WO2009066775A1 - 複素環式化合物の非晶質体、それを含む固体分散体、薬剤、およびその製造法 - Google Patents

複素環式化合物の非晶質体、それを含む固体分散体、薬剤、およびその製造法 Download PDF

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WO2009066775A1
WO2009066775A1 PCT/JP2008/071259 JP2008071259W WO2009066775A1 WO 2009066775 A1 WO2009066775 A1 WO 2009066775A1 JP 2008071259 W JP2008071259 W JP 2008071259W WO 2009066775 A1 WO2009066775 A1 WO 2009066775A1
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same
heterocyclic compound
amorphous form
solid dispersion
medicinal preparation
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PCT/JP2008/071259
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English (en)
French (fr)
Inventor
Tadaaki Sugama
Nobuhiro Ishihara
Yoshiharu Tanaka
Masayuki Takahashi
Shinichi Yaguchi
Tetsuo Watanabe
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Zenyaku Kogyo Kabushikikaisha
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Priority to CN200880117078.4A priority Critical patent/CN101883765B/zh
Priority to CA2706536A priority patent/CA2706536C/en
Priority to US12/744,160 priority patent/US8227463B2/en
Priority to AU2008327095A priority patent/AU2008327095B2/en
Priority to JP2009542608A priority patent/JP5479912B2/ja
Priority to EP08852868A priority patent/EP2218718A1/en
Publication of WO2009066775A1 publication Critical patent/WO2009066775A1/ja

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    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

【課題】　ｓ－トリアジンないしピリミジン誘導体をはじめとする複素環式化合物の、生体内への吸収性の向上を目的とする。 【解決手段】本発明によれば、例えば、一般式（Ｉ）［各Ｒ等は明細書中に定義される］で示されるような、ｓ－トリアジンないしピリミジン誘導体をはじめとする複素環式化合物、その水和物、その溶媒和物もしくはその製薬学的に許容される塩の、非晶質体が提供される。さらには、その非晶質体の製造方法も提供される。また、その非晶質体を含んでなる固体分散体、その固体分散体を含む製剤も提供される。
PCT/JP2008/071259 2007-11-22 2008-11-21 複素環式化合物の非晶質体、それを含む固体分散体、薬剤、およびその製造法 WO2009066775A1 (ja)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN200880117078.4A CN101883765B (zh) 2007-11-22 2008-11-21 杂环化合物的无定形物、含有该无定形物的固体分散体、药剂及其制备方法
CA2706536A CA2706536C (en) 2007-11-22 2008-11-21 Amorphous form of heterocyclic compound, solid dispersion and pharmaceutical preparation each comprising the same, and process for production of the same
US12/744,160 US8227463B2 (en) 2007-11-22 2008-11-21 Amorphous body composed of heterocyclic compound, solid dispersion and pharmaceutical preparation each comprising the same, and process for production of the same
AU2008327095A AU2008327095B2 (en) 2007-11-22 2008-11-21 Amorphous form of heterocyclic compound, solid dispersion and medicinal preparation each comprising the same, and process for production of the same
JP2009542608A JP5479912B2 (ja) 2007-11-22 2008-11-21 複素環式化合物の非晶質体、それを含む固体分散体、薬剤、およびその製造法
EP08852868A EP2218718A1 (en) 2007-11-22 2008-11-21 Amorphous form of heterocyclic compound, solid dispersion and medicinal preparation each comprising the same, and process for production of the same

Applications Claiming Priority (2)

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JP2007303332 2007-11-22
JP2007-303332 2007-11-22

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WO2009066775A1 true WO2009066775A1 (ja) 2009-05-28

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PCT/JP2008/071259 WO2009066775A1 (ja) 2007-11-22 2008-11-21 複素環式化合物の非晶質体、それを含む固体分散体、薬剤、およびその製造法

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US (1) US8227463B2 (ja)
EP (2) EP2409975B1 (ja)
JP (1) JP5479912B2 (ja)
KR (1) KR101576695B1 (ja)
CN (1) CN101883765B (ja)
AU (1) AU2008327095B2 (ja)
CA (1) CA2706536C (ja)
DK (1) DK2409975T3 (ja)
ES (1) ES2539714T3 (ja)
HK (1) HK1163079A1 (ja)
PT (1) PT2409975E (ja)
TW (1) TWI482768B (ja)
WO (1) WO2009066775A1 (ja)

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WO2012020762A1 (ja) * 2010-08-10 2012-02-16 アステラス製薬株式会社 へテロ環化合物
US8461158B2 (en) 2009-03-27 2013-06-11 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
US8486939B2 (en) 2009-07-07 2013-07-16 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
JPWO2012002547A1 (ja) * 2010-07-06 2013-12-12 富士化学工業株式会社 ボセンタン固体分散体
US9056852B2 (en) 2011-03-28 2015-06-16 Mei Pharma, Inc. (Alpha-substituted aralkylamino and heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, pharmaceutical compositions thereof, and their use in treating proliferative diseases
JP2015127334A (ja) * 2010-03-25 2015-07-09 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ （Ｒ）−１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）−Ｎ−（１−（２，３−ジヒドロキシプロピル）−６−フルオロ−２−（１−ヒドロキシ−２−メチルプロパン−２−イル）−１Ｈ−インドール−５−イル）シクロプロパンカルボキサミドの固体形態
US9732080B2 (en) 2006-11-03 2017-08-15 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US9758510B2 (en) 2006-04-07 2017-09-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9974781B2 (en) 2006-04-07 2018-05-22 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10058546B2 (en) 2012-07-16 2018-08-28 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxo1-5-y1)-N-(1-(2,3-dihydroxypropy1)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-y1)-1H-indol-5-y1) cyclopropanecarbox-amide and administration thereof
US10071979B2 (en) 2010-04-22 2018-09-11 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
US10081621B2 (en) 2010-03-25 2018-09-25 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
US10206877B2 (en) 2014-04-15 2019-02-19 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
JP2020502086A (ja) * 2016-12-23 2020-01-23 ユニバーシティ オブ コペンハーゲン 物質及びタンパク質の共アモルファス形態
US11304953B2 (en) 2017-05-23 2022-04-19 Mei Pharma, Inc. Combination therapy
US11351176B2 (en) 2017-08-14 2022-06-07 Mei Pharma, Inc. Combination therapy

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HUE064331T2 (hu) * 2014-09-12 2024-03-28 Biohaven Therapeutics Ltd Benzoimidazol-1,2-il amidok mint KV7 csatorna aktivátorok
MX2020009693A (es) 2018-03-19 2021-01-08 Knopp Biosciences Llc Composiciones y metodos de uso de los activadores del canal kv7.
JP7280111B2 (ja) 2019-05-28 2023-05-23 ファナック株式会社 モータ制御装置

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WO1999005138A1 (fr) 1997-07-24 1999-02-04 Zenyaku Kogyo Kabushiki Kaisha Composes heterocycliques et agent antitumoral contenant lesdits composes utilises comme ingredients actifs
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Cited By (37)

* Cited by examiner, † Cited by third party
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US11639347B2 (en) 2006-04-07 2023-05-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10987348B2 (en) 2006-04-07 2021-04-27 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10975061B2 (en) 2006-04-07 2021-04-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10239867B2 (en) 2006-04-07 2019-03-26 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9974781B2 (en) 2006-04-07 2018-05-22 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
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