AU2017376441B2 - Oxazine derivatives as beta-secretase inhibitors and methods of use - Google Patents
Oxazine derivatives as beta-secretase inhibitors and methods of use Download PDFInfo
- Publication number
- AU2017376441B2 AU2017376441B2 AU2017376441A AU2017376441A AU2017376441B2 AU 2017376441 B2 AU2017376441 B2 AU 2017376441B2 AU 2017376441 A AU2017376441 A AU 2017376441A AU 2017376441 A AU2017376441 A AU 2017376441A AU 2017376441 B2 AU2017376441 B2 AU 2017376441B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- tautomer
- oxazin
- dihydro
- pharmaceutically acceptable
- 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.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D413/02—Heterocyclic 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
- C07D413/10—Heterocyclic 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 carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D413/14—Heterocyclic 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Psychiatry (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434711P | 2016-12-15 | 2016-12-15 | |
| US62/434,711 | 2016-12-15 | ||
| US201762570425P | 2017-10-10 | 2017-10-10 | |
| US62/570,425 | 2017-10-10 | ||
| PCT/US2017/066177 WO2018112081A1 (en) | 2016-12-15 | 2017-12-13 | Oxazine derivatives as beta-secretase inhibitors and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2017376441A1 AU2017376441A1 (en) | 2019-07-04 |
| AU2017376441B2 true AU2017376441B2 (en) | 2021-10-14 |
Family
ID=60888744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017376441A Active AU2017376441B2 (en) | 2016-12-15 | 2017-12-13 | Oxazine derivatives as beta-secretase inhibitors and methods of use |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10947223B2 (enExample) |
| EP (1) | EP3555080B1 (enExample) |
| JP (1) | JP7177773B2 (enExample) |
| AU (1) | AU2017376441B2 (enExample) |
| CA (1) | CA3047286A1 (enExample) |
| MA (1) | MA52722A (enExample) |
| MX (1) | MX388696B (enExample) |
| WO (1) | WO2018112081A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2012129168A (ru) † | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| MX388697B (es) | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| MX386618B (es) | 2016-12-15 | 2025-03-19 | Amgen Inc | Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso. |
| 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. |
| AU2017376445B2 (en) | 2016-12-15 | 2021-09-30 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| BR112020021728A2 (pt) | 2018-04-27 | 2021-01-26 | Shionogi & Co., Ltd. | derivados de tetra-hidropiranooxazina tendo atividade inibitória de bace1 seletiva |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1942105A1 (en) * | 2005-10-25 | 2008-07-09 | Shionogi Co., Ltd. | Aminodihydrothiazine derivative |
| EP2151435A1 (en) * | 2007-04-24 | 2010-02-10 | Shionogi&Co., Ltd. | Pharmaceutical composition for treatment of alzheimer's disease |
| WO2013142613A1 (en) * | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| WO2014138484A1 (en) * | 2013-03-08 | 2014-09-12 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Family Cites Families (56)
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|---|---|---|---|---|
| US5441870A (en) | 1992-04-15 | 1995-08-15 | Athena Neurosciences, Inc. | Methods for monitoring cellular processing of β-amyloid precursor protein |
| SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
| JPH11507538A (ja) | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
| ES2318902T3 (es) | 1998-09-24 | 2009-05-01 | PHARMACIA & UPJOHN COMPANY LLC | Secretasa en la enfermedad del alzheimer. |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| BRPI0906962B8 (pt) | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| 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 |
| AU2009277485B2 (en) | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| 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 |
| US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| CN102686584A (zh) | 2009-11-13 | 2012-09-19 | 盐野义制药株式会社 | 具有氨基连接基的氨基噻嗪或氨基噁嗪衍生物 |
| US20120245154A1 (en) | 2009-12-09 | 2012-09-27 | Shionogi & Co., Ltd. | Substituted aminothiazine derivative |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| CN103429589A (zh) * | 2011-01-12 | 2013-12-04 | 诺瓦提斯公司 | 噁嗪衍生物及其在治疗神经障碍中的用途 |
| KR101569260B1 (ko) | 2011-01-13 | 2015-11-13 | 노파르티스 아게 | 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도 |
| 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 |
| WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| BR112013026341A2 (pt) | 2011-04-13 | 2019-09-24 | Merck Sharp & Dohe Corp. | composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia |
| WO2012147762A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | ピリジン誘導体およびそれを含有するbace1阻害剤 |
| EP2517898A1 (de) | 2011-04-29 | 2012-10-31 | Lanxess Deutschland GmbH | Kieselsäurehaltige Kautschukmischungen mit schwefelhaltigen Additiven |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| US8604024B2 (en) | 2011-05-24 | 2013-12-10 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| 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 |
| US8927535B2 (en) | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds |
| WO2013164730A1 (en) | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| WO2013182638A1 (en) | 2012-06-08 | 2013-12-12 | H. Lundbeck A/S | 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease |
| GB201212871D0 (en) | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
| JP2015529239A (ja) | 2012-09-20 | 2015-10-05 | ファイザー・インク | アルキル置換ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
| EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014062553A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | 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 |
| CA2886507C (en) | 2012-10-26 | 2016-09-20 | Eli Lilly And Company | Bace inhibitors |
| US9447085B2 (en) | 2012-12-14 | 2016-09-20 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use |
| CA2893333C (en) | 2012-12-19 | 2017-10-24 | Pfizer Inc. | Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| EP2935256B1 (en) | 2012-12-19 | 2018-01-24 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production |
| CN104870000A (zh) | 2012-12-20 | 2015-08-26 | 默沙东公司 | 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途 |
| US9580396B2 (en) | 2012-12-21 | 2017-02-28 | Merck Sharp & Dohme Corp. | C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use |
| 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 |
| MX381482B (es) | 2014-08-08 | 2025-03-12 | Amgen Inc | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. |
| JP6765681B2 (ja) | 2015-04-21 | 2020-10-07 | オールジェネシス バイオセラピューティクス インコーポレイテッド | Bace1阻害剤としての化合物およびそれらの使用 |
| US10246429B2 (en) | 2015-08-06 | 2019-04-02 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| MX388697B (es) * | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| AU2017376445B2 (en) * | 2016-12-15 | 2021-09-30 | 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. |
| MX386618B (es) | 2016-12-15 | 2025-03-19 | Amgen Inc | Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso. |
-
2017
- 2017-12-13 AU AU2017376441A patent/AU2017376441B2/en active Active
- 2017-12-13 CA CA3047286A patent/CA3047286A1/en active Pending
- 2017-12-13 MA MA052722A patent/MA52722A/fr unknown
- 2017-12-13 JP JP2019531733A patent/JP7177773B2/ja active Active
- 2017-12-13 MX MX2019007101A patent/MX388696B/es unknown
- 2017-12-13 US US16/466,211 patent/US10947223B2/en active Active
- 2017-12-13 EP EP17822984.5A patent/EP3555080B1/en active Active
- 2017-12-13 WO PCT/US2017/066177 patent/WO2018112081A1/en not_active Ceased
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1942105A1 (en) * | 2005-10-25 | 2008-07-09 | Shionogi Co., Ltd. | Aminodihydrothiazine derivative |
| EP2151435A1 (en) * | 2007-04-24 | 2010-02-10 | Shionogi&Co., Ltd. | Pharmaceutical composition for treatment of alzheimer's disease |
| WO2013142613A1 (en) * | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| WO2014138484A1 (en) * | 2013-03-08 | 2014-09-12 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2019007101A (es) | 2019-12-16 |
| WO2018112081A1 (en) | 2018-06-21 |
| US20200207747A1 (en) | 2020-07-02 |
| AU2017376441A1 (en) | 2019-07-04 |
| MX388696B (es) | 2025-03-20 |
| EP3555080A1 (en) | 2019-10-23 |
| JP2020503293A (ja) | 2020-01-30 |
| CA3047286A1 (en) | 2018-06-21 |
| US10947223B2 (en) | 2021-03-16 |
| JP7177773B2 (ja) | 2022-11-24 |
| MA52722A (fr) | 2021-04-14 |
| EP3555080B1 (en) | 2023-09-20 |
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