AU2014281032B2 - Bace inhibitors - Google Patents

Bace inhibitors Download PDF

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Publication number
AU2014281032B2
AU2014281032B2 AU2014281032A AU2014281032A AU2014281032B2 AU 2014281032 B2 AU2014281032 B2 AU 2014281032B2 AU 2014281032 A AU2014281032 A AU 2014281032A AU 2014281032 A AU2014281032 A AU 2014281032A AU 2014281032 B2 AU2014281032 B2 AU 2014281032B2
Authority
AU
Australia
Prior art keywords
mmol
fluoro
compound
added
mixture
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.)
Ceased
Application number
AU2014281032A
Other languages
English (en)
Other versions
AU2014281032A1 (en
Inventor
Steven James Green
Erik James Hembre
Dustin James Mergott
Yuan Shi
Brian Morgan Watson
Leonard Larry Winneroski Jr.
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of AU2014281032A1 publication Critical patent/AU2014281032A1/en
Application granted granted Critical
Publication of AU2014281032B2 publication Critical patent/AU2014281032B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2014281032A 2013-06-18 2014-06-11 Bace inhibitors Ceased AU2014281032B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361836175P 2013-06-18 2013-06-18
US61/836,175 2013-06-18
US201361877373P 2013-09-13 2013-09-13
US61/877,373 2013-09-13
PCT/US2014/041825 WO2014204730A1 (en) 2013-06-18 2014-06-11 Bace inhibitors

Publications (2)

Publication Number Publication Date
AU2014281032A1 AU2014281032A1 (en) 2015-11-12
AU2014281032B2 true AU2014281032B2 (en) 2016-09-29

Family

ID=51059662

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2014281032A Ceased AU2014281032B2 (en) 2013-06-18 2014-06-11 Bace inhibitors

Country Status (14)

Country Link
US (2) US9029367B2 (enExample)
EP (1) EP3010925B1 (enExample)
JP (1) JP2016522254A (enExample)
KR (1) KR101780140B1 (enExample)
CN (1) CN105324385A (enExample)
AU (1) AU2014281032B2 (enExample)
BR (1) BR112015029348A8 (enExample)
CA (1) CA2910415C (enExample)
EA (1) EA027880B1 (enExample)
ES (1) ES2657905T3 (enExample)
JO (1) JO3318B1 (enExample)
MX (1) MX2015017156A (enExample)
TW (1) TWI639607B (enExample)
WO (1) WO2014204730A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
AR103680A1 (es) * 2015-02-23 2017-05-24 Lilly Co Eli Inhibidores selectivos de bace1
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
US20180244645A1 (en) 2015-08-12 2018-08-30 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
EP3334738A1 (en) * 2015-08-12 2018-06-20 H. Lundbeck A/S 2-amino-7a-phenyl-3,4,4a,5,7,7a-hexahydrofuro[3,4-b]pyridines as bace1 inhibitors
JOP20170106A1 (ar) * 2016-05-20 2017-11-20 Lilly Co Eli مركبات تترا هيدرو فوروكسازين واستخداماتها كمثبطات bace1 انتقائية
JP6889466B2 (ja) * 2016-12-09 2021-06-18 学校法人 名城大学 アミド基を含む単離された化合物の塩、その製造方法及びこれを用いたアミド化合物の合成方法
CN107892697B (zh) 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物
CN111217709A (zh) * 2018-11-27 2020-06-02 南京药石科技股份有限公司 一种（1-氟环丙基）甲胺盐酸盐的制备方法

Citations (2)

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Publication number Priority date Publication date Assignee Title
US20090209755A1 (en) * 2008-01-18 2009-08-20 Yuichi Suzuki Fused aminodihydrothiazine derivatives
WO2011009898A1 (en) * 2009-07-22 2011-01-27 Eisai R&D Management Co., Ltd Fused aminodihydro-oxazine derivatives

Family Cites Families (28)

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CN101228163A (zh) 2005-06-14 2008-07-23 先灵公司 天冬氨酰蛋白酶抑制剂
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
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
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
EP2514747A4 (en) 2009-12-09 2013-05-08 Shionogi & Co SUBSTITUTED AMINOTHIAZINE DERIVATIVE
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
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
JPWO2011071109A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
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
BR112013016241A2 (pt) 2011-01-21 2016-07-12 Eisai R&D Man Co Ltd composto, e, método para fabricar um composto
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
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
MX2013014007A (es) 2011-06-07 2014-03-12 Hoffmann La Roche [1,3] oxazinas.
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
UA120278C2 (uk) 2011-11-25 2019-11-11 Адверіо Фарма Гмбх Заміщені 5-фтор-1н-піразолопіридини в кристалічній формі
EP2841423B1 (en) 2012-04-27 2016-11-30 Eisai R&D Management Co., Ltd. Method for producing 5-(difluoromethyl)pyrazine-2-carboxilic acid and production intermediate 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
WO2014015125A1 (en) 2012-07-19 2014-01-23 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivative salts and uses thereof
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090209755A1 (en) * 2008-01-18 2009-08-20 Yuichi Suzuki Fused aminodihydrothiazine derivatives
WO2011009898A1 (en) * 2009-07-22 2011-01-27 Eisai R&D Management Co., Ltd Fused aminodihydro-oxazine derivatives

Also Published As

Publication number Publication date
BR112015029348A8 (pt) 2020-03-17
US20140371212A1 (en) 2014-12-18
TWI639607B (zh) 2018-11-01
US9029367B2 (en) 2015-05-12
KR101780140B1 (ko) 2017-09-19
EP3010925B1 (en) 2017-10-04
BR112015029348A2 (pt) 2017-07-25
ES2657905T3 (es) 2018-03-07
US20150210716A1 (en) 2015-07-30
WO2014204730A1 (en) 2014-12-24
EP3010925A1 (en) 2016-04-27
CA2910415C (en) 2017-09-05
CN105324385A (zh) 2016-02-10
KR20160009052A (ko) 2016-01-25
JP2016522254A (ja) 2016-07-28
CA2910415A1 (en) 2014-12-24
AU2014281032A1 (en) 2015-11-12
TW201536793A (zh) 2015-10-01
US9169271B2 (en) 2015-10-27
JO3318B1 (ar) 2019-03-13
EA201592183A1 (ru) 2016-05-31
MX2015017156A (es) 2016-03-16
EA027880B1 (ru) 2017-09-29

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired