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PE20142376A1 - Fluormetil-5,6-dihidro-4h-[1,3]oxazinas - Google Patents

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

Info

Publication number
PE20142376A1
PE20142376A1 PE2014001177A PE2014001177A PE20142376A1 PE 20142376 A1 PE20142376 A1 PE 20142376A1 PE 2014001177 A PE2014001177 A PE 2014001177A PE 2014001177 A PE2014001177 A PE 2014001177A PE 20142376 A1 PE20142376 A1 PE 20142376A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
fluormethyl
dihydro
oxazines
Prior art date
Application number
PE2014001177A
Other languages
English (en)
Inventor
Hans Hilpert
Roland Humm
Thomas Johannes Woltering
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 PE20142376A1 publication Critical patent/PE20142376A1/es

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    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Transplantation (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

REFERIDA A UN COMPUESTO DERIVADO DE FLUORMETIL-5,6-DIHIDRO-4H-[1,3]OXAZINA DE FORMULA (I), DONDE R1 ES ARILO, HETEROARILO, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, HALOGENO; R3 ES ALQUILO C1-C6, HALOGENO-ALQUILO C1-C6; R4 ES HALOGENO-ALQUILO C1-C6. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA BACE1 QUE ES LA ENZIMA QUE ROMPE LA PROTEINA PRECURSORA DEL AMILOIDE BETA POR EL SITIO BETA Y SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, ENTRE OTRAS
PE2014001177A 2012-01-26 2013-01-23 Fluormetil-5,6-dihidro-4h-[1,3]oxazinas PE20142376A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20142376A1 true PE20142376A1 (es) 2015-01-17

Family

ID=47603713

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014001177A PE20142376A1 (es) 2012-01-26 2013-01-23 Fluormetil-5,6-dihidro-4h-[1,3]oxazinas

Country Status (23)

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)
IL (1) IL232764A (es)
MA (1) MA35748B1 (es)
MX (1) MX354173B (es)
NZ (1) NZ625684A (es)
PE (1) PE20142376A1 (es)
PH (1) PH12014501334B1 (es)
SG (1) SG11201403956VA (es)
TW (1) TWI472528B (es)
UA (1) UA113538C2 (es)
WO (1) WO2013110622A1 (es)

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EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
CN102834384A (zh) 2009-12-11 2012-12-19 盐野义制药株式会社 *嗪衍生物
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
RU2015132181A (ru) * 2013-01-22 2017-03-02 Ф. Хоффманн-Ля Рош Аг Фтор-[1,3]-оксазины в качестве ингибиторов васе1
MX366855B (es) * 2013-03-01 2019-07-26 Amgen Inc Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.
MX374512B (es) 2013-03-08 2025-03-06 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso.
EA027860B1 (ru) 2013-04-11 2017-09-29 Ф. Хоффманн-Ля Рош Аг ИНГИБИТОРЫ β-СЕКРЕТАЗЫ 1 (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 (en) 2014-07-04 2016-01-07 F. Hoffmann-La Roche Ag Fluoro-[1,3]oxazines as bace1 inhibitors
EP3177618A1 (en) 2014-08-08 2017-06-14 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
MX2017008083A (es) * 2014-12-18 2017-10-31 Janssen Pharmaceutica Nv Compuestos 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2h-pirrol-5-amina inhibidores de beta-secretasa.
JP6674960B2 (ja) 2015-03-20 2020-04-01 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Bace1阻害剤
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

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ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
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
EP2689780A1 (en) * 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
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GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
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UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
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CN102834384A (zh) * 2009-12-11 2012-12-19 盐野义制药株式会社 *嗪衍生物
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
IL232764A0 (en) 2014-07-31
EA027059B1 (ru) 2017-06-30
WO2013110622A1 (en) 2013-08-01
NZ625684A (en) 2016-02-26
CN104066727A (zh) 2014-09-24
CA2856892A1 (en) 2013-08-01
CR20140306A (es) 2014-11-17
PH12014501334A1 (en) 2014-09-15
CO6960553A2 (es) 2014-05-30
CL2014001838A1 (es) 2014-11-07
UA113538C2 (xx) 2017-02-10
MA35748B1 (fr) 2014-12-01
KR101669349B1 (ko) 2016-10-25
MX354173B (es) 2018-02-16
EP2807155A1 (en) 2014-12-03
EP2807155B1 (en) 2017-04-12
JP5869151B2 (ja) 2016-02-24
US9067926B2 (en) 2015-06-30
HK1197242A1 (en) 2015-01-09
AU2013211646A1 (en) 2014-06-05
CN104066727B (zh) 2019-04-26
BR112014015630A8 (pt) 2021-03-16
IL232764A (en) 2015-10-29
JP2015504906A (ja) 2015-02-16
AR089781A1 (es) 2014-09-17
PH12014501334B1 (en) 2014-09-15
BR112014015630B1 (pt) 2022-05-17
EA201491321A1 (ru) 2014-11-28
SG11201403956VA (en) 2014-10-30
KR20140117625A (ko) 2014-10-07
AU2013211646B2 (en) 2017-09-14
US20150031690A1 (en) 2015-01-29
TWI472528B (zh) 2015-02-11
CA2856892C (en) 2020-05-12
MX2014008446A (es) 2015-02-24
BR112014015630A2 (pt) 2017-06-13
TW201335153A (zh) 2013-09-01

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