JP2015535247A5 - - Google Patents
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- Publication number
- JP2015535247A5 JP2015535247A5 JP2015539666A JP2015539666A JP2015535247A5 JP 2015535247 A5 JP2015535247 A5 JP 2015535247A5 JP 2015539666 A JP2015539666 A JP 2015539666A JP 2015539666 A JP2015539666 A JP 2015539666A JP 2015535247 A5 JP2015535247 A5 JP 2015535247A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- salt
- pharmaceutical composition
- acceptable salt
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 102100021257 Beta-secretase 1 Human genes 0.000 description 4
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 description 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699660 Mus musculus Species 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000005013 brain tissue Anatomy 0.000 description 1
- 210000003710 cerebral cortex Anatomy 0.000 description 1
- 210000001320 hippocampus Anatomy 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 230000009261 transgenic effect Effects 0.000 description 1
- 238000011830 transgenic mouse model Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261718728P | 2012-10-26 | 2012-10-26 | |
| US61/718,728 | 2012-10-26 | ||
| PCT/US2013/065418 WO2014066132A1 (en) | 2012-10-26 | 2013-10-17 | Bace inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015535247A JP2015535247A (ja) | 2015-12-10 |
| JP2015535247A5 true JP2015535247A5 (enExample) | 2016-12-01 |
| JP6243921B2 JP6243921B2 (ja) | 2017-12-06 |
Family
ID=49515508
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015539666A Expired - Fee Related JP6243921B2 (ja) | 2012-10-26 | 2013-10-17 | Ｂａｃｅ阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9328124B2 (enExample) |
| EP (1) | EP2912041B1 (enExample) |
| JP (1) | JP6243921B2 (enExample) |
| CN (1) | CN104755484B (enExample) |
| CA (1) | CA2886507C (enExample) |
| CY (1) | CY1118623T1 (enExample) |
| DK (1) | DK2912041T3 (enExample) |
| ES (1) | ES2616835T3 (enExample) |
| HR (1) | HRP20170025T1 (enExample) |
| HU (1) | HUE031764T2 (enExample) |
| LT (1) | LT2912041T (enExample) |
| ME (1) | ME02576B (enExample) |
| PL (1) | PL2912041T3 (enExample) |
| PT (1) | PT2912041T (enExample) |
| RS (1) | RS55561B1 (enExample) |
| SI (1) | SI2912041T1 (enExample) |
| WO (1) | WO2014066132A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| AU2014225604B2 (en) | 2013-03-08 | 2018-05-17 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| TWI684452B (zh) * | 2014-03-14 | 2020-02-11 | 美國禮來大藥廠 | 胺基噻嗪化合物 |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| MA54100A (fr) | 2016-12-15 | 2021-10-20 | Amgen Inc | Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| MX387729B (es) | 2016-12-15 | 2025-03-18 | Amgen Inc | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
| CA3047285A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CN106632001A (zh) * | 2016-12-28 | 2017-05-10 | 山东诚汇双达药业有限公司 | 一种4‑（溴乙酰基）吡啶氢溴酸盐的制备方法 |
| CN110452179A (zh) * | 2019-06-25 | 2019-11-15 | 南京普锐达医药科技有限公司 | 一种2-氯-4-甲氧基-5-氰基嘧啶的合成方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101228163A (zh) | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
| 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 |
| ES2548774T3 (es) | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Derivado de aminodihidrotiazina condensado |
| CL2009000954A1 (es) * | 2008-04-22 | 2010-12-31 | Schering Corp | Compuestos derivados de 2-imino-3-metil pirrolo pirimidinona,inhibidores de bace-1; composicion farmaceutica; y su uso para tratar, prevenir y/o retardar el inicio de una patologia de beta-amiloide seleccionada de enfermedad de alzheimer, enfermedad de parkinson, perdida de la memoria, sindrome de down, entre otras. |
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 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 |
| AU2009300836B2 (en) | 2008-09-30 | 2014-02-27 | Eisai R&D Management Co., Ltd. | Novel fused aminodihydrothiazine derivative |
| 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 |
| 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 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| TW201302763A (zh) | 2011-05-24 | 2013-01-16 | 必治妥美雅史谷比公司 | 用於減少β－類澱粉產生之化合物 |
| JO3143B1 (ar) * | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| GB201212871D0 (en) * | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
-
2013
- 2013-10-17 HU HUE13785730A patent/HUE031764T2/en unknown
- 2013-10-17 PL PL13785730T patent/PL2912041T3/pl unknown
- 2013-10-17 CN CN201380055699.5A patent/CN104755484B/zh not_active Expired - Fee Related
- 2013-10-17 EP EP13785730.6A patent/EP2912041B1/en active Active
- 2013-10-17 HR HRP20170025TT patent/HRP20170025T1/hr unknown
- 2013-10-17 JP JP2015539666A patent/JP6243921B2/ja not_active Expired - Fee Related
- 2013-10-17 RS RS20170016A patent/RS55561B1/sr unknown
- 2013-10-17 CA CA2886507A patent/CA2886507C/en not_active Expired - Fee Related
- 2013-10-17 WO PCT/US2013/065418 patent/WO2014066132A1/en not_active Ceased
- 2013-10-17 DK DK13785730.6T patent/DK2912041T3/en active
- 2013-10-17 SI SI201330463T patent/SI2912041T1/sl unknown
- 2013-10-17 PT PT137857306T patent/PT2912041T/pt unknown
- 2013-10-17 US US14/427,648 patent/US9328124B2/en not_active Expired - Fee Related
- 2013-10-17 LT LTEP13785730.6T patent/LT2912041T/lt unknown
- 2013-10-17 ES ES13785730.6T patent/ES2616835T3/es active Active
-
2017
- 2017-02-10 CY CY20171100191T patent/CY1118623T1/el unknown
- 2017-02-10 ME MEP-2017-4A patent/ME02576B/me unknown
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