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
- Authority
- JP
- Japan
- Prior art keywords
- thia
- azabicyclo
- hept
- ethynyl
- 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.)
- Active
Links
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
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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Psychiatry (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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (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 (enExample) | 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 (enExample) |
| EP (1) | EP3555085B1 (enExample) |
| JP (1) | JP7159161B2 (enExample) |
| AU (1) | AU2017378316B2 (enExample) |
| MX (1) | MX386618B (enExample) |
| WO (1) | WO2018112086A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine 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 |
| CA3047286A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555106B1 (en) | 2016-12-15 | 2022-03-09 | 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. |
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 |
Family Cites Families (59)
| 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 |
| KR100768381B1 (ko) | 1998-09-24 | 2007-10-18 | 파마시아 앤드 업존 캄파니 엘엘씨 | 알츠하이머병 세크레타제 |
| ES2476027T3 (es) | 2005-10-25 | 2014-07-11 | Shionogi & Co., Ltd. | Derivados de aminodihidrotriazina |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 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 |
| HRP20151030T1 (hr) | 2008-01-18 | 2015-11-06 | Eisai R&D Management Co., Ltd. | Kondenzirani derivat aminodihidrotiazina |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| MX2010013256A (es) | 2008-06-13 | 2010-12-21 | Shionogi & Co | Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa. |
| 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 |
| WO2010038686A1 (ja) | 2008-09-30 | 2010-04-08 | 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 | |
| EP2500344A4 (en) | 2009-11-13 | 2013-05-01 | Shionogi & Co | AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION |
| 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 |
| JPWO2011071135A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | オキサジン誘導体 |
| CA2824097A1 (en) | 2011-01-12 | 2012-07-19 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| MA34898B1 (fr) | 2011-01-13 | 2014-02-01 | Novartis Ag | Nouveaux dérivés hétérocycliques et leur utilisation dans le traitement de troubles neurologiques |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (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 |
| WO2012139425A1 (en) | 2011-04-13 | 2012-10-18 | Schering Corporation | 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use |
| CN103649082A (zh) | 2011-04-26 | 2014-03-19 | 盐野义制药株式会社 | 吡啶衍生物和含有该吡啶衍生物的bace1抑制剂 |
| 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 |
| BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
| 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 |
| WO2013142613A1 (en) | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | 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 |
| 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 |
| WO2014062553A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | 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 |
| US9328124B2 (en) | 2012-10-26 | 2016-05-03 | 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 |
| WO2014098831A1 (en) | 2012-12-19 | 2014-06-26 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production |
| CA2893333C (en) | 2012-12-19 | 2017-10-24 | Pfizer Inc. | Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| 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 |
| EP2934534B1 (en) | 2012-12-21 | 2017-12-13 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | 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過フッ素化シクロプロピル縮合1,3−オキサジン−2−アミン化合物、及び使用方法 |
| 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 |
| SG11201708027XA (en) | 2015-04-21 | 2017-11-29 | Allgenesis Biotherapeutics Inc | Compounds and their use as bace1 inhibitors |
| 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 |
| CA3047286A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555106B1 (en) | 2016-12-15 | 2022-03-09 | 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 |
| 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. |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
-
2017
- 2017-12-13 EP EP17822987.8A patent/EP3555085B1/en active Active
- 2017-12-13 MX MX2019007103A patent/MX386618B/es unknown
- 2017-12-13 JP JP2019531735A patent/JP7159161B2/ja active Active
- 2017-12-13 AU AU2017378316A patent/AU2017378316B2/en active Active
- 2017-12-13 US US16/466,199 patent/US10889581B2/en active Active
- 2017-12-13 WO PCT/US2017/066184 patent/WO2018112086A1/en not_active Ceased
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 |
|---|---|
| MX386618B (es) | 2025-03-19 |
| AU2017378316B2 (en) | 2021-04-01 |
| EP3555085A1 (en) | 2019-10-23 |
| EP3555085B1 (en) | 2020-12-02 |
| JP2020503295A (ja) | 2020-01-30 |
| WO2018112086A1 (en) | 2018-06-21 |
| US20200231585A1 (en) | 2020-07-23 |
| CA3047287A1 (en) | 2018-06-21 |
| MX2019007103A (es) | 2019-11-05 |
| US10889581B2 (en) | 2021-01-12 |
| AU2017378316A1 (en) | 2019-07-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6483146B2 (ja) | アルツハイマー病治療用のbace1阻害剤としての2−アミノ−3,5,5−トリフルオロ−3,4,5,6−テトラヒドロピリジン | |
| JP7159161B2 (ja) | 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) | 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 | |
| EP3515897B1 (en) | Piperazine carbamates as modulators of magl and/or abhd6 and their use | |
| JP7149271B2 (ja) | 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 | |
| JP7148518B2 (ja) | β-セクレターゼ阻害剤としての二環式チアジンおよびオキサジン誘導体ならびに使用方法 | |
| JP7149272B2 (ja) | β-セクレターゼ阻害剤としてのチアジン誘導体および使用方法 | |
| TW201321384A (zh) | 作為鈣通道阻斷劑之經取代之八氫吡咯并[1,2-a]吡□磺醯胺 | |
| CA3047287C (en) | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use | |
| US20180230160A1 (en) | 2-amino-7a-phenyl-3,4,4a,5,7,7a-hexahydrofuro[3,4-b]pyridines as bace1 inhibitors | |
| HK40010192B (en) | Piperazine carbamates as modulators of magl and/or abhd6 and their use | |
| HK40010192A (en) | Piperazine carbamates as modulators of magl and/or abhd6 and their use | |
| OA18264A (en) | 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl3,4,5,6-tetrahydropyridines as bacel inhibitors for treating Alzheimer's disease. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20201210 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20201210 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20211118 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20211207 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20220301 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20221004 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20221012 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7159161 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |