ME02576B - Derivati tetrahidropirolotiazina kao inhibitori bace - Google Patents
Derivati tetrahidropirolotiazina kao inhibitori baceInfo
- Publication number
- ME02576B ME02576B MEP-2017-4A MEP20174A ME02576B ME 02576 B ME02576 B ME 02576B ME P20174 A MEP20174 A ME P20174A ME 02576 B ME02576 B ME 02576B
- Authority
- ME
- Montenegro
- Prior art keywords
- compound
- salt
- pharmaceutically acceptable
- acceptable salt
- group
- Prior art date
Links
- 102100021257 Beta-secretase 1 Human genes 0.000 title 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- IKIJFJKFIYFTBZ-BTDLBPIBSA-N 2-[2-[(4ar,7ar)-2-amino-7a-pyrazin-2-yl-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-6-yl]-5-fluoropyrimidin-4-yl]propan-2-ol Chemical compound C1=C(F)C(C(C)(O)C)=NC(N2C[C@@]3(N=C(N)SC[C@@H]3C2)C=2N=CC=NC=2)=N1 IKIJFJKFIYFTBZ-BTDLBPIBSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 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 | |
| PCT/US2013/065418 WO2014066132A1 (en) | 2012-10-26 | 2013-10-17 | Bace inhibitors |
| EP13785730.6A EP2912041B1 (en) | 2012-10-26 | 2013-10-17 | Tetrahydropyrrolothiazine derivatives as bace inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02576B true ME02576B (me) | 2017-06-20 |
Family
ID=49515508
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2017-4A ME02576B (me) | 2012-10-26 | 2017-02-10 | Derivati tetrahidropirolotiazina kao inhibitori bace |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9328124B2 (enExample) |
| EP (1) | EP2912041B1 (enExample) |
| JP (1) | JP6243921B2 (enExample) |
| CN (1) | CN104755484B (enExample) |
| CA (1) | CA2886507C (enExample) |
| CY (1) | CY1118623T1 (enExample) |
| DK (1) | DK2912041T3 (enExample) |
| ES (1) | ES2616835T3 (enExample) |
| HR (1) | HRP20170025T1 (enExample) |
| HU (1) | HUE031764T2 (enExample) |
| LT (1) | LT2912041T (enExample) |
| ME (1) | ME02576B (enExample) |
| PL (1) | PL2912041T3 (enExample) |
| PT (1) | PT2912041T (enExample) |
| RS (1) | RS55561B1 (enExample) |
| SI (1) | SI2912041T1 (enExample) |
| WO (1) | WO2014066132A1 (enExample) |
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 |
| 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 |
| JP6576433B2 (ja) | 2014-08-08 | 2019-09-18 | 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−２−アミン化合物及び使用方法 |
| 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 |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| CA3047287A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| JP7148518B2 (ja) | 2016-12-15 | 2022-10-05 | 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 |
| 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. |
| WO2018112083A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Thiazine 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 |
|---|---|---|---|---|
| SG162790A1 (en) | 2005-06-14 | 2010-07-29 | Schering Corp | 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 |
| ES2548774T3 (es) | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Derivado de aminodihidrotiazina condensado |
| US8541427B2 (en) | 2008-04-22 | 2013-09-24 | Merck, Sharp & Dohme, Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| 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 |
| JPWO2011071109A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
| 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 LT LTEP13785730.6T patent/LT2912041T/lt unknown
- 2013-10-17 DK DK13785730.6T patent/DK2912041T3/en active
- 2013-10-17 EP EP13785730.6A patent/EP2912041B1/en active Active
- 2013-10-17 CA CA2886507A patent/CA2886507C/en not_active Expired - Fee Related
- 2013-10-17 HR HRP20170025TT patent/HRP20170025T1/hr unknown
- 2013-10-17 RS RS20170016A patent/RS55561B1/sr unknown
- 2013-10-17 WO PCT/US2013/065418 patent/WO2014066132A1/en not_active Ceased
- 2013-10-17 HU HUE13785730A patent/HUE031764T2/en unknown
- 2013-10-17 US US14/427,648 patent/US9328124B2/en not_active Expired - Fee Related
- 2013-10-17 PL PL13785730T patent/PL2912041T3/pl unknown
- 2013-10-17 SI SI201330463T patent/SI2912041T1/sl unknown
- 2013-10-17 ES ES13785730.6T patent/ES2616835T3/es active Active
- 2013-10-17 CN CN201380055699.5A patent/CN104755484B/zh not_active Expired - Fee Related
- 2013-10-17 JP JP2015539666A patent/JP6243921B2/ja not_active Expired - Fee Related
- 2013-10-17 PT PT137857306T patent/PT2912041T/pt unknown
-
2017
- 2017-02-10 CY CY20171100191T patent/CY1118623T1/el unknown
- 2017-02-10 ME MEP-2017-4A patent/ME02576B/me unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RS55561B1 (sr) | 2017-05-31 |
| EP2912041A1 (en) | 2015-09-02 |
| SI2912041T1 (sl) | 2017-02-28 |
| CA2886507A1 (en) | 2014-05-01 |
| PL2912041T3 (pl) | 2017-06-30 |
| CN104755484A (zh) | 2015-07-01 |
| LT2912041T (lt) | 2017-03-10 |
| CY1118623T1 (el) | 2017-07-12 |
| US9328124B2 (en) | 2016-05-03 |
| ES2616835T3 (es) | 2017-06-14 |
| DK2912041T3 (en) | 2017-02-27 |
| JP6243921B2 (ja) | 2017-12-06 |
| WO2014066132A1 (en) | 2014-05-01 |
| PT2912041T (pt) | 2017-02-13 |
| CN104755484B (zh) | 2016-02-17 |
| JP2015535247A (ja) | 2015-12-10 |
| HRP20170025T1 (hr) | 2017-03-10 |
| US20150232483A1 (en) | 2015-08-20 |
| EP2912041B1 (en) | 2016-12-14 |
| CA2886507C (en) | 2016-09-20 |
| HUE031764T2 (en) | 2017-07-28 |
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