AU2017376444B2 - Thiazine derivatives as beta-secretase inhibitors and methods of use - Google Patents

Thiazine derivatives as beta-secretase inhibitors and methods of use Download PDF

Info

Publication number
AU2017376444B2
AU2017376444B2 AU2017376444A AU2017376444A AU2017376444B2 AU 2017376444 B2 AU2017376444 B2 AU 2017376444B2 AU 2017376444 A AU2017376444 A AU 2017376444A AU 2017376444 A AU2017376444 A AU 2017376444A AU 2017376444 B2 AU2017376444 B2 AU 2017376444B2
Authority
AU
Australia
Prior art keywords
tautomer
compound
amino
dihydro
pharmaceutically acceptable
Prior art date
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.)
Active
Application number
AU2017376444A
Other languages
English (en)
Other versions
AU2017376444A1 (en
Inventor
Matthew P. Bourbeau
Paul E. Harrington
Qingyian Liu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Amgen Inc
Original Assignee
Amgen Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of AU2017376444A1 publication Critical patent/AU2017376444A1/en
Application granted granted Critical
Publication of AU2017376444B2 publication Critical patent/AU2017376444B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • 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)
AU2017376444A 2016-12-15 2017-12-13 Thiazine derivatives as beta-secretase inhibitors and methods of use Active AU2017376444B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662434714P 2016-12-15 2016-12-15
US62/434,714 2016-12-15
PCT/US2017/066179 WO2018112083A1 (en) 2016-12-15 2017-12-13 Thiazine derivatives as beta-secretase inhibitors and methods of use

Publications (2)

Publication Number Publication Date
AU2017376444A1 AU2017376444A1 (en) 2019-07-04
AU2017376444B2 true AU2017376444B2 (en) 2021-09-30

Family

ID=60888745

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017376444A Active AU2017376444B2 (en) 2016-12-15 2017-12-13 Thiazine derivatives as beta-secretase inhibitors and methods of use

Country Status (9)

Country Link
US (1) US10889579B2 (enExample)
EP (1) EP3555084B1 (enExample)
JP (1) JP7149272B2 (enExample)
AU (1) AU2017376444B2 (enExample)
CA (1) CA3047288A1 (enExample)
ES (1) ES2910791T3 (enExample)
MA (1) MA54100A (enExample)
MX (1) MX388697B (enExample)
WO (1) WO2018112083A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017376441B2 (en) * 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
MX394391B (es) 2016-12-15 2025-03-24 Amgen Inc Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso.
CA3047290A1 (en) 2016-12-15 2018-06-21 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2305672A1 (en) * 2008-06-13 2011-04-06 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY

Family Cites Families (59)

* 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
JPH11507538A (ja) 1995-06-07 1999-07-06 アテナ ニューロサイエンシズ インコーポレイティド β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ
PL205294B1 (pl) 1998-09-24 2010-03-31 Upjohn Co Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta
CA2628074C (en) 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
JP5383484B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
PL2233474T3 (pl) 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
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
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
JP5666304B2 (ja) 2008-09-30 2015-02-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
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
US20120238557A1 (en) 2009-11-13 2012-09-20 Shionogi & Co., Ltd. Aminothiazine or aminooxazine derivative having amino linker
JPWO2011070781A1 (ja) 2009-12-09 2013-04-22 塩野義製薬株式会社 置換アミノチアジン誘導体
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
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
CA2824097A1 (en) 2011-01-12 2012-07-19 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
MY162413A (en) 2011-01-13 2017-06-15 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
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
BR112013026341A2 (pt) 2011-04-13 2019-09-24 Merck Sharp & Dohe Corp composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
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
AR086539A1 (es) 2011-05-24 2014-01-08 Bristol Myers Squibb Co COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE
US8927535B2 (en) 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
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
EP2827857A4 (en) 2012-03-20 2016-03-30 Elan Pharm Inc SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE AND COMPOSITIONS AND USES THEREOF
WO2013164730A1 (en) 2012-05-04 2013-11-07 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2.
WO2013182638A1 (en) 2012-06-08 2013-12-12 H. Lundbeck A/S 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
EP2897964A1 (en) 2012-09-20 2015-07-29 Pfizer Inc. Alkyl-substituted hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
EP2908824B1 (en) 2012-10-17 2018-05-02 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
SI2912041T1 (sl) 2012-10-26 2017-02-28 Eli Lilly And Company Derivati tetrahidropirolotiazina kot inhibitorji beta sekretaze (bace)
WO2014093190A1 (en) 2012-12-14 2014-06-19 Merck Sharp & Dohme Corp. Bace inhibitors of iminothiadiazine dioxides
US9403846B2 (en) 2012-12-19 2016-08-02 Pfizer Inc. Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
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
EP2934539B1 (en) 2012-12-20 2019-03-27 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
WO2014099788A1 (en) 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
MX374512B (es) 2013-03-08 2025-03-06 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso.
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
CN106795147B (zh) 2014-08-08 2020-09-22 美国安进公司 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
ES2942308T3 (es) 2015-04-21 2023-05-31 Allgenesis Biotherapeutics Inc Compuestos y su uso como inhibidores de BACE1
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
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
MX394391B (es) 2016-12-15 2025-03-24 Amgen Inc Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso.
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CN108064136B (zh) 2016-12-23 2019-09-20 深圳市柔宇科技有限公司 一种智能雨伞

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2305672A1 (en) * 2008-06-13 2011-04-06 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY

Also Published As

Publication number Publication date
US10889579B2 (en) 2021-01-12
JP2020503292A (ja) 2020-01-30
JP7149272B2 (ja) 2022-10-06
ES2910791T3 (es) 2022-05-13
US20200062743A1 (en) 2020-02-27
CA3047288A1 (en) 2018-06-21
WO2018112083A1 (en) 2018-06-21
EP3555084B1 (en) 2022-03-16
AU2017376444A1 (en) 2019-07-04
EP3555084A1 (en) 2019-10-23
MX388697B (es) 2025-03-20
MX2019007102A (es) 2019-12-16
MA54100A (fr) 2021-10-20

Similar Documents

Publication Publication Date Title
AU2017376441B2 (en) Oxazine derivatives as beta-secretase inhibitors and methods of use
AU2017376444B2 (en) Thiazine derivatives as beta-secretase inhibitors and methods of use
AU2017376445B2 (en) Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
US11021493B2 (en) 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
EP3177622A1 (en) Novel compounds for use in cognition improvement
AU2017378316B2 (en) Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CA2911693C (en) 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
CA3047287C (en) Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
GB2504615A (en) Fused aminodihydrothiazine derivatives
EP3334738A1 (en) 2-amino-7a-phenyl-3,4,4a,5,7,7a-hexahydrofuro[3,4-b]pyridines as bace1 inhibitors

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)