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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Canada
Prior art keywords
dementia
compound
acid
compounds
mmol
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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
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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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    • 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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  • 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 2011-12-05
EP11191997.3 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) PH12014501235A1 (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
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
AR081587A1 (es) 2010-06-09 2012-10-03 Janssen Pharmaceutica Nv DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE)
ES2648143T3 (es) 2010-12-22 2017-12-28 Janssen Pharmaceutica Nv Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE)
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
CN103974940B (zh) * 2011-12-06 2016-08-24 詹森药业有限公司 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
EP3008067B1 (en) 2013-06-12 2017-03-29 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
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
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)
JP2017538753A (ja) 2014-12-18 2017-12-28 ヤンセン ファーマシューティカ エヌ.ベー. 2,3,4,5−テトラヒドロピリジン−6−アミンおよび3,4−ジヒドロ−2H−ピロール−5−アミンの化合物のβセクレターゼ阻害剤
WO2021154599A1 (en) * 2020-01-27 2021-08-05 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
AR081587A1 (es) 2010-06-09 2012-10-03 Janssen Pharmaceutica Nv DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE)
CN103429589A (zh) * 2011-01-12 2013-12-04 诺瓦提斯公司 噁嗪衍生物及其在治疗神经障碍中的用途
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
CN103974940B (zh) * 2011-12-06 2016-08-24 詹森药业有限公司 5-(3-氨基苯基)-5-烷基-5,6-二氢-2h-[1,4]噁嗪-3-胺衍生物

Also Published As

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

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Effective date: 20171109

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Effective date: 20201204