AU2017378316B2 - Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use - Google Patents

Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use Download PDF

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Publication number
AU2017378316B2
AU2017378316B2 AU2017378316A AU2017378316A AU2017378316B2 AU 2017378316 B2 AU2017378316 B2 AU 2017378316B2 AU 2017378316 A AU2017378316 A AU 2017378316A AU 2017378316 A AU2017378316 A AU 2017378316A AU 2017378316 B2 AU2017378316 B2 AU 2017378316B2
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thia
azabicyclo
hept
ethynyl
amino
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AU2017378316A1 (en
Inventor
Jennifer R. Allen
Albert Amegadzie
Matthew P. Bourbeau
Jian J. Chen
Michael J. Frohn
Paul E. Harrington
Jonathan D. Low
Vu V. MA
Thomas T. Nguyen
Alexander J. Pickrell
Corey REEVES
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Amgen Inc
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Amgen Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/041,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/081,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Psychiatry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2017378316A 2016-12-15 2017-12-13 Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use Active AU2017378316B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662434721P 2016-12-15 2016-12-15
US62/434,721 2016-12-15
PCT/US2017/066184 WO2018112086A1 (en) 2016-12-15 2017-12-13 Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use

Publications (2)

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AU2017378316A1 AU2017378316A1 (en) 2019-07-04
AU2017378316B2 true AU2017378316B2 (en) 2021-04-01

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AU2017378316A Active AU2017378316B2 (en) 2016-12-15 2017-12-13 Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use

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US (1) US10889581B2 (enExample)
EP (1) EP3555085B1 (enExample)
JP (1) JP7159161B2 (enExample)
AU (1) AU2017378316B2 (enExample)
MX (1) MX386618B (enExample)
WO (1) WO2018112086A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
MX387729B (es) 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
CA3047285A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014013076A1 (en) * 2012-07-20 2014-01-23 Eisai R&D Management Co., Ltd. Hexahydropyrrolothiazine compounds
US20160046618A1 (en) * 2014-08-08 2016-02-18 Amgen Inc. Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use

Family Cites Families (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
SI9300303A (en) 1993-06-08 1994-12-31 Krka Tovarna Zdravil Process for isolation of hypolipemic effective substance
AU6383396A (en) 1995-06-07 1996-12-30 Athena Neurosciences, Inc. Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition
KR20070013361A (ko) 1998-09-24 2007-01-30 파마시아 앤드 업존 캄파니 엘엘씨 알츠하이머병 세크레타제
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
WO2008133273A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
ES2548774T3 (es) 2008-01-18 2015-10-20 Eisai R&D Management Co., Ltd. Derivado de aminodihidrotiazina condensado
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
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
CN102105475B (zh) 2008-07-28 2014-04-09 卫材R&D管理有限公司 螺氨基二氢噻嗪衍生物
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
AU2009300836B2 (en) 2008-09-30 2014-02-27 Eisai R&D Management Co., Ltd. Novel fused aminodihydrothiazine derivative
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
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
EP2514747A4 (en) 2009-12-09 2013-05-08 Shionogi & Co SUBSTITUTED AMINOTHIAZINE DERIVATIVE
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
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
EA201391029A1 (ru) 2011-01-12 2014-01-30 Новартис Аг Производные оксазина и их применение при лечении неврологических нарушений
CA2824220C (en) 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
MX2013011947A (es) 2011-04-13 2014-01-16 Merck Sharp & Dohme Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.
CN103649082A (zh) 2011-04-26 2014-03-19 盐野义制药株式会社 吡啶衍生物和含有该吡啶衍生物的bace1抑制剂
EP2517898A1 (de) 2011-04-29 2012-10-31 Lanxess Deutschland GmbH Kieselsäurehaltige Kautschukmischungen mit schwefelhaltigen Additiven
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US8604024B2 (en) 2011-05-24 2013-12-10 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TW201302763A (zh) 2011-05-24 2013-01-16 必治妥美雅史谷比公司 用於減少β-類澱粉產生之化合物
US8927535B2 (en) 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
KR20140054295A (ko) 2011-08-22 2014-05-08 머크 샤프 앤드 돔 코포레이션 Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
JP6043355B2 (ja) 2011-08-31 2016-12-14 ファイザー・インク ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物
HK1206597A1 (en) 2012-03-20 2016-01-15 艾朗制药股份有限公司 Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof
ES2585262T3 (es) 2012-05-04 2016-10-04 Pfizer Inc Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2
WO2013182638A1 (en) 2012-06-08 2013-12-12 H. Lundbeck A/S 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease
CA2882389A1 (en) 2012-09-20 2014-03-27 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
EP2908825B1 (en) 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2014062553A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
HUE031764T2 (en) 2012-10-26 2017-07-28 Lilly Co Eli Tetrahydropyrrolothiazine derivatives as BACE inhibitors
EP2931284B1 (en) 2012-12-14 2017-08-23 Merck Sharp & Dohme Corp. Bace inhibitors of iminothiadiazine dioxides
US9475784B2 (en) 2012-12-19 2016-10-25 Bristol-Myers Squibb Company 4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production
CA2893333C (en) 2012-12-19 2017-10-24 Pfizer Inc. Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
CA2894919A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. C5,c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2934534B1 (en) 2012-12-21 2017-12-13 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
HK1210609A1 (en) 2013-01-22 2016-04-29 霍夫曼-拉罗奇有限公司 Fluoro-[1,3]oxazines as bace1 inhibitors
CA2902212C (en) 2013-03-01 2020-10-13 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
AU2014225604B2 (en) 2013-03-08 2018-05-17 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
TWI593692B (zh) 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
WO2016172255A1 (en) 2015-04-21 2016-10-27 Allgenesis Biotherapeutics, Inc. Compounds and their use as bace1 inhibitors
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
MX387729B (es) 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
CA3047285A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014013076A1 (en) * 2012-07-20 2014-01-23 Eisai R&D Management Co., Ltd. Hexahydropyrrolothiazine compounds
US20160046618A1 (en) * 2014-08-08 2016-02-18 Amgen Inc. Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use

Also Published As

Publication number Publication date
CA3047287A1 (en) 2018-06-21
US20200231585A1 (en) 2020-07-23
EP3555085B1 (en) 2020-12-02
JP2020503295A (ja) 2020-01-30
EP3555085A1 (en) 2019-10-23
WO2018112086A1 (en) 2018-06-21
MX2019007103A (es) 2019-11-05
JP7159161B2 (ja) 2022-10-24
AU2017378316A1 (en) 2019-07-04
US10889581B2 (en) 2021-01-12
MX386618B (es) 2025-03-19

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