WO2008133273A1 - アルツハイマー症治療用医薬組成物 - Google Patents

アルツハイマー症治療用医薬組成物 Download PDF

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Publication number
WO2008133273A1
WO2008133273A1 PCT/JP2008/057842 JP2008057842W WO2008133273A1 WO 2008133273 A1 WO2008133273 A1 WO 2008133273A1 JP 2008057842 W JP2008057842 W JP 2008057842W WO 2008133273 A1 WO2008133273 A1 WO 2008133273A1
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Prior art keywords
alzheimer
disease
treatment
pharmaceutical composition
hydrogen
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PCT/JP2008/057842
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English (en)
French (fr)
Inventor
Naotake Kobayashi
Kazuo Ueda
Naohiro Itoh
Shinji Suzuki
Gaku Sakaguchi
Akira Kato
Akira Yukimasa
Akihiro Hori
Yuji Kooriyama
Hidekazu Haraguchi
Ken Yasui
Yasuhiko Kanda
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Shionogi and Co Ltd
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Shionogi and Co Ltd
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Priority to US12/597,470 priority Critical patent/US8653067B2/en
Priority to EP08751980A priority patent/EP2151435A4/en
Priority to JP2009511887A priority patent/JP5383483B2/ja
Publication of WO2008133273A1 publication Critical patent/WO2008133273A1/ja
Anticipated expiration legal-status Critical
Priority to US14/070,202 priority patent/US8895548B2/en
Ceased legal-status Critical Current

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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
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    • 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
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    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
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    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12—Nitrogen atoms not forming part of a nitro radical
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    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
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    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

式(I): (式中、環Aは置換基を有していてもよい炭素環式基または置換基を有していてもよい複素環式基であり、Eは低級アルキレン等であり、XはS、OまたはNR1であり、R1は水素または低級アルキルであり、R2a、R2b、R3a、R3b、R4aおよびR4bは各々独立して水素、ハロゲン、ヒドロキシ等であり、nおよびmは各々独立して0~3の整数であり、n+mは1~3であり、R5は水素、置換基を有していてもよい低級アルキル等である) で示される化合物もしくはその製薬上許容される塩またはそれらの溶媒和物を有効成分とする、アルツハイマー症治療用医薬組成物。
PCT/JP2008/057842 2007-04-24 2008-04-23 アルツハイマー症治療用医薬組成物 Ceased WO2008133273A1 (ja)

Priority Applications (4)

Application Number Priority Date Filing Date Title
US12/597,470 US8653067B2 (en) 2007-04-24 2008-04-23 Pharmaceutical composition for treating Alzheimer's disease
EP08751980A EP2151435A4 (en) 2007-04-24 2008-04-23 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
JP2009511887A JP5383483B2 (ja) 2007-04-24 2008-04-23 アルツハイマー症治療用医薬組成物
US14/070,202 US8895548B2 (en) 2007-04-24 2013-11-01 Pharmaceutical composition for treating alzheimer's disease

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007114764 2007-04-24
JP2007-114764 2007-04-24

Related Child Applications (2)

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US12/597,470 A-371-Of-International US8653067B2 (en) 2007-04-24 2008-04-23 Pharmaceutical composition for treating Alzheimer's disease
US14/070,202 Continuation US8895548B2 (en) 2007-04-24 2013-11-01 Pharmaceutical composition for treating alzheimer's disease

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WO2008133273A1 true WO2008133273A1 (ja) 2008-11-06

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PCT/JP2008/057842 Ceased WO2008133273A1 (ja) 2007-04-24 2008-04-23 アルツハイマー症治療用医薬組成物

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US (2) US8653067B2 (ja)
EP (1) EP2151435A4 (ja)
JP (1) JP5383483B2 (ja)
WO (1) WO2008133273A1 (ja)

Cited By (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009091016A1 (ja) * 2008-01-18 2009-07-23 Eisai R & D Management Co., Ltd. 縮合アミノジヒドロチアジン誘導体
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
US7648983B2 (en) 2008-05-02 2010-01-19 Eli Lilly And Company BACE inhibitors
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
WO2010113848A1 (ja) 2009-03-31 2010-10-07 塩野義製薬株式会社 Bace1阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
WO2010105179A3 (en) * 2009-03-13 2010-11-11 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US7868000B2 (en) 2005-06-14 2011-01-11 Schering Corporation Aspartyl protease inhibitors
WO2011005738A1 (en) 2009-07-09 2011-01-13 Eli Lilly And Company Bace inhibitors
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2011009898A1 (en) 2009-07-22 2011-01-27 Eisai R&D Management Co., Ltd Fused aminodihydro-oxazine derivatives
WO2011029803A1 (en) * 2009-09-11 2011-03-17 F. Hoffmann-La Roche Ag 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes
WO2011058763A1 (ja) 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
WO2011071109A1 (ja) 2009-12-11 2011-06-16 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
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
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