CN102348698B - β-分泌酶的抑制剂 - Google Patents
β-分泌酶的抑制剂 Download PDFInfo
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- CN102348698B CN102348698B CN201080011490.5A CN201080011490A CN102348698B CN 102348698 B CN102348698 B CN 102348698B CN 201080011490 A CN201080011490 A CN 201080011490A CN 102348698 B CN102348698 B CN 102348698B
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- alkyl
- halo
- cycloalkyl
- heteroaryl
- phenyl
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/44—Nitrogen atoms not forming part of a nitro radical
- C07D233/46—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms attached to said nitrogen atoms
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
-
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
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- 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
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Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010021680A2 (en) | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| EP2801570A1 (en) | 2009-03-13 | 2014-11-12 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2539322B1 (en) | 2010-02-24 | 2014-01-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| US8415483B2 (en) * | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| 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 |
| EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use |
| US8962859B2 (en) | 2011-02-15 | 2015-02-24 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| EP2758406A1 (en) | 2011-09-21 | 2014-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9650336B2 (en) | 2011-10-10 | 2017-05-16 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
| TWI557112B (zh) * | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β-分泌酶抑制劑 |
| EP2847177B1 (en) | 2012-05-09 | 2017-10-11 | Boehringer Ingelheim International GmbH | Methods for making oxetan-3-ylmethanamines |
| KR20150023536A (ko) * | 2012-05-30 | 2015-03-05 | 코멘티스, 인코포레이티드 | 크로만 화합물 |
| EP2669286A1 (en) * | 2012-05-31 | 2013-12-04 | Ares Trading S.A. | Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases |
| US9000183B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000182B2 (en) * | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | 2H-imidazol-4-amine compounds and their use as BACE inhibitors |
| US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000185B2 (en) * | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether compounds and their use as BACE inhibitors |
| US10548882B2 (en) * | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β-分泌酶抑制劑 |
| WO2014051653A1 (en) | 2012-09-27 | 2014-04-03 | Portola Pharmaceuticals, Inc. | Bicyclic dihydropyridone kinase inhibitors |
| WO2014052398A1 (en) | 2012-09-28 | 2014-04-03 | Vitae Pharmaceuticals, Inc. | Inhibitor of beta-secretase |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9079832B2 (en) | 2012-11-21 | 2015-07-14 | Boehringer Ingelheim International Gmbh | Process for making N-sulfinyl α-amino amides |
| US10550327B2 (en) | 2012-11-21 | 2020-02-04 | Merck Patent Gmbh | Polymerisable compounds and the use thereof in liquid-crystal displays |
| EP2759310B2 (en) | 2013-01-28 | 2023-11-08 | Mölnlycke Health Care AB | Suction device |
| WO2014160775A1 (en) | 2013-03-26 | 2014-10-02 | Saint Louis University | Compositions and methods for the treatment of malaria |
| WO2016055858A1 (en) * | 2014-10-07 | 2016-04-14 | Astrazeneca Ab | Compounds and their use as bace inhibitors |
| JP6319805B2 (ja) * | 2014-10-08 | 2018-05-09 | 田岡化学工業株式会社 | スピロビフルオレン骨格を有するジオール化合物およびその製造方法 |
| CN106083764B (zh) * | 2016-07-11 | 2018-09-18 | 上海皓元生物医药科技有限公司 | 一种用于制备axl抑制剂的高纯度中间体的手性拆分方法 |
| US11505534B2 (en) | 2017-05-16 | 2022-11-22 | The University Of Chicago | Highly diastereoselective construction of the 4,5-spirocycle via palladium-catalyzed intramolecular alkenylation |
| EP3640244A4 (en) * | 2017-06-14 | 2020-11-25 | Nippon Soda Co., Ltd. | OXADIAZOLINE COMPOUND AND PEST-CONTROLLERS |
| KR101969528B1 (ko) | 2017-09-29 | 2019-04-16 | 에스케이텔레콤 주식회사 | 터치 디스플레이를 제어하는 장치와 방법 및 터치 디스플레이 시스템 |
| US11760701B2 (en) | 2018-02-27 | 2023-09-19 | The Research Foundation For The State University Of New Yrok | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
| CN108675923B (zh) * | 2018-06-27 | 2021-04-27 | 沅江华龙催化科技有限公司 | 一种由环酮化合物与2-芳基丙烯及二甲亚砜共同构建螺环化合物的方法 |
| CN108675922B (zh) * | 2018-06-27 | 2021-04-27 | 沅江华龙催化科技有限公司 | 一种螺环化合物及其合成方法 |
| WO2021065898A1 (ja) | 2019-09-30 | 2021-04-08 | 日本ケミファ株式会社 | アゼパン誘導体 |
| WO2021217508A1 (en) * | 2020-04-29 | 2021-11-04 | Novartis Ag | COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2α AND THEIR METHODS OF USE |
| IL314330A (en) | 2022-01-18 | 2024-09-01 | Maze Therapeutics Inc | Apol1 inhibitors and methods of use |
| TW202517642A (zh) * | 2023-07-11 | 2025-05-01 | 美商梅斯治療股份有限公司 | Apol1抑制劑及其使用方法 |
| WO2025015104A2 (en) * | 2023-07-11 | 2025-01-16 | Maze Therapeutics, Inc. | Apol1 inhibitors and methods of use |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101115482A (zh) * | 2004-12-13 | 2008-01-30 | 先灵公司 | 杂环天冬氨酰蛋白酶抑制剂 |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5745185A (en) * | 1980-07-21 | 1982-03-13 | Eisai Co Ltd | Hydantoin derivative and its preparation |
| AU655666B2 (en) | 1991-08-28 | 1995-01-05 | Pharmacia & Upjohn Company | Spirocyclic benzopyran imidazolines |
| EP0758313A4 (en) | 1994-05-06 | 1999-09-15 | Pharmacopeia Inc | COMBINATORIAL LIBRARY OF DIHYDROBENZOPYRANES |
| US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2153832B1 (en) * | 2003-12-15 | 2016-03-09 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) * | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| DE602005017033D1 (de) * | 2004-06-16 | 2009-11-19 | Wyeth Corp | Amino-5,5-diphenylimidazolon-derivate zur beta-sekretase-hemmung |
| MXPA06014792A (es) * | 2004-06-16 | 2007-02-16 | Wyeth Corp | Difenilimidazopirimidina y aminas imidazol como inhibidores de ??-secretasa. |
| CN101068545A (zh) | 2004-10-13 | 2007-11-07 | 默克公司 | 作为β-分泌酶抑制剂用于治疗阿尔茨海默病的螺哌啶化合物 |
| CN101198609A (zh) * | 2005-06-14 | 2008-06-11 | 先灵公司 | 天冬氨酰基蛋白酶抑制剂 |
| US7759353B2 (en) * | 2005-06-14 | 2010-07-20 | Schering Corporation | Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment |
| MX2008000212A (es) * | 2005-06-30 | 2008-03-24 | Wyeth Corp | Compuestos amino-5-(6 miembros)heteroarilimidazolona y el uso de estos para la modulacion de la (-secretasa. |
| 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 |
| EP1913193B1 (en) | 2005-07-29 | 2018-12-05 | Koninklijke Philips N.V. | Steam ironing devive for generating a burst of steam |
| KR20080050430A (ko) | 2005-09-26 | 2008-06-05 | 와이어쓰 | 베타-세크레타제 (bace) 억제제로서아미노-5-[4-(디플루오로메톡시)페닐]-5-페닐이미다졸론화합물 |
| CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| US7872009B2 (en) * | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
| DE102005057688A1 (de) | 2005-12-01 | 2007-06-14 | Endress + Hauser Flowtec Ag | Vorrichtung zur Bestimmung und/oder Überwachung des Massedurchflusses eines gasförmigen Mediums |
| CN101360737A (zh) | 2005-12-19 | 2009-02-04 | 惠氏公司 | 2-氨基-5-哌啶咪唑酮化合物和其用于β分泌酶调节的用途 |
| EP1974278A4 (en) | 2005-12-20 | 2012-01-04 | Fieldbus Foundation | SYSTEM AND METHOD FOR IMPLEMENTING INSTRUMENTED SAFETY SYSTEMS |
| WO2007100536A1 (en) * | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| CA2653650A1 (en) * | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| PT2042480E (pt) * | 2006-07-18 | 2013-06-24 | Astellas Pharma Inc | Derivado de aminoindano ou um seu sal |
| WO2008030412A2 (en) | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| WO2008076043A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5,5-diaryl-imidazol-4-ones |
| CL2008000784A1 (es) | 2007-03-20 | 2008-05-30 | Wyeth Corp | Compuestos amino-5-[-4-(diflourometoxi) fenil sustituido]-5-fenilmidazolona, inhibidores de b-secretasa; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar alzheimer, deterioro cognitivo, sindrome de down, disminucion co |
| AR065814A1 (es) | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
| RU2476430C2 (ru) | 2007-04-24 | 2013-02-27 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина, замещенные циклической группой |
| WO2008133273A1 (ja) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| WO2009103626A1 (en) * | 2008-02-18 | 2009-08-27 | F. Hoffmann-La Roche Ag | 4, 5-dihydro-oxazol-2-yl amine derivatives |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| 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 |
| WO2010021680A2 (en) * | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| KR20110073511A (ko) * | 2008-09-11 | 2011-06-29 | 암젠 인크 | 베타세크레타제 조절제로서의 스피로-테트라사이클릭 고리 화합물 및 사용 방법 |
| KR20110086769A (ko) | 2008-11-23 | 2011-07-29 | 화이자 인코포레이티드 | 베타 세크레타제 억제제로서의 락탐 |
| EP2801570A1 (en) * | 2009-03-13 | 2014-11-12 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| WO2011072064A1 (en) | 2009-12-08 | 2011-06-16 | Array Biopharma Inc. | S piro [chroman - 4, 4 ' - imidazol] ones as beta - secretase inhibitors |
| EP2539322B1 (en) * | 2010-02-24 | 2014-01-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β-分泌酶抑制劑 |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β-分泌酶抑制劑 |
| WO2014052398A1 (en) * | 2012-09-28 | 2014-04-03 | Vitae Pharmaceuticals, Inc. | Inhibitor of beta-secretase |
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| CN101115482A (zh) * | 2004-12-13 | 2008-01-30 | 先灵公司 | 杂环天冬氨酰蛋白酶抑制剂 |
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