TW201221128A - Crystalline forms of a factor Xa inhibitor - Google Patents

Crystalline forms of a factor Xa inhibitor Download PDF

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Publication number
TW201221128A
TW201221128A TW100131157A TW100131157A TW201221128A TW 201221128 A TW201221128 A TW 201221128A TW 100131157 A TW100131157 A TW 100131157A TW 100131157 A TW100131157 A TW 100131157A TW 201221128 A TW201221128 A TW 201221128A
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TW
Taiwan
Prior art keywords
crystalline form
stroke
doc
water
solvent
Prior art date
Application number
TW100131157A
Other languages
English (en)
Chinese (zh)
Inventor
Vincent R Capodanno
Liam Corcoran
Michael Mcnevin
Itzia Zoraida Arroyo
Robert M Wenslow
Richard G Ball
Eric L Margelefsky
Timothy K Maher
Anjali Pandey
Original Assignee
Portola Pharm Inc
Merck Sharp & Amp Dohme Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Portola Pharm Inc, Merck Sharp & Amp Dohme Corp filed Critical Portola Pharm Inc
Publication of TW201221128A publication Critical patent/TW201221128A/zh

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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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW100131157A 2010-09-01 2011-08-30 Crystalline forms of a factor Xa inhibitor TW201221128A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37933910P 2010-09-01 2010-09-01
US201161454396P 2011-03-18 2011-03-18

Publications (1)

Publication Number Publication Date
TW201221128A true TW201221128A (en) 2012-06-01

Family

ID=45773260

Family Applications (1)

Application Number Title Priority Date Filing Date
TW100131157A TW201221128A (en) 2010-09-01 2011-08-30 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)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (16)

* 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
WO2013033370A1 (en) 2011-08-31 2013-03-07 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
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
US20190300483A1 (en) * 2016-06-02 2019-10-03 Dr. Reddy's Laboratories Limited POLYMORPHS OF BETRlXABAN & 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

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
MXPA02006660A (es) * 2000-01-07 2002-12-13 Transform Pharmaceuticals Inc Formacion, identificacion y analisis de diversas formas solidas de alto rendimiento.
AU2001245353A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of 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
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
CN1968922A (zh) 2004-06-18 2007-05-23 米伦纽姆医药公司 因子xa抑制剂
KR101358574B1 (ko) * 2005-11-08 2014-02-04 밀레니엄 파머슈티컬스 인코퍼레이티드 Xa 인자 억제제, n­(5­클로로­2­피리디닐)­2­[[4­[(디메틸아미노)이미노메틸]벤조일]아미노]­5­메톡시­벤자마이드의 약제학적 염 및 다형체
TW200813017A (en) 2006-05-05 2008-03-16 Millennium Pharm Inc Factor XA inhibitors
US20080051578A1 (en) 2006-08-24 2008-02-28 Georg Dahmann Substituted biaryls, process for their manufacture and use thereof as medicaments
PT2404906E (pt) 2006-11-02 2015-11-02 Millennium Pharm Inc Métodos de sintetizar sais farmacêuticos de um inibidor de fator xa
CA2913963A1 (en) 2006-12-08 2008-06-19 Millenium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
EP2114930A2 (en) 2007-01-05 2009-11-11 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
AU2008239659B2 (en) 2007-04-13 2013-09-05 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
EP2586439A1 (en) * 2007-05-02 2013-05-01 Portola Pharmaceuticals, Inc. Combination therapy with a compound acting as a platelet ADP receptor inhibitor
SI2915564T1 (sl) 2007-09-28 2021-03-31 Alexion Pharmaceuticals, Inc. Antidoti za zaviralce dejavnika Ksa in postopki njihove uporabe
US8455439B2 (en) * 2008-11-14 2013-06-04 Portola Pharmaceuticals, Inc. Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
JP5766204B2 (ja) 2009-12-17 2015-08-19 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. 第Xa因子阻害剤の合成方法
AR082803A1 (es) 2010-09-01 2013-01-09 Portola Pharm Inc Metodos y formulaciones para el tratamiento de la trombosis con betrixaban y un inhibidor de la glicoproteina p

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
WO2012031017A1 (en) 2012-03-08
AR082804A1 (es) 2013-01-09
CA2810004C (en) 2019-09-10
CA2810004A1 (en) 2012-03-08
AU2011295909B2 (en) 2015-05-21
PT2611779T (pt) 2016-11-21
JP2015232046A (ja) 2015-12-24
ES2603084T3 (es) 2017-02-23
EP2611779A1 (en) 2013-07-10
AU2011295909A1 (en) 2013-04-04
JP2013536864A (ja) 2013-09-26
NZ608442A (en) 2015-04-24
CN103261161A (zh) 2013-08-21
CN103261161B (zh) 2016-04-27
US8946269B2 (en) 2015-02-03
JP2018024709A (ja) 2018-02-15
EP2611779B1 (en) 2016-08-10
JP2019135258A (ja) 2019-08-15
IL224698A (en) 2017-01-31
US20120071519A1 (en) 2012-03-22

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