CN103974940B - 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 - Google Patents

5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 Download PDF

Info

Publication number
CN103974940B
CN103974940B CN201280060009.0A CN201280060009A CN103974940B CN 103974940 B CN103974940 B CN 103974940B CN 201280060009 A CN201280060009 A CN 201280060009A CN 103974940 B CN103974940 B CN 103974940B
Authority
CN
China
Prior art keywords
compound
fluoro
alkyl
phenyl
dihydro
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
CN201280060009.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN103974940A (zh
Inventor
H.J.M.吉森
S.F.A.范布兰特
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.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of CN103974940A publication Critical patent/CN103974940A/zh
Application granted granted Critical
Publication of CN103974940B publication Critical patent/CN103974940B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201280060009.0A 2011-12-06 2012-12-04 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 Expired - Fee Related CN103974940B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11192171.4 2011-12-06
EP11192171 2011-12-06
PCT/EP2012/074349 WO2013083556A1 (en) 2011-12-06 2012-12-04 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives

Publications (2)

Publication Number Publication Date
CN103974940A CN103974940A (zh) 2014-08-06
CN103974940B true CN103974940B (zh) 2016-08-24

Family

ID=47278316

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280060009.0A Expired - Fee Related CN103974940B (zh) 2011-12-06 2012-12-04 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物

Country Status (12)

Country Link
US (1) US20140364428A1 (https=)
EP (1) EP2788335B1 (https=)
JP (1) JP5989130B2 (https=)
KR (1) KR102002345B1 (https=)
CN (1) CN103974940B (https=)
AU (1) AU2012347396B2 (https=)
CA (1) CA2853891C (https=)
EA (1) EA024716B1 (https=)
ES (1) ES2582473T3 (https=)
IL (1) IL232917A (https=)
MX (1) MX357383B (https=)
WO (1) WO2013083556A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
MX339640B (es) 2010-06-09 2016-06-01 Janssen Pharmaceutica Nv * Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace).
EP2655376B1 (en) 2010-12-22 2017-08-23 Janssen Pharmaceutica NV 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
AU2012224632B2 (en) 2011-03-09 2016-06-16 Janssen Pharmaceutica Nv 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
KR102243134B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체
MX368326B (es) 2013-06-12 2019-09-27 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace).
BR112015030597A2 (pt) 2013-06-12 2017-07-25 Janssen Pharmaceutica Nv derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace)
ES2768823T3 (es) * 2014-12-18 2020-06-23 Janssen Pharmaceutica Nv Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa
US20190359609A1 (en) * 2016-12-16 2019-11-28 Janssen Pharmaceutica Nv Bicyclic oga inhibitor compounds
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
CN108440320A (zh) * 2018-05-09 2018-08-24 上海凌凯医药科技有限公司 一种高手性选择性合成α-双取代α-氨基酸的方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101687827A (zh) * 2007-04-24 2010-03-31 盐野义制药株式会社 环状基团取代的氨基二氢噻嗪衍生物
US20100160290A1 (en) * 2007-04-24 2010-06-24 Shionogi & Co., Ltd. Pharmaceutical composition for treating alzheimer's disease
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2011020806A1 (en) * 2009-08-19 2011-02-24 F. Hoffmann-La Roche Ag 3-amino-5-phenyl-5,6-dihydro-2h-[1,4]oxazine derivatives
WO2011058763A1 (ja) * 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
WO2011071135A1 (ja) * 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
WO2012098064A1 (en) * 2011-01-18 2012-07-26 F. Hoffmann-La Roche Ag 1,4 oxazines as bace1 and/or bace2 inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX339640B (es) * 2010-06-09 2016-06-01 Janssen Pharmaceutica Nv * Derivados de 5, 6-dihidro-2h-[1, 4] oxazin-3-il-amina utiles como inhibidores de la beta-secretasa (bace).
US9284284B2 (en) * 2011-10-13 2016-03-15 Novartis Ag Oxazine derivatives and their use in the treatment of disease
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101687827A (zh) * 2007-04-24 2010-03-31 盐野义制药株式会社 环状基团取代的氨基二氢噻嗪衍生物
US20100160290A1 (en) * 2007-04-24 2010-06-24 Shionogi & Co., Ltd. Pharmaceutical composition for treating alzheimer's disease
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2011020806A1 (en) * 2009-08-19 2011-02-24 F. Hoffmann-La Roche Ag 3-amino-5-phenyl-5,6-dihydro-2h-[1,4]oxazine derivatives
WO2011058763A1 (ja) * 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
WO2011071135A1 (ja) * 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
WO2012098064A1 (en) * 2011-01-18 2012-07-26 F. Hoffmann-La Roche Ag 1,4 oxazines as bace1 and/or bace2 inhibitors

Also Published As

Publication number Publication date
CN103974940A (zh) 2014-08-06
IL232917A (en) 2016-07-31
JP5989130B2 (ja) 2016-09-07
CA2853891A1 (en) 2013-06-13
WO2013083556A1 (en) 2013-06-13
IL232917A0 (en) 2014-08-03
EA201491102A1 (ru) 2014-09-30
EP2788335B1 (en) 2016-04-13
JP2015500257A (ja) 2015-01-05
CA2853891C (en) 2020-03-10
US20140364428A1 (en) 2014-12-11
MX357383B (es) 2018-07-06
AU2012347396B2 (en) 2017-02-16
HK1198535A1 (en) 2015-05-15
KR102002345B1 (ko) 2019-07-22
ES2582473T3 (es) 2016-09-13
KR20140106541A (ko) 2014-09-03
EA024716B1 (ru) 2016-10-31
NZ623858A (en) 2015-05-29
EP2788335A1 (en) 2014-10-15
MX2014006752A (es) 2014-07-14
AU2012347396A1 (en) 2014-05-08

Similar Documents

Publication Publication Date Title
CN103974940B (zh) 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物
EP2588466B1 (en) 5-Amino-3,6-dihydro-1H-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (BACE)
CN103974951B (zh) 6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物
US20130102618A1 (en) 3-amino-5,6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia
CN107108582B (zh) β-分泌酶的2，3，4，5-四氢吡啶-6-胺化合物抑制剂
HK1198535B (en) 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4] oxazin-3-amine derivatives
NZ623858B2 (en) 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives
HK1198586B (zh) 6-二氟甲基-5，6-二氢-2h-[1，4]恶嗪-3-胺衍生物
AU2011263836A1 (en) 5-amino-3,6-dihydro-1H-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (BACE)

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1198535

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1198535

Country of ref document: HK

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

Granted publication date: 20160824