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 |
|---|---|---|---|---|
| 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 |
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | 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 |
| JP6576433B2 (ja) | 2014-08-08 | 2019-09-18 | アムジエン・インコーポレーテツド | 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 |
| 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 |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| CA3047287A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| JP7148518B2 (ja) | 2016-12-15 | 2022-10-05 | アムジエン・インコーポレーテツド | β－セクレターゼ阻害剤としての二環式チアジンおよびオキサジン誘導体ならびに使用方法 |
| 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. |
| WO2018112083A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine 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 |
|---|---|---|---|---|
| SG162790A1 (en) | 2005-06-14 | 2010-07-29 | Schering Corp | Aspartyl protease inhibitors |
| JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
| ES2548774T3 (es) | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Derivado de aminodihidrotiazina condensado |
| US8541427B2 (en) | 2008-04-22 | 2013-09-24 | Merck, Sharp & Dohme, Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| KR20110076965A (ko) | 2008-09-30 | 2011-07-06 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신규한 축합 아미노 디하이드로티아진 유도체 |
| 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 |
| WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| 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 LT LTEP13785730.6T patent/LT2912041T/lt unknown
- 2013-10-17 DK DK13785730.6T patent/DK2912041T3/en active
- 2013-10-17 EP EP13785730.6A patent/EP2912041B1/en active Active
- 2013-10-17 CA CA2886507A patent/CA2886507C/en not_active Expired - Fee Related
- 2013-10-17 HR HRP20170025TT patent/HRP20170025T1/hr unknown
- 2013-10-17 RS RS20170016A patent/RS55561B1/sr unknown
- 2013-10-17 WO PCT/US2013/065418 patent/WO2014066132A1/en not_active Ceased
- 2013-10-17 HU HUE13785730A patent/HUE031764T2/en unknown
- 2013-10-17 US US14/427,648 patent/US9328124B2/en not_active Expired - Fee Related
- 2013-10-17 PL PL13785730T patent/PL2912041T3/pl unknown
- 2013-10-17 SI SI201330463T patent/SI2912041T1/sl unknown
- 2013-10-17 ES ES13785730.6T patent/ES2616835T3/es active Active
- 2013-10-17 CN CN201380055699.5A patent/CN104755484B/zh not_active Expired - Fee Related
- 2013-10-17 JP JP2015539666A patent/JP6243921B2/ja not_active Expired - Fee Related
- 2013-10-17 PT PT137857306T patent/PT2912041T/pt unknown
-
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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