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AR082804A1 - Formas cristalinas de un inhibidor del factor xa - Google Patents

Formas cristalinas de un inhibidor del factor xa

Info

Publication number
AR082804A1
AR082804A1 ARP110103159A ARP110103159A AR082804A1 AR 082804 A1 AR082804 A1 AR 082804A1 AR P110103159 A ARP110103159 A AR P110103159A AR P110103159 A ARP110103159 A AR P110103159A AR 082804 A1 AR082804 A1 AR 082804A1
Authority
AR
Argentina
Prior art keywords
degrees
crystalline form
crystal forms
factor inhibitor
betrixaban maleate
Prior art date
Application number
ARP110103159A
Other languages
English (en)
Original Assignee
Portola Pharm Inc
Merck Sharp & Dohme
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 & Dohme filed Critical Portola Pharm Inc
Publication of AR082804A1 publication Critical patent/AR082804A1/es

Links

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

Landscapes

  • 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)

Abstract

La presente proporciona formas cristalinas de una sal maleato de betrixaban, composiciones y métodos de preparación o uso de las mismas.Reivindicación 1: Una forma cristalina de maleato de betrixaban que es la Forma II. Reivindicación 2: La forma cristalina de acuerdo con la reivindicación 1, que tiene un patrón de difracción de polvo de rayos X que tiene por lo menos las siguientes posiciones de picos característicos aproximados 5,0, 9,7, 10,1, 15,3, 17,5 y 19,6 grados 2q (cada uno ± 0,1 grados 2q). Reivindicación 10: Una forma cristalina de maleato de betrixaban, la cual es la Forma III. Reivindicación 11: La forma cristalina de acuerdo con la reivindicación 10, que tiene un patrón de difracción de polvo de rayos X que tiene por lo menos las siguientes posiciones de picos característicos aproximados 2,2, 4,9, 10,0, 15,1, 17,4, y 22,4 grados 2q (cada uno ± 0,1 grados 2q).
ARP110103159A 2010-09-01 2011-08-30 Formas cristalinas de un inhibidor del factor xa AR082804A1 (es)

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
AR082804A1 true AR082804A1 (es) 2013-01-09

Family

ID=45773260

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103159A AR082804A1 (es) 2010-09-01 2011-08-30 Formas cristalinas de un inhibidor del factor xa

Country Status (13)

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

Families Citing this family (17)

* 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
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
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
CN113905715A (zh) 2019-06-28 2022-01-07 宝洁公司 光增强处理方法

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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
EP1248869A2 (en) * 2000-01-07 2002-10-16 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
US6376515B2 (en) 2000-02-29 2002-04-23 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor Xa
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JP5227178B2 (ja) * 2005-11-08 2013-07-03 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 Ｎ−（５−クロロ−２−ピリジニル）−２−［［４−［（ジメチルアミノ）イミノメチル］ベンゾイル］アミノ］−５−メトキシ−ベンズアミド、第Ｘａ因子阻害剤の薬学的な塩および多形体
MX2008014193A (es) 2006-05-05 2009-03-31 Millennium Pharm Inc Inhibidores del factor xa.
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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

Also Published As

Publication number Publication date
ES2603084T3 (es) 2017-02-23
US20120071519A1 (en) 2012-03-22
PT2611779T (pt) 2016-11-21
EP2611779A1 (en) 2013-07-10
JP2019135258A (ja) 2019-08-15
CN103261161A (zh) 2013-08-21
JP2015232046A (ja) 2015-12-24
US8946269B2 (en) 2015-02-03
AU2011295909A1 (en) 2013-04-04
TW201221128A (en) 2012-06-01
CA2810004C (en) 2019-09-10
JP2013536864A (ja) 2013-09-26
JP2018024709A (ja) 2018-02-15
EP2611779B1 (en) 2016-08-10
CA2810004A1 (en) 2012-03-08
AU2011295909B2 (en) 2015-05-21
CN103261161B (zh) 2016-04-27
WO2012031017A1 (en) 2012-03-08
IL224698A (en) 2017-01-31
NZ608442A (en) 2015-04-24

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