CN103974951B - 6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 - Google Patents
6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 Download PDFInfo
- Publication number
- CN103974951B CN103974951B CN201280059719.1A CN201280059719A CN103974951B CN 103974951 B CN103974951 B CN 103974951B CN 201280059719 A CN201280059719 A CN 201280059719A CN 103974951 B CN103974951 B CN 103974951B
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- Prior art keywords
- dementia
- compound
- acid
- compounds
- mmol
- 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
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- 0 CC*C(*CC)([C@@](C=CC)(c1cc(C=C)ccc1*CC)P)OCC(C)=C Chemical compound CC*C(*CC)([C@@](C=CC)(c1cc(C=C)ccc1*CC)P)OCC(C)=C 0.000 description 4
- HAWDTKBFCJAHLH-UHFFFAOYSA-N CC(c1cc(Br)ccc1F)(C(OC1)=C(F)F)NC1=S Chemical compound CC(c1cc(Br)ccc1F)(C(OC1)=C(F)F)NC1=S HAWDTKBFCJAHLH-UHFFFAOYSA-N 0.000 description 1
- VCPJSDSVWYLHEU-UHFFFAOYSA-N COC(C(c(cc(cc1)Br)c1F)=O)=O Chemical compound COC(C(c(cc(cc1)Br)c1F)=O)=O VCPJSDSVWYLHEU-UHFFFAOYSA-N 0.000 description 1
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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- 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)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (2)
| Publication Number | Publication Date |
|---|---|
| CN103974951A CN103974951A (zh) | 2014-08-06 |
| CN103974951B true CN103974951B (zh) | 2016-04-13 |
Family
ID=47278317
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280059719.1A Expired - Fee Related CN103974951B (zh) | 2011-12-05 | 2012-12-04 | 6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 |
Country Status (18)
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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011009943A1 (en) * | 2009-07-24 | 2011-01-27 | Novartis Ag | Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
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
-
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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011009943A1 (en) * | 2009-07-24 | 2011-01-27 | Novartis Ag | Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders |
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 |
| JP6169095B2 (ja) | 2017-07-26 |
| 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 |
| 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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| CN103415521B (zh) | 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 | |
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| CN103974940B (zh) | 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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| HK1198535B (en) | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4] oxazin-3-amine derivatives | |
| HK1189223B (en) | 3-4-dihydro-pyrrolo[1,2-a] pyrazin-1-ylamine derivatives useful as inhibitors of betasecretase(bace) | |
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| NZ626662B2 (en) | 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
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| PB01 | Publication | ||
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| REG | Reference to a national code |
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| 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: 20160413 Termination date: 20201204 |