JP5767214B2 - オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用 - Google Patents

オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用 Download PDF

Info

Publication number
JP5767214B2
JP5767214B2 JP2012521053A JP2012521053A JP5767214B2 JP 5767214 B2 JP5767214 B2 JP 5767214B2 JP 2012521053 A JP2012521053 A JP 2012521053A JP 2012521053 A JP2012521053 A JP 2012521053A JP 5767214 B2 JP5767214 B2 JP 5767214B2
Authority
JP
Japan
Prior art keywords
phenyl
amino
dihydro
amide
carboxylic acid
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2012521053A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013500247A5 (enExample
JP2013500247A (ja
Inventor
サンガメシュ・バディジェル
ムラリ・チェブロル
マティアス・フレデリクセン
フィリップ・ホルツァー
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
ヘンリク・メビッツ
ウルフ・ノイマン
リタ・ラモス
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
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42629546&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5767214(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ノバルティス アーゲー, ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2013500247A publication Critical patent/JP2013500247A/ja
Publication of JP2013500247A5 publication Critical patent/JP2013500247A5/ja
Application granted granted Critical
Publication of JP5767214B2 publication Critical patent/JP5767214B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2012521053A 2009-07-24 2010-07-23 オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用 Expired - Fee Related JP5767214B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US22847209P 2009-07-24 2009-07-24
US61/228,472 2009-07-24
US25891109P 2009-11-06 2009-11-06
US61/258,911 2009-11-06
US36370210P 2010-07-13 2010-07-13
US61/363,702 2010-07-13
PCT/EP2010/060718 WO2011009943A1 (en) 2009-07-24 2010-07-23 Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

Publications (3)

Publication Number Publication Date
JP2013500247A JP2013500247A (ja) 2013-01-07
JP2013500247A5 JP2013500247A5 (enExample) 2013-02-28
JP5767214B2 true JP5767214B2 (ja) 2015-08-19

Family

ID=42629546

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012521053A Expired - Fee Related JP5767214B2 (ja) 2009-07-24 2010-07-23 オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用

Country Status (26)

Country Link
US (5) US8207164B2 (enExample)
EP (1) EP2456763B1 (enExample)
JP (1) JP5767214B2 (enExample)
KR (2) KR101422965B1 (enExample)
CN (1) CN102471293B (enExample)
AR (1) AR077328A1 (enExample)
AU (1) AU2010274913B2 (enExample)
CA (1) CA2768980A1 (enExample)
CL (1) CL2012000185A1 (enExample)
CO (1) CO6491058A2 (enExample)
CR (1) CR20120002A (enExample)
CU (1) CU24083B1 (enExample)
EA (1) EA201200174A1 (enExample)
EC (1) ECSP12011622A (enExample)
ES (1) ES2534315T3 (enExample)
GT (1) GT201200016A (enExample)
IL (1) IL217378A (enExample)
MA (1) MA33450B1 (enExample)
MX (1) MX2012001070A (enExample)
NZ (1) NZ597529A (enExample)
PE (1) PE20121440A1 (enExample)
SG (1) SG177397A1 (enExample)
TW (1) TW201107316A (enExample)
UY (1) UY32799A (enExample)
WO (1) WO2011009943A1 (enExample)
ZA (1) ZA201200155B (enExample)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
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
CA2683887A1 (en) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein
JP5490692B2 (ja) 2008-06-13 2014-05-14 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
WO2010047372A1 (ja) 2008-10-22 2010-04-29 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２－アミノピリミジン－４－オンおよび２－アミノピリジン誘導体
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
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
JPWO2011071135A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 オキサジン誘導体
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
NZ600136A (en) * 2009-12-31 2013-09-27 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
AU2011227501B9 (en) 2010-03-15 2013-08-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as Beta - secretase modulators and their medical use
US8673894B2 (en) * 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
EA021240B1 (ru) 2010-06-09 2015-05-29 Янссен Фармацевтика Нв Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)
PL2483255T3 (pl) * 2010-07-13 2014-03-31 Novartis Ag Pochodne oksazyny i ich zastosowanie w leczeniu zaburzeń neurologicznych
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
EP2655376B1 (en) 2010-12-22 2017-08-23 Janssen Pharmaceutica NV 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
US8524897B2 (en) * 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
US20130281449A1 (en) * 2011-01-12 2013-10-24 Novartis Ag Oxazine Derivatives and their Use in the Treatment of Neurological Disorders
JP2014505689A (ja) * 2011-01-13 2014-03-06 ノバルティス アーゲー 代謝障害の処置用ｂａｃｅ−２阻害剤
CA2824220C (en) * 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US9242943B2 (en) * 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8399459B2 (en) * 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8815841B2 (en) * 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
CA2824360C (en) * 2011-03-01 2020-01-14 Janssen Pharmaceutica Nv 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace)
US9067924B2 (en) * 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
JP5853035B2 (ja) * 2011-03-09 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体
US8748418B2 (en) * 2011-03-18 2014-06-10 Hoffmann-La Roche Inc. 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
US8877744B2 (en) * 2011-04-04 2014-11-04 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
MX2013011947A (es) 2011-04-13 2014-01-16 Merck Sharp & Dohme Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
US9079919B2 (en) * 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
JP2014516063A (ja) * 2011-06-07 2014-07-07 エフ．ホフマン−ラ ロシュ アーゲー Ｂａｃｅ１及び／又はｂａｃｅ２阻害剤としてのハロゲン−アルキル−１，３オキサジン
BR112013031510A2 (pt) * 2011-06-07 2016-12-27 Hoffmann La Roche [1,3]oxazinas
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
JP2014526560A (ja) 2011-09-21 2014-10-06 アムジエン・インコーポレーテツド β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法
WO2013054291A1 (en) * 2011-10-13 2013-04-18 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
MX357383B (es) * 2011-12-06 2018-07-06 Janssen Pharmaceutica Nv Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2h-[1,4]oxazin- 3-amina.
CA2856892C (en) * 2012-01-26 2020-05-12 F. Hoffmann-La Roche Ag Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
US9556135B2 (en) 2012-10-12 2017-01-31 Amgen, Inc. Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CA2894919A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. C5,c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors, compositions, and their use
TW201512171A (zh) 2013-04-19 2015-04-01 Pfizer Ltd 化學化合物
KR102243134B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체
MX368326B (es) 2013-06-12 2019-09-27 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace).
ES2721073T3 (es) 2013-06-12 2019-07-26 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)
FR3025591B1 (fr) * 2014-09-05 2016-10-14 Technofan Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe
KR20170095881A (ko) 2014-12-18 2017-08-23 얀센 파마슈티카 엔.브이. 베타―세크레타제의 ２,３,４,５―테트라히드로피리딘―６―아민 및 ３,４―디히드로―２ｈ―피롤―５―아민 화합물 억제제
TW201726651A (zh) * 2015-09-23 2017-08-01 健生藥品公司 ２，３，４，５－四氫吡啶－６－胺衍生物
JP2019524825A (ja) * 2016-08-26 2019-09-05 イーライ リリー アンド カンパニー 選択的ｂａｃｅ１阻害剤として有用な１，４−オキサジン
US10159191B2 (en) 2016-09-23 2018-12-25 Deere & Company Harvester grain unloader
CN110018266B (zh) * 2019-02-15 2022-03-04 广州市妇女儿童医疗中心 一种快速定量分析48种氨基酸的方法
CN112250580A (zh) * 2020-10-28 2021-01-22 上海昂卓新材料科技有限公司 一种2-硝基-2-取代苯基丙烷-1,3-二醇的制备方法

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL6911868A (enExample) 1968-08-31 1970-03-03
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
TW200502221A (en) * 2002-10-03 2005-01-16 Astrazeneca Ab Novel lactams and uses thereof
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
AU2004309287B2 (en) 2003-12-29 2008-07-31 Banyu Pharmaceutical Co., Ltd Novel 2-heteroaryl-substituted benzimidazole derivative
CN1933838A (zh) 2004-02-12 2007-03-21 默克公司 作为代谢型谷氨酸受体－5调节剂的联吡啶酰胺
TW200624426A (en) 2004-09-21 2006-07-16 Lilly Co Eli BACE inhibitors
US7888374B2 (en) 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
EP2612854B1 (en) * 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
CN101679266B (zh) 2007-03-01 2015-05-06 诺华股份有限公司 Pim激酶抑制剂及其应用方法
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
CA2683887A1 (en) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
TWI423970B (zh) 2008-01-18 2014-01-21 衛材Ｒ＆Ｄ企管股份有限公司 經稠合之胺基二氫噻衍生物
US20100197688A1 (en) 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
JP5490692B2 (ja) 2008-06-13 2014-05-14 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
WO2010007756A1 (ja) 2008-07-14 2010-01-21 塩野義製薬株式会社 Ｔｔｋ阻害作用を有するピリジン誘導体
WO2010047372A1 (ja) 2008-10-22 2010-04-29 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２－アミノピリミジン－４－オンおよび２－アミノピリジン誘導体
US9237972B2 (en) 2008-12-16 2016-01-19 Kimberly-Clark Worldwide, Inc. Liquid surfactant compositions that adhere to surfaces and solidify and swell in the presence of water and articles using the same
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
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
EP2500344A4 (en) 2009-11-13 2013-05-01 Shionogi & Co AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
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
JPWO2011071135A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 オキサジン誘導体
US8673894B2 (en) * 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
MX2012014382A (es) 2010-06-09 2013-01-29 Janssen Pharmaceutica Nv Derivados de 5-amino-3, 6-dihidro-1h-pirazin-2-ona utiles como inhibidores de beta-secretasa (bace).
EA021240B1 (ru) 2010-06-09 2015-05-29 Янссен Фармацевтика Нв Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)
PL2483255T3 (pl) * 2010-07-13 2014-03-31 Novartis Ag Pochodne oksazyny i ich zastosowanie w leczeniu zaburzeń neurologicznych
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
US20130281449A1 (en) 2011-01-12 2013-10-24 Novartis Ag Oxazine Derivatives and their Use in the Treatment of Neurological Disorders
JP2014505689A (ja) 2011-01-13 2014-03-06 ノバルティス アーゲー 代謝障害の処置用ｂａｃｅ−２阻害剤
CA2824220C (en) 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
WO2013054291A1 (en) 2011-10-13 2013-04-18 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease

Also Published As

Publication number Publication date
CL2012000185A1 (es) 2012-10-12
PE20121440A1 (es) 2012-11-06
US20140088084A1 (en) 2014-03-27
CO6491058A2 (es) 2012-07-31
KR20140004810A (ko) 2014-01-13
EP2456763B1 (en) 2015-01-21
EA201200174A1 (ru) 2012-08-30
US20150018338A1 (en) 2015-01-15
US20110021520A1 (en) 2011-01-27
US8846658B2 (en) 2014-09-30
MA33450B1 (fr) 2012-07-03
US20140113894A1 (en) 2014-04-24
ECSP12011622A (es) 2012-02-29
HK1166314A1 (en) 2012-10-26
KR101422965B1 (ko) 2014-07-23
SG177397A1 (en) 2012-02-28
UY32799A (es) 2011-02-28
CN102471293B (zh) 2014-10-01
WO2011009943A1 (en) 2011-01-27
IL217378A0 (en) 2012-03-01
GT201200016A (es) 2013-09-23
ES2534315T3 (es) 2015-04-21
CU24083B1 (es) 2015-03-30
CR20120002A (es) 2012-02-15
CU20120013A7 (es) 2012-04-15
US8207164B2 (en) 2012-06-26
KR20120039655A (ko) 2012-04-25
AU2010274913A1 (en) 2012-02-02
ZA201200155B (en) 2012-09-26
TW201107316A (en) 2011-03-01
AR077328A1 (es) 2011-08-17
US20120238560A1 (en) 2012-09-20
EP2456763A1 (en) 2012-05-30
JP2013500247A (ja) 2013-01-07
CN102471293A (zh) 2012-05-23
CA2768980A1 (en) 2011-01-27
NZ597529A (en) 2013-11-29
AU2010274913B2 (en) 2013-09-19
MX2012001070A (es) 2012-03-16
IL217378A (en) 2015-02-26

Similar Documents

Publication Publication Date Title
JP5767214B2 (ja) オキサジン誘導体および神経障害の処置のためのｂａｃｅ阻害剤としてのその使用
JP5128019B1 (ja) 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
US8338413B1 (en) Oxazine derivatives and their use in the treatment of neurological disorders
EP2663559B1 (en) Oxazine derivatives and their use in the treatment of neurological disorders
HK1166314B (en) Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
AU2013273640A1 (en) Oxazine derivatives and their use as BACE inhibitors for the treatment of neurological disorders

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130110

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20130110

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20131105

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140203

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140210

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140220

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140227

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140328

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140404

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140502

RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20140815

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20140902

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A132

Effective date: 20141216

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141222

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20150602

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20150618

R150 Certificate of patent or registration of utility model

Ref document number: 5767214

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees