NZ608442A - Crystalline forms of a factor xa inhibitor - Google Patents

Crystalline forms of a factor xa inhibitor

Info

Publication number
NZ608442A
NZ608442A NZ60844211A NZ60844211A NZ608442A NZ 608442 A NZ608442 A NZ 608442A NZ 60844211 A NZ60844211 A NZ 60844211A NZ 60844211 A NZ60844211 A NZ 60844211A NZ 608442 A NZ608442 A NZ 608442A
Authority
NZ
New Zealand
Prior art keywords
crystalline forms
inhibitor
factor
betrixaban
maleate
Prior art date
Application number
NZ60844211A
Other languages
English (en)
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
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 filed Critical Portola Pharm Inc
Publication of NZ608442A publication Critical patent/NZ608442A/en

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)
  • 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)
NZ60844211A 2010-09-01 2011-08-31 Crystalline forms of a factor xa inhibitor NZ608442A (en)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
NZ608442A true NZ608442A (en) 2015-04-24

Family

ID=45773260

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ60844211A NZ608442A (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)

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
WO2013033370A1 (en) 2011-08-31 2013-03-07 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
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
WO2020264076A1 (en) 2019-06-28 2020-12-30 The Procter & Gamble Company Light augmented treatment method

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
IL150524A0 (en) * 2000-01-07 2003-02-12 Transform Pharmaceuticals Inc High-throughput formation, identification, and analysis of diverse solid-forms
WO2001064642A2 (en) 2000-02-29 2001-09-07 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
KR101195801B1 (ko) 2004-06-18 2012-11-05 밀레니엄 파머슈티컬스 인코퍼레이티드 Ｘａ 인자 억제제
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
CN101304971B (zh) 2005-11-08 2011-09-07 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
EP2016072B1 (en) 2006-05-05 2014-07-16 Millennium Pharmaceuticals, 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
EP2077995B1 (en) 2006-11-02 2012-02-08 Millennium Pharmaceuticals, Inc. Methods of synthesizing pharmaceutical salts of a factor xa inhibitor
PT2101760E (pt) 2006-12-08 2013-05-07 Millennium Pharm Inc Formulações de dose unitária e métodos de tratamento da trombose com um inibidor oral do fator xa
CA2674924A1 (en) 2007-01-05 2008-07-17 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
EP2155195B1 (en) 2007-04-13 2014-07-16 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
KR101509829B1 (ko) * 2007-05-02 2015-04-06 포톨라 파마슈티컬스, 인코포레이티드 혈소판 ａｄｐ 수용체 억제제로 작용하는 화합물을 이용한 병용요법
KR102069498B1 (ko) 2007-09-28 2020-01-23 포톨라 파마슈티컬스, 인코포레이티드 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법
CA2743496C (en) * 2008-11-14 2018-03-27 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

Also Published As

Publication number Publication date
US20120071519A1 (en) 2012-03-22
IL224698A (en) 2017-01-31
JP2013536864A (ja) 2013-09-26
CN103261161B (zh) 2016-04-27
WO2012031017A1 (en) 2012-03-08
JP2019135258A (ja) 2019-08-15
CA2810004C (en) 2019-09-10
JP2015232046A (ja) 2015-12-24
AU2011295909B2 (en) 2015-05-21
CN103261161A (zh) 2013-08-21
EP2611779A1 (en) 2013-07-10
JP2018024709A (ja) 2018-02-15
PT2611779T (pt) 2016-11-21
CA2810004A1 (en) 2012-03-08
US8946269B2 (en) 2015-02-03
EP2611779B1 (en) 2016-08-10
ES2603084T3 (es) 2017-02-23
TW201221128A (en) 2012-06-01
AR082804A1 (es) 2013-01-09
AU2011295909A1 (en) 2013-04-04

Similar Documents

Publication Publication Date Title
LTC2618831I2 (lt) Makrocikliniai iš prolino gauti HCV serino proteazės inhibitoriai
MX345259B (es) Inhibidores de serina proteasas similares a tripsina, y su preparación y uso.
MX2011011272A (es) Procesos e intermediarios.
AU2012214029A8 (en) Rorgammat inhibitors
MX344025B (es) Inhibidores de proteínas quinasas.
MX338327B (es) Inhibidores de cdk.
TNSN07466A1 (en) Formulation of a thienopyridine platelet aggregation inhibitor
MX2013005826A (es) Benzoxazepinas como inhibidores de fosfatidilinositol 3-cinasa/objetivo de rapamicina en mamiferos (p13k/mtor) y metodos de uso y fabricacion.
MY160675A (en) Composition and method for polishing polysilicon
MY150542A (en) Cmet inhibitors
NZ594403A (en) Amorphous salt of a macrocyclic inhibitor of hcv
WO2012071509A3 (en) Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture
GB0907698D0 (en) Method of modifying serine protease inhibitors
IN2012DN01968A (enExample)
MX2011006764A (es) Procedimiento y compuestos intermedios para preparar un inhibidor de proteasa macrociclico del vhc.
MY155330A (en) Methods for salt production
MX2012007341A (es) Inhibidores de proteasoma y procesos para su preparacion, purificacion y uso.
CR20140128A (es) Inhibidores de la enzima activadora de nedd 8
MX2013005819A (es) Benzoxazepinas como inhibidores de 3-cinasa/objetivo mamífero de rapamicina (pi3k/mtor) metodos de uso y fabricacion.
TW200700064A (en) Novel compounds
MX359399B (es) Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
EA201200017A1 (ru) Новая кристаллическая форма пемироласта
MX2013005825A (es) Benzoxazepinas como inhibidores de objetivo de rapamicina en mamiferos (mtor) y metodos de uso y fabricacion.
GB0809068D0 (en) The use of serine protease inhibitors
MX2009001150A (es) Aditivo que contiene titanio.

Legal Events

Date Code Title Description
PSEA Patent sealed
RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 31 AUG 2016 BY DENNEMEYER + CO.

Effective date: 20150811

RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 31 AUG 2017 BY DENNEMEYER + CO.

Effective date: 20160722

RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 31 AUG 2018 BY DENNEMEYER + CO

Effective date: 20170726

RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 31 AUG 2019 BY DENNEMEYER + CO

Effective date: 20180803

RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 31 AUG 2020 BY DENNEMEYER + CO.

Effective date: 20190719

LAPS Patent lapsed