JP2014505688A - オキサジン誘導体および神経障害の処置におけるその使用 - Google Patents

オキサジン誘導体および神経障害の処置におけるその使用 Download PDF

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JP2014505688A
JP2014505688A JP2013548830A JP2013548830A JP2014505688A JP 2014505688 A JP2014505688 A JP 2014505688A JP 2013548830 A JP2013548830 A JP 2013548830A JP 2013548830 A JP2013548830 A JP 2013548830A JP 2014505688 A JP2014505688 A JP 2014505688A
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amino
phenyl
fluoro
dihydro
pyridine
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JP2014505688A5 (enExample
Inventor
コンスタンツェ・フルト
ライナー・マルティン・リュエント
ライナー・マッハウアー
ウルフ・ノイマン
ハインリッヒ・リューガー
ミヒャエル・シェーファー
マリナ・ティンテルノート−ブロムライ
シーム・ヤコブ・フェーンストラ
マルクス・フェーグトレ
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ノバルティス アーゲー
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Publication of JP2014505688A5 publication Critical patent/JP2014505688A5/ja
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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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/28—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2013548830A 2011-01-12 2012-01-11 オキサジン誘導体および神経障害の処置におけるその使用 Ceased JP2014505688A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161432037P 2011-01-12 2011-01-12
US61/432,037 2011-01-12
PCT/EP2012/050387 WO2012095463A1 (en) 2011-01-12 2012-01-11 Oxazine derivatives and their use in the treatment of neurological disorders

Publications (2)

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JP2014505688A true JP2014505688A (ja) 2014-03-06
JP2014505688A5 JP2014505688A5 (enExample) 2015-03-05

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JP2013548830A Ceased JP2014505688A (ja) 2011-01-12 2012-01-11 オキサジン誘導体および神経障害の処置におけるその使用

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Country Link
US (1) US20130281449A1 (enExample)
EP (1) EP2663559B1 (enExample)
JP (1) JP2014505688A (enExample)
KR (1) KR20140051822A (enExample)
CN (1) CN103429589A (enExample)
AU (1) AU2012206555A1 (enExample)
BR (1) BR112013017779A2 (enExample)
CA (1) CA2824097A1 (enExample)
EA (1) EA201391029A1 (enExample)
MX (1) MX2013008111A (enExample)
WO (1) WO2012095463A1 (enExample)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015500223A (ja) * 2011-12-05 2015-01-05 ヤンセン ファーマシューティカ エヌ．ベー． ６−ジフルオロメチル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体
US9751886B2 (en) 2013-06-12 2017-09-05 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE)
US9828350B2 (en) 2010-06-09 2017-11-28 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
US9834559B2 (en) 2013-06-12 2017-12-05 Janssen Pharmaceutica Nv 4-Amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase (BACE)
US9840507B2 (en) 2010-12-22 2017-12-12 Janssen Pharmaceutica, Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
US9845326B2 (en) 2011-03-09 2017-12-19 Janssen Pharmaceutica Nv Substituted 3,4-dihydropyrrolo[1,2-A]pyrazines as beta-secretase (BACE) inhibitors
US10106524B2 (en) 2014-12-18 2018-10-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase
JP2020503293A (ja) * 2016-12-15 2020-01-30 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
JP2020520352A (ja) * 2017-08-11 2020-07-09 エルジー・ケム・リミテッド ハロゲン置換のスチレンモノマーの製造方法

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KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
MY162413A (en) 2011-01-13 2017-06-15 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US9284284B2 (en) 2011-10-13 2016-03-15 Novartis Ag Oxazine derivatives and their use in the treatment of disease
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
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
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.
KR20160115936A (ko) 2014-02-19 2016-10-06 하. 룬드벡 아크티에셀스카브 알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘
CN106795147B (zh) 2014-08-08 2020-09-22 美国安进公司 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
EP3334720A1 (en) 2015-08-12 2018-06-20 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
WO2018039062A1 (en) 2016-08-26 2018-03-01 Eli Lilly And Company 1,4-oxazines useful as selective bace1 inhibitors
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CA3047290A1 (en) 2016-12-15 2018-06-21 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MX394391B (es) 2016-12-15 2025-03-24 Amgen Inc Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso.
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
CN111675708A (zh) * 2020-06-10 2020-09-18 南京合巨药业有限公司 一种6-氰基-7-氮杂吲哚及其衍生物的制备方法
CN111943947B (zh) * 2020-07-24 2021-04-30 重庆文理学院 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用

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NL6911868A (enExample) 1968-08-31 1970-03-03
DE19725802A1 (de) 1996-07-10 1998-01-15 Lonza Ag Verfahren zur Herstellung von (S)- oder (R)-3,3,3-trifluor-2-hydroxy-2-methylpropionsäure
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
BRPI0418212A (pt) 2003-12-29 2007-04-27 Banyu Pharma Co Ltd composto ou um sal deste farmaceuticamente aceitável, ativador da glicocinase, e, medicamentos para a terapia e/ou prevenção da diabete, e da obesidade
CA2628074C (en) * 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
PL2233474T3 (pl) 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
CN102186841A (zh) * 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
UY32799A (es) * 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
DK2483255T3 (da) * 2010-07-13 2014-01-20 Novartis Ag Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9828350B2 (en) 2010-06-09 2017-11-28 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
US9840507B2 (en) 2010-12-22 2017-12-12 Janssen Pharmaceutica, Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
US9845326B2 (en) 2011-03-09 2017-12-19 Janssen Pharmaceutica Nv Substituted 3,4-dihydropyrrolo[1,2-A]pyrazines as beta-secretase (BACE) inhibitors
JP2015500223A (ja) * 2011-12-05 2015-01-05 ヤンセン ファーマシューティカ エヌ．ベー． ６−ジフルオロメチル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体
US9751886B2 (en) 2013-06-12 2017-09-05 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE)
US9834559B2 (en) 2013-06-12 2017-12-05 Janssen Pharmaceutica Nv 4-Amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase (BACE)
US10106524B2 (en) 2014-12-18 2018-10-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase
JP2020503293A (ja) * 2016-12-15 2020-01-30 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
JP7177773B2 (ja) 2016-12-15 2022-11-24 アムジエン・インコーポレーテツド β－セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
JP2020520352A (ja) * 2017-08-11 2020-07-09 エルジー・ケム・リミテッド ハロゲン置換のスチレンモノマーの製造方法
US10988424B2 (en) 2017-08-11 2021-04-27 Lg Chem, Ltd. Method for preparing halogen-substituted styrene monomer

Also Published As

Publication number Publication date
BR112013017779A2 (pt) 2016-10-11
EP2663559B1 (en) 2015-07-01
CA2824097A1 (en) 2012-07-19
CN103429589A (zh) 2013-12-04
WO2012095463A1 (en) 2012-07-19
AU2012206555A1 (en) 2013-08-01
MX2013008111A (es) 2013-10-30
KR20140051822A (ko) 2014-05-02
US20130281449A1 (en) 2013-10-24
EP2663559A1 (en) 2013-11-20
EA201391029A1 (ru) 2014-01-30

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