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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
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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 |
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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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| CA (1) | CA2852366C (enExample) |
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| UA (1) | UA111749C2 (enExample) |
| WO (1) | WO2013083557A1 (enExample) |
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Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| PH12012502377A1 (en) | 2010-06-09 | 2014-10-14 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| NZ610948A (en) | 2010-12-22 | 2014-06-27 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| BR112013022917A2 (pt) | 2011-03-09 | 2016-12-06 | Janssen Pharmaceutica Nv | derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de beta-secretase (bace) |
| JP5989130B2 (ja) * | 2011-12-06 | 2016-09-07 | ヤンセン ファーマシューティカ エヌ．ベー． | ５−（３−アミノフェニル）−５−アルキル−５，６−ジヒドロ−２ｈ−［１，４］オキサジン−３−アミン誘導体 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| JP6325092B2 (ja) | 2013-06-12 | 2018-05-16 | ヤンセン ファーマシューティカ エヌ．ベー． | βーセクレターゼ（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］ピラジン誘導体 |
| KR102243133B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체 |
| KR102243135B1 (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-3(2h)-온 유도체 |
| EP3233834B1 (en) | 2014-12-18 | 2019-11-13 | Janssen Pharmaceutica NV | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase |
| 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 |
| PH12012502377A1 (en) * | 2010-06-09 | 2014-10-14 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| MX2013008111A (es) * | 2011-01-12 | 2013-10-30 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos. |
| CN103608345A (zh) * | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| JP5989130B2 (ja) * | 2011-12-06 | 2016-09-07 | ヤンセン ファーマシューティカ エヌ．ベー． | ５−（３−アミノフェニル）−５−アルキル−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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2012
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- 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 KR KR1020147013840A patent/KR102060379B1/ko not_active Expired - Fee Related
- 2012-12-04 JP JP2014543939A patent/JP6169095B2/ja not_active Expired - Fee Related
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- 2012-12-04 EA EA201491116A patent/EA023909B1/ru not_active IP Right Cessation
- 2012-12-04 MY MYPI2014700925A patent/MY165209A/en unknown
- 2012-12-04 WO PCT/EP2012/074351 patent/WO2013083557A1/en not_active Ceased
- 2012-12-04 EP EP12794731.5A patent/EP2788346B1/en active Active
- 2012-12-04 AU AU2012347397A patent/AU2012347397B2/en not_active Ceased
- 2012-12-04 SG SG11201402734XA patent/SG11201402734XA/en unknown
- 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 BR BR112014013310A patent/BR112014013310A2/pt not_active Application Discontinuation
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2014
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- 2014-06-02 IL IL232916A patent/IL232916A/en active IP Right Grant
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Also Published As
| Publication number | Publication date |
|---|---|
| UA111749C2 (uk) | 2016-06-10 |
| US20140343048A1 (en) | 2014-11-20 |
| IL232916A (en) | 2016-07-31 |
| WO2013083557A1 (en) | 2013-06-13 |
| MY165209A (en) | 2018-03-05 |
| ES2558604T3 (es) | 2016-02-05 |
| EA201491116A1 (ru) | 2014-12-30 |
| KR102060379B1 (ko) | 2019-12-30 |
| IL232916A0 (en) | 2014-08-03 |
| SG11201402734XA (en) | 2014-06-27 |
| JP2015500223A (ja) | 2015-01-05 |
| KR20140107209A (ko) | 2014-09-04 |
| HK1198586A1 (zh) | 2015-04-30 |
| CN103974951B (zh) | 2016-04-13 |
| MX357384B (es) | 2018-07-06 |
| NZ626662A (en) | 2015-05-29 |
| PH12014501235B1 (en) | 2014-09-08 |
| AU2012347397B2 (en) | 2016-09-22 |
| CA2852366A1 (en) | 2013-06-13 |
| ZA201404074B (en) | 2016-10-26 |
| BR112014013310A2 (pt) | 2017-06-13 |
| EP2788346A1 (en) | 2014-10-15 |
| AU2012347397A1 (en) | 2014-04-24 |
| EP2788346B1 (en) | 2015-10-28 |
| CN103974951A (zh) | 2014-08-06 |
| CA2852366C (en) | 2020-02-18 |
| PH12014501235A1 (en) | 2014-09-08 |
| EA023909B1 (ru) | 2016-07-29 |
| MX2014006689A (es) | 2014-09-04 |
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