JP6389830B2 - ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法 - Google Patents

ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法 Download PDF

Info

Publication number
JP6389830B2
JP6389830B2 JP2015560325A JP2015560325A JP6389830B2 JP 6389830 B2 JP6389830 B2 JP 6389830B2 JP 2015560325 A JP2015560325 A JP 2015560325A JP 2015560325 A JP2015560325 A JP 2015560325A JP 6389830 B2 JP6389830 B2 JP 6389830B2
Authority
JP
Japan
Prior art keywords
alkyl
independently
amino
methyl
dihydro
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.)
Active
Application number
JP2015560325A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016511258A (ja
JP2016511258A5 (enExample
Inventor
ミナッチ，アナ・エレナ
ロウ，ジョナサン・ディー
アレン，ジェニファー・アール
チェン，ジエン
チェン，ニン
チュヨン，ユアン
ジャッド，テッド
リウ，チンイェン
ロペス，パトリシア
チェン，ウェンユエン
ラムフェルト，シャノン
ルザサ，ロバート・エム
タマヨ，ヌリア・エイ
シュエ，チウフェン
ヤン，ブライアント
ジョン，ウェンジ
Original Assignee
アムジエン・インコーポレーテツド
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 アムジエン・インコーポレーテツド filed Critical アムジエン・インコーポレーテツド
Publication of JP2016511258A publication Critical patent/JP2016511258A/ja
Publication of JP2016511258A5 publication Critical patent/JP2016511258A5/ja
Application granted granted Critical
Publication of JP6389830B2 publication Critical patent/JP6389830B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • C07D413/14—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
    • 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
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2015560325A 2013-03-01 2014-02-27 ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法 Active JP6389830B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361771615P 2013-03-01 2013-03-01
US61/771,615 2013-03-01
US201361826431P 2013-05-22 2013-05-22
US61/826,431 2013-05-22
US201461928898P 2014-01-17 2014-01-17
US61/928,898 2014-01-17
PCT/US2014/019100 WO2014134341A1 (en) 2013-03-01 2014-02-27 Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Publications (3)

Publication Number Publication Date
JP2016511258A JP2016511258A (ja) 2016-04-14
JP2016511258A5 JP2016511258A5 (enExample) 2017-03-30
JP6389830B2 true JP6389830B2 (ja) 2018-09-12

Family

ID=50349866

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015560325A Active JP6389830B2 (ja) 2013-03-01 2014-02-27 ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法

Country Status (9)

Country Link
US (1) US9296734B2 (enExample)
EP (1) EP2961749B1 (enExample)
JP (1) JP6389830B2 (enExample)
AU (2) AU2014223334C1 (enExample)
CA (1) CA2902212C (enExample)
MX (1) MX366855B (enExample)
TW (1) TW201446758A (enExample)
UY (1) UY35361A (enExample)
WO (1) WO2014134341A1 (enExample)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
PE20151794A1 (es) 2013-03-08 2015-12-03 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso
BR112015019412A8 (pt) * 2013-04-11 2019-11-12 Hoffmann La Roche inibidores de bace1, seus usos, e composição farmacêutica
CR20160352A (es) 2014-02-19 2016-10-20 H Lundbeck As 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
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
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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
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
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
MX2018001699A (es) 2015-08-12 2018-05-07 H Lundbeck As 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1.
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
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
AU2016375540A1 (en) 2015-12-25 2018-07-19 Shionogi & Co., Ltd. Process and intermediates for preparation of thiazine derivatives
JP6616525B2 (ja) * 2016-03-01 2019-12-04 エフ．ホフマン−ラ ロシュ アーゲー Ｂａｃｅ１阻害剤
MX386618B (es) * 2016-12-15 2025-03-19 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso.
MY199348A (en) * 2017-04-27 2023-10-24 Basf Se Process for preparing optically active 2,3-dihydrothiazolo[3,2-a]pyrimidin-4-ium compounds
CN112313238B (zh) 2018-04-27 2025-01-17 盐野义制药株式会社 具有选择性bace1抑制活性的四氢吡喃并噁嗪衍生物
TWI797167B (zh) * 2018-09-28 2023-04-01 德商巴地斯顏料化工廠 用於製備光學活性嘧啶鎓化合物之方法
TWI780230B (zh) * 2018-09-28 2022-10-11 德商巴地斯顏料化工廠 用於製備含硫之嘧啶鎓化合物之方法
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Ａｌｋ﹘５抑制劑和彼之用途
CN113979993B (zh) * 2021-11-29 2023-10-13 云南萃精生物科技有限责任公司 一种不对称合成（s）-烟碱的方法
CN114561435B (zh) * 2022-04-27 2022-08-30 南京科力硕生物科技有限公司 利用磁性碳纳米管固定化酶催化制备4-氯-3-乙基-1-甲基吡唑-5-甲酸的方法

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
SI9300303A (en) 1993-06-08 1994-12-31 Krka Tovarna Zdravil Process for isolation of hypolipemic effective substance
US5942400A (en) 1995-06-07 1999-08-24 Elan Pharmaceuticals, Inc. Assays for detecting β-secretase
DK1115874T3 (da) 1998-09-24 2009-04-20 Pharmacia & Upjohn Co Llc Alzheimer's sygdom-sekretase
US20040234976A1 (en) 1998-09-24 2004-11-25 Gurney Mark E. Alzheimer's disease secretase, app substrates therefor, and uses therefor
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP2343069B1 (en) 2003-12-15 2016-03-02 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
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
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
CA2692713A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
CA2695114A1 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
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
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
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
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
KR20110048491A (ko) 2008-07-28 2011-05-11 에자이 알앤드디 매니지먼트 가부시키가이샤 스피로아미노디하이드로티아진 유도체들
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
EP2500344A4 (en) * 2009-11-13 2013-05-01 Shionogi & Co AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION
US20120245154A1 (en) 2009-12-09 2012-09-27 Shionogi & Co., Ltd. Substituted aminothiazine derivative
JP5554346B2 (ja) 2009-12-09 2014-07-23 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
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
EP2511269A4 (en) 2009-12-11 2013-04-24 Shionogi & Co FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP
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
WO2012078994A1 (en) 2010-12-09 2012-06-14 Janssen Pharmaceutica Nv Imidazo [1, 2-a] pyridine sulfonamides as trpm8 modulators
US20130281449A1 (en) 2011-01-12 2013-10-24 Novartis Ag Oxazine Derivatives and their Use in the Treatment of Neurological Disorders
CA2824220C (en) 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic 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
US8404680B2 (en) 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
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
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
US8785436B2 (en) * 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US8604024B2 (en) 2011-05-24 2013-12-10 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
US8598161B2 (en) 2011-05-24 2013-12-03 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
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
JP2012250933A (ja) 2011-06-03 2012-12-20 Shionogi & Co Ltd オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物
BR112013031510A2 (pt) 2011-06-07 2016-12-27 Hoffmann La Roche [1,3]oxazinas
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
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
UY34278A (es) * 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
WO2013030713A1 (en) 2011-08-31 2013-03-07 Pfizer Inc. Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds
US20130073953A1 (en) 2011-09-21 2013-03-21 Timothy Onyenobi News headline screenshot viewing system
WO2013054291A1 (en) 2011-10-13 2013-04-18 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease
CA2853221A1 (en) 2011-10-24 2013-05-02 Tohru Yamashita Bicyclic compound
CA2856892C (en) * 2012-01-26 2020-05-12 F. Hoffmann-La Roche Ag Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
EP2827857A4 (en) 2012-03-20 2016-03-30 Elan Pharm Inc SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE AND COMPOSITIONS AND USES THEREOF
ES2585262T3 (es) 2012-05-04 2016-10-04 Pfizer Inc Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2
WO2013182638A1 (en) 2012-06-08 2013-12-12 H. Lundbeck A/S 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease
SG11201407576YA (en) 2012-06-26 2015-03-30 Hoffmann La Roche Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
JP2015529239A (ja) 2012-09-20 2015-10-05 ファイザー・インク アルキル置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
WO2014062553A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2014062549A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
HUE031764T2 (en) 2012-10-26 2017-07-28 Lilly Co Eli Tetrahydropyrrolothiazine derivatives as BACE inhibitors
WO2014093190A1 (en) 2012-12-14 2014-06-19 Merck Sharp & Dohme Corp. Bace inhibitors of iminothiadiazine dioxides
US9475784B2 (en) 2012-12-19 2016-10-25 Bristol-Myers Squibb Company 4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production
CA2893333C (en) 2012-12-19 2017-10-24 Pfizer Inc. Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
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
EP2934534B1 (en) 2012-12-21 2017-12-13 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
MX2015008957A (es) * 2013-01-22 2015-09-29 Siena Biotech Spa Fluoro-[1,3]oxazinas como inhibidores de beta-secretasa 1 (bace1).
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
PE20151794A1 (es) 2013-03-08 2015-12-03 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso
BR112015019412A8 (pt) * 2013-04-11 2019-11-12 Hoffmann La Roche inibidores de bace1, seus usos, e composição farmacêutica
HK1213562A1 (zh) 2013-04-26 2016-07-08 豪夫迈‧罗氏有限公司 Bace抑制剂的合成

Also Published As

Publication number Publication date
JP2016511258A (ja) 2016-04-14
UY35361A (es) 2014-09-30
US20140249104A1 (en) 2014-09-04
AU2014223334B2 (en) 2018-04-05
MX2015011313A (es) 2015-12-03
AU2014223334C1 (en) 2018-10-18
CA2902212C (en) 2020-10-13
EP2961749A1 (en) 2016-01-06
EP2961749B1 (en) 2019-10-09
MX366855B (es) 2019-07-26
US9296734B2 (en) 2016-03-29
TW201446758A (zh) 2014-12-16
AU2014223334A1 (en) 2015-09-10
CA2902212A1 (en) 2014-09-04
WO2014134341A1 (en) 2014-09-04
AU2018204589A1 (en) 2018-07-12

Similar Documents

Publication Publication Date Title
JP6389830B2 (ja) ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法
JP6374889B2 (ja) β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法
US9556135B2 (en) Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
CA2905012C (en) Substituted 7-azabicycles and their use as orexin receptor modulators
US8921363B2 (en) Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors
EP2526092B1 (en) Amino heteroaryl compounds as beta-secretase modulators and methods of use
US8497264B2 (en) Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US10246429B2 (en) Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JP6576433B2 (ja) β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−２−アミン化合物及び使用方法
JP7149271B2 (ja) β－セクレターゼ阻害剤としての１，４－チアジンジオキシドおよび１，２，４－チアジアジンジオキシド誘導体ならびに使用方法
JP2014526560A (ja) 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
US9309263B2 (en) Fused multi-cyclic sulfone compounds as inhibitors of beta-secretase and methods of use thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151119

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170224

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170224

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20171212

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20171214

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20180221

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180611

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: 20180807

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20180820

R150 Certificate of patent or registration of utility model

Ref document number: 6389830

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