AU2017376444B2 - Thiazine derivatives as beta-secretase inhibitors and methods of use - Google Patents
Thiazine derivatives as beta-secretase inhibitors and methods of use Download PDFInfo
- Publication number
- AU2017376444B2 AU2017376444B2 AU2017376444A AU2017376444A AU2017376444B2 AU 2017376444 B2 AU2017376444 B2 AU 2017376444B2 AU 2017376444 A AU2017376444 A AU 2017376444A AU 2017376444 A AU2017376444 A AU 2017376444A AU 2017376444 B2 AU2017376444 B2 AU 2017376444B2
- Authority
- AU
- Australia
- Prior art keywords
- tautomer
- compound
- amino
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434714P | 2016-12-15 | 2016-12-15 | |
| US62/434,714 | 2016-12-15 | ||
| PCT/US2017/066179 WO2018112083A1 (en) | 2016-12-15 | 2017-12-13 | Thiazine derivatives as beta-secretase inhibitors and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2017376444A1 AU2017376444A1 (en) | 2019-07-04 |
| AU2017376444B2 true AU2017376444B2 (en) | 2021-09-30 |
Family
ID=60888745
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017376444A Active AU2017376444B2 (en) | 2016-12-15 | 2017-12-13 | Thiazine derivatives as beta-secretase inhibitors and methods of use |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10889579B2 (OSRAM) |
| EP (1) | EP3555084B1 (OSRAM) |
| JP (1) | JP7149272B2 (OSRAM) |
| AU (1) | AU2017376444B2 (OSRAM) |
| CA (1) | CA3047288A1 (OSRAM) |
| ES (1) | ES2910791T3 (OSRAM) |
| MA (1) | MA54100A (OSRAM) |
| MX (1) | MX388697B (OSRAM) |
| WO (1) | WO2018112083A1 (OSRAM) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA54100A (fr) | 2016-12-15 | 2021-10-20 | Amgen Inc | Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| JP7177773B2 (ja) * | 2016-12-15 | 2022-11-24 | 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オキサジン誘導体および使用方法 |
| JP7149271B2 (ja) | 2016-12-15 | 2022-10-06 | 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1,4-チアジンジオキシドおよび1,2,4-チアジアジンジオキシド誘導体ならびに使用方法 |
| JP7159161B2 (ja) | 2016-12-15 | 2022-10-24 | 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誘導体および使用方法 |
| WO2018112084A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2305672A1 (en) * | 2008-06-13 | 2011-04-06 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
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| SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
| WO1996040885A2 (en) | 1995-06-07 | 1996-12-19 | Athena Neurosciences, Inc. | β-SECRETASE, ANTIBODIES TO β-SECRETASE, AND ASSAYS FOR DETECTING β-SECRETASE INHIBITION |
| CN1198936C (zh) | 1998-09-24 | 2005-04-27 | 法玛西雅厄普约翰美国公司 | 阿尔茨海默氏疾病分泌酶 |
| RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
| TW200902526A (en) | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
| 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 |
| JP4520533B2 (ja) | 2008-01-18 | 2010-08-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 縮合アミノジヒドロチアジン誘導体 |
| 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 |
| WO2010013794A1 (en) | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| CN102171221B (zh) | 2008-09-30 | 2013-11-06 | 卫材R&D管理有限公司 | 新的稠合的氨基二氢噻嗪衍生物 |
| 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 | |
| WO2011058763A1 (ja) | 2009-11-13 | 2011-05-19 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
| WO2011070781A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 置換アミノチアジン誘導体 |
| 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 |
| KR20120104570A (ko) | 2009-12-11 | 2012-09-21 | 시오노기세야쿠 가부시키가이샤 | 옥사진 유도체 |
| JP2014505688A (ja) | 2011-01-12 | 2014-03-06 | ノバルティス アーゲー | 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 |
| DK2663561T3 (en) | 2011-01-13 | 2016-06-06 | Novartis Ag | New heterocyclic derivatives and their use in treating neurological disorders |
| 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 |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9499502B2 (en) | 2011-04-13 | 2016-11-22 | Merck Sharp & Dohme Corp. | 5-substituted iminothiazines and their mono- and dioxides as BACE inhibitors, compositions, and their use |
| 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 |
| US8598161B2 (en) | 2011-05-24 | 2013-12-03 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| US8927535B2 (en) | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
| 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 |
| AU2013235117A1 (en) | 2012-03-20 | 2014-10-16 | Dean R. Artis | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| 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 |
| US9260455B2 (en) | 2012-09-20 | 2016-02-16 | Pfizer Inc. | Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9422277B2 (en) | 2012-10-17 | 2016-08-23 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
| EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| SI2912041T1 (sl) | 2012-10-26 | 2017-02-28 | Eli Lilly And Company | Derivati tetrahidropirolotiazina kot inhibitorji beta sekretaze (bace) |
| EP2931284B1 (en) | 2012-12-14 | 2017-08-23 | Merck Sharp & Dohme Corp. | Bace inhibitors of iminothiadiazine dioxides |
| 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 |
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| CA2894919A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5,c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9580396B2 (en) | 2012-12-21 | 2017-02-28 | Merck Sharp & Dohme Corp. | C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use |
| SG11201507196WA (en) | 2013-03-08 | 2015-10-29 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of 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 |
| 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 |
| JP7159161B2 (ja) | 2016-12-15 | 2022-10-24 | 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誘導体および使用方法 |
| JP7177773B2 (ja) | 2016-12-15 | 2022-11-24 | 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オキサジン誘導体および使用方法 |
| MA54100A (fr) | 2016-12-15 | 2021-10-20 | Amgen Inc | Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| WO2018112084A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CN108064136B (zh) | 2016-12-23 | 2019-09-20 | 深圳市柔宇科技有限公司 | 一种智能雨伞 |
-
2017
- 2017-12-13 MA MA054100A patent/MA54100A/fr unknown
- 2017-12-13 MX MX2019007102A patent/MX388697B/es unknown
- 2017-12-13 AU AU2017376444A patent/AU2017376444B2/en active Active
- 2017-12-13 ES ES17822985T patent/ES2910791T3/es active Active
- 2017-12-13 US US16/466,209 patent/US10889579B2/en active Active
- 2017-12-13 JP JP2019531722A patent/JP7149272B2/ja active Active
- 2017-12-13 EP EP17822985.2A patent/EP3555084B1/en active Active
- 2017-12-13 WO PCT/US2017/066179 patent/WO2018112083A1/en not_active Ceased
- 2017-12-13 CA CA3047288A patent/CA3047288A1/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2305672A1 (en) * | 2008-06-13 | 2011-04-06 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
Also Published As
| Publication number | Publication date |
|---|---|
| US10889579B2 (en) | 2021-01-12 |
| MA54100A (fr) | 2021-10-20 |
| EP3555084A1 (en) | 2019-10-23 |
| EP3555084B1 (en) | 2022-03-16 |
| JP7149272B2 (ja) | 2022-10-06 |
| ES2910791T3 (es) | 2022-05-13 |
| MX388697B (es) | 2025-03-20 |
| MX2019007102A (es) | 2019-12-16 |
| JP2020503292A (ja) | 2020-01-30 |
| WO2018112083A1 (en) | 2018-06-21 |
| AU2017376444A1 (en) | 2019-07-04 |
| US20200062743A1 (en) | 2020-02-27 |
| CA3047288A1 (en) | 2018-06-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |