TWI564034B - 含1-(β-D-葡萄吡喃糖苷)-3-(苯基噻吩基甲基)苯化合物之錠劑 - Google Patents

含1-(β-D-葡萄吡喃糖苷)-3-(苯基噻吩基甲基)苯化合物之錠劑 Download PDF

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TWI564034B
TWI564034B TW100116437A TW100116437A TWI564034B TW I564034 B TWI564034 B TW I564034B TW 100116437 A TW100116437 A TW 100116437A TW 100116437 A TW100116437 A TW 100116437A TW I564034 B TWI564034 B TW I564034B
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TW100116437A
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TW201200164A (en
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杉本昌陽
木下肇
德田卓之
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田邊三菱製藥股份有限公司
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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
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • 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
    • 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
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P27/02Ophthalmic agents
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    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW100116437A 2010-05-11 2011-05-11 含1-(β-D-葡萄吡喃糖苷)-3-(苯基噻吩基甲基)苯化合物之錠劑 TWI564034B (zh)

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US33331210P 2010-05-11 2010-05-11

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TW201200164A TW201200164A (en) 2012-01-01
TWI564034B true TWI564034B (zh) 2017-01-01

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US (2) US20130052266A1 (enExample)
EP (1) EP2568971B1 (enExample)
JP (1) JP5596799B2 (enExample)
KR (1) KR101869110B1 (enExample)
CN (3) CN105769792A (enExample)
ES (1) ES2836952T3 (enExample)
TW (1) TWI564034B (enExample)
WO (1) WO2011142478A1 (enExample)

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US20110009347A1 (en) 2009-07-08 2011-01-13 Yin Liang Combination therapy for the treatment of diabetes
EP2979698A4 (en) 2013-03-29 2016-11-16 Astellas Pharma Inc PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION
WO2014195966A2 (en) * 2013-05-30 2014-12-11 Cadila Healthcare Limited Amorphous form of canagliflozin and process for preparing thereof
CN103641822B (zh) * 2013-10-21 2016-06-08 江苏奥赛康药业股份有限公司 一种卡格列净化合物及其药物组合物
WO2015071761A2 (en) * 2013-11-11 2015-05-21 Crystal Pharmatech Co., Ltd. Crystalline forms b, c, and d of canagliflozin
CN103655539B (zh) * 2013-12-13 2019-09-13 重庆医药工业研究院有限责任公司 一种卡格列净的口服固体制剂及其制备方法
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
CN103980262B (zh) * 2014-04-01 2016-06-22 天津大学 卡格列净的b晶型及其结晶制备方法
CN103980261B (zh) * 2014-04-01 2016-06-29 天津大学 卡格列净的a晶型及其结晶制备方法
EP2947077A1 (en) 2014-05-19 2015-11-25 LEK Pharmaceuticals d.d. Stereoselective synthesis of intermediates in the preparation of ß-C-arylglucosides
EP3148513B1 (en) * 2014-05-29 2020-02-26 Novartis AG Ceritinib formulation
CN105330706B (zh) * 2014-06-05 2019-04-16 江苏豪森药业集团有限公司 卡格列净中间体的制备方法
US20160002275A1 (en) * 2014-07-03 2016-01-07 Cadila Healthcare Limited Process for preparation and purification of canagliflozin
EP2990029A1 (en) 2014-08-29 2016-03-02 Sandoz Ag Pharmaceutical compositions comprising Canagliflozin
CN104402946B (zh) * 2014-11-17 2018-01-02 连云港恒运药业有限公司 卡格列净中间体及其无定形的制备方法
CN105769803A (zh) * 2014-12-16 2016-07-20 康普药业股份有限公司 一种用于治疗2型糖尿病的药物组合物及其制备方法
WO2016104643A1 (ja) * 2014-12-25 2016-06-30 田辺三菱製薬株式会社 糖尿病治療用固形製剤
CN104523573A (zh) * 2014-12-29 2015-04-22 成都恒瑞制药有限公司 一种卡格列净快速释放片剂及其制备方法
WO2016142950A1 (en) * 2015-03-11 2016-09-15 Harman Finochem Limited A novel process for preparing (2s,3r,4r,5s,6r)-2-{3-[5-[4-fluoro-phenyl)- thiophen-2-ylmethyl]-4-methyl-phenyl}-6-hydroxymethyl-tetrahydro-pyran-3,4,5- triol and its stable amorphous hemihydrate form
CN106279134A (zh) * 2015-06-23 2017-01-04 中美华世通生物医药科技(武汉)有限公司 卡格列净单晶及其制备方法和用途
US20170071970A1 (en) * 2015-09-15 2017-03-16 Janssen Pharmaceutica Nv Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders
CN106749212A (zh) * 2015-11-24 2017-05-31 重庆圣华曦药业股份有限公司 一种卡格列净中间体的精制方法
CN105503845A (zh) * 2015-12-01 2016-04-20 北京普德康利医药科技发展有限公司 去氟卡格列净化合物及其制备方法和应用
TWI835735B (zh) * 2017-06-12 2024-03-21 比利時商健生藥品公司 減少或預防第ii型糖尿病患者中心血管事件之方法
CN109553609B (zh) * 2017-09-26 2020-09-04 北大方正集团有限公司 一种卡格列净的制备方法
CN109553649B (zh) * 2017-09-26 2020-12-04 北大方正集团有限公司 一种卡格列净中间体的制备方法
US11857559B2 (en) 2018-09-10 2024-01-02 Aurobindo Pharma Ltd. Pharmaceutical composition comprising Canagliflozin, process of preparation and use thereof
CN110946840B (zh) * 2019-12-31 2021-11-26 常州恒邦药业有限公司 一种卡格列净药物组合物及其制备方法
JPWO2024053680A1 (enExample) * 2022-09-07 2024-03-14
CN115531376A (zh) * 2022-10-26 2022-12-30 河南省人民医院 卡格列净在菌群调节方面的新应用

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Publication number Publication date
KR20130106279A (ko) 2013-09-27
US9655852B2 (en) 2017-05-23
JP5596799B2 (ja) 2014-09-24
TW201200164A (en) 2012-01-01
ES2836952T3 (es) 2021-06-28
CN105769792A (zh) 2016-07-20
WO2011142478A1 (en) 2011-11-17
US20130052266A1 (en) 2013-02-28
EP2568971A1 (en) 2013-03-20
JP2013526482A (ja) 2013-06-24
CN106890147A (zh) 2017-06-27
KR101869110B1 (ko) 2018-06-19
EP2568971B1 (en) 2020-10-14
CN102985075A (zh) 2013-03-20
US20160228375A1 (en) 2016-08-11

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