MX2014008446A - Fluorometil-5,6-dihidro-4h-[1,3]oxazinas. - Google Patents

Fluorometil-5,6-dihidro-4h-[1,3]oxazinas.

Info

Publication number
MX2014008446A
MX2014008446A MX2014008446A MX2014008446A MX2014008446A MX 2014008446 A MX2014008446 A MX 2014008446A MX 2014008446 A MX2014008446 A MX 2014008446A MX 2014008446 A MX2014008446 A MX 2014008446A MX 2014008446 A MX2014008446 A MX 2014008446A
Authority
MX
Mexico
Prior art keywords
oxazines
fluoromethyl
dihydro
present
alzheimer
Prior art date
Application number
MX2014008446A
Other languages
English (en)
Other versions
MX354173B (es
Inventor
Thomas Woltering
Hans Hilpert
Roland Humm
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 MX2014008446A publication Critical patent/MX2014008446A/es
Publication of MX354173B publication Critical patent/MX354173B/es

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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

Abstract

La presente invención se refiere a un compuesto de la fórmula I (ver Fórmula) que tiene actividad inhibidora de la BACE1, su producción, composiciones farmacéuticas que lo contienen y su uso como sustancias terapéuticamente activas. Los compuestos activos de la presente invención son útiles para el tratamiento terapéutico y/o profiláctico por ejemplo de la enfermedad de Alzheimer.
MX2014008446A 2012-01-26 2013-01-23 Fluorometil-5,6-dihidro-4h-[1,3]oxazinas. MX354173B (es)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
MX2014008446A true MX2014008446A (es) 2015-02-24
MX354173B MX354173B (es) 2018-02-16

Family

ID=47603713

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014008446A MX354173B (es) 2012-01-26 2013-01-23 Fluorometil-5,6-dihidro-4h-[1,3]oxazinas.

Country Status (24)

Country Link
US (1) US9067926B2 (es)
EP (1) EP2807155B1 (es)
JP (1) JP5869151B2 (es)
KR (1) KR101669349B1 (es)
CN (1) CN104066727B (es)
AR (1) AR089781A1 (es)
AU (1) AU2013211646B2 (es)
BR (1) BR112014015630B1 (es)
CA (1) CA2856892C (es)
CL (1) CL2014001838A1 (es)
CO (1) CO6960553A2 (es)
CR (1) CR20140306A (es)
EA (1) EA027059B1 (es)
HK (1) HK1197242A1 (es)
IL (1) IL232764A (es)
MA (1) MA35748B1 (es)
MX (1) MX354173B (es)
NZ (1) NZ625684A (es)
PE (1) PE20142376A1 (es)
PH (1) PH12014501334A1 (es)
SG (1) SG11201403956VA (es)
TW (1) TWI472528B (es)
UA (1) UA113538C2 (es)
WO (1) WO2013110622A1 (es)

Families Citing this family (15)

* 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
BR112012013854A2 (pt) 2009-12-11 2019-09-24 Shionogi & Co derivados de oxazina.
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
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
WO2014134341A1 (en) * 2013-03-01 2014-09-04 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP2964644B1 (en) 2013-03-08 2018-12-26 Amgen, Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CA2900433C (en) 2013-04-11 2021-06-22 F. Hoffmann-La Roche Ag 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 (en) 2014-07-04 2016-01-07 F. Hoffmann-La Roche Ag Fluoro-[1,3]oxazines as bace1 inhibitors
WO2016022724A1 (en) 2014-08-08 2016-02-11 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
SG11201707050VA (en) 2015-03-20 2017-10-30 Hoffmann La Roche Bace1 inhibitors
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
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
KR20210003872A (ko) 2018-04-27 2021-01-12 시오노기 앤드 컴파니, 리미티드 선택적 bace1 억제 활성을 갖는 테트라하이드로피라노옥사진 유도체
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
JP2010523540A (ja) * 2007-04-03 2010-07-15 ファイザー・インク スルホンアミドおよびその医薬組成物
JP5383483B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
JP5383484B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
CA2711655C (en) 2008-01-18 2013-03-05 Eisai R&D Management Co., Ltd. Condensed aminodihydrothiazine derivative
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
US20120238557A1 (en) * 2009-11-13 2012-09-20 Shionogi & Co., Ltd. Aminothiazine or aminooxazine derivative having amino linker
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
US20120245155A1 (en) * 2009-12-11 2012-09-27 Shionogi & Co., Ltd. Fused heterocyclic compound having amino group
BR112012013854A2 (pt) * 2009-12-11 2019-09-24 Shionogi & Co derivados de oxazina.
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
PH12014501334B1 (en) 2014-09-15
AU2013211646B2 (en) 2017-09-14
PH12014501334A1 (en) 2014-09-15
BR112014015630A8 (pt) 2021-03-16
NZ625684A (en) 2016-02-26
PE20142376A1 (es) 2015-01-17
EP2807155B1 (en) 2017-04-12
JP2015504906A (ja) 2015-02-16
MA35748B1 (fr) 2014-12-01
HK1197242A1 (en) 2015-01-09
CL2014001838A1 (es) 2014-11-07
MX354173B (es) 2018-02-16
CA2856892A1 (en) 2013-08-01
US9067926B2 (en) 2015-06-30
BR112014015630A2 (pt) 2017-06-13
EP2807155A1 (en) 2014-12-03
SG11201403956VA (en) 2014-10-30
EA027059B1 (ru) 2017-06-30
CA2856892C (en) 2020-05-12
TW201335153A (zh) 2013-09-01
AU2013211646A1 (en) 2014-06-05
TWI472528B (zh) 2015-02-11
IL232764A0 (en) 2014-07-31
US20150031690A1 (en) 2015-01-29
CO6960553A2 (es) 2014-05-30
CR20140306A (es) 2014-11-17
UA113538C2 (xx) 2017-02-10
JP5869151B2 (ja) 2016-02-24
CN104066727A (zh) 2014-09-24
KR20140117625A (ko) 2014-10-07
WO2013110622A1 (en) 2013-08-01
KR101669349B1 (ko) 2016-10-25
EA201491321A1 (ru) 2014-11-28
IL232764A (en) 2015-10-29
BR112014015630B1 (pt) 2022-05-17
AR089781A1 (es) 2014-09-17
CN104066727B (zh) 2019-04-26

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