CA3047285A1 - Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use - Google Patents
Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use Download PDFInfo
- Publication number
- CA3047285A1 CA3047285A1 CA3047285A CA3047285A CA3047285A1 CA 3047285 A1 CA3047285 A1 CA 3047285A1 CA 3047285 A CA3047285 A CA 3047285A CA 3047285 A CA3047285 A CA 3047285A CA 3047285 A1 CA3047285 A1 CA 3047285A1
- Authority
- CA
- Canada
- Prior art keywords
- fluoro
- tautomer
- compound
- thiazin
- amino
- 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.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434719P | 2016-12-15 | 2016-12-15 | |
| US62/434,719 | 2016-12-15 | ||
| US201762570429P | 2017-10-10 | 2017-10-10 | |
| US62/570,429 | 2017-10-10 | ||
| PCT/US2017/066180 WO2018112084A1 (en) | 2016-12-15 | 2017-12-13 | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3047285A1 true CA3047285A1 (en) | 2018-06-21 |
Family
ID=60888746
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3047285A Pending CA3047285A1 (en) | 2016-12-15 | 2017-12-13 | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US11548903B2 (enExample) |
| EP (1) | EP3555106B1 (enExample) |
| JP (1) | JP7148518B2 (enExample) |
| AU (1) | AU2017376445B2 (enExample) |
| CA (1) | CA3047285A1 (enExample) |
| ES (1) | ES2910367T3 (enExample) |
| MA (1) | MA54101A (enExample) |
| MX (1) | MX394391B (enExample) |
| WO (1) | WO2018112084A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2012006491A (es) † | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| AU2017376441B2 (en) * | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| MX394391B (es) | 2016-12-15 | 2025-03-24 | Amgen Inc | Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso. |
| CA3047290A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| CA3047288A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
Family Cites Families (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| PL205294B1 (pl) | 1998-09-24 | 2010-03-31 | Upjohn Co | Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta |
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
| US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
| PL2233474T3 (pl) | 2008-01-18 | 2015-12-31 | Eisai R&D Man Co Ltd | Skondensowana pochodna aminodihydrotiazyny |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| 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 |
| CN102105475B (zh) | 2008-07-28 | 2014-04-09 | 卫材R&D管理有限公司 | 螺氨基二氢噻嗪衍生物 |
| JP5666304B2 (ja) * | 2008-09-30 | 2015-02-12 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
| 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 | |
| US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
| JPWO2011070781A1 (ja) | 2009-12-09 | 2013-04-22 | 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 |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| CA2824097A1 (en) | 2011-01-12 | 2012-07-19 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| MY162413A (en) | 2011-01-13 | 2017-06-15 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of 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 |
| 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 |
| US20140235626A1 (en) | 2011-04-26 | 2014-08-21 | Shionogi & Co., Ltd. | Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them |
| 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 |
| AR086539A1 (es) | 2011-05-24 | 2014-01-08 | Bristol Myers Squibb Co | COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE |
| US8927535B2 (en) | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | 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 |
| EP2827857A4 (en) | 2012-03-20 | 2016-03-30 | Elan Pharm Inc | SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE 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 |
| EP2897964A1 (en) | 2012-09-20 | 2015-07-29 | Pfizer Inc. | Alkyl-substituted hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
| EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9422277B2 (en) | 2012-10-17 | 2016-08-23 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| SI2912041T1 (sl) | 2012-10-26 | 2017-02-28 | Eli Lilly And Company | Derivati tetrahidropirolotiazina kot inhibitorji beta sekretaze (bace) |
| WO2014093190A1 (en) | 2012-12-14 | 2014-06-19 | Merck Sharp & Dohme Corp. | Bace inhibitors of iminothiadiazine dioxides |
| US9475784B2 (en) | 2012-12-19 | 2016-10-25 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production |
| US9403846B2 (en) | 2012-12-19 | 2016-08-02 | Pfizer Inc. | Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| EP2934539B1 (en) | 2012-12-20 | 2019-03-27 | Merck Sharp & Dohme Corp. | C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors |
| WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| MX374512B (es) | 2013-03-08 | 2025-03-06 | Amgen Inc | Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso. |
| 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 |
| CN106795147B (zh) | 2014-08-08 | 2020-09-22 | 美国安进公司 | 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法 |
| ES2942308T3 (es) | 2015-04-21 | 2023-05-31 | Allgenesis Biotherapeutics Inc | Compuestos y su uso como inhibidores de BACE1 |
| 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 |
| MX394391B (es) | 2016-12-15 | 2025-03-24 | Amgen Inc | Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso. |
| CA3047288A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| CA3047290A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
-
2017
- 2017-12-13 MX MX2019007100A patent/MX394391B/es unknown
- 2017-12-13 AU AU2017376445A patent/AU2017376445B2/en active Active
- 2017-12-13 US US16/466,202 patent/US11548903B2/en active Active
- 2017-12-13 CA CA3047285A patent/CA3047285A1/en active Pending
- 2017-12-13 WO PCT/US2017/066180 patent/WO2018112084A1/en not_active Ceased
- 2017-12-13 JP JP2019531734A patent/JP7148518B2/ja active Active
- 2017-12-13 EP EP17822986.0A patent/EP3555106B1/en active Active
- 2017-12-13 ES ES17822986T patent/ES2910367T3/es active Active
- 2017-12-13 MA MA054101A patent/MA54101A/fr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX394391B (es) | 2025-03-24 |
| WO2018112084A1 (en) | 2018-06-21 |
| EP3555106A1 (en) | 2019-10-23 |
| US11548903B2 (en) | 2023-01-10 |
| ES2910367T3 (es) | 2022-05-12 |
| JP7148518B2 (ja) | 2022-10-05 |
| MX2019007100A (es) | 2019-12-16 |
| AU2017376445A1 (en) | 2019-07-04 |
| JP2020503294A (ja) | 2020-01-30 |
| AU2017376445B2 (en) | 2021-09-30 |
| MA54101A (fr) | 2021-10-27 |
| EP3555106B1 (en) | 2022-03-09 |
| US20200199153A1 (en) | 2020-06-25 |
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| AU2017376445B2 (en) | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use | |
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| EP3555086B1 (en) | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use | |
| US10889579B2 (en) | Thiazine derivatives as β-secretase inhibitors and methods of use | |
| US10889581B2 (en) | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use | |
| EP4568975A1 (en) | Heterocyclic compound | |
| CA3047287C (en) | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
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