CN104755484B - Bace抑制剂 - Google Patents
Bace抑制剂 Download PDFInfo
- Publication number
- CN104755484B CN104755484B CN201380055699.5A CN201380055699A CN104755484B CN 104755484 B CN104755484 B CN 104755484B CN 201380055699 A CN201380055699 A CN 201380055699A CN 104755484 B CN104755484 B CN 104755484B
- Authority
- CN
- China
- Prior art keywords
- mmol
- compound
- methanol
- solution
- dichloromethane
- 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.)
- Expired - Fee Related
Links
- 0 CC(*)(N)NC=N Chemical compound CC(*)(N)NC=N 0.000 description 1
- RRSMEKPXGFJQKE-UHFFFAOYSA-N CC(C)(C)OC(N(CC=C)CC(c(nc1)ccc1F)=N)=O Chemical compound CC(C)(C)OC(N(CC=C)CC(c(nc1)ccc1F)=N)=O RRSMEKPXGFJQKE-UHFFFAOYSA-N 0.000 description 1
- OBZDPELYPGXTMH-UHFFFAOYSA-N CC(C)(c1nc(Cl)ncc1F)F Chemical compound CC(C)(c1nc(Cl)ncc1F)F OBZDPELYPGXTMH-UHFFFAOYSA-N 0.000 description 1
- MEFRYHOZPXPLCB-GTNSWQLSSA-N CC(C)c(nc(N1C[C@]2(c3nccnc3)N=C(N)SC[C@@H]2C1)nc1)c1F Chemical compound CC(C)c(nc(N1C[C@]2(c3nccnc3)N=C(N)SC[C@@H]2C1)nc1)c1F MEFRYHOZPXPLCB-GTNSWQLSSA-N 0.000 description 1
- DLGBSWPDPPRBII-QFYYESIMSA-N NC(SC[C@@H]1CN(C2)c3nccc(CF)n3)=N[C@]12c(nc1)ccc1F Chemical compound NC(SC[C@@H]1CN(C2)c3nccc(CF)n3)=N[C@]12c(nc1)ccc1F DLGBSWPDPPRBII-QFYYESIMSA-N 0.000 description 1
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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261718728P | 2012-10-26 | 2012-10-26 | |
| US61/718,728 | 2012-10-26 | ||
| PCT/US2013/065418 WO2014066132A1 (en) | 2012-10-26 | 2013-10-17 | Bace inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104755484A CN104755484A (zh) | 2015-07-01 |
| CN104755484B true CN104755484B (zh) | 2016-02-17 |
Family
ID=49515508
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380055699.5A Expired - Fee Related CN104755484B (zh) | 2012-10-26 | 2013-10-17 | Bace抑制剂 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9328124B2 (https=) |
| EP (1) | EP2912041B1 (https=) |
| JP (1) | JP6243921B2 (https=) |
| CN (1) | CN104755484B (https=) |
| CA (1) | CA2886507C (https=) |
| CY (1) | CY1118623T1 (https=) |
| DK (1) | DK2912041T3 (https=) |
| ES (1) | ES2616835T3 (https=) |
| HR (1) | HRP20170025T1 (https=) |
| HU (1) | HUE031764T2 (https=) |
| LT (1) | LT2912041T (https=) |
| ME (1) | ME02576B (https=) |
| PL (1) | PL2912041T3 (https=) |
| PT (1) | PT2912041T (https=) |
| RS (1) | RS55561B1 (https=) |
| SI (1) | SI2912041T1 (https=) |
| WO (1) | WO2014066132A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | 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 |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| 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 |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| 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 |
| WO2018112084A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| 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 |
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101228163A (zh) * | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
| EP2511269A1 (en) * | 2009-12-11 | 2012-10-17 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| RU2476431C2 (ru) * | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
| US8450331B2 (en) | 2008-04-22 | 2013-05-28 | Merck Sharp & Dohme Corp. | Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| KR20110076965A (ko) | 2008-09-30 | 2011-07-06 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신규한 축합 아미노 디하이드로티아진 유도체 |
| 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 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| 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 PL PL13785730T patent/PL2912041T3/pl unknown
- 2013-10-17 WO PCT/US2013/065418 patent/WO2014066132A1/en not_active Ceased
- 2013-10-17 EP EP13785730.6A patent/EP2912041B1/en active Active
- 2013-10-17 RS RS20170016A patent/RS55561B1/sr unknown
- 2013-10-17 HR HRP20170025TT patent/HRP20170025T1/hr unknown
- 2013-10-17 CA CA2886507A patent/CA2886507C/en not_active Expired - Fee Related
- 2013-10-17 DK DK13785730.6T patent/DK2912041T3/en active
- 2013-10-17 ES ES13785730.6T patent/ES2616835T3/es active Active
- 2013-10-17 SI SI201330463T patent/SI2912041T1/sl unknown
- 2013-10-17 LT LTEP13785730.6T patent/LT2912041T/lt unknown
- 2013-10-17 US US14/427,648 patent/US9328124B2/en not_active Expired - Fee Related
- 2013-10-17 PT PT137857306T patent/PT2912041T/pt unknown
- 2013-10-17 JP JP2015539666A patent/JP6243921B2/ja not_active Expired - Fee Related
- 2013-10-17 CN CN201380055699.5A patent/CN104755484B/zh not_active Expired - Fee Related
- 2013-10-17 HU HUE13785730A patent/HUE031764T2/en unknown
-
2017
- 2017-02-10 CY CY20171100191T patent/CY1118623T1/el unknown
- 2017-02-10 ME MEP-2017-4A patent/ME02576B/me unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101228163A (zh) * | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
| EP2511269A1 (en) * | 2009-12-11 | 2012-10-17 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
Also Published As
| Publication number | Publication date |
|---|---|
| HRP20170025T1 (hr) | 2017-03-10 |
| WO2014066132A1 (en) | 2014-05-01 |
| CA2886507A1 (en) | 2014-05-01 |
| EP2912041B1 (en) | 2016-12-14 |
| HUE031764T2 (en) | 2017-07-28 |
| JP2015535247A (ja) | 2015-12-10 |
| DK2912041T3 (en) | 2017-02-27 |
| ES2616835T3 (es) | 2017-06-14 |
| SI2912041T1 (sl) | 2017-02-28 |
| RS55561B1 (sr) | 2017-05-31 |
| LT2912041T (lt) | 2017-03-10 |
| CN104755484A (zh) | 2015-07-01 |
| PT2912041T (pt) | 2017-02-13 |
| US20150232483A1 (en) | 2015-08-20 |
| EP2912041A1 (en) | 2015-09-02 |
| CA2886507C (en) | 2016-09-20 |
| JP6243921B2 (ja) | 2017-12-06 |
| PL2912041T3 (pl) | 2017-06-30 |
| US9328124B2 (en) | 2016-05-03 |
| ME02576B (me) | 2017-06-20 |
| CY1118623T1 (el) | 2017-07-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160217 Termination date: 20191017 |