WO2009001730A1 - βセクレターゼ阻害活性を有する新規化合物 - Google Patents

βセクレターゼ阻害活性を有する新規化合物 Download PDF

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Publication number
WO2009001730A1
WO2009001730A1 PCT/JP2008/061141 JP2008061141W WO2009001730A1 WO 2009001730 A1 WO2009001730 A1 WO 2009001730A1 JP 2008061141 W JP2008061141 W JP 2008061141W WO 2009001730 A1 WO2009001730 A1 WO 2009001730A1
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group
substituted
unsubstituted
atom
alkyl
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PCT/JP2008/061141
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English (en)
French (fr)
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Yoshiaki Kiso
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Yoshiaki Kiso
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Publication date
Application filed by Yoshiaki Kiso filed Critical Yoshiaki Kiso
Priority to JP2009520510A priority Critical patent/JP5410278B2/ja
Priority to US12/452,234 priority patent/US8344002B2/en
Priority to EP08777340A priority patent/EP2168947A4/en
Publication of WO2009001730A1 publication Critical patent/WO2009001730A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

　下記式（１）で示されるβセクレターゼ阻害活性を有する新規化合物 　［式中、Ａｒは置換もしくは無置換の５～６員の単環性芳香族環基を示し；Ｒ1、Ｒ2およびＲ3は水素原子、置換もしくは無置換のアルキル基などを示し、あるいはＲ２とＲ３は、それぞれ隣接する炭素原子および窒素原子と共に３～６員環を形成してもよく； Ｒ4は、炭素数１～６のアルキル、フェニル、フェニルチオもしくはヘテロ環のいずれかで置換された炭素数１～６のアルキルなどを示し； Ａは次式（２） （式中、ＸおよびＹは酸素原子、ＮＨまたは硫黄原子を示し、Ｚは水素原子、置換されていてもよい水酸基、アミノ基、またはチオール基などを示す。）で示される基を示し；そして Ｂは水酸基、置換もしくは無置換のアミノ基、置換もしくは無置換の脂肪族もしくは芳香族アミノ基などを示す。］ またはその薬学上許容される塩もしくはそのプロドラッグ。
PCT/JP2008/061141 2007-06-22 2008-06-18 βセクレターゼ阻害活性を有する新規化合物 WO2009001730A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2009520510A JP5410278B2 (ja) 2007-06-22 2008-06-18 βセクレターゼ阻害活性を有する新規化合物
US12/452,234 US8344002B2 (en) 2007-06-22 2008-06-18 Compound having β-secretase inhibitory activity
EP08777340A EP2168947A4 (en) 2007-06-22 2008-06-18 NOVEL COMPOUND HAVING SECRETASE INHIBITING ACTIVITY

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007164845 2007-06-22
JP2007-164845 2007-06-22

Publications (1)

Publication Number Publication Date
WO2009001730A1 true WO2009001730A1 (ja) 2008-12-31

Family

ID=40185549

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/061141 WO2009001730A1 (ja) 2007-06-22 2008-06-18 βセクレターゼ阻害活性を有する新規化合物

Country Status (4)

Country Link
US (1) US8344002B2 (ja)
EP (1) EP2168947A4 (ja)
JP (1) JP5410278B2 (ja)
WO (1) WO2009001730A1 (ja)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011004778A1 (ja) * 2009-07-08 2011-01-13 住友化学株式会社 光学活性化合物の製造方法
CN102344485A (zh) * 2010-08-05 2012-02-08 中国人民解放军军事医学科学院毒物药物研究所 用于治疗阿尔茨海默病的肽类β分泌酶抑制剂及其用途
JP2012521421A (ja) * 2009-03-25 2012-09-13 コメンティス，インコーポレーテッド β−セクレターゼ活性を阻害するピロリジン化合物及びその使用方法
US9714252B2 (en) 2012-12-20 2017-07-25 Purdue Pharma L.P. Cyclic sulfonamides as sodium channel blockers
US9718780B2 (en) 2012-03-16 2017-08-01 Purdue Pharma L.P. Substituted pyridines as sodium channel blockers
US10730866B2 (en) 2014-04-07 2020-08-04 Purdue Pharma L.P. Indole derivatives and use thereof

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2593434A1 (en) 2010-07-16 2013-05-22 Purdue Pharma LP Pyridine compounds as sodium channel blockers
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001000665A2 (en) 1999-06-28 2001-01-04 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
WO2004076478A1 (ja) 2003-02-28 2004-09-10 Yoshiaki Kiso βセクレターゼ阻害活性を有するペプチド誘導体
WO2007029587A1 (ja) * 2005-09-05 2007-03-15 Dainippon Sumitomo Pharma Co., Ltd. βセクレターゼ阻害剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001000665A2 (en) 1999-06-28 2001-01-04 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
WO2004076478A1 (ja) 2003-02-28 2004-09-10 Yoshiaki Kiso βセクレターゼ阻害活性を有するペプチド誘導体
WO2007029587A1 (ja) * 2005-09-05 2007-03-15 Dainippon Sumitomo Pharma Co., Ltd. βセクレターゼ阻害剤

Non-Patent Citations (11)

* Cited by examiner, † Cited by third party
Title
"JIKKEN KAGAKU KOUZA", vol. 14, MARUZEN, article "Synthesis of Organic compounds II"
GREEN: "Protective Groups in Organic Synthesis", 1981, JOHN WILEY & SONS, INC.
J. MED. CHEM., vol. 45, 2002, pages 259 - 262
J. MED. CHEM., vol. 47, 2004, pages 158
J. MED. CHEM., vol. 47, 2004, pages 6447
JOURNAL OF MEDICINAL CHEMISTRY, vol. 20, 1977, pages 510 - 515
KIMURA, T. ET AL.: "Design and synthesis of potent beta-secretase (BACE1) inhibitorswith P1' carboxylic acid bioisosteres", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 9, 1 May 2006 (2006-05-01), pages 2380 - 2386, XP025106867 *
NATURE, vol. 402, 1999, pages 537 - 540
NOBUO IZUMIYA ET AL.: "Base and Experiment of Peptide Synthesis", 1985, MARUZEN
SCHRODER; LUHKER: "The Peptides", vol. 1, 1966, ACADEMIC PRESS
See also references of EP2168947A4

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012521421A (ja) * 2009-03-25 2012-09-13 コメンティス，インコーポレーテッド β−セクレターゼ活性を阻害するピロリジン化合物及びその使用方法
WO2011004778A1 (ja) * 2009-07-08 2011-01-13 住友化学株式会社 光学活性化合物の製造方法
CN102471266A (zh) * 2009-07-08 2012-05-23 住友化学株式会社 光学活性化合物的制造方法
CN102344485A (zh) * 2010-08-05 2012-02-08 中国人民解放军军事医学科学院毒物药物研究所 用于治疗阿尔茨海默病的肽类β分泌酶抑制剂及其用途
US9718780B2 (en) 2012-03-16 2017-08-01 Purdue Pharma L.P. Substituted pyridines as sodium channel blockers
US9714252B2 (en) 2012-12-20 2017-07-25 Purdue Pharma L.P. Cyclic sulfonamides as sodium channel blockers
US10730866B2 (en) 2014-04-07 2020-08-04 Purdue Pharma L.P. Indole derivatives and use thereof

Also Published As

Publication number Publication date
US20100137606A1 (en) 2010-06-03
EP2168947A1 (en) 2010-03-31
EP2168947A4 (en) 2010-07-28
JPWO2009001730A1 (ja) 2010-08-26
JP5410278B2 (ja) 2014-02-05
US8344002B2 (en) 2013-01-01

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