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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Expired - Fee Related legal-status Critical Current
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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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (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 (enExample)
EP (1) EP2788346B1 (enExample)
JP (1) JP6169095B2 (enExample)
KR (1) KR102060379B1 (enExample)
CN (1) CN103974951B (enExample)
AU (1) AU2012347397B2 (enExample)
BR (1) BR112014013310A2 (enExample)
CA (1) CA2852366C (enExample)
EA (1) EA023909B1 (enExample)
ES (1) ES2558604T3 (enExample)
IL (1) IL232916A (enExample)
MX (1) MX357384B (enExample)
MY (1) MY165209A (enExample)
PH (1) PH12014501235B1 (enExample)
SG (1) SG11201402734XA (enExample)
UA (1) UA111749C2 (enExample)
WO (1) WO2013083557A1 (enExample)
ZA (1) ZA201404074B (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
AU2011263797B2 (en) 2010-06-09 2014-06-05 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
JP5834091B2 (ja) 2010-12-22 2015-12-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap ベータ−セクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−イミダゾ[1,2−a]ピラジン−8−イルアミン誘導体
JP5853035B2 (ja) 2011-03-09 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap β−セクレターゼ(BACE)の阻害剤として有用な3,4−ジヒドロ−ピロロ[1,2−a]ピラジン−1−イルアミン誘導体
US20140364428A1 (en) * 2011-12-06 2014-12-11 Janssen Pharmaceutica Nv 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
CA2911693C (en) 2013-06-12 2021-08-24 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
AU2014280124B2 (en) 2013-06-12 2018-11-01 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE)
CA2967164A1 (en) 2014-12-18 2016-06-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase
US20230074641A1 (en) * 2020-01-27 2023-03-09 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
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
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
AU2011263797B2 (en) * 2010-06-09 2014-06-05 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
EA201391029A1 (ru) * 2011-01-12 2014-01-30 Новартис Аг Производные оксазина и их применение при лечении неврологических нарушений
WO2012147763A1 (ja) * 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するbace1阻害剤
US20140364428A1 (en) * 2011-12-06 2014-12-11 Janssen Pharmaceutica Nv 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives

Also Published As

Publication number Publication date
EP2788346A1 (en) 2014-10-15
WO2013083557A1 (en) 2013-06-13
PH12014501235A1 (en) 2014-09-08
MX2014006689A (es) 2014-09-04
BR112014013310A2 (pt) 2017-06-13
JP2015500223A (ja) 2015-01-05
UA111749C2 (uk) 2016-06-10
MY165209A (en) 2018-03-05
MX357384B (es) 2018-07-06
EA201491116A1 (ru) 2014-12-30
NZ626662A (en) 2015-05-29
AU2012347397B2 (en) 2016-09-22
EA023909B1 (ru) 2016-07-29
IL232916A (en) 2016-07-31
IL232916A0 (en) 2014-08-03
KR102060379B1 (ko) 2019-12-30
JP6169095B2 (ja) 2017-07-26
EP2788346B1 (en) 2015-10-28
ES2558604T3 (es) 2016-02-05
AU2012347397A1 (en) 2014-04-24
PH12014501235B1 (en) 2014-09-08
KR20140107209A (ko) 2014-09-04
ZA201404074B (en) 2016-10-26
US20140343048A1 (en) 2014-11-20
CN103974951B (zh) 2016-04-13
CN103974951A (zh) 2014-08-06
CA2852366A1 (en) 2013-06-13
SG11201402734XA (en) 2014-06-27
HK1198586A1 (zh) 2015-04-30

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Effective date: 20171109

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Effective date: 20201204