DK2912041T3 - Tetrahydropyrrolothiazinderivater som bace-inhibitorer - Google Patents
Tetrahydropyrrolothiazinderivater som bace-inhibitorer Download PDFInfo
- Publication number
- DK2912041T3 DK2912041T3 DK13785730.6T DK13785730T DK2912041T3 DK 2912041 T3 DK2912041 T3 DK 2912041T3 DK 13785730 T DK13785730 T DK 13785730T DK 2912041 T3 DK2912041 T3 DK 2912041T3
- Authority
- DK
- Denmark
- Prior art keywords
- mmol
- compound
- give
- solution
- added
- Prior art date
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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (11)
1. Forbindelse
med formlen: hvor A er udvalgt fra gruppen bestående af;
R1 er H eller F; R2 er H, -OCH3, C1-C3 alkyl,
R3 er H, -CH3 eller -OCH3; og R4 er H eller F; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse eller salt ifølge krav 1, hvor A er udvalgt fra gruppen bestående af:
3. Forbindelse eller salt ifølge krav 1 eller krav 2, hvor A er udvalgt fra gruppen bestående af:
4. Forbindelse eller salt ifølge et af kravene 1-3, hvor A er:
5. Forbindelse eller salt ifølge et af kravene 1 til 4, hvor R2 er
6. Forbindelse eller salt ifølge et af kravene 1 til 5, hvor R1 er F.
7. Forbindelse eller salt ifølge krav 1, som er 2-[2-[(4aR,7aR)-2-amino-7a- pyrazin-2-yl-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-6-yl]-5-fluor-pyrimidin-4-yl]propan-2-ol.
8. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge et af kravene 1-7 til anvendelse inden for terapi.
9. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge et af kravene 1-7 til anvendelse inden for behandlingen af Alzheimers sygdom.
10. Farmaceutisk sammensætning omfattende en forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge et af kravene 1-7 med et eller flere farmaceutisk acceptable bærestoffer, fortyndingsmidler eller hjælpestoffer.
11. Farmaceutisk sammensætning ifølge krav 10, yderligere omfattende et eller flere andre terapeutiske midler.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261718728P | 2012-10-26 | 2012-10-26 | |
| PCT/US2013/065418 WO2014066132A1 (en) | 2012-10-26 | 2013-10-17 | Bace inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2912041T3 true DK2912041T3 (da) | 2017-02-27 |
Family
ID=49515508
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK13785730.6T DK2912041T3 (da) | 2012-10-26 | 2013-10-17 | Tetrahydropyrrolothiazinderivater som bace-inhibitorer |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9328124B2 (da) |
| EP (1) | EP2912041B1 (da) |
| JP (1) | JP6243921B2 (da) |
| CN (1) | CN104755484B (da) |
| CA (1) | CA2886507C (da) |
| CY (1) | CY1118623T1 (da) |
| DK (1) | DK2912041T3 (da) |
| ES (1) | ES2616835T3 (da) |
| HR (1) | HRP20170025T1 (da) |
| HU (1) | HUE031764T2 (da) |
| LT (1) | LT2912041T (da) |
| ME (1) | ME02576B (da) |
| PL (1) | PL2912041T3 (da) |
| PT (1) | PT2912041T (da) |
| RS (1) | RS55561B1 (da) |
| SI (1) | SI2912041T1 (da) |
| WO (1) | WO2014066132A1 (da) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014134341A1 (en) | 2013-03-01 | 2014-09-04 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of 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 |
| TWI684452B (zh) * | 2014-03-14 | 2020-02-11 | 美國禮來大藥廠 | 胺基噻嗪化合物 |
| MX2017001794A (es) | 2014-08-08 | 2017-06-29 | Amgen Inc | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. |
| 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 |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| JP7149272B2 (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チアジン誘導体および使用方法 |
| MX2019007104A (es) | 2016-12-15 | 2019-11-05 | Amgen Inc | Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso. |
| US11548903B2 (en) | 2016-12-15 | 2023-01-10 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CN106632001A (zh) * | 2016-12-28 | 2017-05-10 | 山东诚汇双达药业有限公司 | 一种4‑（溴乙酰基）吡啶氢溴酸盐的制备方法 |
| CN110452179A (zh) * | 2019-06-25 | 2019-11-15 | 南京普锐达医药科技有限公司 | 一种2-氯-4-甲氧基-5-氰基嘧啶的合成方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006138264A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
| RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
| AR071385A1 (es) * | 2008-04-22 | 2010-06-16 | Schering Corp | Compuestos de 2-imino-3-metil pirrolopirimidinona sustituida con tiofenilo,composiciones farmaceuticas que los contienen,y uso de los mismos para el tratamiento de patologias asociadas con la proteina beta amiloide,tales como alzheimer y otros formas de demencia. |
| ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
| AR073406A1 (es) | 2008-09-30 | 2010-11-03 | Eisai R&D Man Co Ltd | Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer. |
| 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 |
| EP2511269A4 (en) * | 2009-12-11 | 2013-04-24 | Shionogi & Co | FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| 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 |
| JO3143B1 (ar) | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| GB201212871D0 (en) | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
| 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 |
-
2013
- 2013-10-17 PT PT137857306T patent/PT2912041T/pt unknown
- 2013-10-17 WO PCT/US2013/065418 patent/WO2014066132A1/en active Application Filing
- 2013-10-17 ES ES13785730.6T patent/ES2616835T3/es active Active
- 2013-10-17 US US14/427,648 patent/US9328124B2/en not_active Expired - Fee Related
- 2013-10-17 SI SI201330463T patent/SI2912041T1/sl unknown
- 2013-10-17 HU HUE13785730A patent/HUE031764T2/en unknown
- 2013-10-17 LT LTEP13785730.6T patent/LT2912041T/lt unknown
- 2013-10-17 DK DK13785730.6T patent/DK2912041T3/da active
- 2013-10-17 PL PL13785730T patent/PL2912041T3/pl unknown
- 2013-10-17 JP JP2015539666A patent/JP6243921B2/ja not_active Expired - Fee Related
- 2013-10-17 EP EP13785730.6A patent/EP2912041B1/en active Active
- 2013-10-17 RS RS20170016A patent/RS55561B1/sr unknown
- 2013-10-17 CN CN201380055699.5A patent/CN104755484B/zh not_active Expired - Fee Related
- 2013-10-17 CA CA2886507A patent/CA2886507C/en not_active Expired - Fee Related
-
2017
- 2017-01-10 HR HRP20170025TT patent/HRP20170025T1/hr unknown
- 2017-02-10 ME MEP-2017-4A patent/ME02576B/me unknown
- 2017-02-10 CY CY20171100191T patent/CY1118623T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN104755484A (zh) | 2015-07-01 |
| CA2886507A1 (en) | 2014-05-01 |
| CN104755484B (zh) | 2016-02-17 |
| HRP20170025T1 (hr) | 2017-03-10 |
| HUE031764T2 (en) | 2017-07-28 |
| SI2912041T1 (sl) | 2017-02-28 |
| CA2886507C (en) | 2016-09-20 |
| ES2616835T3 (es) | 2017-06-14 |
| LT2912041T (lt) | 2017-03-10 |
| US20150232483A1 (en) | 2015-08-20 |
| WO2014066132A1 (en) | 2014-05-01 |
| PL2912041T3 (pl) | 2017-06-30 |
| EP2912041B1 (en) | 2016-12-14 |
| JP2015535247A (ja) | 2015-12-10 |
| US9328124B2 (en) | 2016-05-03 |
| JP6243921B2 (ja) | 2017-12-06 |
| EP2912041A1 (en) | 2015-09-02 |
| ME02576B (me) | 2017-06-20 |
| CY1118623T1 (el) | 2017-07-12 |
| PT2912041T (pt) | 2017-02-13 |
| RS55561B1 (sr) | 2017-05-31 |
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