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 PDF

Info

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
Authority
CN
China
Prior art keywords
compound
salt
mixture
formula
alkyl
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.)
Pending
Application number
CN201280004193.7A
Other languages
English (en)
Chinese (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
Priority to CN201610875412.9A priority Critical patent/CN106632401B/zh
Publication of CN103502231A publication Critical patent/CN103502231A/zh
Pending legal-status Critical Current

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)
  • 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)
CN201280004193.7A 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 Pending CN103502231A (zh)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (33)

* Cited by examiner, † Cited by third party
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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
EP2781519B1 (en) Novel antiviral pyrrolopyridine derivative and a production method for same
TW201623236A (zh) 吡唑醯胺衍生物
JPWO2008156159A1 (ja) ジアミン誘導体の製造法
WO2014098831A1 (en) 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production
CA2804137C (en) Fused heterocyclic derivatives as s1p modulators
WO2019036441A1 (en) PROCESSES FOR PREPARING NIRAPARIB AND INTERMEDIATES THEREOF
US20230416252A1 (en) Process toward the manufacture of (6r,10s)-10-{4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)-pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b][1,7]diazacyclotetradecin-5(6h)-one
EP1817312A1 (en) Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of alzheimer's disease
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
TW200530178A (en) Processes for preparing bicyclo [3.1.0] hexane derivatives, and intermediates thereto
JPWO2012157504A1 (ja) β−ラクタム化合物およびその製造方法
JPH05221947A (ja) シクロプロパン誘導体の製法
TW202607005A (zh) 用於治療與apj受體活性相關的病狀的化合物及組成物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C12 Rejection of a patent application after its publication
RJ01 Rejection of invention patent application after publication

Application publication date: 20140108