BRPI1007768A2 - processo para a preparação de riv aroxabano e seus intermediários. - Google Patents

processo para a preparação de riv aroxabano e seus intermediários.

Info

Publication number
BRPI1007768A2
BRPI1007768A2 BRPI1007768A BRPI1007768A BRPI1007768A2 BR PI1007768 A2 BRPI1007768 A2 BR PI1007768A2 BR PI1007768 A BRPI1007768 A BR PI1007768A BR PI1007768 A BRPI1007768 A BR PI1007768A BR PI1007768 A2 BRPI1007768 A2 BR PI1007768A2
Authority
BR
Brazil
Prior art keywords
aroxaban
riv
intermediates
preparation
riv aroxaban
Prior art date
Application number
BRPI1007768A
Other languages
English (en)
Inventor
Weeratunga Gamini
Bodhuri Prabhudas
Original Assignee
Apotex Pharmachem 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 Apotex Pharmachem Inc filed Critical Apotex Pharmachem Inc
Publication of BRPI1007768A2 publication Critical patent/BRPI1007768A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
BRPI1007768A 2009-04-28 2010-04-28 processo para a preparação de riv aroxabano e seus intermediários. BRPI1007768A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12/431,272 US7816355B1 (en) 2009-04-28 2009-04-28 Processes for the preparation of rivaroxaban and intermediates thereof
PCT/CA2010/000656 WO2010124385A1 (en) 2009-04-28 2010-04-28 Processes for the preparation of rivaroxaban and intermediates thereof

Publications (1)

Publication Number Publication Date
BRPI1007768A2 true BRPI1007768A2 (pt) 2018-03-06

Family

ID=42941191

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1007768A BRPI1007768A2 (pt) 2009-04-28 2010-04-28 processo para a preparação de riv aroxabano e seus intermediários.

Country Status (12)

Country Link
US (2) US7816355B1 (pt)
EP (1) EP2424847B1 (pt)
JP (1) JP2012525337A (pt)
KR (1) KR20120104077A (pt)
CN (1) CN102844309A (pt)
AU (1) AU2010242496B2 (pt)
BR (1) BRPI1007768A2 (pt)
CA (1) CA2759828C (pt)
IL (1) IL215999A (pt)
MX (1) MX2011011328A (pt)
NZ (1) NZ595942A (pt)
WO (1) WO2010124385A1 (pt)

Families Citing this family (32)

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Publication number Priority date Publication date Assignee Title
AU2011300365A1 (en) * 2010-09-07 2013-05-02 Symed Labs Limited Processes for the preparation of 4-{4-[5(S)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl} morpholin-3-one
WO2012051692A1 (en) * 2010-10-18 2012-04-26 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
CN104693139B (zh) * 2011-01-07 2017-04-19 浙江九洲药业股份有限公司 一种合成利伐沙班中间体的新工艺
CN102584738B (zh) * 2011-01-07 2015-04-29 浙江九洲药业股份有限公司 一种合成利伐沙班中间体的工艺
US9221771B2 (en) * 2011-04-11 2015-12-29 Sandoz Ag Method for the preparation of substituted oxazolidinones
UA114601C2 (uk) * 2011-05-06 2017-07-10 Егіш Дьйодьсердьяр Нільваношан Мюкеде Ресвеньтаршашаг Спосіб одержання ривароксабану та проміжних сполук, які одержано в даному способі
ES2395304B1 (es) 2011-05-20 2014-01-16 Interquim, S.A. Procedimiento de obtención de una tiofen-2-carboxamida.
CN102827154B (zh) 2011-06-14 2015-04-22 上海科胜药物研发有限公司 一种合成利伐沙班中间体4-{4-[(5s)-5-(氨基甲基)-2-氧代-1,3-恶唑烷-3-基]苯基}吗啉-3-酮的方法
WO2013105100A1 (en) * 2012-01-09 2013-07-18 Symed Labs Limited Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide and intermediates thereof
CZ2012111A3 (cs) * 2012-02-16 2013-08-28 Zentiva, K.S. Zpusob prípravy rivaroxabanu zalozený na vyuzití (S)-epichlorhydrinu
CN103288814B (zh) 2012-02-24 2016-07-06 国药集团国瑞药业有限公司 一种利伐沙班中间体的制备方法
JP2015514114A (ja) * 2012-04-06 2015-05-18 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ リバーロキサバンを調製するためのプロセス
EP2844654B1 (en) 2012-05-02 2021-03-10 Symed Labs Limited Improved process for preparing rivaroxaban using novel intermediates
CN102702186B (zh) * 2012-06-20 2014-11-19 安润医药科技（苏州）有限公司 利伐沙班的合成方法
CN102786516B (zh) * 2012-08-21 2014-10-01 湖南师范大学 一种利伐沙班的合成方法
HK1217101A1 (zh) 2012-12-26 2016-12-23 Wanbury有限公司 取代的恶唑烷酮类的醛衍生物
ES2610020T3 (es) 2012-12-26 2017-04-25 Wanbury Limited Producto intermedio de rivaroxabán y preparación del mismo
IN2013MU01113A (pt) 2013-03-25 2015-06-19 Glenmark Generics Ltd
CN104098556B (zh) * 2013-04-09 2019-01-08 浙江九洲药物科技有限公司 一种利伐沙班的合成工艺
CN104370854B (zh) * 2013-08-12 2016-07-06 四川大学 3-卤-2-羟基丙基-1-酰基苯胺类化合物其制备方法和用途
WO2015026761A1 (en) 2013-08-19 2015-02-26 Amneal Pharmaceuticals Llc A process for the preparation of rivaroxaban
CN104447726B (zh) * 2013-09-18 2017-10-10 深圳翰宇药业股份有限公司 一种利伐沙班的制备方法
IN2014MU00072A (pt) 2014-01-08 2015-08-21 Wockhardt Ltd
IN2014CH00290A (pt) 2014-01-23 2015-08-14 Symed Labs Ltd
CN103804315B (zh) * 2014-02-20 2015-12-09 四川大学 一种5-氨甲基噁唑烷酮类化合物的制备方法
CN104860904B (zh) * 2014-02-20 2016-08-17 四川大学 N-环氧丙基-n-酰基苯胺类化合物其制备方法和用途
CN103951661B (zh) * 2014-04-28 2017-06-23 南京斯贝源医药科技有限公司 一种利伐沙班的制备方法
CN104844588B (zh) * 2015-03-24 2018-08-24 辽宁上药好护士药业（集团）有限公司 一种利伐沙班相关物质二胺的合成方法
CN104833740A (zh) * 2015-05-13 2015-08-12 成都百裕科技制药有限公司 利伐沙班中间体的高效液相色谱检测方法
WO2016199027A1 (en) * 2015-06-08 2016-12-15 Mehta Api Pvt. Ltd. An improved process for preparation of rivaroxaban
CN105130976A (zh) * 2015-08-26 2015-12-09 浙江车头制药股份有限公司 一种利伐沙班中间体的合成方法
CN108690010A (zh) * 2018-06-29 2018-10-23 苏州中联化学制药有限公司 利伐沙班的制备工艺

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Publication number Priority date Publication date Assignee Title
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10300111A1 (de) 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid
DE10342570A1 (de) * 2003-09-15 2005-04-14 Bayer Healthcare Ag Verfahren zur Herstellung von 4-(4-Aminophenyl)-3-morpholinon
DE10355461A1 (de) * 2003-11-27 2005-06-23 Bayer Healthcare Ag Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung
DE102004002044A1 (de) * 2004-01-15 2005-08-04 Bayer Healthcare Ag Herstellverfahren
DE102004062475A1 (de) * 2004-12-24 2006-07-06 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit modifizierter Freisetzung
EP1685841A1 (en) * 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention and treatment of thromboembolic disorders
DE102005047561A1 (de) 2005-10-04 2007-04-05 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung
CA2823159C (en) 2005-10-04 2014-10-21 Bayer Intellectual Property Gmbh Polymorphic form of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide
DE102005047564A1 (de) * 2005-10-04 2007-05-31 Bayer Healthcare Ag Amorphe Form von 5-Chlor-N-({(5S)2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl)-methyl)-2-thiophencarboxamid
DE102005048824A1 (de) 2005-10-10 2007-04-12 Bayer Healthcare Ag Behandlung und Prophylaxe von Mikroangiopathien
DE102006007146A1 (de) 2006-02-16 2007-08-23 Bayer Healthcare Ag Aminoacyl-Prodrugs
DE102006039589A1 (de) 2006-08-24 2008-03-06 Bayer Healthcare Ag Aminoacyl-Prodrugs II
DE102007018662A1 (de) 2007-04-20 2008-10-23 Bayer Healthcare Ag Oxazolidinone zur Behandlung und Prophylaxe von pulmonaler Hypertonie
DE102007032345A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Aminoacyl-Prodrugs
EP2190841B1 (en) 2007-08-14 2013-05-15 Concert Pharmaceuticals Inc. Substituted oxazolidinone derivatives
US20100168111A1 (en) 2008-12-31 2010-07-01 Apotex Pharmachem Inc. Polymorphic form of 5 chloro n {[(5s) 2 oxo 3 [4 (3 oxomorpholin 4 yl)phenyl]oxa-zolidin 5 yl]-methyl}thiophene 2 carboxamide

Also Published As

Publication number Publication date
US20100273798A1 (en) 2010-10-28
CN102844309A (zh) 2012-12-26
IL215999A (en) 2017-01-31
NZ595942A (en) 2013-11-29
CA2759828C (en) 2018-08-21
MX2011011328A (es) 2012-01-20
KR20120104077A (ko) 2012-09-20
CA2759828A1 (en) 2010-11-04
JP2012525337A (ja) 2012-10-22
US8101609B2 (en) 2012-01-24
AU2010242496B2 (en) 2015-08-27
US20100273790A1 (en) 2010-10-28
EP2424847A1 (en) 2012-03-07
WO2010124385A1 (en) 2010-11-04
EP2424847B1 (en) 2016-04-06
US7816355B1 (en) 2010-10-19
IL215999A0 (en) 2012-01-31
EP2424847A4 (en) 2012-10-03
AU2010242496A1 (en) 2011-11-17

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]