KR101780140B1 - Bace 억제제 - Google Patents

Bace 억제제 Download PDF

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Publication number
KR101780140B1
KR101780140B1 KR1020157035519A KR20157035519A KR101780140B1 KR 101780140 B1 KR101780140 B1 KR 101780140B1 KR 1020157035519 A KR1020157035519 A KR 1020157035519A KR 20157035519 A KR20157035519 A KR 20157035519A KR 101780140 B1 KR101780140 B1 KR 101780140B1
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mmol
added
fluoro
give
compound
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KR20160009052A (ko
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스티븐 제임스 그린
에릭 제임스 헴브레
더스틴 제임스 머고트
유안 쉬
브라이언 모건 왓슨
레오나르드 래리 위너로스키 주니어
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일라이 릴리 앤드 캄파니
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/5415Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/542Heterocyclic 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 heterocyclic ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020157035519A 2013-06-18 2014-06-11 Bace 억제제 Expired - Fee Related KR101780140B1 (ko)

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
KR20160009052A KR20160009052A (ko) 2016-01-25
KR101780140B1 true KR101780140B1 (ko) 2017-09-19

Family

ID=51059662

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020157035519A Expired - Fee Related KR101780140B1 (ko) 2013-06-18 2014-06-11 Bace 억제제

Country Status (14)

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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)

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Publication number Priority date Publication date Assignee Title
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
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
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
JP2018531889A (ja) 2015-08-12 2018-11-01 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−3−フルオロ−3−(フルオロメチル)−6−メチル−6−フェニル−3,4,5,6−テトラヒドロピリジン
WO2017025565A1 (en) * 2015-08-12 2017-02-16 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 Eli Lilly And Company 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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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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SG162790A1 (en) 2005-06-14 2010-07-29 Schering Corp Aspartyl protease inhibitors
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EP2689780A1 (en) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 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
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
WO2010038686A1 (ja) 2008-09-30 2010-04-08 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
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WO2011009898A1 (en) * 2009-07-22 2011-01-27 Eisai R&D Management Co., Ltd Fused aminodihydro-oxazine derivatives

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Also Published As

Publication number Publication date
CA2910415C (en) 2017-09-05
AU2014281032A1 (en) 2015-11-12
US9169271B2 (en) 2015-10-27
JO3318B1 (ar) 2019-03-13
CN105324385A (zh) 2016-02-10
US9029367B2 (en) 2015-05-12
BR112015029348A8 (pt) 2020-03-17
EP3010925B1 (en) 2017-10-04
US20140371212A1 (en) 2014-12-18
EP3010925A1 (en) 2016-04-27
MX2015017156A (es) 2016-03-16
US20150210716A1 (en) 2015-07-30
EA027880B1 (ru) 2017-09-29
TWI639607B (zh) 2018-11-01
AU2014281032B2 (en) 2016-09-29
KR20160009052A (ko) 2016-01-25
JP2016522254A (ja) 2016-07-28
BR112015029348A2 (pt) 2017-07-25
WO2014204730A1 (en) 2014-12-24
TW201536793A (zh) 2015-10-01
CA2910415A1 (en) 2014-12-24
EA201592183A1 (ru) 2016-05-31
ES2657905T3 (es) 2018-03-07

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