MA28290A1 - Procede de preparation - Google Patents

Procede de preparation

Info

Publication number
MA28290A1
MA28290A1 MA29179A MA29179A MA28290A1 MA 28290 A1 MA28290 A1 MA 28290A1 MA 29179 A MA29179 A MA 29179A MA 29179 A MA29179 A MA 29179A MA 28290 A1 MA28290 A1 MA 28290A1
Authority
MA
Morocco
Prior art keywords
preparation
oxo
thiophenecarboxamide
oxiranylmethyl
morpholinone
Prior art date
Application number
MA29179A
Other languages
English (en)
Inventor
Mathias Berwe
Christian Thomas
Joachim Rehse
Dirk Grotjohann
Original Assignee
Bayer Schering Pharma Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34716548&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA28290(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of MA28290A1 publication Critical patent/MA28290A1/fr

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
    • C07D413/14—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61P9/10—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Epidemiology (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)

Abstract

Procédé de préparation La présente invention se rapporte à un procédé de préparation du 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]-l,3-oxazolidine-5-yl}méthyl)-2-thiophènecarboxamide à partir du 2-[(2S)-2-oxiranylméthyl]-lH-isoindole-l,3(2H)-dione, de la 4-(4-aminophényl)-3-morpholinone et du chlorure de 5-chlorothiophène-2-carbonyl.
MA29179A 2004-01-15 2006-07-10 Procede de preparation MA28290A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004002044A DE102004002044A1 (de) 2004-01-15 2004-01-15 Herstellverfahren

Publications (1)

Publication Number Publication Date
MA28290A1 true MA28290A1 (fr) 2006-11-01

Family

ID=34716548

Family Applications (1)

Application Number Title Priority Date Filing Date
MA29179A MA28290A1 (fr) 2004-01-15 2006-07-10 Procede de preparation

Country Status (32)

Country Link
US (1) US7351823B2 (fr)
EP (1) EP1720866B1 (fr)
JP (2) JP5311742B2 (fr)
KR (1) KR20130004257A (fr)
CN (1) CN1906191B (fr)
AR (1) AR047389A1 (fr)
AT (1) ATE518856T1 (fr)
AU (1) AU2004313694B2 (fr)
BR (1) BRPI0418405B8 (fr)
CA (1) CA2553237C (fr)
CY (1) CY1112565T1 (fr)
DE (1) DE102004002044A1 (fr)
DK (1) DK1720866T3 (fr)
EC (1) ECSP066703A (fr)
ES (1) ES2369140T3 (fr)
GT (1) GT200400277A (fr)
HN (1) HN2005000016A (fr)
HR (1) HRP20110796T1 (fr)
IL (1) IL176767A (fr)
MA (1) MA28290A1 (fr)
MY (1) MY138944A (fr)
NO (1) NO335553B1 (fr)
NZ (1) NZ548506A (fr)
PE (1) PE20050763A1 (fr)
PL (1) PL1720866T3 (fr)
PT (1) PT1720866E (fr)
RU (1) RU2383540C2 (fr)
SI (1) SI1720866T1 (fr)
TW (1) TWI340137B (fr)
UY (1) UY28718A1 (fr)
WO (1) WO2005068456A1 (fr)
ZA (1) ZA200605747B (fr)

Families Citing this family (82)

* Cited by examiner, † Cited by third party
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DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10129725A1 (de) * 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
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
DE10355461A1 (de) 2003-11-27 2005-06-23 Bayer Healthcare Ag Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung
DE102004062475A1 (de) * 2004-12-24 2006-07-06 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit modifizierter Freisetzung
EP1685841A1 (fr) 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention et traitement de troubles thromboemboliques
DE102005045518A1 (de) 2005-09-23 2007-03-29 Bayer Healthcare Ag 2-Aminoethoxyessigsäure-Derivate und ihre Verwendung
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
DE102005047558A1 (de) * 2005-10-04 2008-02-07 Bayer Healthcare Ag Kombinationstherapie substituierter Oxazolidinone zur Prophylaxe und Behandlung von cerebralen Durchblutungsstörungen
DE102005047561A1 (de) 2005-10-04 2007-04-05 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung
PT1934208E (pt) * 2005-10-04 2011-06-01 Bayer Schering Pharma Ag Nova forma polimorfa de 5-cloro-n-({(5s)-2-oxo-3-[4-(3- oxo-4-morfolinil)-fenil]-1,3-oxazolidin-5-il}-metil)-2- tiofenocarboxamida
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
DE102006051625A1 (de) * 2006-11-02 2008-05-08 Bayer Materialscience Ag Kombinationstherapie substituierter Oxazolidinone
DE102007028407A1 (de) * 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
DE102007028319A1 (de) * 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
WO2009018807A1 (fr) * 2007-08-06 2009-02-12 Schebo Biotech Ag Oxazolidinones utilisées comme inhibiteurs du facteur xa, procédé pour leur production et leur utilisation thérapeutique
US8706950B2 (en) 2008-03-01 2014-04-22 Kabushiki Kaisha Toshiba Memory system
DE102008028071A1 (de) 2008-06-12 2009-12-17 Bayer Schering Pharma Aktiengesellschaft Neue Cokristall-Verbindung von Rivaroxaban und Malonsäure
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
US8435989B2 (en) * 2009-04-28 2013-05-07 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
US7816355B1 (en) 2009-04-28 2010-10-19 Apotex Pharmachem Inc Processes for the preparation of rivaroxaban and intermediates thereof
US8309547B2 (en) * 2009-04-28 2012-11-13 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
WO2011012321A1 (fr) 2009-07-31 2011-02-03 Krka, D.D., Novo Mesto Méthodes de cristallisation de rivaroxaban
WO2011080341A1 (fr) * 2010-01-04 2011-07-07 Enantia, S.L. Procédé de préparation de rivaroxaban et ses intermédiaires
DE102010028362A1 (de) 2010-04-29 2011-11-03 Bayer Schering Pharma Aktiengesellschaft Herstellverfahren
EP2388260A1 (fr) 2010-05-21 2011-11-23 Archimica GmbH Procédé de fabrication pour un inhibiteur d'un facteur de coagulation sanguine
CN102311400A (zh) * 2010-06-29 2012-01-11 翔真生物科技股份有限公司 制备5-左旋-氨甲基-3-芳基-2-恶唑烷酮类的方法
EP2404920A1 (fr) 2010-07-06 2012-01-11 Sandoz AG Form cristalline de Rivaroxaban dihydrate
US20130253187A1 (en) 2010-09-14 2013-09-26 Medichem, S.A. Process for Determining the Suitability for Distribution of a Batch of Thiophene-2-Carboxamide Derivative
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CA2815063C (fr) 2010-10-18 2016-11-22 Apotex Pharmachem Inc. Procedes de preparation de rivaroxaban et ses intermediaires
GEP20156397B (en) * 2011-05-06 2015-11-10 Egis Gyógyszergyár Nyilvánosan Működő Részvénytársaság Process for the preparation of a rivaroxaban and intermediates formed in said process
WO2012156983A1 (fr) * 2011-05-16 2012-11-22 Symed Labs Limited Procédés pour la préparation de 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]-1,3-oxazolidin-5-yl}méthyl)-2-thiophènecarboxamide
ES2395304B1 (es) 2011-05-20 2014-01-16 Interquim, S.A. Procedimiento de obtención de una tiofen-2-carboxamida.
CN102250076A (zh) * 2011-05-27 2011-11-23 横店集团家园化工有限公司 一种利伐沙班中间体及利伐沙班的制备方法
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
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WO2013053739A1 (fr) 2011-10-10 2013-04-18 Laboratorios Lesvi, S. L. Procédé de préparation d'inhibiteurs du facteur xa
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CN102757424B (zh) * 2012-07-09 2014-10-15 云南大学 2-苄基取代苯并呋喃—咪唑盐类化合物及其制备方法
CN102746288B (zh) * 2012-07-24 2015-04-08 常州制药厂有限公司 一种抗凝血药及其关键中间体的制备方法
WO2014020458A1 (fr) * 2012-08-01 2014-02-06 Alembic Pharmaceuticals Limited Procédé amélioré de préparation du rivaroxaban
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
CN103833724A (zh) * 2012-11-20 2014-06-04 上海医药工业研究院 一种5-氯噻吩-2-甲酰氯的制备方法
CN103864771A (zh) * 2012-12-13 2014-06-18 北京京卫信康医药科技发展有限公司 一种利伐沙班的制备方法
CN103864772A (zh) * 2012-12-13 2014-06-18 北京京卫信康医药科技发展有限公司 一种利伐沙班及其中间体的制备方法
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PT2895176T (pt) 2012-12-26 2017-01-27 Wanbury Ltd Intermediário de rivaroxabano e a sua preparação
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CN104109158A (zh) * 2013-04-16 2014-10-22 上海医药工业研究院 一种纯化利伐沙班的方法
CN103275061A (zh) * 2013-06-04 2013-09-04 上海同昌生物医药科技有限公司 一种生产5-氯噻吩-2-羧酸的方法
CN103351385A (zh) * 2013-06-28 2013-10-16 浙江燎原药业有限公司 一种利伐沙班中间体的制备方法
CN103709116B (zh) * 2013-12-10 2015-09-23 四川大学 一种4-(4-烷氧羰氨基)苯基-3-吗啉酮的制备方法
CN103724336B (zh) * 2013-12-24 2015-10-21 悦康药业集团有限公司 一种新型抗凝血药物的合成方法
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CN105085370B (zh) * 2014-04-22 2017-04-12 北大方正集团有限公司 (s)‑1‑卤代‑2‑[2‑(1,3‑二氧异吲哚)基]乙基氯甲酸酯及其制备方法
WO2015188787A1 (fr) * 2014-06-14 2015-12-17 Sunshine Lake Pharma Co., Ltd. Procédé de préparation de composé d'oxazolidinone et intermédiaires de celui-ci
CN104086539A (zh) * 2014-07-17 2014-10-08 天津炜捷制药有限公司 一种利伐沙班的制备方法
CN104211693B (zh) * 2014-08-07 2017-02-22 成都百裕制药股份有限公司 一种利伐沙班晶型及其制备方法与用途
CN104211694A (zh) * 2014-08-14 2014-12-17 广东东阳光药业有限公司 一种改进的制备Xa因子抑制剂的方法
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EP3209661B1 (fr) 2014-10-22 2021-02-17 Zaklady Farmaceutyczne Polpharma SA Procédé de préparation d'un polymorphe de rivaroxaban
CN104807934B (zh) * 2015-04-30 2017-01-18 成都百裕制药股份有限公司 异吲哚二酮类化合物的正相高效液相色谱检测方法
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
CN105440028B (zh) * 2015-12-07 2018-03-13 石家庄康贺威药业有限公司 一种利伐沙班化合物及其制备方法
CN106008490B (zh) * 2016-01-11 2019-01-04 南京生命能科技开发有限公司 一种利伐沙班的新晶体及其制备方法
CN106977507A (zh) * 2017-04-21 2017-07-25 上海华源医药科技发展有限公司 一种利伐沙班的制备方法
CN109553611A (zh) * 2017-09-23 2019-04-02 齐鲁制药有限公司 利伐沙班中间体的制备方法和用途
JP7205529B2 (ja) * 2018-02-26 2023-01-17 住友化学株式会社 オキサゾリジノン化合物の製造方法
JP7339754B2 (ja) * 2019-03-27 2023-09-06 ダイト株式会社 中間体の製造方法
CN112521380A (zh) * 2020-12-14 2021-03-19 哈尔滨珍宝制药有限公司 一种利伐沙班中间体a的合成方法及其在制备利伐沙班中的应用
CN117500806A (zh) * 2021-05-28 2024-02-02 默沙东有限责任公司 Btk抑制剂及其中间体的合成
BR112023024807A2 (pt) * 2021-05-28 2024-02-15 Merck Sharp & Dohme Llc Síntese de inibidor de btk e intermediários do mesmo
EP4201933A1 (fr) * 2021-12-23 2023-06-28 Zaklady Farmaceutyczne Polpharma S.A. Processus de cristallisation de rivaroxaban

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19962924A1 (de) * 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10129725A1 (de) * 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
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

Also Published As

Publication number Publication date
IL176767A0 (en) 2006-10-31
JP2012097106A (ja) 2012-05-24
IL176767A (en) 2011-04-28
CY1112565T1 (el) 2016-02-10
CA2553237A1 (fr) 2005-07-28
CN1906191B (zh) 2010-05-26
PL1720866T3 (pl) 2012-01-31
CA2553237C (fr) 2012-04-17
HK1103722A1 (en) 2007-12-28
RU2006129341A (ru) 2008-02-20
PE20050763A1 (es) 2005-12-02
MY138944A (en) 2009-08-28
ECSP066703A (es) 2006-10-31
AU2004313694B2 (en) 2011-06-02
GT200400277A (es) 2005-08-18
PT1720866E (pt) 2011-10-12
AR047389A1 (es) 2006-01-18
DK1720866T3 (da) 2011-11-21
SI1720866T1 (sl) 2012-01-31
KR20130004257A (ko) 2013-01-09
BRPI0418405B8 (pt) 2021-05-25
RU2383540C2 (ru) 2010-03-10
TW200604195A (en) 2006-02-01
EP1720866B1 (fr) 2011-08-03
WO2005068456A1 (fr) 2005-07-28
BRPI0418405A (pt) 2007-05-15
BRPI0418405B1 (pt) 2018-03-13
EP1720866A1 (fr) 2006-11-15
CN1906191A (zh) 2007-01-31
ZA200605747B (en) 2007-10-31
NZ548506A (en) 2009-06-26
JP5311742B2 (ja) 2013-10-09
AU2004313694A1 (en) 2005-07-28
HRP20110796T1 (hr) 2011-12-31
NO20063677L (no) 2006-10-11
JP2007517816A (ja) 2007-07-05
HN2005000016A (es) 2009-06-01
US20050182055A1 (en) 2005-08-18
DE102004002044A1 (de) 2005-08-04
ATE518856T1 (de) 2011-08-15
TWI340137B (en) 2011-04-11
NO335553B1 (no) 2014-12-29
US7351823B2 (en) 2008-04-01
ES2369140T3 (es) 2011-11-25
UY28718A1 (es) 2005-08-31

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