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 PDF

Info

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
Authority
CN
China
Prior art keywords
compound
mixture
formula
added
equiv
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
Application number
CN201610875412.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN106632401A (zh
Inventor
B.米塔塞夫
金大式
张慧明
M.J.施纳德贝克
C.N.法兴
K.尤施扎瓦
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanitary Material R&d Management Co ltd
Original Assignee
Sanitary Material R&d Management Co ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sanitary Material R&d Management Co ltd filed Critical Sanitary Material R&d Management Co ltd
Publication of CN106632401A publication Critical patent/CN106632401A/zh
Application granted granted Critical
Publication of CN106632401B publication Critical patent/CN106632401B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic 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
    • C07D307/18Heterocyclic 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
    • C07D307/22Nitrogen atoms not forming part of a nitro radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

Landscapes

  • 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)
CN201610875412.9A 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 Expired - Fee Related CN106632401B (zh)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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

Similar Documents

Publication Publication Date Title
CN106632401B (zh) 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物
AU2009205072C1 (en) Condensed aminodihydrothiazine derivative
EP1925611B1 (en) Optically active diamine derivative and process for producing the same
JP6093770B2 (ja) 癌の治療のためのmdm2阻害剤としての複素環化合物
EP2935256A1 (en) 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production
EP3177618A1 (en) Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JP2024542610A (ja) 神経学的状態の治療のためのスルホンアミド化合物
WO2014015125A1 (en) Fused aminodihydrothiazine derivative salts and uses thereof
JP6723250B2 (ja) N−[3−[(4ar,7as)−2−アミノ−6−(5−フルオロピリミジン−2−イル)−4,4a,5,7−テトラヒドロピロロ[3,4−d][1,3]チアジン−7a−イル]−4−フルオロ−フェニル]−5−メトキシ−ピラジン−2−カルボキサミドのトシル酸塩
JP6353977B2 (ja) Bace阻害剤としてのテトラヒドロピロロ[3,4−d][1,3]チアジン誘導体

Legal Events

Date Code Title Description
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

CF01 Termination of patent right due to non-payment of annual fee