JP2013536864A - 第Xa因子阻害剤の結晶形態 - Google Patents

第Xa因子阻害剤の結晶形態 Download PDF

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JP2013536864A
JP2013536864A JP2013527286A JP2013527286A JP2013536864A JP 2013536864 A JP2013536864 A JP 2013536864A JP 2013527286 A JP2013527286 A JP 2013527286A JP 2013527286 A JP2013527286 A JP 2013527286A JP 2013536864 A JP2013536864 A JP 2013536864A
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crystalline form
patient
betrixaban
thrombosis
stroke
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JP2013536864A5 (enExample
Inventor
ビンセント アール. カポダノ,
リアム コルコラン,
マイケル マクネビン,
イツィア ソロイダ アロジョ,
ロバート エム. ウェンスロー,
リチャード ジー. ボール,
エリック エル. マーゲレフスキー,
ティモシー ケー. メイヤー,
アンジャリ ペンディー,
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ポートラ ファーマシューティカルズ, インコーポレイテッド
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Publication of JP2013536864A publication Critical patent/JP2013536864A/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
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2013527286A 2010-09-01 2011-08-31 第Xa因子阻害剤の結晶形態 Pending JP2013536864A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US37933910P 2010-09-01 2010-09-01
US61/379,339 2010-09-01
US201161454396P 2011-03-18 2011-03-18
US61/454,396 2011-03-18
PCT/US2011/050057 WO2012031017A1 (en) 2010-09-01 2011-08-31 CRYSTALLINE FORMS OF A FACTOR Xa INHIBITOR

Related Child Applications (2)

Application Number Title Priority Date Filing Date
JP2015187427A Division JP2015232046A (ja) 2010-09-01 2015-09-24 第Xa因子阻害剤の結晶形態
JP2017221050A Division JP2018024709A (ja) 2010-09-01 2017-11-16 第Xa因子阻害剤の結晶形態

Publications (2)

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JP2013536864A true JP2013536864A (ja) 2013-09-26
JP2013536864A5 JP2013536864A5 (enExample) 2014-10-09

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JP2013527286A Pending JP2013536864A (ja) 2010-09-01 2011-08-31 第Xa因子阻害剤の結晶形態
JP2015187427A Pending JP2015232046A (ja) 2010-09-01 2015-09-24 第Xa因子阻害剤の結晶形態
JP2017221050A Pending JP2018024709A (ja) 2010-09-01 2017-11-16 第Xa因子阻害剤の結晶形態
JP2019081907A Pending JP2019135258A (ja) 2010-09-01 2019-04-23 第Xa因子阻害剤の結晶形態

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JP2015187427A Pending JP2015232046A (ja) 2010-09-01 2015-09-24 第Xa因子阻害剤の結晶形態
JP2017221050A Pending JP2018024709A (ja) 2010-09-01 2017-11-16 第Xa因子阻害剤の結晶形態
JP2019081907A Pending JP2019135258A (ja) 2010-09-01 2019-04-23 第Xa因子阻害剤の結晶形態

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US (1) US8946269B2 (enExample)
EP (1) EP2611779B1 (enExample)
JP (4) JP2013536864A (enExample)
CN (1) CN103261161B (enExample)
AR (1) AR082804A1 (enExample)
AU (1) AU2011295909B2 (enExample)
CA (1) CA2810004C (enExample)
ES (1) ES2603084T3 (enExample)
IL (1) IL224698A (enExample)
NZ (1) NZ608442A (enExample)
PT (1) PT2611779T (enExample)
TW (1) TW201221128A (enExample)
WO (1) WO2012031017A1 (enExample)

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US8980876B2 (en) 2010-10-28 2015-03-17 The Procter & Gamble Company Inhibition of microbial growth by aconitase inhibition

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US20150224091A1 (en) * 2011-08-31 2015-08-13 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
TWI502689B (zh) * 2012-03-16 2015-10-01 Luxtera Inc 光子材料中介層的方法及系統
US20140346397A1 (en) 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US9200268B2 (en) 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
CN104693114B (zh) * 2013-12-10 2019-08-16 四川海思科制药有限公司 一种贝曲西班的改进的制备方法
CN105085387A (zh) * 2014-05-20 2015-11-25 四川海思科制药有限公司 贝曲西班盐及其制备方法和用途
WO2017091757A1 (en) 2015-11-24 2017-06-01 Portola Pharmaceuticals, Inc. Isotopically enriched betrixaban
CN106995405A (zh) * 2016-01-25 2017-08-01 重庆医药工业研究院有限责任公司 一种贝曲西班马来酸盐无定型物及其制备方法
WO2017208169A1 (en) * 2016-06-02 2017-12-07 Dr. Reddy’S Laboratories Limited Polymorphs of betrixaban & its maleate salt
EP3254674A1 (en) 2016-06-08 2017-12-13 Sandoz Ag Pharmaceutical compositions of betrixaban maleate
EP3293174A1 (en) 2016-09-09 2018-03-14 Sandoz Ag Crystalline salts of betrixaban
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
CN107382897B (zh) * 2017-07-10 2021-05-04 浙江宏元药业股份有限公司 一种贝曲西班的中间体及其制备方法和应用
EP3510996A1 (en) * 2018-01-11 2019-07-17 Sandoz AG Pharmaceutical compositions of betrixaban
CN108570003A (zh) * 2018-06-01 2018-09-25 浙江宏元药业股份有限公司 一种贝曲西班马来酸盐的一水无定形及其制备方法
WO2020264076A1 (en) 2019-06-28 2020-12-30 The Procter & Gamble Company Light augmented treatment method

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8980876B2 (en) 2010-10-28 2015-03-17 The Procter & Gamble Company Inhibition of microbial growth by aconitase inhibition

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JP2019135258A (ja) 2019-08-15
JP2015232046A (ja) 2015-12-24
AU2011295909B2 (en) 2015-05-21
JP2018024709A (ja) 2018-02-15
AR082804A1 (es) 2013-01-09
US8946269B2 (en) 2015-02-03
PT2611779T (pt) 2016-11-21
US20120071519A1 (en) 2012-03-22
IL224698A (en) 2017-01-31
EP2611779B1 (en) 2016-08-10
WO2012031017A1 (en) 2012-03-08
NZ608442A (en) 2015-04-24
TW201221128A (en) 2012-06-01
CA2810004C (en) 2019-09-10
CN103261161A (zh) 2013-08-21
EP2611779A1 (en) 2013-07-10
AU2011295909A1 (en) 2013-04-04
ES2603084T3 (es) 2017-02-23
CA2810004A1 (en) 2012-03-08
CN103261161B (zh) 2016-04-27

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