ES2582473T3 - Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa - Google Patents
Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa Download PDFInfo
- Publication number
- ES2582473T3 ES2582473T3 ES12794730.7T ES12794730T ES2582473T3 ES 2582473 T3 ES2582473 T3 ES 2582473T3 ES 12794730 T ES12794730 T ES 12794730T ES 2582473 T3 ES2582473 T3 ES 2582473T3
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- Prior art keywords
- fluoro
- compound
- alkyl
- phenyl
- mmol
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- LJGHYPLBDBRCRZ-UHFFFAOYSA-N 3-(3-aminophenyl)sulfonylaniline Chemical group NC1=CC=CC(S(=O)(=O)C=2C=C(N)C=CC=2)=C1 LJGHYPLBDBRCRZ-UHFFFAOYSA-N 0.000 title description 3
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 7
- 125000004076 pyridyl group Chemical group 0.000 claims abstract description 7
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- PCZXVLXHPWLNDS-UKRRQHHQSA-N (5r,6r)-5-[2-fluoro-5-(pyrimidin-2-ylamino)phenyl]-5-methyl-6-(trifluoromethyl)-2,6-dihydro-1,4-oxazin-3-amine Chemical compound C=1C(NC=2N=CC=CN=2)=CC=C(F)C=1[C@@]1(C)N=C(N)CO[C@H]1C(F)(F)F PCZXVLXHPWLNDS-UKRRQHHQSA-N 0.000 claims description 2
- VJQVDJKEAGOIJY-HZPDHXFCSA-N (5r,6r)-5-[2-fluoro-5-[(3-methoxypyrazin-2-yl)amino]phenyl]-5-methyl-6-(trifluoromethyl)-2,6-dihydro-1,4-oxazin-3-amine Chemical compound COC1=NC=CN=C1NC1=CC=C(F)C([C@]2(C)[C@@H](OCC(N)=N2)C(F)(F)F)=C1 VJQVDJKEAGOIJY-HZPDHXFCSA-N 0.000 claims description 2
- XIRMZGFOPCKMTN-IAGOWNOFSA-N (5r,6r)-5-[2-fluoro-5-[(3-methoxypyridin-2-yl)amino]phenyl]-5-methyl-6-(trifluoromethyl)-2,6-dihydro-1,4-oxazin-3-amine Chemical compound COC1=CC=CN=C1NC1=CC=C(F)C([C@]2(C)[C@@H](OCC(N)=N2)C(F)(F)F)=C1 XIRMZGFOPCKMTN-IAGOWNOFSA-N 0.000 claims description 2
- AZTLHEQHXVOHHJ-DZGCQCFKSA-N (5r,6r)-6-fluoro-5-[2-fluoro-5-(pyrimidin-2-ylamino)phenyl]-5-methyl-2,6-dihydro-1,4-oxazin-3-amine Chemical compound C=1C(NC=2N=CC=CN=2)=CC=C(F)C=1[C@@]1(C)N=C(N)CO[C@@H]1F AZTLHEQHXVOHHJ-DZGCQCFKSA-N 0.000 claims description 2
- QZDGAPNXFGXMQG-JKSUJKDBSA-N (5r,6r)-6-fluoro-5-[2-fluoro-5-[(3-methoxypyrazin-2-yl)amino]phenyl]-5-methyl-2,6-dihydro-1,4-oxazin-3-amine Chemical compound COC1=NC=CN=C1NC1=CC=C(F)C([C@]2(C)[C@H](OCC(N)=N2)F)=C1 QZDGAPNXFGXMQG-JKSUJKDBSA-N 0.000 claims description 2
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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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11192171 | 2011-12-06 | ||
| EP11192171 | 2011-12-06 | ||
| PCT/EP2012/074349 WO2013083556A1 (en) | 2011-12-06 | 2012-12-04 | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
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| 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) |
| UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| 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 |
| US20190359609A1 (en) * | 2016-12-16 | 2019-11-28 | Janssen Pharmaceutica Nv | Bicyclic oga inhibitor compounds |
| WO2019025250A1 (en) | 2017-08-04 | 2019-02-07 | Basf Se | SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI |
| CN108440320A (zh) * | 2018-05-09 | 2018-08-24 | 上海凌凯医药科技有限公司 | 一种高手性选择性合成α-双取代α-氨基酸的方法 |
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| ES2476605T3 (es) * | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
| 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 |
| 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 |
| US20120238557A1 (en) * | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
| 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) |
| US9242943B2 (en) * | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| IN2014DN03206A (enExample) * | 2011-10-13 | 2015-05-22 | Novartis Ag | |
| UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
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Also Published As
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| KR20140106541A (ko) | 2014-09-03 |
| EA024716B1 (ru) | 2016-10-31 |
| NZ623858A (en) | 2015-05-29 |
| HK1198535A1 (en) | 2015-05-15 |
| CA2853891C (en) | 2020-03-10 |
| CA2853891A1 (en) | 2013-06-13 |
| EP2788335A1 (en) | 2014-10-15 |
| MX2014006752A (es) | 2014-07-14 |
| IL232917A (en) | 2016-07-31 |
| MX357383B (es) | 2018-07-06 |
| IL232917A0 (en) | 2014-08-03 |
| US20140364428A1 (en) | 2014-12-11 |
| CN103974940B (zh) | 2016-08-24 |
| AU2012347396A1 (en) | 2014-05-08 |
| CN103974940A (zh) | 2014-08-06 |
| AU2012347396B2 (en) | 2017-02-16 |
| KR102002345B1 (ko) | 2019-07-22 |
| JP5989130B2 (ja) | 2016-09-07 |
| WO2013083556A1 (en) | 2013-06-13 |
| EP2788335B1 (en) | 2016-04-13 |
| EA201491102A1 (ru) | 2014-09-30 |
| JP2015500257A (ja) | 2015-01-05 |
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