AU2011295909B2 - Crystalline forms of a factor Xa inhibitor - Google Patents

Crystalline forms of a factor Xa inhibitor Download PDF

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Publication number
AU2011295909B2
AU2011295909B2 AU2011295909A AU2011295909A AU2011295909B2 AU 2011295909 B2 AU2011295909 B2 AU 2011295909B2 AU 2011295909 A AU2011295909 A AU 2011295909A AU 2011295909 A AU2011295909 A AU 2011295909A AU 2011295909 B2 AU2011295909 B2 AU 2011295909B2
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AU
Australia
Prior art keywords
crystalline form
thrombotic
betrixaban
stroke
water
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2011295909A
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English (en)
Other versions
AU2011295909A1 (en
Inventor
Itzia Zoraida Arroyo
Richard G. Ball
Vincent R. Capodanno
Liam Corcoran
Timothy K. Maher
Eric L. Margelefsky
Michael Mcnevin
Anjali Pandey
Robert M. Wenslow
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Portola Pharmaceuticals LLC
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Portola Pharmaceuticals LLC
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Filing date
Publication date
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Publication of AU2011295909A1 publication Critical patent/AU2011295909A1/en
Application granted granted Critical
Publication of AU2011295909B2 publication Critical patent/AU2011295909B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2011295909A 2010-09-01 2011-08-31 Crystalline forms of a factor Xa inhibitor Ceased AU2011295909B2 (en)

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
AU2011295909A1 AU2011295909A1 (en) 2013-04-04
AU2011295909B2 true AU2011295909B2 (en) 2015-05-21

Family

ID=45773260

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011295909A Ceased AU2011295909B2 (en) 2010-09-01 2011-08-31 Crystalline forms of a factor Xa inhibitor

Country Status (13)

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
TWI616987B (zh) * 2012-03-16 2018-03-01 樂仕特拉公司 光子材料中介層的方法及系統
US9200268B2 (en) 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US20140346397A1 (en) 2012-12-27 2014-11-27 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
EP3463352A4 (en) * 2016-06-02 2019-10-30 Dr. Reddy S Laboratories Limited POLYMORPH OF BETRIXABAN AND 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

Citations (1)

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Publication number Priority date Publication date Assignee Title
US7598276B2 (en) * 2005-11-08 2009-10-06 Millenium Pharmaceuticals, Inc. Pharmaceutical salts and polymorphs of a factor Xa inhibitor

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GB9226238D0 (en) 1992-12-16 1993-02-10 Scherer Ltd R P Encapsulation apparatus and process
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
SK9742002A3 (en) * 2000-01-07 2003-02-04 Transform Pharmaceuticals Inc High-throughput formation, identification, and analysis of diverse solid-forms
ES2254385T3 (es) 2000-02-29 2006-06-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
US6627646B2 (en) 2001-07-17 2003-09-30 Sepracor Inc. Norastemizole polymorphs
DE10322469A1 (de) 2003-05-19 2004-12-16 Bayer Healthcare Ag Heterocyclische Verbindungen
JP5020073B2 (ja) 2004-06-18 2012-09-05 ミレニアム ファーマシューティカルズ インク． 第Ｘａ因子阻害剤
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EA015942B1 (ru) 2006-05-05 2011-12-30 Милленниум Фамэсьютикэлс, Инк. Замещенные имидазолы, композиция на их основе, способ профилактики или лечения нежелательного тромбообразования с их помощью и способ ингибирования коагуляции образцов крови
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NZ599556A (en) 2007-05-02 2013-10-25 Portola Pharm Inc Combination therapy with a compound acting as a platelet adp receptor inhibitor
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EP2364165B1 (en) * 2008-11-14 2018-01-03 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
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US7598276B2 (en) * 2005-11-08 2009-10-06 Millenium Pharmaceuticals, Inc. Pharmaceutical salts and polymorphs of a factor Xa inhibitor

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Also Published As

Publication number Publication date
PT2611779T (pt) 2016-11-21
US8946269B2 (en) 2015-02-03
AR082804A1 (es) 2013-01-09
JP2013536864A (ja) 2013-09-26
CA2810004A1 (en) 2012-03-08
CN103261161A (zh) 2013-08-21
CA2810004C (en) 2019-09-10
ES2603084T3 (es) 2017-02-23
TW201221128A (en) 2012-06-01
CN103261161B (zh) 2016-04-27
EP2611779A1 (en) 2013-07-10
JP2018024709A (ja) 2018-02-15
JP2019135258A (ja) 2019-08-15
NZ608442A (en) 2015-04-24
US20120071519A1 (en) 2012-03-22
WO2012031017A1 (en) 2012-03-08
EP2611779B1 (en) 2016-08-10
IL224698A (en) 2017-01-31
JP2015232046A (ja) 2015-12-24
AU2011295909A1 (en) 2013-04-04

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired