AR089781A1 - Fluorometil-5,6-dihidro-4h-[1,3]oxazinas - Google Patents

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

Info

Publication number
AR089781A1
AR089781A1 ARP130100195A ARP130100195A AR089781A1 AR 089781 A1 AR089781 A1 AR 089781A1 AR P130100195 A ARP130100195 A AR P130100195A AR P130100195 A ARP130100195 A AR P130100195A AR 089781 A1 AR089781 A1 AR 089781A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
alkoxy
alkynyl
cyano
Prior art date
Application number
ARP130100195A
Other languages
English (en)
Inventor
Hilpert Hans
Humm Roland
Woltering Thomas
Original Assignee
Hoffmann La Roche
Siena Biotech Spa
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, Siena Biotech Spa filed Critical Hoffmann La Roche
Publication of AR089781A1 publication Critical patent/AR089781A1/es

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Classifications

    • 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

Con actividad inhibidora de la BACE1, su obtención, composiciones farmacéuticas que lo contienen y su utilización como sustancias terapéuticamente activas, son útiles para el tratamiento terapéutico y/o profiláctico p. ej. de la enfermedad de Alzheimer. Reivindicación 1: Un compuesto de la fórmula (1), en la que: R¹ se elige entre el grupo formado por: i) arilo, ii) arilo sustituido por 1 - 4 sustituyentes elegidos individualmente entre ciano, ciano-alquilo C₁₋₆, halógeno, halógeno-alcoxi C₁₋₆, halógeno-alquilo C₁₋₆, alcoxi C₁₋₆, (alcoxi C₁₋₆)-alquilo C₁₋₆, (alquinil C₂₋₆)-alcoxi C₁₋₆, alquinilo C₂₋₆ y alquilo C₁₋₆, iii) heteroarilo y iv) heteroarilo sustituido por 1 - 4 sustituyentes elegidos individualmente entre ciano, ciano-alquilo C₁₋₆, halógeno, halógeno-alcoxi C₁₋₆, halógeno-alquilo C₁₋₆, alcoxi C₁₋₆, (alcoxi C₁₋₆)-alquilo C₁₋₆, (alquinil C₂₋₆)-alcoxi C₁₋₆, alquinilo C₂₋₆ y alquilo C₁₋₆; R² se elige entre el grupo formado por: i) hidrógeno, ii) alquilo C₁₋₆ y iii) halógeno; R³ se elige entre el grupo formado por: i) alquilo C₁₋₆ y ii) halógeno-alquilo C₁₋₆; R⁴ es halógeno-alquilo C₁₋₆; o las sales farmacéuticamente aceptables del mismo.
ARP130100195A 2012-01-26 2013-01-23 Fluorometil-5,6-dihidro-4h-[1,3]oxazinas AR089781A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12152686 2012-01-26

Publications (1)

Publication Number Publication Date
AR089781A1 true AR089781A1 (es) 2014-09-17

Family

ID=47603713

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130100195A AR089781A1 (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)

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KR20130018370A (ko) 2008-06-13 2013-02-20 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
WO2011071135A1 (ja) † 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
CA2896185A1 (en) * 2013-01-22 2014-07-31 F. Hoffmann-La Roche Ag Fluoro-[1,3]oxazines as bace1 inhibitors
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
WO2014166906A1 (en) 2013-04-11 2014-10-16 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
MX2017001794A (es) 2014-08-08 2017-06-29 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
RU2712272C2 (ru) 2015-03-20 2020-01-28 Ф. Хоффманн-Ля Рош Аг Ингибиторы бета-секретазы
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
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

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CN103936690B (zh) * 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
US20100035865A1 (en) * 2007-04-03 2010-02-11 Pfizer Inc Sulfonamides and Pharmaceutical Compositions Thereof
EP2151435A4 (en) * 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Also Published As

Publication number Publication date
US9067926B2 (en) 2015-06-30
AU2013211646B2 (en) 2017-09-14
JP2015504906A (ja) 2015-02-16
IL232764A (en) 2015-10-29
MX354173B (es) 2018-02-16
NZ625684A (en) 2016-02-26
WO2013110622A1 (en) 2013-08-01
TW201335153A (zh) 2013-09-01
TWI472528B (zh) 2015-02-11
IL232764A0 (en) 2014-07-31
BR112014015630A2 (pt) 2017-06-13
EA201491321A1 (ru) 2014-11-28
CL2014001838A1 (es) 2014-11-07
CA2856892A1 (en) 2013-08-01
CO6960553A2 (es) 2014-05-30
US20150031690A1 (en) 2015-01-29
EP2807155B1 (en) 2017-04-12
BR112014015630B1 (pt) 2022-05-17
BR112014015630A8 (pt) 2021-03-16
KR20140117625A (ko) 2014-10-07
CR20140306A (es) 2014-11-17
SG11201403956VA (en) 2014-10-30
PH12014501334B1 (en) 2014-09-15
MA35748B1 (fr) 2014-12-01
PH12014501334A1 (en) 2014-09-15
CN104066727B (zh) 2019-04-26
UA113538C2 (xx) 2017-02-10
EP2807155A1 (en) 2014-12-03
JP5869151B2 (ja) 2016-02-24
AU2013211646A1 (en) 2014-06-05
CA2856892C (en) 2020-05-12
PE20142376A1 (es) 2015-01-17
HK1197242A1 (en) 2015-01-09
EA027059B1 (ru) 2017-06-30
CN104066727A (zh) 2014-09-24
MX2014008446A (es) 2015-02-24
KR101669349B1 (ko) 2016-10-25

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