WO2009019815A1 - 新規γセクレターゼ阻害剤 - Google Patents

新規γセクレターゼ阻害剤 Download PDF

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Publication number
WO2009019815A1
WO2009019815A1 PCT/JP2008/001728 JP2008001728W WO2009019815A1 WO 2009019815 A1 WO2009019815 A1 WO 2009019815A1 JP 2008001728 W JP2008001728 W JP 2008001728W WO 2009019815 A1 WO2009019815 A1 WO 2009019815A1
Authority
WO
WIPO (PCT)
Prior art keywords
linear
carbon atoms
alkyl group
branched alkyl
novel
Prior art date
Application number
PCT/JP2008/001728
Other languages
English (en)
French (fr)
Inventor
Atsuhiro Abe
Hideaki Shimizu
Seigo Sawada
Hiroshi Kodaira
Original Assignee
Kabushiki Kaisha Yakult Honsha
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 Kabushiki Kaisha Yakult Honsha filed Critical Kabushiki Kaisha Yakult Honsha
Priority to CN2008801027042A priority Critical patent/CN101970458B/zh
Priority to US12/672,326 priority patent/US8501813B2/en
Priority to CA2695877A priority patent/CA2695877A1/en
Priority to EA201070245A priority patent/EA017495B1/ru
Priority to EP08790127A priority patent/EP2177529B1/en
Priority to JP2009526326A priority patent/JP5374370B2/ja
Publication of WO2009019815A1 publication Critical patent/WO2009019815A1/ja

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

　優れたγセクレターゼ阻害効果を有し、かつ、Ａβの生成を特異的に阻害する新規な化合物を提供すること。 　下記式（１）の化合物又はその薬学的に許容し得る塩。 ［式中、Ｒ1は炭素数１～４の直鎖若しくは分岐鎖のアルキル基又はフェニル基を示し；Ｒ2は１つ以上のフェニル基又はハロゲノフェニル基により置換されていてもよい炭素数１～４の直鎖又は分岐鎖のアルキル基を示し；Ｒ3は１つ以上の水酸基により置換されていてもよい炭素数１～４の直鎖又は分岐鎖のアルキル基を示し；Ｒ4は炭素数１～４の直鎖又は分岐鎖のアルキル基を示し、「*」はキラル中心を示す。］
PCT/JP2008/001728 2007-08-09 2008-07-01 新規γセクレターゼ阻害剤 WO2009019815A1 (ja)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN2008801027042A CN101970458B (zh) 2007-08-09 2008-07-01 新型γ分泌酶抑制剂
US12/672,326 US8501813B2 (en) 2007-08-09 2008-07-01 γ-secretase inhibitor
CA2695877A CA2695877A1 (en) 2007-08-09 2008-07-01 Novel .gamma.-secretase inhibitor
EA201070245A EA017495B1 (ru) 2007-08-09 2008-07-01 ИНГИБИТОРЫ γ-СЕКРЕТАЗЫ
EP08790127A EP2177529B1 (en) 2007-08-09 2008-07-01 Gamma-secretase inhibitor
JP2009526326A JP5374370B2 (ja) 2007-08-09 2008-07-01 新規γセクレターゼ阻害剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-207521 2007-08-09
JP2007207521 2007-08-09

Publications (1)

Publication Number Publication Date
WO2009019815A1 true WO2009019815A1 (ja) 2009-02-12

Family

ID=40341060

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/001728 WO2009019815A1 (ja) 2007-08-09 2008-07-01 新規γセクレターゼ阻害剤

Country Status (8)

Country Link
US (1) US8501813B2 (ja)
EP (1) EP2177529B1 (ja)
JP (1) JP5374370B2 (ja)
KR (1) KR20100045458A (ja)
CN (1) CN101970458B (ja)
CA (1) CA2695877A1 (ja)
EA (1) EA017495B1 (ja)
WO (1) WO2009019815A1 (ja)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012520875A (ja) * 2009-03-19 2012-09-10 ブリストル−マイヤーズ スクイブ カンパニー ベータアミロイドペプチド産生阻害剤としての新規アルファ−（ｎ−スルホンアミド）アセトアミド化合物
JP2016204397A (ja) * 2016-09-14 2016-12-08 国立大学法人京都大学 アルツハイマー病予防薬

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102201638B1 (ko) 2013-06-11 2021-01-13 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 SC-β 세포 및 조성물 그리고 그 생성 방법
CA3108275A1 (en) 2018-08-10 2020-02-13 Vertex Pharmaceuticals Incorporated Stem cell derived islet differentiation
AU2022377078A1 (en) 2021-11-01 2024-04-04 Vertex Pharmaceuticals Incorporated Stem cell derived pancreatic islet differentiation

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002053594A2 (en) * 2000-12-28 2002-07-11 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
WO2003039454A2 (en) 2001-10-23 2003-05-15 Oklahoma Medical Research Foundation Beta-secretase inhibitors and methods of use
WO2003091278A1 (fr) 2002-04-24 2003-11-06 Hiroshi Mori Inhibiteurs de gamma secretase

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040121947A1 (en) 2000-12-28 2004-06-24 Oklahoma Medical Research Foundation Compounds which inhibit beta-secretase activity and methods of use thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002053594A2 (en) * 2000-12-28 2002-07-11 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
WO2003039454A2 (en) 2001-10-23 2003-05-15 Oklahoma Medical Research Foundation Beta-secretase inhibitors and methods of use
WO2003091278A1 (fr) 2002-04-24 2003-11-06 Hiroshi Mori Inhibiteurs de gamma secretase
EP1498421A1 (en) 2002-04-24 2005-01-19 Hiroshi Mori Gamma-secretase inhibitors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BIOCHEMISTRY, vol. 39, no. 30, 2000, pages 8698 - 8704
J. BIOL. CHEM., vol. 254, no. 10, 1979, pages 4027 - 4032
J. MED. CHEM., vol. 41, no. 1, 1998, pages 6 - 9
See also references of EP2177529A4 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012520875A (ja) * 2009-03-19 2012-09-10 ブリストル−マイヤーズ スクイブ カンパニー ベータアミロイドペプチド産生阻害剤としての新規アルファ−（ｎ−スルホンアミド）アセトアミド化合物
JP2016204397A (ja) * 2016-09-14 2016-12-08 国立大学法人京都大学 アルツハイマー病予防薬

Also Published As

Publication number Publication date
US20110071224A1 (en) 2011-03-24
CN101970458B (zh) 2013-08-28
JP5374370B2 (ja) 2013-12-25
CA2695877A1 (en) 2009-02-12
EP2177529A1 (en) 2010-04-21
JPWO2009019815A1 (ja) 2010-10-28
KR20100045458A (ko) 2010-05-03
CN101970458A (zh) 2011-02-09
EA017495B1 (ru) 2012-12-28
EP2177529A4 (en) 2011-04-20
EP2177529B1 (en) 2013-03-27
EA201070245A1 (ru) 2010-10-29
US8501813B2 (en) 2013-08-06

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