JP2016536321A - カナグリフロジンのb形結晶、c形およびd形 - Google Patents

カナグリフロジンのb形結晶、c形およびd形 Download PDF

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JP2016536321A
JP2016536321A JP2016530967A JP2016530967A JP2016536321A JP 2016536321 A JP2016536321 A JP 2016536321A JP 2016530967 A JP2016530967 A JP 2016530967A JP 2016530967 A JP2016530967 A JP 2016530967A JP 2016536321 A JP2016536321 A JP 2016536321A
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ray diffraction
diffraction pattern
measured
canagliflozin
values
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JP2016530967A
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JP2016536321A5 (https=
Inventor
チェン、ミンホア
チャン、イェンフォン
チャオ、イー
チャオ、イェー
チャン、シアオユイ
ヤン、チャオホイ
ルー、フェイ
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Crystal Pharmatech Co Ltd
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Crystal Pharmatech Co Ltd
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Priority claimed from CN201310556655.2A external-priority patent/CN103554092A/zh
Priority claimed from CN201310617597.XA external-priority patent/CN103588762A/zh
Application filed by Crystal Pharmatech Co Ltd filed Critical Crystal Pharmatech Co Ltd
Publication of JP2016536321A publication Critical patent/JP2016536321A/ja
Publication of JP2016536321A5 publication Critical patent/JP2016536321A5/ja
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/06Heterocyclic radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
JP2016530967A 2013-11-11 2014-11-11 カナグリフロジンのb形結晶、c形およびd形 Pending JP2016536321A (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN201310556655.2A CN103554092A (zh) 2013-11-11 2013-11-11 1-(β-D-吡喃葡糖基)-4-甲基-3-[5-(4-氟苯基)-2-噻吩基甲基]苯的新晶型B及其制备方法
CN201310556655.2 2013-11-11
CN201310617597.X 2013-11-27
CN201310617597.XA CN103588762A (zh) 2013-11-27 2013-11-27 坎格列净的新晶型及其制备方法
CN201410542984.6A CN104356121A (zh) 2013-11-11 2014-10-14 1-(β-D-吡喃葡糖基)-4-甲基-3-[5-(4-氟苯基)-2-噻吩基甲基]苯的晶型B及其制备方法
CN201410542984.6 2014-10-14
CN201410593413.5A CN104356122B (zh) 2013-11-27 2014-10-29 坎格列净的晶型及其制备方法
CN201410593413.5 2014-10-29
PCT/IB2014/003013 WO2015071761A2 (en) 2013-11-11 2014-11-11 Crystalline forms b, c, and d of canagliflozin

Publications (2)

Publication Number Publication Date
JP2016536321A true JP2016536321A (ja) 2016-11-24
JP2016536321A5 JP2016536321A5 (https=) 2017-12-07

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JP2016530967A Pending JP2016536321A (ja) 2013-11-11 2014-11-11 カナグリフロジンのb形結晶、c形およびd形

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Country Link
US (1) US20160280731A1 (https=)
EP (1) EP3068779A4 (https=)
JP (1) JP2016536321A (https=)
WO (1) WO2015071761A2 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015139386A1 (zh) 2014-03-19 2015-09-24 杭州普晒医药科技有限公司 坎格列净一水合物及其晶型、它们的制备方法和用途
WO2016016774A1 (en) * 2014-07-31 2016-02-04 Sun Pharmaceutical Industries Limited Crystalline forms of canagliflozin
CN104530024B (zh) * 2015-02-04 2017-08-08 上海迪赛诺药业有限公司 1‑(β‑D‑吡喃葡糖基)‑4‑甲基‑3‑[5‑(4‑氟苯基)‑2‑噻吩基甲基]苯的晶型及其制备方法
ES2896101T3 (es) 2015-09-15 2022-02-23 Laurus Labs Ltd Cocristales de inhibidores de SGLT2, procedimiento para su preparación y composiciones farmacéuticas de los mismos
CZ2015824A3 (cs) 2015-11-20 2017-05-31 Zentiva, K.S. Krystalická forma Canagliflozinu a způsob její přípravy

Citations (7)

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Publication number Priority date Publication date Assignee Title
JP2003519698A (ja) * 2000-01-07 2003-06-24 トランスフォーム ファーマスーティカルズ,インコーポレイテッド 多様な固体形態のハイスループットでの形成、同定および分析
JP2010511602A (ja) * 2006-12-04 2010-04-15 田辺三菱製薬株式会社 1−(β−D−グルコピラノシル)−4−メチル−3−[5−(4−フルオロフェニル)−2−チエニルメチル]ベンゼン1/2水和物の結晶形
JP2010539092A (ja) * 2007-09-10 2010-12-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Sgltの阻害物質として有用な化合物の製造方法
JP2013508284A (ja) * 2009-10-14 2013-03-07 ヤンセン ファーマシューティカ エヌ.ベー. Sglt2の阻害物質として有用な化合物の調製プロセス
JP2013526482A (ja) * 2010-05-11 2013-06-24 田辺三菱製薬株式会社 カナグリフロジン含有錠剤
CN103980262A (zh) * 2014-04-01 2014-08-13 天津大学 卡格列净的b晶型及其结晶制备方法
CN104119324A (zh) * 2014-07-23 2014-10-29 齐鲁天和惠世制药有限公司 一种卡格列净的制备方法

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* Cited by examiner, † Cited by third party
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CA2911261A1 (en) * 2013-05-08 2014-11-13 Lek Pharmaceuticals D.D. Novel crystalline hydrates of 1-(.beta.-d-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene
CN103588762A (zh) * 2013-11-27 2014-02-19 苏州晶云药物科技有限公司 坎格列净的新晶型及其制备方法
CN103554092A (zh) * 2013-11-11 2014-02-05 苏州晶云药物科技有限公司 1-(β-D-吡喃葡糖基)-4-甲基-3-[5-(4-氟苯基)-2-噻吩基甲基]苯的新晶型B及其制备方法
WO2016016774A1 (en) * 2014-07-31 2016-02-04 Sun Pharmaceutical Industries Limited Crystalline forms of canagliflozin

Patent Citations (7)

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Publication number Priority date Publication date Assignee Title
JP2003519698A (ja) * 2000-01-07 2003-06-24 トランスフォーム ファーマスーティカルズ,インコーポレイテッド 多様な固体形態のハイスループットでの形成、同定および分析
JP2010511602A (ja) * 2006-12-04 2010-04-15 田辺三菱製薬株式会社 1−(β−D−グルコピラノシル)−4−メチル−3−[5−(4−フルオロフェニル)−2−チエニルメチル]ベンゼン1/2水和物の結晶形
JP2010539092A (ja) * 2007-09-10 2010-12-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Sgltの阻害物質として有用な化合物の製造方法
JP2013508284A (ja) * 2009-10-14 2013-03-07 ヤンセン ファーマシューティカ エヌ.ベー. Sglt2の阻害物質として有用な化合物の調製プロセス
JP2013526482A (ja) * 2010-05-11 2013-06-24 田辺三菱製薬株式会社 カナグリフロジン含有錠剤
CN103980262A (zh) * 2014-04-01 2014-08-13 天津大学 卡格列净的b晶型及其结晶制备方法
CN104119324A (zh) * 2014-07-23 2014-10-29 齐鲁天和惠世制药有限公司 一种卡格列净的制备方法

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BYRN S: "PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS", PHARMACEUTICAL RESEARCH, vol. V12 N7, JPN5013009960, 1 July 1995 (1995-07-01), US, pages 945 - 954, ISSN: 0003838782 *
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US20160280731A1 (en) 2016-09-29
EP3068779A4 (en) 2017-06-28
EP3068779A2 (en) 2016-09-21
WO2015071761A3 (en) 2015-09-24
WO2015071761A2 (en) 2015-05-21

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