JP6169095B2 - ６−ジフルオロメチル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体 - Google Patents
６−ジフルオロメチル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体 Download PDFInfo
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- JP6169095B2 JP6169095B2 JP2014543939A JP2014543939A JP6169095B2 JP 6169095 B2 JP6169095 B2 JP 6169095B2 JP 2014543939 A JP2014543939 A JP 2014543939A JP 2014543939 A JP2014543939 A JP 2014543939A JP 6169095 B2 JP6169095 B2 JP 6169095B2
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- UNMQQOQNRVQEOT-UHFFFAOYSA-N 2-(difluoromethyl)-3,6-dihydro-2h-1,4-oxazin-5-amine Chemical class NC1=NCC(C(F)F)OC1 UNMQQOQNRVQEOT-UHFFFAOYSA-N 0.000 title 1
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- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 9
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
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- FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 description 6
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- BMTZEAOGFDXDAD-UHFFFAOYSA-M 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholin-4-ium;chloride Chemical compound [Cl-].COC1=NC(OC)=NC([N+]2(C)CCOCC2)=N1 BMTZEAOGFDXDAD-UHFFFAOYSA-M 0.000 description 4
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Classifications
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- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
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| EP11191997 | 2011-12-05 | ||
| EP11191997.3 | 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 (3)
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| JP2015500223A JP2015500223A (ja) | 2015-01-05 |
| JP2015500223A5 JP2015500223A5 (enExample) | 2015-12-17 |
| JP6169095B2 true JP6169095B2 (ja) | 2017-07-26 |
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| JP2014543939A Expired - Fee Related JP6169095B2 (ja) | 2011-12-05 | 2012-12-04 | ６−ジフルオロメチル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体 |
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| EP (1) | EP2788346B1 (enExample) |
| JP (1) | JP6169095B2 (enExample) |
| KR (1) | KR102060379B1 (enExample) |
| CN (1) | CN103974951B (enExample) |
| AU (1) | AU2012347397B2 (enExample) |
| BR (1) | BR112014013310A2 (enExample) |
| CA (1) | CA2852366C (enExample) |
| EA (1) | EA023909B1 (enExample) |
| ES (1) | ES2558604T3 (enExample) |
| IL (1) | IL232916A (enExample) |
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| UA (1) | UA111749C2 (enExample) |
| WO (1) | WO2013083557A1 (enExample) |
| ZA (1) | ZA201404074B (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| AR081587A1 (es) | 2010-06-09 | 2012-10-03 | Janssen Pharmaceutica Nv | DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE) |
| ES2648143T3 (es) | 2010-12-22 | 2017-12-28 | Janssen Pharmaceutica Nv | Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE) |
| JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体 |
| CN103974940B (zh) * | 2011-12-06 | 2016-08-24 | 詹森药业有限公司 | 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| EP3008067B1 (en) | 2013-06-12 | 2017-03-29 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| KR102243134B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체 |
| BR112015030597A2 (pt) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace) |
| JP2017538753A (ja) | 2014-12-18 | 2017-12-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ２，３，４，５−テトラヒドロピリジン−６−アミンおよび３，４−ジヒドロ−２Ｈ−ピロール−５−アミンの化合物のβセクレターゼ阻害剤 |
| 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 (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 |
| AR081587A1 (es) | 2010-06-09 | 2012-10-03 | Janssen Pharmaceutica Nv | DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE) |
| CN103429589A (zh) * | 2011-01-12 | 2013-12-04 | 诺瓦提斯公司 | 噁嗪衍生物及其在治疗神经障碍中的用途 |
| WO2012147763A1 (ja) * | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| CN103974940B (zh) * | 2011-12-06 | 2016-08-24 | 詹森药业有限公司 | 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 |
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2012
- 2012-04-12 UA UAA201403502A patent/UA111749C2/uk unknown
- 2012-12-04 SG SG11201402734XA patent/SG11201402734XA/en unknown
- 2012-12-04 KR KR1020147013840A patent/KR102060379B1/ko not_active Expired - Fee Related
- 2012-12-04 ES ES12794731.5T patent/ES2558604T3/es active Active
- 2012-12-04 EP EP12794731.5A patent/EP2788346B1/en active Active
- 2012-12-04 EA EA201491116A patent/EA023909B1/ru not_active IP Right Cessation
- 2012-12-04 AU AU2012347397A patent/AU2012347397B2/en not_active Ceased
- 2012-12-04 WO PCT/EP2012/074351 patent/WO2013083557A1/en not_active Ceased
- 2012-12-04 MX MX2014006689A patent/MX357384B/es active IP Right Grant
- 2012-12-04 CA CA2852366A patent/CA2852366C/en not_active Expired - Fee Related
- 2012-12-04 JP JP2014543939A patent/JP6169095B2/ja 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 CN CN201280059719.1A patent/CN103974951B/zh not_active Expired - Fee Related
- 2012-12-04 BR BR112014013310A patent/BR112014013310A2/pt not_active Application Discontinuation
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2014
- 2014-06-02 PH PH12014501235A patent/PH12014501235A1/en unknown
- 2014-06-02 IL IL232916A patent/IL232916A/en active IP Right Grant
- 2014-06-04 ZA ZA2014/04074A patent/ZA201404074B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PH12014501235B1 (en) | 2014-09-08 |
| ZA201404074B (en) | 2016-10-26 |
| SG11201402734XA (en) | 2014-06-27 |
| US20140343048A1 (en) | 2014-11-20 |
| CA2852366C (en) | 2020-02-18 |
| CA2852366A1 (en) | 2013-06-13 |
| BR112014013310A2 (pt) | 2017-06-13 |
| IL232916A0 (en) | 2014-08-03 |
| UA111749C2 (uk) | 2016-06-10 |
| EP2788346A1 (en) | 2014-10-15 |
| ES2558604T3 (es) | 2016-02-05 |
| AU2012347397B2 (en) | 2016-09-22 |
| MX2014006689A (es) | 2014-09-04 |
| EA201491116A1 (ru) | 2014-12-30 |
| KR102060379B1 (ko) | 2019-12-30 |
| JP2015500223A (ja) | 2015-01-05 |
| EP2788346B1 (en) | 2015-10-28 |
| PH12014501235A1 (en) | 2014-09-08 |
| MX357384B (es) | 2018-07-06 |
| CN103974951B (zh) | 2016-04-13 |
| HK1198586A1 (zh) | 2015-04-30 |
| MY165209A (en) | 2018-03-05 |
| AU2012347397A1 (en) | 2014-04-24 |
| IL232916A (en) | 2016-07-31 |
| NZ626662A (en) | 2015-05-29 |
| WO2013083557A1 (en) | 2013-06-13 |
| EA023909B1 (ru) | 2016-07-29 |
| CN103974951A (zh) | 2014-08-06 |
| KR20140107209A (ko) | 2014-09-04 |
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