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
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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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (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
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
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
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
RU2018104868A (ru) 2015-08-12 2019-09-13 Х. Лундбекк А/С 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1
JP2018527338A (ja) * 2015-08-12 2018-09-20 ハー・ルンドベック・アクチエゼルスカベット ＢＡＣＥ１阻害剤としての２−アミノ−７ａ−フェニル−３，４，４ａ，５，７，７ａ−ヘキサヒドロフロ［３，４−ｂ］ピリジン
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)

* 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

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WO2006138264A2 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
AU2008245082B8 (en) 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
KR20110076965A (ko) 2008-09-30 2011-07-06 에자이 알앤드디 매니지먼트 가부시키가이샤 신규한 축합 아미노 디하이드로티아진 유도체
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
US20120245154A1 (en) 2009-12-09 2012-09-27 Shionogi & Co., Ltd. Substituted aminothiazine derivative
US20120245155A1 (en) 2009-12-11 2012-09-27 Shionogi & Co., Ltd. Fused heterocyclic compound having amino group
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
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
EP2665716B1 (en) 2011-01-21 2017-03-08 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
EP2694521B1 (en) 2011-04-07 2015-11-25 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
EP2718287A1 (en) 2011-06-07 2014-04-16 F.Hoffmann-La Roche Ag [1,3]oxazines
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
WO2013030713A1 (en) 2011-08-31 2013-03-07 Pfizer Inc. Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds
HUE053745T2 (hu) 2011-11-25 2021-07-28 Adverio Pharma Gmbh Helyettesített 5-fluor-1H-pirazolopiridin kristályos formában
HUE030534T2 (hu) 2012-04-27 2017-05-29 Eisai R&D Man Co Ltd Eljárás 5-(difluormetil)pirazin-2-karbonsav elõállítására és elõállítási intermediere
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.
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Patent 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

Also Published As

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

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