CN103502231A - 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
- CN103502231A CN103502231A CN201280004193.7A CN201280004193A CN103502231A CN 103502231 A CN103502231 A CN 103502231A CN 201280004193 A CN201280004193 A CN 201280004193A CN 103502231 A CN103502231 A CN 103502231A
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- compound
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- Prior art date
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- 0 C*=CC=*(C)C(C(COC(*)C=C)=NO)=C* Chemical compound C*=CC=*(C)C(C(COC(*)C=C)=NO)=C* 0.000 description 3
- IAYLALGUBGQKKY-UHFFFAOYSA-N C=C1OCC(c(cccc2)c2F)=C1CO Chemical compound C=C1OCC(c(cccc2)c2F)=C1CO IAYLALGUBGQKKY-UHFFFAOYSA-N 0.000 description 1
- USYBRPZRFIAESY-UHFFFAOYSA-N CC(C=C)OCC(N1CCOCC1)=O Chemical compound CC(C=C)OCC(N1CCOCC1)=O USYBRPZRFIAESY-UHFFFAOYSA-N 0.000 description 1
- FAMVOZPGRWJEJE-HLUHBDAQSA-N C[C@H]([C@H]1CO)OC[C@]1(c(cccc1)c1F)N Chemical compound C[C@H]([C@H]1CO)OC[C@]1(c(cccc1)c1F)N FAMVOZPGRWJEJE-HLUHBDAQSA-N 0.000 description 1
- KEAXHJHDEOLCCG-MFAVDMRSSA-N NC1([C@H](CO)C(C(F)(F)F)OC1)c(cccc1)c1F Chemical compound NC1([C@H](CO)C(C(F)(F)F)OC1)c(cccc1)c1F KEAXHJHDEOLCCG-MFAVDMRSSA-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
- YONLFQNRGZXBBF-KBPBESRZSA-N OC([C@H]([C@@H](C(O)=O)OC(c1ccccc1)=O)OC(c1ccccc1)=O)=O Chemical compound OC([C@H]([C@@H](C(O)=O)OC(c1ccccc1)=O)OC(c1ccccc1)=O)=O YONLFQNRGZXBBF-KBPBESRZSA-N 0.000 description 1
Images
Classifications
-
- 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)
- 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)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610875412.9A 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 |
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 |
|---|---|---|---|
| CN201610875412.9A Division 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103502231A true CN103502231A (zh) | 2014-01-08 |
Family
ID=45563570
Family Applications (2)
| 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 |
| 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 |
Family Applications After (1)
| 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 |
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) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107106568A (zh) * | 2014-10-10 | 2017-08-29 | 卫材R&D管理有限公司 | 稠合氨基二氢噻嗪衍生物的药物组合物 |
Families Citing this family (11)
| 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 |
| GB201101139D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (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 |
| CN110214146B (zh) * | 2016-10-27 | 2023-08-29 | 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 |
| US20210324056A1 (en) | 2018-07-24 | 2021-10-21 | Eisai R&D Management Co., Ltd. | Methods of treatment and prevention of alzheimer's disease |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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| 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 |
| WO2001087293A1 (en) | 2000-05-19 | 2001-11-22 | 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 |
| 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 |
| 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 |
| ATE443043T1 (de) | 2002-11-12 | 2009-10-15 | Merck & Co Inc | Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer |
| SG163508A1 (en) | 2003-12-15 | 2010-08-30 | Schering Corp | Heterocyclic aspartyl protease inhibitors |
| WO2005097767A1 (en) | 2004-03-30 | 2005-10-20 | Merck & Co., Inc. | 2-aminothiazole compounds useful as aspartyl protease inhibitors |
| 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 |
| DE602006021535D1 (de) | 2005-01-19 | 2011-06-09 | Merck Sharp & Dohme | Als inhibitoren von beta-secretase aktive tertiäre carbinamine mit substituierten heterocyclen zur behandlung der alzheimer-krankheit |
| SG162790A1 (en) | 2005-06-14 | 2010-07-29 | Schering Corp | Aspartyl protease inhibitors |
| WO2007011810A1 (en) | 2005-07-18 | 2007-01-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| CN101460480A (zh) | 2006-04-05 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途 |
| BRPI0712721A2 (pt) | 2006-05-31 | 2012-11-20 | Asubio Pharma Co Ltd | composto de anel de 7 membros e mÉtodo de produÇço e aplicaÇço farmacÊutica do mesmo |
| MX2009006228A (es) | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| 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 |
| WO2008146871A1 (ja) | 2007-05-29 | 2008-12-04 | Santen Pharmaceutical Co., Ltd. | グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド構造を導入したフェニル基を置換基として有する新規1,2,3,4-テトラヒドロキノキサリン誘導体 |
| 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 |
| WO2010013794A1 (en) | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| WO2010038686A1 (ja) | 2008-09-30 | 2010-04-08 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
| 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 |
| EP2588467A1 (en) | 2010-07-01 | 2013-05-08 | Amgen Inc. | Heterocyclic compounds and their use as inhibitors of pi3k activity |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
-
2012
- 2012-01-20 SG SG2013027461A patent/SG191710A1/en unknown
- 2012-01-20 EP EP12702690.4A patent/EP2665716B1/en active Active
- 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 CA CA2814014A patent/CA2814014A1/en not_active Abandoned
- 2012-01-20 SG SG10201601516QA patent/SG10201601516QA/en unknown
- 2012-01-20 WO PCT/US2012/022053 patent/WO2012100179A1/en not_active Ceased
- 2012-01-20 RU RU2013138226/04A patent/RU2013138226A/ru not_active Application Discontinuation
- 2012-01-20 ES ES12702690.4T patent/ES2624288T3/es active Active
- 2012-01-20 BR BR112013016241A patent/BR112013016241A2/pt not_active IP Right Cessation
- 2012-01-20 JP JP2013550622A patent/JP5993875B2/ja not_active Expired - Fee Related
- 2012-01-20 US US13/355,030 patent/US8426584B2/en not_active Expired - Fee Related
- 2012-01-20 MX MX2013005115A patent/MX2013005115A/es active IP Right Grant
-
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 (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Non-Patent Citations (1)
| Title |
|---|
| LINDA DOYLE ET AL.: "An investigation of structure-reactivity relationships of d-alkenyl oximes; competitive thermal reactions leading to cyclic nitrones and/or N-unsubstituted bicyclic isoxazolidines", 《TETRAHEDRON》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107106568A (zh) * | 2014-10-10 | 2017-08-29 | 卫材R&D管理有限公司 | 稠合氨基二氢噻嗪衍生物的药物组合物 |
| CN107106568B (zh) * | 2014-10-10 | 2023-09-26 | 卫材R&D管理有限公司 | 稠合氨基二氢噻嗪衍生物的药物组合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016121177A (ja) | 2016-07-07 |
| US20140309429A1 (en) | 2014-10-16 |
| MX2013005115A (es) | 2013-06-03 |
| IL226405A0 (en) | 2013-07-31 |
| WO2012100179A1 (en) | 2012-07-26 |
| JP6087005B2 (ja) | 2017-03-01 |
| CA2814014A1 (en) | 2012-07-26 |
| US8802871B2 (en) | 2014-08-12 |
| RU2013138226A (ru) | 2015-02-27 |
| ES2624288T3 (es) | 2017-07-13 |
| SG10201601516QA (en) | 2016-03-30 |
| EP2665716A1 (en) | 2013-11-27 |
| CN106632401B (zh) | 2020-12-29 |
| US20120190848A1 (en) | 2012-07-26 |
| JP5993875B2 (ja) | 2016-09-14 |
| JP2014503001A (ja) | 2014-02-06 |
| SG191710A1 (en) | 2013-08-30 |
| BR112013016241A2 (pt) | 2016-07-12 |
| CN106632401A (zh) | 2017-05-10 |
| US8426584B2 (en) | 2013-04-23 |
| US8962858B2 (en) | 2015-02-24 |
| EP2665716B1 (en) | 2017-03-08 |
| US20130197244A1 (en) | 2013-08-01 |
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| C06 | Publication | ||
| PB01 | Publication | ||
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| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20140108 |