CN106632401B - 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 - Google Patents
用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 Download PDFInfo
- Publication number
- CN106632401B CN106632401B CN201610875412.9A CN201610875412A CN106632401B CN 106632401 B CN106632401 B CN 106632401B CN 201610875412 A CN201610875412 A CN 201610875412A CN 106632401 B CN106632401 B CN 106632401B
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-
- 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
-
- 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
- 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)
- Hydrogenated Pyridines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434849P | 2011-01-21 | 2011-01-21 | |
| US61/434849 | 2011-01-21 | ||
| CN201280004193.7A CN103502231A (zh) | 2011-01-21 | 2012-01-20 | 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280004193.7A Division CN103502231A (zh) | 2011-01-21 | 2012-01-20 | 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106632401A CN106632401A (zh) | 2017-05-10 |
| CN106632401B true CN106632401B (zh) | 2020-12-29 |
Family
ID=45563570
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610875412.9A Expired - Fee Related CN106632401B (zh) | 2011-01-21 | 2012-01-20 | 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 |
| CN201280004193.7A Pending CN103502231A (zh) | 2011-01-21 | 2012-01-20 | 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280004193.7A Pending CN103502231A (zh) | 2011-01-21 | 2012-01-20 | 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US8426584B2 (https=) |
| EP (1) | EP2665716B1 (https=) |
| JP (2) | JP5993875B2 (https=) |
| CN (2) | CN106632401B (https=) |
| BR (1) | BR112013016241A2 (https=) |
| CA (1) | CA2814014A1 (https=) |
| ES (1) | ES2624288T3 (https=) |
| IL (1) | IL226405A0 (https=) |
| MX (1) | MX2013005115A (https=) |
| RU (1) | RU2013138226A (https=) |
| SG (2) | SG10201601516QA (https=) |
| WO (1) | WO2012100179A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
| 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 |
| JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
| SG11201702632QA (en) * | 2014-10-10 | 2017-05-30 | Eisai R&D Man Co Ltd | Pharmaceutical composition of fused aminodihydrothiazine derivative |
| CN117244056A (zh) | 2016-10-27 | 2023-12-19 | 卫材研究发展管理有限公司 | 用于治疗阿尔茨海默病的含有抗Aβ初原纤维抗体和β-分泌酶BACE1抑制剂的组合物 |
| MX2021000778A (es) | 2018-07-24 | 2021-03-31 | Eisai R&D Man Co Ltd | Metodos de tratamiento y prevencion de la enfermedad de alzheimer. |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2151435A1 (en) * | 2007-04-24 | 2010-02-10 | Shionogi&Co., Ltd. | Pharmaceutical composition for treatment of alzheimer's disease |
| CN101910143A (zh) * | 2008-01-18 | 2010-12-08 | 卫材R&D管理有限公司 | 稠合的氨基二氢噻嗪衍生物 |
| WO2011005738A1 (en) * | 2009-07-09 | 2011-01-13 | Eli Lilly And Company | Bace inhibitors |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3227713A (en) | 1966-01-04 | Azine derivatives | ||
| US3235551A (en) | 1966-02-15 | Novel derivatives of | ||
| 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 |
| CN1251671C (zh) | 2000-05-19 | 2006-04-19 | 武田药品工业株式会社 | β分泌酶抑制剂 |
| US6562783B2 (en) | 2001-05-30 | 2003-05-13 | Neurologic, Inc. | Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors |
| WO2004014843A1 (ja) | 2002-08-09 | 2004-02-19 | Takeda Chemical Industries, Ltd. | 置換アミノ化合物およびその用途 |
| WO2004037212A2 (en) | 2002-10-24 | 2004-05-06 | 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 |
| CA2505098A1 (en) | 2002-11-12 | 2004-05-27 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
| PT1699455E (pt) | 2003-12-15 | 2013-08-27 | Merck Sharp & Dohme | Inibidores de protease de aspartilo heterocíclicos |
| 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 |
| EP1802587A4 (en) | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS |
| WO2006041405A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-pyrimidones and uses thereof |
| CA2594946A1 (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 |
| MX2007016180A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Inhibidores de aspartil proteasas. |
| US8211904B2 (en) | 2005-07-18 | 2012-07-03 | Merck, Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
| US20090099217A1 (en) | 2006-04-05 | 2009-04-16 | Astex Therapeutics Ltd. | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies |
| 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 |
| AU2007332754A1 (en) | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| ES2419239T3 (es) | 2007-05-29 | 2013-08-20 | Santen Pharmaceutical Co., Ltd | Nuevo derivado de 1,2,3,4-tetrahidroquinoxalina que tiene como sustituyente un grupo fenilo con una estructura de éster de ácido sulfónico o una estructura de amida de ácido sulfónico introducida en el mismo y que tienen una actividad de unión al receptor de glucocorticoides |
| PE20091236A1 (es) | 2007-11-22 | 2009-09-16 | Astrazeneca Ab | Derivados de pirimidina como immunomoduladores de tlr7 |
| 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 |
| EP2318416B1 (en) | 2008-07-28 | 2013-09-04 | 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 |
| 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 |
| JP2013530238A (ja) | 2010-07-01 | 2013-07-25 | アムジエン・インコーポレーテツド | Pi3k活性の阻害剤としての複素環化合物及びその使用 |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
-
2012
- 2012-01-20 US US13/355,030 patent/US8426584B2/en not_active Expired - Fee Related
- 2012-01-20 SG SG10201601516QA patent/SG10201601516QA/en unknown
- 2012-01-20 BR BR112013016241A patent/BR112013016241A2/pt not_active IP Right Cessation
- 2012-01-20 ES ES12702690.4T patent/ES2624288T3/es active Active
- 2012-01-20 JP JP2013550622A patent/JP5993875B2/ja not_active Expired - Fee Related
- 2012-01-20 WO PCT/US2012/022053 patent/WO2012100179A1/en not_active Ceased
- 2012-01-20 EP EP12702690.4A patent/EP2665716B1/en active Active
- 2012-01-20 RU RU2013138226/04A patent/RU2013138226A/ru not_active Application Discontinuation
- 2012-01-20 CN CN201610875412.9A patent/CN106632401B/zh not_active Expired - Fee Related
- 2012-01-20 CN CN201280004193.7A patent/CN103502231A/zh active Pending
- 2012-01-20 MX MX2013005115A patent/MX2013005115A/es active IP Right Grant
- 2012-01-20 CA CA2814014A patent/CA2814014A1/en not_active Abandoned
- 2012-01-20 SG SG2013027461A patent/SG191710A1/en unknown
-
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
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2151435A1 (en) * | 2007-04-24 | 2010-02-10 | Shionogi&Co., Ltd. | Pharmaceutical composition for treatment of alzheimer's disease |
| CN101910143A (zh) * | 2008-01-18 | 2010-12-08 | 卫材R&D管理有限公司 | 稠合的氨基二氢噻嗪衍生物 |
| WO2011005738A1 (en) * | 2009-07-09 | 2011-01-13 | Eli Lilly And Company | Bace inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| US8426584B2 (en) | 2013-04-23 |
| US20130197244A1 (en) | 2013-08-01 |
| EP2665716B1 (en) | 2017-03-08 |
| CN106632401A (zh) | 2017-05-10 |
| JP2016121177A (ja) | 2016-07-07 |
| EP2665716A1 (en) | 2013-11-27 |
| US20140309429A1 (en) | 2014-10-16 |
| IL226405A0 (en) | 2013-07-31 |
| JP2014503001A (ja) | 2014-02-06 |
| BR112013016241A2 (pt) | 2016-07-12 |
| JP6087005B2 (ja) | 2017-03-01 |
| CN103502231A (zh) | 2014-01-08 |
| ES2624288T3 (es) | 2017-07-13 |
| US20120190848A1 (en) | 2012-07-26 |
| US8802871B2 (en) | 2014-08-12 |
| SG10201601516QA (en) | 2016-03-30 |
| MX2013005115A (es) | 2013-06-03 |
| JP5993875B2 (ja) | 2016-09-14 |
| WO2012100179A1 (en) | 2012-07-26 |
| RU2013138226A (ru) | 2015-02-27 |
| US8962858B2 (en) | 2015-02-24 |
| SG191710A1 (en) | 2013-08-30 |
| CA2814014A1 (en) | 2012-07-26 |
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Legal Events
| Date | Code | Title | Description |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20201229 |
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| CF01 | Termination of patent right due to non-payment of annual fee |