JP2016501827A - Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 - Google Patents

Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 Download PDF

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JP2016501827A
JP2016501827A JP2015516335A JP2015516335A JP2016501827A JP 2016501827 A JP2016501827 A JP 2016501827A JP 2015516335 A JP2015516335 A JP 2015516335A JP 2015516335 A JP2015516335 A JP 2015516335A JP 2016501827 A JP2016501827 A JP 2016501827A
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JP2016501827A5 (https=
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兼一 日下部
兼一 日下部
周平 吉田
周平 吉田
中原 健二
健二 中原
長谷川 剛
剛 長谷川
元太 只野
元太 只野
光記 渕野
光記 渕野
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Shionogi and Co Ltd
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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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/04Heterocyclic 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
    • 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
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/10Spiro-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2015516335A 2012-10-24 2013-10-23 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 Pending JP2016501827A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2015516335A JP2016501827A (ja) 2012-10-24 2013-10-23 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP2012234461 2012-10-24
JP2012234461 2012-10-24
JP2013154451 2013-07-25
JP2013154451 2013-07-25
JP2015516335A JP2016501827A (ja) 2012-10-24 2013-10-23 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
PCT/JP2013/079472 WO2014065434A1 (en) 2012-10-24 2013-10-23 Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity

Publications (2)

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JP2016501827A true JP2016501827A (ja) 2016-01-21
JP2016501827A5 JP2016501827A5 (https=) 2016-10-13

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JP2015516335A Pending JP2016501827A (ja) 2012-10-24 2013-10-23 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体

Country Status (4)

Country Link
US (2) US9540359B2 (https=)
EP (1) EP2912035A4 (https=)
JP (1) JP2016501827A (https=)
WO (1) WO2014065434A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019507164A (ja) * 2016-03-01 2019-03-14 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Bace1阻害剤

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
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.
AU2014253275B2 (en) 2013-04-11 2018-10-18 F. Hoffmann-La Roche Ag BACE1 inhibitors
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
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
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
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
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.
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
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
AU2019258575A1 (en) 2018-04-27 2020-10-29 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
CN111592557A (zh) * 2020-05-09 2020-08-28 河北合佳医药科技集团股份有限公司 一种7-氨基-3-乙烯基头孢烷酸的一步法环保制备方法

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007049532A1 (ja) * 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体
WO2011070029A1 (en) * 2009-12-10 2011-06-16 F. Hoffmann-La Roche Ag Amino oxazine derivatives
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
WO2011069934A1 (en) * 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors
WO2012107371A1 (en) * 2011-02-08 2012-08-16 F. Hoffmann-La Roche Ag 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
WO2012139993A1 (en) * 2011-04-11 2012-10-18 F. Hoffmann-La Roche Ag 1,3 oxazines as bace1 and/or bace2 inhibitors
WO2013110622A1 (en) * 2012-01-26 2013-08-01 F. Hoffmann-La Roche Ag Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
WO2013142613A1 (en) * 2012-03-20 2013-09-26 Elan Pharmaceuticals, Inc. Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof
JP2014513702A (ja) * 2011-05-16 2014-06-05 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1,3−オキサジン
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
JP2014518895A (ja) * 2011-06-07 2014-08-07 エフ.ホフマン−ラ ロシュ アーゲー [1,3]オキサジン
JP2014524463A (ja) * 2011-08-25 2014-09-22 ノバルティス アーゲー 2−アミノ−4−(ピリジン−2−イル)−5,6−ジヒドロ−4h−1,3−オキサジン誘導体およびbace−1および/またはbace−2阻害剤としてのそれらの使用
JP2014526534A (ja) * 2011-09-21 2014-10-06 エフ.ホフマン−ラ ロシュ アーゲー BACE1阻害剤としてのN−(3−(2−アミノ−6,6−ジフルオロ−4,4a,5,6,7,7a−ヘキサヒドロ−シクロペンタ[e][1,3]オキサジン−4−イル)−フェニル)−アミド

Family Cites Families (201)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3235551A (en) 1966-02-15 Novel derivatives of
US2899426A (en) 1959-08-11 Synthesis of l
US3227713A (en) 1966-01-04 Azine derivatives
JPH09504278A (ja) 1944-06-01 1997-04-28 ザ、ウェルカム、ファンデーション、リミテッド Noシンターゼインヒビターとしての置換尿素およびイソチオ尿素誘導体
US3115494A (en) 1961-10-13 1963-12-24 Mcneilab Inc 2-amino-5, 6-dihydro-4ii-1, 3-oxazines and a process for their preparation
BE637923A (https=) 1962-09-29
US3636116A (en) 1968-09-03 1972-01-18 Dow Chemical Co 1 2-substituted indene compounds
SU465792A3 (ru) 1968-11-06 1975-03-30 Хиноин Гиогисцер-Ес Вегиесцети Термекек Гиара Рт (Фирма) Способ получени гетероциклических соединений
US3577428A (en) 1969-04-14 1971-05-04 Colgate Palmolive Co 2-amino-4-aryloxyalkyl-4-alkyl-2-oxazolines
US3719674A (en) 1971-02-08 1973-03-06 Dow Chemical Co 1,2-substituted indene compounds
DE2426653C3 (de) 1974-06-01 1982-05-06 Bayer Ag, 5090 Leverkusen Derivate des 2-Amino-1,3-thiazins
DD140144A1 (de) 1978-11-08 1980-02-13 Horst Hartmann Verfahren zur herstellung von p-aminophenylsubstituierten 2-amino-1,3-thiaziniumsalzen
US4311840A (en) 1980-11-13 1982-01-19 E. R. Squibb & Sons, Inc. 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones
JPS62120374A (ja) 1985-11-20 1987-06-01 Yoshitomi Pharmaceut Ind Ltd 1,3−チアジンまたは1,3−オキサジン誘導体
JPH0231792Y2 (https=) 1986-01-21 1990-08-28
FI95572C (fi) 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
CA1332151C (en) 1988-01-28 1994-09-27 Roman Amrein Use of a benzamide to treat cognitive disorder
US5236942A (en) 1990-04-19 1993-08-17 Merrell Dow Pharmaceuticals Inc. 5-aryl-4-alkyl-3H-1,2,4-triazole-3-thiones useful in the treatment of Altzheimer's dementia
US5328915A (en) 1992-09-17 1994-07-12 E. I. Du Pont De Nemours And Company Arthropodicidal amidrazone ureas
EP0670720A1 (en) 1992-11-27 1995-09-13 The Wellcome Foundation Limited Enzyme inhibitors
GB9418912D0 (en) 1994-09-20 1994-11-09 Fisons Corp Pharmaceutically active compounds
AU4149696A (en) 1994-11-15 1996-06-06 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
DE4442116A1 (de) 1994-11-25 1996-05-30 Cassella Ag 2-Amino-1,3-thiazine als Hemmstoffe der Stickstoffmonoxid-Synthase
WO1996018607A1 (en) 1994-12-12 1996-06-20 Chugai Seiyaku Kabushiki Kaisha Aniline derivative having the effect of inhibiting nitrogen monoxide synthase
JPH08333258A (ja) 1994-12-14 1996-12-17 Japan Tobacco Inc チアジン又はチアゼピン誘導体及びそれら化合物を含有してなる一酸化窒素合成酵素阻害剤
DE4444930A1 (de) 1994-12-16 1996-06-27 Cassella Ag 2-Amino-1,3-thiazepine und deren Verwendung als Hemmstoffe der Stickstoffmonoxid-Synthase
DK0843661T3 (da) 1995-08-11 2002-07-22 Pfizer (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanolmethansulfonat-trihydrat
JPH0967355A (ja) 1995-08-31 1997-03-11 Tokyo Tanabe Co Ltd チアジン誘導体、チアゾール誘導体及びそれらの製造方法
HUP9602538A3 (en) 1995-09-18 1997-08-28 Sankyo Co New urea and amide derivatives having acat inhibitory activity, their preparation and their use
TR199800697T2 (xx) 1995-10-17 1998-07-21 Astra Pharmaceuticals Limited Farmas�tik olarak aktif kinazolin bile�imleri.
CZ327698A3 (cs) 1996-04-13 1999-05-12 Astra Pharmaceuticals Ltd. Aminoisochinolinový a aminothienopyridinový derivát a jejich použití jako protizánětlivých přípravků
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US5952374A (en) 1997-09-29 1999-09-14 Protein Technologies International, Inc. Method for inhibiting the development of Alzheimer's disease and related dementias- and for preserving cognitive function
SE9703693D0 (sv) 1997-10-10 1997-10-10 Astra Pharma Prod Novel combination
TW460460B (en) 1997-11-04 2001-10-21 Chugai Pharmaceutical Co Ltd Heterocyclic compounds having NOS inhibitory activities
US6294695B1 (en) 1998-03-26 2001-09-25 Mount Sinai School Of Medicine Of The City University Of New York Aminobenzoic acid derivatives having anti-tumorigenic activity methods of making and using the same
AUPP285898A0 (en) 1998-04-07 1998-04-30 Fujisawa Pharmaceutical Co., Ltd. Amido derivatives
SE9802333D0 (sv) 1998-06-29 1998-06-29 Astra Pharma Prod Novel combination
US7375125B2 (en) 1999-08-04 2008-05-20 Ore Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
ES2316383T3 (es) 1999-09-17 2009-04-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
US20030060487A1 (en) 2000-04-12 2003-03-27 Bamdad R. Shoshana Treatment of neurodegenerative disease
CA2407088A1 (en) 2000-05-19 2001-11-22 Takeda Chemical Industries, Ltd. Beta-secretase inhibitors
US6420566B2 (en) 2000-06-09 2002-07-16 Aventis Pharma S.A. Pharmaceutical compositions containing a 4, 5-dihydro-1, 3-thiazol-2-ylamine derivative, novel derivatives and preparation thereof
US6713276B2 (en) 2000-06-28 2004-03-30 Scios, Inc. Modulation of Aβ levels by β-secretase BACE2
WO2002062766A2 (en) 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
EP1389194A2 (en) 2001-04-27 2004-02-18 Vertex Pharmaceuticals Incorporated Inhibitors of bace
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
AU2002359376B2 (en) 2001-11-08 2008-01-10 Elan Pharmaceuticals, Inc. N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives
JP4342309B2 (ja) 2001-11-09 2009-10-14 アベンティス・ファーマ・ソシエテ・アノニム 誘導型no−シンターゼ阻害剤としての2−アミノ−4−ピリジルメチル−チアゾリン誘導体の使用
PT1446393E (pt) 2001-11-09 2006-05-31 Aventis Pharma Sa Derivados de 2-amino-tiazolina e sua utilizacao como inibidores da sintase de no indutivel
ES2250731T3 (es) 2001-11-09 2006-04-16 Aventis Pharma S.A. Derivados de 2-amino-4-heteroariletil tiazolina y su utilizacion como inhibidores de no-sintasa inductible.
EP1492784A4 (en) 2002-03-28 2006-03-29 Merck & Co Inc SUBSTITUTED 2,3-DIPHENYLPYRIDINES
WO2004000312A2 (de) 2002-06-19 2003-12-31 Solvay Pharmaceuticals Gmbh Arzneimittel zur behandlung von eine inhibition oder aktivitätsverminderung von ph-wert-regulierenden bikarbonat-transporter-proteinen erfordernden erkrangungen
WO2004009549A2 (en) 2002-07-18 2004-01-29 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
WO2004014843A1 (ja) 2002-08-09 2004-02-19 Takeda Chemical Industries, Ltd. 置換アミノ化合物およびその用途
TW200502221A (en) 2002-10-03 2005-01-16 Astrazeneca Ab Novel lactams and uses thereof
JP2004149429A (ja) 2002-10-29 2004-05-27 Takeda Chem Ind Ltd インドール化合物およびその用途
JP2006096665A (ja) 2002-10-29 2006-04-13 Ono Pharmaceut Co Ltd 脊柱管狭窄症治療剤
ATE443043T1 (de) 2002-11-12 2009-10-15 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
RU2252936C2 (ru) 2002-12-05 2005-05-27 Институт физиологически активных веществ РАН S-замещенные n-1-[(гетеро)арил]алкил-n`-[(гетеро)арил]алкилизотиомочевины, способ их получения, фармацевтическая композиция, способ изучения глутаматэргической системы, способы лечения (варианты)
MXPA05011503A (es) 2003-04-25 2006-05-31 Johnson & Johnson Inhibidores de la c-fms cinasa.
GB0324498D0 (en) 2003-07-21 2003-11-26 Aventis Pharma Inc Heterocyclic compounds as P2X7 ion channel blockers
MXPA06003949A (es) 2003-10-07 2006-06-27 Renovis Inc Compuestos amida como ligandos del canal de ion y su uso.
EP2335701B1 (en) 2003-12-15 2012-07-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
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
US20050216196A1 (en) 2003-12-24 2005-09-29 Ridvan Akkurt Contamination estimation using fluid analysis models
JP2007530696A (ja) 2004-03-30 2007-11-01 メルク エンド カムパニー インコーポレーテッド アスパラギン酸プロテアーゼ阻害剤として有用な2−アミノチアゾール化合物
CA2564751A1 (en) 2004-04-30 2005-11-24 Schering Corporation Neuropeptide receptor modulators
RU2006144075A (ru) 2004-06-16 2008-07-27 Вайет (Us) ДИФЕНИЛИМИДАЗОПИРИМИДИН И -ИМИДАЗОЛАМИНЫ КАК ИНГИБИТОРЫ β-СЕКРЕТАЗЫ
EP1784188B1 (en) 2004-08-23 2010-07-14 Merck Sharp & Dohme Corp. Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006029850A1 (en) 2004-09-14 2006-03-23 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
EP1802588A4 (en) 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINOPYRIMIDONE AND APPLICATIONS THEREOF
JP2008516945A (ja) 2004-10-15 2008-05-22 アストラゼネカ・アクチエボラーグ 置換されたアミノ化合物およびそれらの使用
US20080287399A1 (en) 2004-12-14 2008-11-20 Astrazeneca Ab Substituted Aminopyridines and Uses Thereof
KR20140018997A (ko) 2005-01-07 2014-02-13 신타 파마슈티칼스 코프. 염증 및 면역 관련 용도를 위한 화합물
CA2593515A1 (en) 2005-01-14 2006-07-20 Wyeth Amino-imidazolones for the inhibition of beta-secretase
WO2006088694A1 (en) 2005-02-14 2006-08-24 Wyeth SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS
WO2006088705A1 (en) 2005-02-14 2006-08-24 Wyeth Terphenyl guanidines as [beta symbol] -secretase inhibitors
BRPI0606902A2 (pt) 2005-02-14 2009-07-28 Wyeth Corp composto; método para o tratamento de uma doença ou distúrbio associado a atividade excessiva de bace em um paciente que dele necessite; método para modular a atividade de bace; composição farmacêutica
US20060223849A1 (en) 2005-03-14 2006-10-05 Mjalli Adnan M Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors
NZ564222A (en) 2005-06-14 2011-10-28 Taigen Biotechnology Co Ltd Pyrimidine compounds
AU2006259675A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
WO2006138265A2 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
KR20080025079A (ko) 2005-06-14 2008-03-19 쉐링 코포레이션 아스파르틸 프로테아제 억제제
US7273882B2 (en) 2005-06-21 2007-09-25 Bristol-Myers Squibb Company Aminoacetamide acyl guanidines as β-secretase inhibitors
AU2006266167A1 (en) 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
TW200730523A (en) 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
JP2009509957A (ja) 2005-09-26 2009-03-12 ワイス β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物
CN101360721A (zh) 2005-11-15 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基嘧啶酮衍生物或2-氨基吡啶酮衍生物及其用途
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
EP1951680A4 (en) 2005-11-15 2011-08-10 Astrazeneca Ab NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
WO2007058601A1 (en) 2005-11-21 2007-05-24 Astrazeneca Ab Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia
AU2006333049A1 (en) 2005-12-19 2007-07-12 Wyeth 2-amino-5-piperidinylimidazolone compounds and use thereof for beta-secretase modulation
AR058381A1 (es) 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
UY30118A1 (es) 2006-01-31 2007-06-29 Tanabe Seiyaku Co Compueto amina trisustituido
US7868022B2 (en) 2006-02-06 2011-01-11 Janssen Pharmaceutica Nv 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
US7776882B2 (en) 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
CN101460480A (zh) 2006-04-05 2009-06-17 阿斯利康(瑞典)有限公司 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途
TW200808751A (en) 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
PL2021335T3 (pl) 2006-04-20 2011-10-31 Janssen Pharmaceutica Nv Związki heterocykliczne jako inhibitory kinazy C-FMS
PE20080155A1 (es) 2006-06-12 2008-03-10 Schering Corp Compuestos heterociclicos como inhibidores de aspartil-proteasa
AU2007275221A1 (en) 2006-07-20 2008-01-24 Allen J. Borchardt Benzothiophene inhibitors of RHO kinase
TW200817406A (en) 2006-08-17 2008-04-16 Wyeth Corp Imidazole amines as inhibitors of β-secretase
US20100016341A1 (en) 2006-12-12 2010-01-21 Zhaoning Zhu Aspartyl protease inhibitors containing a tricyclic ring system
JP2010512389A (ja) 2006-12-12 2010-04-22 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
TW200831080A (en) 2006-12-15 2008-08-01 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
KR101222412B1 (ko) 2007-02-15 2013-01-15 에프. 호프만-라 로슈 아게 Taar1 리간드로서의 2-아미노옥사졸린
JP5383484B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
JP4846769B2 (ja) 2007-07-30 2011-12-28 田辺三菱製薬株式会社 医薬組成物
US9986911B2 (en) 2007-10-19 2018-06-05 Smiths Medical Asd, Inc. Wireless telecommunications system adaptable for patient monitoring
WO2009064418A1 (en) 2007-11-14 2009-05-22 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
PL2233474T3 (pl) 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
WO2009097278A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
EP2240472B1 (en) 2008-01-29 2012-11-21 Janssen Pharmaceutica NV 2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace)
SG187502A1 (en) 2008-02-01 2013-02-28 Takeda Pharmaceutical Oxim derivatives as hsp90 inhibitors
EP2245019B1 (en) 2008-02-18 2012-11-14 F. Hoffmann-La Roche AG 4, 5-dihydro-oxazol-2-yl amine derivatives
CA2723222C (en) 2008-04-22 2013-04-02 Schering Corporation Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
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
CN102105475B (zh) 2008-07-28 2014-04-09 卫材R&D管理有限公司 螺氨基二氢噻嗪衍生物
EP2312945A4 (en) 2008-08-13 2012-05-09 Merck Sharp & Dohme PURE DERIVATIVES FOR THE TREATMENT OF MORBUS ALZHEIMER
WO2010019393A1 (en) 2008-08-13 2010-02-18 Merck Sharp & Dohme Corp. Pyrimidine derivatives for treatment of alzheimer's disease
JP5666304B2 (ja) 2008-09-30 2015-02-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
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
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
US20100125081A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
EP2415756A4 (en) 2009-03-31 2012-08-29 Shionogi & Co ISOTHIOROUS DERIVATIVES OR ISO-HARVEST DERIVATIVES WITH BACE1-HEMMENDER EFFECT
KR101123178B1 (ko) 2009-04-09 2012-06-13 (주)에스메디 2-아릴벤조싸이오펜 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
CA2760946C (en) 2009-05-07 2019-06-25 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions for studying, imaging, and treating pain
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
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
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
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace 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
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8354441B2 (en) 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
US20120238557A1 (en) 2009-11-13 2012-09-20 Shionogi & Co., Ltd. Aminothiazine or aminooxazine derivative having amino linker
EP2509983B1 (en) 2009-11-16 2014-09-17 Merck Sharp & Dohme Corp. FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
WO2011071057A1 (ja) 2009-12-09 2011-06-16 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
JPWO2011070781A1 (ja) 2009-12-09 2013-04-22 塩野義製薬株式会社 置換アミノチアジン誘導体
JPWO2011071109A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 4-アミノ-1,3-チアジンまたはオキサジン誘導体
NZ600136A (en) 2009-12-31 2013-09-27 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
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
MX339640B (es) 2010-06-09 2016-06-01 Janssen Pharmaceutica Nv * Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace).
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).
US20130102618A1 (en) 2010-06-28 2013-04-25 Janssen Pharmaceutica Nv 3-amino-5,6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia
DK2483255T3 (da) 2010-07-13 2014-01-20 Novartis Ag Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
BR112013006353A2 (pt) 2010-09-22 2024-01-16 Janssen Pharmaceutica Nv Derivados de 4,7-di-hifro-pirazolo[1,5-a]pirazin-6-ilamina úteis como inibidores de beta-secretase (bace)
JP5816630B2 (ja) 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
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)
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
CA2824097A1 (en) 2011-01-12 2012-07-19 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
MY162413A (en) 2011-01-13 2017-06-15 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
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US8399459B2 (en) 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US20130040971A1 (en) 2011-02-14 2013-02-14 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of cns disorders
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
CN103415519B (zh) 2011-03-01 2016-03-02 詹森药业有限公司 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物
US9067924B2 (en) 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
AU2012224632B2 (en) 2011-03-09 2016-06-16 Janssen Pharmaceutica Nv 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
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
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
US8604024B2 (en) 2011-05-24 2013-12-10 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
AR086539A1 (es) 2011-05-24 2014-01-08 Bristol Myers Squibb Co COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE
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
UA111749C2 (uk) 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
EP2788335B1 (en) 2011-12-06 2016-04-13 Janssen Pharmaceutica, N.V. 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives for the treatment of disorders in which beta-secretase is involved
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
CA2872181A1 (en) 2012-06-26 2014-01-03 F. Hoffmann-La Roche Ag Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
WO2014010748A1 (en) 2012-07-10 2014-01-16 Shionogi & Co., Ltd. Cyclopropane derivative having bace1 inhibiting activity
JP2014101354A (ja) 2012-10-24 2014-06-05 Shionogi & Co Ltd Bace1阻害作用を有するオキサジン誘導体
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
JP2014101353A (ja) 2012-10-26 2014-06-05 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
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
CN104968660A (zh) 2013-01-22 2015-10-07 霍夫曼-拉罗奇有限公司 作为bace1抑制剂的氟-[1,3]噁嗪类化合物
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.
AU2014253275B2 (en) 2013-04-11 2018-10-18 F. Hoffmann-La Roche Ag BACE1 inhibitors

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007049532A1 (ja) * 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体
WO2011070029A1 (en) * 2009-12-10 2011-06-16 F. Hoffmann-La Roche Ag Amino oxazine derivatives
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
WO2011069934A1 (en) * 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors
WO2012107371A1 (en) * 2011-02-08 2012-08-16 F. Hoffmann-La Roche Ag 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
WO2012139993A1 (en) * 2011-04-11 2012-10-18 F. Hoffmann-La Roche Ag 1,3 oxazines as bace1 and/or bace2 inhibitors
JP2014513702A (ja) * 2011-05-16 2014-06-05 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1,3−オキサジン
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
JP2014518895A (ja) * 2011-06-07 2014-08-07 エフ.ホフマン−ラ ロシュ アーゲー [1,3]オキサジン
JP2014524463A (ja) * 2011-08-25 2014-09-22 ノバルティス アーゲー 2−アミノ−4−(ピリジン−2−イル)−5,6−ジヒドロ−4h−1,3−オキサジン誘導体およびbace−1および/またはbace−2阻害剤としてのそれらの使用
JP2014526534A (ja) * 2011-09-21 2014-10-06 エフ.ホフマン−ラ ロシュ アーゲー BACE1阻害剤としてのN−(3−(2−アミノ−6,6−ジフルオロ−4,4a,5,6,7,7a−ヘキサヒドロ−シクロペンタ[e][1,3]オキサジン−4−イル)−フェニル)−アミド
WO2013110622A1 (en) * 2012-01-26 2013-08-01 F. Hoffmann-La Roche Ag Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
WO2013142613A1 (en) * 2012-03-20 2013-09-26 Elan Pharmaceuticals, Inc. Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HANS HILPERT ET AL: "β-Secretase(BACE1) Inhibitors with High in Vivo Efficacy Suitable for Clinical Evaluation in Alzhei", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 10, JPN6017020921, 16 April 2013 (2013-04-16), pages 3980 - 3995, ISSN: 0003647800 *
WOLTERING,T.J. ET AL: "BACE1 inhibitors: A head group scan on a series of amides", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 23, no. 14, JPN6017020923, 18 May 2013 (2013-05-18), pages 4239 - 4243, ISSN: 0003647801 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019507164A (ja) * 2016-03-01 2019-03-14 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Bace1阻害剤

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