JP2014505688A5 - - Google Patents
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- JP2014505688A5 JP2014505688A5 JP2013548830A JP2013548830A JP2014505688A5 JP 2014505688 A5 JP2014505688 A5 JP 2014505688A5 JP 2013548830 A JP2013548830 A JP 2013548830A JP 2013548830 A JP2013548830 A JP 2013548830A JP 2014505688 A5 JP2014505688 A5 JP 2014505688A5
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- JP
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- Prior art keywords
- disease
- bace
- present
- treating
- patent document
- 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.)
- Ceased
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 18
- 201000010099 disease Diseases 0.000 description 11
- 239000003814 drug Substances 0.000 description 10
- 239000003795 chemical substances by application Substances 0.000 description 7
- 208000035475 disorder Diseases 0.000 description 7
- 229940124597 therapeutic agent Drugs 0.000 description 6
- 208000024827 Alzheimer disease Diseases 0.000 description 5
- 210000004556 brain Anatomy 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 108090000765 processed proteins & peptides Proteins 0.000 description 4
- 102000003908 Cathepsin D Human genes 0.000 description 3
- 108090000258 Cathepsin D Proteins 0.000 description 3
- 208000010877 cognitive disease Diseases 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 208000027061 mild cognitive impairment Diseases 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 2
- 102100021257 Beta-secretase 1 Human genes 0.000 description 2
- 101710150192 Beta-secretase 1 Proteins 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 238000004220 aggregation Methods 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 238000002648 combination therapy Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000004770 neurodegeneration Effects 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 230000006641 stabilisation Effects 0.000 description 2
- 238000011105 stabilization Methods 0.000 description 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 description 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 description 1
- 102000035101 Aspartic proteases Human genes 0.000 description 1
- 108091005502 Aspartic proteases Proteins 0.000 description 1
- 208000024806 Brain atrophy Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 230000003044 adaptive effect Effects 0.000 description 1
- 239000003696 aspartic proteinase inhibitor Substances 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 239000013066 combination product Substances 0.000 description 1
- 229940127555 combination product Drugs 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 230000002121 endocytic effect Effects 0.000 description 1
- 238000012224 gene deletion Methods 0.000 description 1
- 210000002288 golgi apparatus Anatomy 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000015654 memory Effects 0.000 description 1
- 230000001394 metastastic effect Effects 0.000 description 1
- 206010061289 metastatic neoplasm Diseases 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000007505 plaque formation Effects 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 210000000225 synapse Anatomy 0.000 description 1
- 230000000946 synaptic effect Effects 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161432037P | 2011-01-12 | 2011-01-12 | |
| US61/432,037 | 2011-01-12 | ||
| PCT/EP2012/050387 WO2012095463A1 (en) | 2011-01-12 | 2012-01-11 | Oxazine derivatives and their use in the treatment of neurological disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014505688A JP2014505688A (ja) | 2014-03-06 |
| JP2014505688A5 true JP2014505688A5 (enExample) | 2015-03-05 |
Family
ID=45476523
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013548830A Ceased JP2014505688A (ja) | 2011-01-12 | 2012-01-11 | オキサジン誘導体および神経障害の処置におけるその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20130281449A1 (enExample) |
| EP (1) | EP2663559B1 (enExample) |
| JP (1) | JP2014505688A (enExample) |
| KR (1) | KR20140051822A (enExample) |
| CN (1) | CN103429589A (enExample) |
| AU (1) | AU2012206555A1 (enExample) |
| BR (1) | BR112013017779A2 (enExample) |
| CA (1) | CA2824097A1 (enExample) |
| EA (1) | EA201391029A1 (enExample) |
| MX (1) | MX2013008111A (enExample) |
| WO (1) | WO2012095463A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| AU2011263797B2 (en) | 2010-06-09 | 2014-06-05 | Janssen Pharmaceutica Nv | 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE) |
| JP5834091B2 (ja) | 2010-12-22 | 2015-12-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | ベータ−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な５，６−ジヒドロ−イミダゾ［１，２−ａ］ピラジン−８−イルアミン誘導体 |
| CA2824220C (en) | 2011-01-13 | 2020-09-01 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体 |
| EA201490774A1 (ru) | 2011-10-13 | 2014-08-29 | Новартис Аг | Новые производные оксазина и их применение при лечении заболевания |
| UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| 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 |
| CA2911693C (en) | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| CA2912156C (en) | 2013-06-12 | 2021-07-20 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| TW201609700A (zh) | 2014-02-19 | 2016-03-16 | Ｈ 朗德貝克公司 | ２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶作爲ｂａｃｅ１抑制劑用於治療阿茲海默症 |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| 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 |
| CA2967164A1 (en) | 2014-12-18 | 2016-06-23 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase |
| 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 |
| US20180244645A1 (en) | 2015-08-12 | 2018-08-30 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
| WO2018039062A1 (en) | 2016-08-26 | 2018-03-01 | Eli Lilly And Company | 1,4-oxazines useful as selective bace1 inhibitors |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| CA3047285A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| 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. |
| MA54100A (fr) | 2016-12-15 | 2021-10-20 | Amgen Inc | Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| KR102093540B1 (ko) | 2017-08-11 | 2020-03-25 | 주식회사 엘지화학 | 할로겐 치환된 스티렌 모노머의 제조방법 |
| CN111675708A (zh) * | 2020-06-10 | 2020-09-18 | 南京合巨药业有限公司 | 一种6-氰基-7-氮杂吲哚及其衍生物的制备方法 |
| CN111943947B (zh) * | 2020-07-24 | 2021-04-30 | 重庆文理学院 | 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6911868A (enExample) | 1968-08-31 | 1970-03-03 | ||
| DE19725802A1 (de) | 1996-07-10 | 1998-01-15 | Lonza Ag | Verfahren zur Herstellung von (S)- oder (R)-3,3,3-trifluor-2-hydroxy-2-methylpropionsäure |
| CA2514733A1 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| US7728025B2 (en) | 2003-12-29 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | 2-heteroaryl-substituted benzimidazole derivative |
| EP2612854B1 (en) * | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors |
| ES2548774T3 (es) | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Derivado de aminodihidrotiazina condensado |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体 |
| AR077328A1 (es) * | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| DK2483255T3 (da) * | 2010-07-13 | 2014-01-20 | Novartis Ag | Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser |
-
2012
- 2012-01-11 EA EA201391029A patent/EA201391029A1/ru unknown
- 2012-01-11 CN CN2012800128201A patent/CN103429589A/zh active Pending
- 2012-01-11 CA CA 2824097 patent/CA2824097A1/en not_active Abandoned
- 2012-01-11 EP EP12700232.7A patent/EP2663559B1/en not_active Not-in-force
- 2012-01-11 WO PCT/EP2012/050387 patent/WO2012095463A1/en not_active Ceased
- 2012-01-11 JP JP2013548830A patent/JP2014505688A/ja not_active Ceased
- 2012-01-11 KR KR20137021073A patent/KR20140051822A/ko not_active Withdrawn
- 2012-01-11 BR BR112013017779A patent/BR112013017779A2/pt not_active IP Right Cessation
- 2012-01-11 US US13/978,885 patent/US20130281449A1/en not_active Abandoned
- 2012-01-11 MX MX2013008111A patent/MX2013008111A/es not_active Application Discontinuation
- 2012-01-11 AU AU2012206555A patent/AU2012206555A1/en not_active Abandoned
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