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)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (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
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
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
CN104968660A (zh) * 2013-01-22 2015-10-07 霍夫曼-拉罗奇有限公司 作为bace1抑制剂的氟-[1,3]噁嗪类化合物
AU2014223334C1 (en) * 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP2964644B1 (fr) 2013-03-08 2018-12-26 Amgen, Inc. Composés perfluorés à base de 1,3-oxazin-2-amine condensée avec un cyclopropyle en tant qu'inhibiteurs de la bêta-secrétase et leurs procédés d'utilisation
MY174747A (en) 2013-04-11 2020-05-13 Hoffmann La Roche Bace1 inhibitors
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
MX381482B (es) 2014-08-08 2025-03-12 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
JP2017538753A (ja) * 2014-12-18 2017-12-28 ヤンセン ファーマシューティカ エヌ．ベー． ２，３，４，５−テトラヒドロピリジン−６−アミンおよび３，４−ジヒドロ−２Ｈ−ピロール−５−アミンの化合物のβセクレターゼ阻害剤
CA2979113A1 (fr) 2015-03-20 2016-09-29 F. Hoffmann-La Roche Ag Inhibiteurs de bace1
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
BR112020021728A2 (pt) 2018-04-27 2021-01-26 Shionogi & Co., Ltd. derivados de tetra-hidropiranooxazina tendo atividade inibitória de bace1 seletiva
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
ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
WO2008120093A1 (fr) * 2007-04-03 2008-10-09 Pfizer Inc. Sulfonamides et compositions pharmaceutiques les contenant
AU2008245082B8 (en) * 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
EP2151435A4 (fr) * 2007-04-24 2011-09-14 Shionogi & Co Composition pharmaceutique pour le traitement de la maladie d'alzheimer
BRPI0906962B8 (pt) 2008-01-18 2021-05-25 Eisai R&D Man Co Ltd composto de aminodiidrotiazina fundido
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
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
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
CN102686584A (zh) * 2009-11-13 2012-09-19 盐野义制药株式会社 具有氨基连接基的氨基噻嗪或氨基噁嗪衍生物
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
RU2012129168A (ru) * 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
US20120245155A1 (en) * 2009-12-11 2012-09-27 Shionogi & Co., Ltd. Fused heterocyclic compound having amino group
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
CR20140306A (es) 2014-11-17
MX354173B (es) 2018-02-16
CL2014001838A1 (es) 2014-11-07
EP2807155B1 (fr) 2017-04-12
KR101669349B1 (ko) 2016-10-25
JP5869151B2 (ja) 2016-02-24
EA201491321A1 (ru) 2014-11-28
CA2856892A1 (fr) 2013-08-01
WO2013110622A1 (fr) 2013-08-01
CN104066727A (zh) 2014-09-24
EA027059B1 (ru) 2017-06-30
PE20142376A1 (es) 2015-01-17
CO6960553A2 (es) 2014-05-30
UA113538C2 (xx) 2017-02-10
AU2013211646A1 (en) 2014-06-05
PH12014501334A1 (en) 2014-09-15
BR112014015630A2 (pt) 2017-06-13
MX2014008446A (es) 2015-02-24
CN104066727B (zh) 2019-04-26
PH12014501334B1 (en) 2014-09-15
CA2856892C (fr) 2020-05-12
KR20140117625A (ko) 2014-10-07
TWI472528B (zh) 2015-02-11
AU2013211646B2 (en) 2017-09-14
TW201335153A (zh) 2013-09-01
NZ625684A (en) 2016-02-26
HK1197242A1 (en) 2015-01-09
IL232764A (en) 2015-10-29
BR112014015630A8 (pt) 2021-03-16
IL232764A0 (en) 2014-07-31
AR089781A1 (es) 2014-09-17
US9067926B2 (en) 2015-06-30
US20150031690A1 (en) 2015-01-29
SG11201403956VA (en) 2014-10-30
EP2807155A1 (fr) 2014-12-03
JP2015504906A (ja) 2015-02-16
BR112014015630B1 (pt) 2022-05-17

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