JP7159161B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP7159161B2 JP7159161B2 JP2019531735A JP2019531735A JP7159161B2 JP 7159161 B2 JP7159161 B2 JP 7159161B2 JP 2019531735 A JP2019531735 A JP 2019531735A JP 2019531735 A JP2019531735 A JP 2019531735A JP 7159161 B2 JP7159161 B2 JP 7159161B2
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- Prior art keywords
- thia
- azabicyclo
- hept
- ethynyl
- amino
- Prior art date
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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
- C07D417/14—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 three or more hetero 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
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
-
- 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
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- 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434721P | 2016-12-15 | 2016-12-15 | |
| US62/434,721 | 2016-12-15 | ||
| PCT/US2017/066184 WO2018112086A1 (en) | 2016-12-15 | 2017-12-13 | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020503295A JP2020503295A (ja) | 2020-01-30 |
| JP2020503295A5 JP2020503295A5 (cg-RX-API-DMAC7.html) | 2021-01-28 |
| JP7159161B2 true JP7159161B2 (ja) | 2022-10-24 |
Family
ID=60888747
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019531735A Active JP7159161B2 (ja) | 2016-12-15 | 2017-12-13 | 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 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10889581B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3555085B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP7159161B2 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2017378316B2 (cg-RX-API-DMAC7.html) |
| MX (1) | MX386618B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2018112086A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11548903B2 (en) | 2016-12-15 | 2023-01-10 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| MA52722A (fr) | 2016-12-15 | 2021-04-14 | Amgen Inc | Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| AU2017376446B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016022724A1 (en) | 2014-08-08 | 2016-02-11 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JP2016505055A (ja) | 2013-01-22 | 2016-02-18 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤としてのフルオロ−[1,3]オキサジン |
| JP2016511258A (ja) | 2013-03-01 | 2016-04-14 | アムジエン・インコーポレーテツド | ベータ−セクレターゼ阻害剤としてのパーフルオロ化5,6−ジヒドロ−4h−1,3−オキサジン−2−アミン化合物および使用方法 |
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| EP1115874B1 (en) | 1998-09-24 | 2009-01-07 | Pharmacia & Upjohn Company LLC | Alzheimer's disease secretase |
| KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
| 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 |
| MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
| US20100317850A1 (en) | 2008-01-18 | 2010-12-16 | Yuichi Suzuki | Condensed aminodihydrothiazine derivative |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting 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 |
| MX2011003189A (es) | 2008-09-30 | 2011-04-27 | Eisai R&D Man Co Ltd | Nuevo derivado de aminodihidrotiazina fusionada. |
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| 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 |
| 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 |
| US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
| EA201391029A1 (ru) | 2011-01-12 | 2014-01-30 | Новартис Аг | Производные оксазина и их применение при лечении неврологических нарушений |
| 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 |
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| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | 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 |
| JPWO2012147762A1 (ja) | 2011-04-26 | 2014-07-28 | 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 |
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| EP2751116B1 (en) | 2011-08-31 | 2016-10-12 | Pfizer Inc | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
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| 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 |
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| CN104755484B (zh) | 2012-10-26 | 2016-02-17 | 伊莱利利公司 | Bace抑制剂 |
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| 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 |
| 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 |
| MA52722A (fr) | 2016-12-15 | 2021-04-14 | Amgen Inc | Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| AU2017376446B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| US11548903B2 (en) | 2016-12-15 | 2023-01-10 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
-
2017
- 2017-12-13 AU AU2017378316A patent/AU2017378316B2/en active Active
- 2017-12-13 MX MX2019007103A patent/MX386618B/es unknown
- 2017-12-13 WO PCT/US2017/066184 patent/WO2018112086A1/en not_active Ceased
- 2017-12-13 US US16/466,199 patent/US10889581B2/en active Active
- 2017-12-13 JP JP2019531735A patent/JP7159161B2/ja active Active
- 2017-12-13 EP EP17822987.8A patent/EP3555085B1/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016505055A (ja) | 2013-01-22 | 2016-02-18 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤としてのフルオロ−[1,3]オキサジン |
| JP2016511258A (ja) | 2013-03-01 | 2016-04-14 | アムジエン・インコーポレーテツド | ベータ−セクレターゼ阻害剤としてのパーフルオロ化5,6−ジヒドロ−4h−1,3−オキサジン−2−アミン化合物および使用方法 |
| WO2016022724A1 (en) | 2014-08-08 | 2016-02-11 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2020503295A (ja) | 2020-01-30 |
| WO2018112086A1 (en) | 2018-06-21 |
| CA3047287A1 (en) | 2018-06-21 |
| AU2017378316A1 (en) | 2019-07-04 |
| US10889581B2 (en) | 2021-01-12 |
| AU2017378316B2 (en) | 2021-04-01 |
| EP3555085B1 (en) | 2020-12-02 |
| EP3555085A1 (en) | 2019-10-23 |
| MX2019007103A (es) | 2019-11-05 |
| US20200231585A1 (en) | 2020-07-23 |
| MX386618B (es) | 2025-03-19 |
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