EA201491116A1 - Производные 6-дифторметил-5,6-дигидро-2h-[1,4]оксазин-3-амина - Google Patents
Производные 6-дифторметил-5,6-дигидро-2h-[1,4]оксазин-3-аминаInfo
- Publication number
- EA201491116A1 EA201491116A1 EA201491116A EA201491116A EA201491116A1 EA 201491116 A1 EA201491116 A1 EA 201491116A1 EA 201491116 A EA201491116 A EA 201491116A EA 201491116 A EA201491116 A EA 201491116A EA 201491116 A1 EA201491116 A1 EA 201491116A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- dementia
- beta
- compounds
- oxazin
- amine
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Изобретение относится к новым производным 6-дифторметил-5,6-дигидро-2Н-[1,4]оксазин-3-амина в качестве ингибиторов бета-секретазы, также известной как фермент, расщепляющий предшественник амилоида по бета-сайту, ВАСЕ, ВАСЕ1, Asp2 или мемапсин 2. Изобретение также относится к фармацевтическим композициям, содержащим такие соединения, к способам получения таких соединений и композиций и применению таких соединений и композиций для предупреждения и лечения нарушений, в которые вовлечена бета-секретаза, таких как болезнь Альцгеймера (AD), умеренное когнитивное нарушение, угасание, деменция, деменция с тельцами Леви, церебральная амилоидная ангиопатия, слабоумие вследствие множественных инфарктов, синдром Дауна, деменция, ассоциированная с инсультом, деменция, ассоциированная с болезнью Паркинсона, и деменция, ассоциированная с бета-амилоидом.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11191997 | 2011-12-05 | ||
| PCT/EP2012/074351 WO2013083557A1 (en) | 2011-12-05 | 2012-12-04 | 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201491116A1 true EA201491116A1 (ru) | 2014-12-30 |
| EA023909B1 EA023909B1 (ru) | 2016-07-29 |
Family
ID=47278317
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201491116A EA023909B1 (ru) | 2011-12-05 | 2012-12-04 | Производные 6-дифторметил-5,6-дигидро-2h-[1,4]оксазин-3-амина |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20140343048A1 (ru) |
| EP (1) | EP2788346B1 (ru) |
| JP (1) | JP6169095B2 (ru) |
| KR (1) | KR102060379B1 (ru) |
| CN (1) | CN103974951B (ru) |
| AU (1) | AU2012347397B2 (ru) |
| BR (1) | BR112014013310A2 (ru) |
| CA (1) | CA2852366C (ru) |
| EA (1) | EA023909B1 (ru) |
| ES (1) | ES2558604T3 (ru) |
| HK (1) | HK1198586A1 (ru) |
| IL (1) | IL232916A (ru) |
| MX (1) | MX357384B (ru) |
| MY (1) | MY165209A (ru) |
| PH (1) | PH12014501235B1 (ru) |
| SG (1) | SG11201402734XA (ru) |
| UA (1) | UA111749C2 (ru) |
| WO (1) | WO2013083557A1 (ru) |
| ZA (1) | ZA201404074B (ru) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
| DK2580200T3 (en) | 2010-06-09 | 2017-01-09 | Janssen Pharmaceutica Nv | 5,6-dihydro-2H- [1,4] oxazin-3-YLAMINDERIVATER THAT COULD BE USED AS INHIBITORS OF BETA-secretase (BACE) |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| EA023824B1 (ru) | 2011-03-09 | 2016-07-29 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) |
| WO2013083556A1 (en) * | 2011-12-06 | 2013-06-13 | Janssen Pharmaceutica Nv | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| JP6387402B2 (ja) | 2013-06-12 | 2018-09-05 | ヤンセン ファーマシューティカ エヌ．ベー． | β−セクレターゼ（ＢＡＣＥ）の阻害剤としての４−アミノ−６−フェニル−５，６−ジヒドロイミダゾ［１，５−Ａ］ピラジン−３（２Ｈ）−オン誘導体 |
| EP3008066B1 (en) | 2013-06-12 | 2018-08-15 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| EP3008065B1 (en) | 2013-06-12 | 2019-01-30 | Janssen Pharmaceutica NV | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
| MX2017008083A (es) | 2014-12-18 | 2017-10-31 | Janssen Pharmaceutica Nv | Compuestos 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2h-pirrol-5-amina inhibidores de beta-secretasa. |
| WO2021154599A1 (en) * | 2020-01-27 | 2021-08-05 | Silcotek Corp. | Biopharmaceutical manufacturing process and product |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY32799A (es) * | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| US8188079B2 (en) * | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| UA103272C2 (ru) * | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-амино-5,5-дифтор-5,6-дигидро-4h-оксазины как ингибиторы bace1 и/или bace2 |
| DK2580200T3 (en) * | 2010-06-09 | 2017-01-09 | Janssen Pharmaceutica Nv | 5,6-dihydro-2H- [1,4] oxazin-3-YLAMINDERIVATER THAT COULD BE USED AS INHIBITORS OF BETA-secretase (BACE) |
| WO2012095463A1 (en) * | 2011-01-12 | 2012-07-19 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| JP2012147763A (ja) * | 2011-01-17 | 2012-08-09 | Toshitaka Kobayashi | 乾物穿孔具 |
| WO2013083556A1 (en) * | 2011-12-06 | 2013-06-13 | Janssen Pharmaceutica Nv | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
-
2012
- 2012-04-12 UA UAA201403502A patent/UA111749C2/uk unknown
- 2012-12-04 MX MX2014006689A patent/MX357384B/es active IP Right Grant
- 2012-12-04 EA EA201491116A patent/EA023909B1/ru not_active IP Right Cessation
- 2012-12-04 CN CN201280059719.1A patent/CN103974951B/zh not_active Expired - Fee Related
- 2012-12-04 US US14/362,523 patent/US20140343048A1/en not_active Abandoned
- 2012-12-04 MY MYPI2014700925A patent/MY165209A/en unknown
- 2012-12-04 BR BR112014013310A patent/BR112014013310A2/pt not_active Application Discontinuation
- 2012-12-04 SG SG11201402734XA patent/SG11201402734XA/en unknown
- 2012-12-04 JP JP2014543939A patent/JP6169095B2/ja not_active Expired - Fee Related
- 2012-12-04 WO PCT/EP2012/074351 patent/WO2013083557A1/en active Application Filing
- 2012-12-04 AU AU2012347397A patent/AU2012347397B2/en not_active Ceased
- 2012-12-04 KR KR1020147013840A patent/KR102060379B1/ko active IP Right Grant
- 2012-12-04 CA CA2852366A patent/CA2852366C/en not_active Expired - Fee Related
- 2012-12-04 EP EP12794731.5A patent/EP2788346B1/en active Active
- 2012-12-04 ES ES12794731.5T patent/ES2558604T3/es active Active
-
2014
- 2014-06-02 IL IL232916A patent/IL232916A/en active IP Right Grant
- 2014-06-02 PH PH12014501235A patent/PH12014501235B1/en unknown
- 2014-06-04 ZA ZA2014/04074A patent/ZA201404074B/en unknown
- 2014-12-01 HK HK14112072A patent/HK1198586A1/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CN103974951A (zh) | 2014-08-06 |
| PH12014501235A1 (en) | 2014-09-08 |
| CA2852366A1 (en) | 2013-06-13 |
| EA023909B1 (ru) | 2016-07-29 |
| EP2788346A1 (en) | 2014-10-15 |
| MY165209A (en) | 2018-03-05 |
| KR102060379B1 (ko) | 2019-12-30 |
| WO2013083557A1 (en) | 2013-06-13 |
| IL232916A0 (en) | 2014-08-03 |
| UA111749C2 (uk) | 2016-06-10 |
| CA2852366C (en) | 2020-02-18 |
| HK1198586A1 (zh) | 2015-04-30 |
| US20140343048A1 (en) | 2014-11-20 |
| NZ626662A (en) | 2015-05-29 |
| IL232916A (en) | 2016-07-31 |
| PH12014501235B1 (en) | 2014-09-08 |
| AU2012347397A1 (en) | 2014-04-24 |
| EP2788346B1 (en) | 2015-10-28 |
| AU2012347397B2 (en) | 2016-09-22 |
| CN103974951B (zh) | 2016-04-13 |
| BR112014013310A2 (pt) | 2017-06-13 |
| SG11201402734XA (en) | 2014-06-27 |
| KR20140107209A (ko) | 2014-09-04 |
| ZA201404074B (en) | 2016-10-26 |
| MX2014006689A (es) | 2014-09-04 |
| MX357384B (es) | 2018-07-06 |
| JP2015500223A (ja) | 2015-01-05 |
| JP6169095B2 (ja) | 2017-07-26 |
| ES2558604T3 (es) | 2016-02-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |