JP5993875B2 - 縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物 - Google Patents
縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物 Download PDFInfo
- Publication number
- JP5993875B2 JP5993875B2 JP2013550622A JP2013550622A JP5993875B2 JP 5993875 B2 JP5993875 B2 JP 5993875B2 JP 2013550622 A JP2013550622 A JP 2013550622A JP 2013550622 A JP2013550622 A JP 2013550622A JP 5993875 B2 JP5993875 B2 JP 5993875B2
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- Expired - Fee Related
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- 0 *CC(C=C)OCC(N1CCOCC1)=O Chemical compound *CC(C=C)OCC(N1CCOCC1)=O 0.000 description 9
- JYDMYZPSZVZHIG-UHFFFAOYSA-N CC(C=C)OC(C(c(cccc1)c1[F]C)=O)C(OC(C)(C)C)=O Chemical compound CC(C=C)OC(C(c(cccc1)c1[F]C)=O)C(OC(C)(C)C)=O JYDMYZPSZVZHIG-UHFFFAOYSA-N 0.000 description 1
- XHNXAPUTQFTIOC-HNJNHCNJSA-N NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)NC(c2cnc(CF)cn2)=O)c1F Chemical compound NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)NC(c2cnc(CF)cn2)=O)c1F XHNXAPUTQFTIOC-HNJNHCNJSA-N 0.000 description 1
- IZRBDNDYENBBIF-UBHAPETDSA-N NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)[N+]([O-])=O)c1F Chemical compound NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)[N+]([O-])=O)c1F IZRBDNDYENBBIF-UBHAPETDSA-N 0.000 description 1
- PLJQOSOPRCJZKY-UBHAPETDSA-N NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cccc1)c1F Chemical compound NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cccc1)c1F PLJQOSOPRCJZKY-UBHAPETDSA-N 0.000 description 1
- FICBLPSPSCLFQS-ZDSQKVDBSA-N NC(SC[C@@H]1[C@@H](CF)OC2)=N[C@]12c(cccc1F)c1F Chemical compound NC(SC[C@@H]1[C@@H](CF)OC2)=N[C@]12c(cccc1F)c1F FICBLPSPSCLFQS-ZDSQKVDBSA-N 0.000 description 1
- YMQRPXBBBOXHNZ-UHFFFAOYSA-N O=C(CCl)N1CCOCC1 Chemical compound O=C(CCl)N1CCOCC1 YMQRPXBBBOXHNZ-UHFFFAOYSA-N 0.000 description 1
- BKUJEHHWQQBLTE-UHFFFAOYSA-N OC(c1cnc(CF)cn1)=O Chemical compound OC(c1cnc(CF)cn1)=O BKUJEHHWQQBLTE-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- 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
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/22—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Furan Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434849P | 2011-01-21 | 2011-01-21 | |
| US61/434,849 | 2011-01-21 | ||
| PCT/US2012/022053 WO2012100179A1 (en) | 2011-01-21 | 2012-01-20 | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016041508A Division JP6087005B2 (ja) | 2011-01-21 | 2016-03-03 | 縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503001A JP2014503001A (ja) | 2014-02-06 |
| JP2014503001A5 JP2014503001A5 (enExample) | 2016-01-28 |
| JP5993875B2 true JP5993875B2 (ja) | 2016-09-14 |
Family
ID=45563570
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013550622A Expired - Fee Related JP5993875B2 (ja) | 2011-01-21 | 2012-01-20 | 縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物 |
| JP2016041508A Expired - Fee Related JP6087005B2 (ja) | 2011-01-21 | 2016-03-03 | 縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016041508A Expired - Fee Related JP6087005B2 (ja) | 2011-01-21 | 2016-03-03 | 縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US8426584B2 (enExample) |
| EP (1) | EP2665716B1 (enExample) |
| JP (2) | JP5993875B2 (enExample) |
| CN (2) | CN103502231A (enExample) |
| BR (1) | BR112013016241A2 (enExample) |
| CA (1) | CA2814014A1 (enExample) |
| ES (1) | ES2624288T3 (enExample) |
| IL (1) | IL226405A0 (enExample) |
| MX (1) | MX2013005115A (enExample) |
| RU (1) | RU2013138226A (enExample) |
| SG (2) | SG191710A1 (enExample) |
| WO (1) | WO2012100179A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0906962B8 (pt) | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| GB201212816D0 (en) * | 2012-07-19 | 2012-09-05 | Eisai Ltd | Novel compounds |
| TWI639607B (zh) | 2013-06-18 | 2018-11-01 | 美國禮來大藥廠 | Bace抑制劑 |
| CA2963761C (en) * | 2014-10-10 | 2023-10-17 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition of fused aminodihydrothiazine derivative |
| KR102630042B1 (ko) | 2016-10-27 | 2024-01-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 알츠하이머병의 치료를 위한 항-a베타 원시섬유 항체 및 베타-세크레타제 bace1 억제제를 포함하는 조성물 |
| WO2020023530A2 (en) | 2018-07-24 | 2020-01-30 | Eisai R&D Management Co., Ltd. | Methods of treatment and prevention of alzheimer's disease |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3235551A (en) | 1966-02-15 | Novel derivatives of | ||
| US3227713A (en) | 1966-01-04 | Azine derivatives | ||
| JPH0967355A (ja) | 1995-08-31 | 1997-03-11 | Tokyo Tanabe Co Ltd | チアジン誘導体、チアゾール誘導体及びそれらの製造方法 |
| AU2001258771A1 (en) | 2000-05-19 | 2001-11-26 | Takeda Chemical Industries Ltd. | -secretase inhibitors |
| US6562783B2 (en) | 2001-05-30 | 2003-05-13 | Neurologic, Inc. | Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors |
| AU2003254844A1 (en) | 2002-08-09 | 2004-02-25 | Takeda Chemical Industries, Ltd. | Substituted amino compounds and use thereof |
| AU2003285012A1 (en) | 2002-10-24 | 2004-05-13 | Sepracor, Inc. | Compositions comprising zopiclone derivatives and methods of making and using the same |
| JP2004149429A (ja) | 2002-10-29 | 2004-05-27 | Takeda Chem Ind Ltd | インドール化合物およびその用途 |
| DE60329316D1 (de) | 2002-11-12 | 2009-10-29 | Merck & Co Inc | Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer |
| CA2548388A1 (en) | 2003-12-15 | 2005-06-30 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP2007530696A (ja) | 2004-03-30 | 2007-11-01 | メルク エンド カムパニー インコーポレーテッド | アスパラギン酸プロテアーゼ阻害剤として有用な2−アミノチアゾール化合物 |
| PE20060664A1 (es) | 2004-09-15 | 2006-08-04 | Novartis Ag | Amidas biciclicas como inhibidores de cinasa |
| CN101084198A (zh) | 2004-10-15 | 2007-12-05 | 阿斯利康(瑞典)有限公司 | 取代的氨基-嘧啶酮及其用途 |
| US20090221579A1 (en) | 2004-10-15 | 2009-09-03 | Jeffrey Scott Albert | Substituted Amino-Compounds and Uses Thereof |
| WO2006078577A1 (en) | 2005-01-19 | 2006-07-27 | Merck & Co., Inc. | Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of alzheimer's disease |
| WO2006138264A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| CA2615656A1 (en) | 2005-07-18 | 2007-01-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| JP2009532464A (ja) | 2006-04-05 | 2009-09-10 | アストラゼネカ・アクチエボラーグ | 2−アミノピリミジン−4−オン及びAβ−関連の病理を治療又は予防するためのその使用 |
| JP5117382B2 (ja) | 2006-05-31 | 2013-01-16 | 第一三共株式会社 | 7員環化合物の製造方法 |
| MX2009006228A (es) | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
| EP2151435A4 (en) * | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| EP2151436B1 (en) | 2007-05-29 | 2013-04-24 | Santen Pharmaceutical Co., Ltd | Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein and has glucocorticoid receptor-binding activity |
| PE20091236A1 (es) | 2007-11-22 | 2009-09-16 | Astrazeneca Ab | Derivados de pirimidina como immunomoduladores de tlr7 |
| BRPI0906962B8 (pt) | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| WO2010013302A1 (ja) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| AU2009277485B2 (en) | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| KR20110076965A (ko) | 2008-09-30 | 2011-07-06 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신규한 축합 아미노 디하이드로티아진 유도체 |
| AR077277A1 (es) * | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| GB0912778D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| MX2012015135A (es) | 2010-07-01 | 2013-05-06 | Amgen Inc | Compuestos heterociclicos y su uso como inhibidores de la actividad pi3k. |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
-
2012
- 2012-01-20 EP EP12702690.4A patent/EP2665716B1/en active Active
- 2012-01-20 CA CA2814014A patent/CA2814014A1/en not_active Abandoned
- 2012-01-20 US US13/355,030 patent/US8426584B2/en not_active Expired - Fee Related
- 2012-01-20 BR BR112013016241A patent/BR112013016241A2/pt not_active IP Right Cessation
- 2012-01-20 SG SG2013027461A patent/SG191710A1/en unknown
- 2012-01-20 RU RU2013138226/04A patent/RU2013138226A/ru not_active Application Discontinuation
- 2012-01-20 SG SG10201601516QA patent/SG10201601516QA/en unknown
- 2012-01-20 MX MX2013005115A patent/MX2013005115A/es active IP Right Grant
- 2012-01-20 JP JP2013550622A patent/JP5993875B2/ja not_active Expired - Fee Related
- 2012-01-20 CN CN201280004193.7A patent/CN103502231A/zh active Pending
- 2012-01-20 CN CN201610875412.9A patent/CN106632401B/zh not_active Expired - Fee Related
- 2012-01-20 WO PCT/US2012/022053 patent/WO2012100179A1/en not_active Ceased
- 2012-01-20 ES ES12702690.4T patent/ES2624288T3/es active Active
-
2013
- 2013-03-12 US US13/795,308 patent/US8802871B2/en active Active
- 2013-05-16 IL IL226405A patent/IL226405A0/en unknown
-
2014
- 2014-06-26 US US14/316,321 patent/US8962858B2/en not_active Expired - Fee Related
-
2016
- 2016-03-03 JP JP2016041508A patent/JP6087005B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| MX2013005115A (es) | 2013-06-03 |
| US8802871B2 (en) | 2014-08-12 |
| JP2016121177A (ja) | 2016-07-07 |
| BR112013016241A2 (pt) | 2016-07-12 |
| RU2013138226A (ru) | 2015-02-27 |
| EP2665716B1 (en) | 2017-03-08 |
| CN106632401A (zh) | 2017-05-10 |
| WO2012100179A1 (en) | 2012-07-26 |
| US8426584B2 (en) | 2013-04-23 |
| JP6087005B2 (ja) | 2017-03-01 |
| CA2814014A1 (en) | 2012-07-26 |
| JP2014503001A (ja) | 2014-02-06 |
| ES2624288T3 (es) | 2017-07-13 |
| US20130197244A1 (en) | 2013-08-01 |
| IL226405A0 (en) | 2013-07-31 |
| CN106632401B (zh) | 2020-12-29 |
| US20120190848A1 (en) | 2012-07-26 |
| US20140309429A1 (en) | 2014-10-16 |
| SG191710A1 (en) | 2013-08-30 |
| US8962858B2 (en) | 2015-02-24 |
| EP2665716A1 (en) | 2013-11-27 |
| CN103502231A (zh) | 2014-01-08 |
| SG10201601516QA (en) | 2016-03-30 |
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