CN103261161B - 凝血因子Xa抑制剂的结晶形式 - Google Patents

凝血因子Xa抑制剂的结晶形式 Download PDF

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Publication number
CN103261161B
CN103261161B CN201180052042.4A CN201180052042A CN103261161B CN 103261161 B CN103261161 B CN 103261161B CN 201180052042 A CN201180052042 A CN 201180052042A CN 103261161 B CN103261161 B CN 103261161B
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China
Prior art keywords
crystalline form
betrixaban
thrombosis
water
thrombotic
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Expired - Fee Related
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CN201180052042.4A
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English (en)
Chinese (zh)
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CN103261161A (zh
Inventor
V.R.卡波达诺
L.科科伦
M.麦克内文
I.Z.阿罗约
R.M.温斯罗
R.G.鲍尔
E.L.马杰里夫斯基
T.K.马厄
A.潘迪
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Portola Pharmaceuticals LLC
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Portola Pharmaceuticals LLC
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino 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)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201180052042.4A 2010-09-01 2011-08-31 凝血因子Xa抑制剂的结晶形式 Expired - Fee Related CN103261161B (zh)

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

Publications (2)

Publication Number Publication Date
CN103261161A CN103261161A (zh) 2013-08-21
CN103261161B true CN103261161B (zh) 2016-04-27

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CN201180052042.4A Expired - Fee Related CN103261161B (zh) 2010-09-01 2011-08-31 凝血因子Xa抑制剂的结晶形式

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Country Link
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
US20150224091A1 (en) * 2011-08-31 2015-08-13 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
TWI686904B (zh) * 2012-03-16 2020-03-01 美商樂仕特拉公司 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
CN113905715B (zh) 2019-06-28 2025-04-15 宝洁公司 光增强处理方法

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CN101304971A (zh) * 2005-11-08 2008-11-12 米伦纽姆医药公司 Xa因子抑制剂n-(5-氯-2-吡啶基)-2-[[4-[(二甲氨基)亚氨基甲基]苯甲酰基]氨基]-5-甲氧基-苯甲酰胺的医药盐和多晶型
CN101686959A (zh) * 2007-05-02 2010-03-31 波托拉医药品公司 作为血小板adp受体抑制剂的化合物的组合疗法
WO2010056765A2 (en) * 2008-11-14 2010-05-20 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents

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BRPI0809655B8 (pt) 2007-04-13 2021-05-25 Millennium Pharm Inc uso de um composto e um agente terapêutico,composição farmacêutica,e,kit
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CN101304971A (zh) * 2005-11-08 2008-11-12 米伦纽姆医药公司 Xa因子抑制剂n-(5-氯-2-吡啶基)-2-[[4-[(二甲氨基)亚氨基甲基]苯甲酰基]氨基]-5-甲氧基-苯甲酰胺的医药盐和多晶型
CN101686959A (zh) * 2007-05-02 2010-03-31 波托拉医药品公司 作为血小板adp受体抑制剂的化合物的组合疗法
WO2010056765A2 (en) * 2008-11-14 2010-05-20 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents

Also Published As

Publication number Publication date
CA2810004C (en) 2019-09-10
US8946269B2 (en) 2015-02-03
JP2018024709A (ja) 2018-02-15
AU2011295909B2 (en) 2015-05-21
US20120071519A1 (en) 2012-03-22
JP2015232046A (ja) 2015-12-24
AR082804A1 (es) 2013-01-09
EP2611779A1 (en) 2013-07-10
CA2810004A1 (en) 2012-03-08
EP2611779B1 (en) 2016-08-10
JP2013536864A (ja) 2013-09-26
TW201221128A (en) 2012-06-01
NZ608442A (en) 2015-04-24
IL224698A (en) 2017-01-31
AU2011295909A1 (en) 2013-04-04
ES2603084T3 (es) 2017-02-23
CN103261161A (zh) 2013-08-21
WO2012031017A1 (en) 2012-03-08
JP2019135258A (ja) 2019-08-15
PT2611779T (pt) 2016-11-21

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Granted publication date: 20160427

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CF01 Termination of patent right due to non-payment of annual fee