CA2852366C - 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives - Google Patents

6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives Download PDF

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Publication number
CA2852366C
CA2852366C CA2852366A CA2852366A CA2852366C CA 2852366 C CA2852366 C CA 2852366C CA 2852366 A CA2852366 A CA 2852366A CA 2852366 A CA2852366 A CA 2852366A CA 2852366 C CA2852366 C CA 2852366C
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Prior art keywords
dementia
compound
acid
compounds
mmol
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Expired - Fee Related
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CA2852366A
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English (en)
French (fr)
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CA2852366A1 (en
Inventor
Andres Avelino Trabanco-Suarez
Henricus Jacobus Maria Gijsen
Michel Surkyn
Hana PROKOPCOVA
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Janssen Pharmaceutica NV
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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)
CA2852366A 2011-12-05 2012-12-04 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives Expired - Fee Related CA2852366C (en)

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
CA2852366A1 CA2852366A1 (en) 2013-06-13
CA2852366C true CA2852366C (en) 2020-02-18

Family

ID=47278317

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2852366A Expired - Fee Related CA2852366C (en) 2011-12-05 2012-12-04 6-difluoromethyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives

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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
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

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
CN103974951B (zh) 2016-04-13
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
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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Effective date: 20171109

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