CN103974951B - 6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 - Google Patents

6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 Download PDF

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Publication number
CN103974951B
CN103974951B CN201280059719.1A CN201280059719A CN103974951B CN 103974951 B CN103974951 B CN 103974951B CN 201280059719 A CN201280059719 A CN 201280059719A CN 103974951 B CN103974951 B CN 103974951B
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dementia
compound
acid
compounds
mmol
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Chinese (zh)
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CN103974951A (zh
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A.A.特拉班科-苏亚雷兹
H.J.M.吉森
M.苏克恩
H.普罗科科瓦
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Janssen Pharmaceutica NV
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    • 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
    • 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
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201280059719.1A 2011-12-05 2012-12-04 6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物 Expired - Fee Related CN103974951B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11191997.3 2011-12-05
EP11191997 2011-12-05
PCT/EP2012/074351 WO2013083557A1 (en) 2011-12-05 2012-12-04 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives

Publications (2)

Publication Number Publication Date
CN103974951A CN103974951A (zh) 2014-08-06
CN103974951B true CN103974951B (zh) 2016-04-13

Family

ID=47278317

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CN201280059719.1A Expired - Fee Related CN103974951B (zh) 2011-12-05 2012-12-04 6-二氟甲基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物

Country Status (18)

Country Link
US (1) US20140343048A1 (https=)
EP (1) EP2788346B1 (https=)
JP (1) JP6169095B2 (https=)
KR (1) KR102060379B1 (https=)
CN (1) CN103974951B (https=)
AU (1) AU2012347397B2 (https=)
BR (1) BR112014013310A2 (https=)
CA (1) CA2852366C (https=)
EA (1) EA023909B1 (https=)
ES (1) ES2558604T3 (https=)
IL (1) IL232916A (https=)
MX (1) MX357384B (https=)
MY (1) MY165209A (https=)
PH (1) PH12014501235A1 (https=)
SG (1) SG11201402734XA (https=)
UA (1) UA111749C2 (https=)
WO (1) WO2013083557A1 (https=)
ZA (1) ZA201404074B (https=)

Families Citing this family (12)

* 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)
EP2788335B1 (en) * 2011-12-06 2016-04-13 Janssen Pharmaceutica, N.V. 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives for the treatment of disorders in which beta-secretase is involved
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
EP4096920A1 (en) * 2020-01-27 2022-12-07 Silcotek Corp. Biopharmaceutical manufacturing process and product

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8188079B2 (en) * 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
UA103272C2 (uk) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
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).
CA2824097A1 (en) * 2011-01-12 2012-07-19 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
US8883779B2 (en) * 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
EP2788335B1 (en) * 2011-12-06 2016-04-13 Janssen Pharmaceutica, N.V. 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives for the treatment of disorders in which beta-secretase is involved

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

Also Published As

Publication number Publication date
UA111749C2 (uk) 2016-06-10
SG11201402734XA (en) 2014-06-27
EA023909B1 (ru) 2016-07-29
MX357384B (es) 2018-07-06
PH12014501235B1 (en) 2014-09-08
CN103974951A (zh) 2014-08-06
MY165209A (en) 2018-03-05
EA201491116A1 (ru) 2014-12-30
EP2788346B1 (en) 2015-10-28
ZA201404074B (en) 2016-10-26
AU2012347397B2 (en) 2016-09-22
MX2014006689A (es) 2014-09-04
IL232916A (en) 2016-07-31
KR20140107209A (ko) 2014-09-04
BR112014013310A2 (pt) 2017-06-13
PH12014501235A1 (en) 2014-09-08
EP2788346A1 (en) 2014-10-15
HK1198586A1 (zh) 2015-04-30
IL232916A0 (en) 2014-08-03
CA2852366C (en) 2020-02-18
US20140343048A1 (en) 2014-11-20
CA2852366A1 (en) 2013-06-13
ES2558604T3 (es) 2016-02-05
JP2015500223A (ja) 2015-01-05
JP6169095B2 (ja) 2017-07-26
KR102060379B1 (ko) 2019-12-30
NZ626662A (en) 2015-05-29
WO2013083557A1 (en) 2013-06-13
AU2012347397A1 (en) 2014-04-24

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