant une activité inhibitrice de bace1
HK1210609A1 (en) * 2013-01-22 2016-04-29 霍夫曼-拉罗奇有限公司 Fluoro-[1,3]oxazines as bace1 inhibitors
CA2902212C (fr) * 2013-03-01 2020-10-13 Amgen Inc. Composes perfluores 5,6-dihydro-4h-1,3-oxazine-2-amine substitues en tant qu'inhibiteurs de la beta-secretase et procedes d'utilisation correspondants
AU2014225604B2 (en) 2013-03-08 2018-05-17 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
PE20151748A1 (es) 2013-04-11 2015-12-02 Hoffmann La Roche Inhibidores de bace1
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
WO2016001266A1 (fr) 2014-07-04 2016-01-07 F. Hoffmann-La Roche Ag Fluoro-[1,3]oxazines en tant qu'inhibiteurs de bace1
AU2015301028B2 (en) 2014-08-08 2019-09-26 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
CA2967164A1 (fr) * 2014-12-18 2016-06-23 Janssen Pharmaceutica Nv Composes fr 2,3,4,5-tetrahydropyridine-6-amine et 3,4-dihydro-2 h-pyrrol-5-amine inhibiteurs de la beta-secretase
AU2016236402B2 (en) 2015-03-20 2019-08-01 F. Hoffmann-La Roche Ag BACE1 inhibitors
WO2017061534A1 (fr) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dérivés de dihydrothiazine
JP2017071603A (ja) * 2015-10-09 2017-04-13 塩野義製薬株式会社 ジヒドロチアジンまたはジヒドロオキサジン誘導体を含有する医薬組成物
US11629154B2 (en) 2018-04-27 2023-04-18 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
CN111892550B (zh) * 2020-08-25 2022-07-19 苏州大学 4-苯基-6h-1,3-噁嗪-6-酮衍生物及其制备和应用

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2612854B1 (fr) * 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Dérivés d'aminothiazolidine et d'aminotétrahydrothiazepine comme inhibiteurs de BACE 1
EP2142505A1 (fr) * 2007-04-03 2010-01-13 Pfizer, Inc. Sulfonamides et compositions pharmaceutiques les contenant
WO2008133273A1 (fr) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. Composition pharmaceutique pour le traitement de la maladie d'alzheimer
TW200902526A (en) * 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
ES2548774T3 (es) 2008-01-18 2015-10-20 Eisai R&D Management Co., Ltd. Derivado de aminodihidrotiazina condensado
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
AR077328A1 (es) * 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8188079B2 (en) * 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011058763A1 (fr) * 2009-11-13 2011-05-19 塩野義製薬株式会社 Dérivé d'aminothiazine ou d'aminooxazine contenant un lieur amino
UA110467C2 (uk) * 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
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
JPWO2011071109A1 (ja) * 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
US8415483B2 (en) 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
US9067924B2 (en) 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors

Also Published As

Publication number Publication date
AR089781A1 (es) 2014-09-17
CN104066727B (zh) 2019-04-26
JP2015504906A (ja) 2015-02-16
KR101669349B1 (ko) 2016-10-25
BR112014015630A2 (pt) 2017-06-13
EP2807155A1 (fr) 2014-12-03
CA2856892C (fr) 2020-05-12
US9067926B2 (en) 2015-06-30
PH12014501334A1 (en) 2014-09-15
CO6960553A2 (es) 2014-05-30
IL232764A (en) 2015-10-29
MX2014008446A (es) 2015-02-24
BR112014015630A8 (pt) 2021-03-16
US20150031690A1 (en) 2015-01-29
CR20140306A (es) 2014-11-17
NZ625684A (en) 2016-02-26
HK1197242A1 (en) 2015-01-09
UA113538C2 (xx) 2017-02-10
BR112014015630B1 (pt) 2022-05-17
PH12014501334B1 (en) 2014-09-15
JP5869151B2 (ja) 2016-02-24
EA201491321A1 (ru) 2014-11-28
KR20140117625A (ko) 2014-10-07
IL232764A0 (en) 2014-07-31
AU2013211646A1 (en) 2014-06-05
CA2856892A1 (fr) 2013-08-01
TW201335153A (zh) 2013-09-01
EP2807155B1 (fr) 2017-04-12
CL2014001838A1 (es) 2014-11-07
PE20142376A1 (es) 2015-01-17
SG11201403956VA (en) 2014-10-30
EA027059B1 (ru) 2017-06-30
CN104066727A (zh) 2014-09-24
AU2013211646B2 (en) 2017-09-14
WO2013110622A1 (fr) 2013-08-01
MX354173B (es) 2018-02-16
TWI472528B (zh) 2015-02-11

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