MD4557C1 - Procedeu de obţinere a rivaroxabanului şi un compus intermediar utilizat în acest procedeu - Google Patents
Procedeu de obţinere a rivaroxabanului şi un compus intermediar utilizat în acest procedeuInfo
- Publication number
- MD4557C1 MD4557C1 MDA20130094A MD20130094A MD4557C1 MD 4557 C1 MD4557 C1 MD 4557C1 MD A20130094 A MDA20130094 A MD A20130094A MD 20130094 A MD20130094 A MD 20130094A MD 4557 C1 MD4557 C1 MD 4557C1
- Authority
- MD
- Moldova
- Prior art keywords
- rivaroxaban
- preparation
- oxo
- intermediate used
- relates
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- KGFYHTZWPPHNLQ-AWEZNQCLSA-N rivaroxaban Chemical compound S1C(Cl)=CC=C1C(=O)NC[C@@H]1OC(=O)N(C=2C=CC(=CC=2)N2C(COCC2)=O)C1 KGFYHTZWPPHNLQ-AWEZNQCLSA-N 0.000 title abstract 3
- 229960001148 rivaroxaban Drugs 0.000 title abstract 2
- 239000002050 international nonproprietary name Substances 0.000 abstract 2
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 208000031104 Arterial Occlusive disease Diseases 0.000 abstract 1
- 206010051113 Arterial restenosis Diseases 0.000 abstract 1
- 206010051055 Deep vein thrombosis Diseases 0.000 abstract 1
- 208000010378 Pulmonary Embolism Diseases 0.000 abstract 1
- 206010047249 Venous thrombosis Diseases 0.000 abstract 1
- 208000021328 arterial occlusion Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
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
-
- 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
- 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
- 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
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Invenţia se referă la un procedeu de obţinere a compusului farmaceutic activ 5-clor-N-({(5S)-2-oxo-3-[4-(3-oxo-morfolin-4-il)-fenil]-l,3-oxazolidin-5-il}-metil)tiofen-2-carboxamidei cu formula:având denumirea comună internaţională (INN) rivaroxaban, care poate fi utilizat în tratamentul infarctului miocardic, în tromboza venelor profunde, în angina pectorală, în ocluzia arterială, restenoza arterială şi în embolismul pulmonar.Invenţia se referă, de asemenea, la un compus intermediar, utilizat în acest procedeu.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
HU1100239A HU230984B1 (hu) | 2011-05-06 | 2011-05-06 | Új eljárás gyógyszerhatóanyag előállítására és az eljárás során keletkező intermedierek |
HU1100240A HU230985B1 (hu) | 2011-05-06 | 2011-05-06 | Új kapcsolási eljárás gyógyszerhatóanyag előállítására |
HU1100238A HU230961B1 (hu) | 2011-05-06 | 2011-05-06 | Új eljárás gyógyszerhatóanyag előállítására és az eljárás során keletkező intermedierek |
PCT/HU2012/000033 WO2012153155A1 (en) | 2011-05-06 | 2012-05-04 | Process for the preparation of a rivaroxaban and intermediates formed in said process |
Publications (3)
Publication Number | Publication Date |
---|---|
MD20130094A2 MD20130094A2 (ro) | 2014-04-30 |
MD4557B1 MD4557B1 (ro) | 2018-03-31 |
MD4557C1 true MD4557C1 (ro) | 2018-10-31 |
Family
ID=89990276
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MDA20130094A MD4557C1 (ro) | 2011-05-06 | 2012-05-04 | Procedeu de obţinere a rivaroxabanului şi un compus intermediar utilizat în acest procedeu |
Country Status (8)
Country | Link |
---|---|
US (1) | US9556163B2 (ro) |
EP (1) | EP2705028B1 (ro) |
JP (1) | JP6325978B2 (ro) |
EA (1) | EA024685B1 (ro) |
GE (1) | GEP20156397B (ro) |
MD (1) | MD4557C1 (ro) |
UA (1) | UA114601C2 (ro) |
WO (1) | WO2012153155A1 (ro) |
Families Citing this family (11)
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 |
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 |
HUE037188T2 (hu) | 2012-12-21 | 2018-08-28 | Farma Grs D O O | Eljárás rivaroxaban elõállítására |
US9394292B2 (en) | 2012-12-26 | 2016-07-19 | Wanbury Ltd. | Rivaroxaban intermediate and preparation thereof |
EP2897619A4 (en) | 2012-12-26 | 2016-08-17 | Wanbury Ltd | ALDEHYDE DERIVATIVE FROM SUBSTITUTED OXAZOLIDINONES |
CN103360380B (zh) * | 2013-03-13 | 2016-01-20 | 浙江天宇药业股份有限公司 | 一种利伐沙班的合成方法和利伐沙班的中间体及其制备 |
IN2014MU00072A (ro) | 2014-01-08 | 2015-08-21 | Wockhardt Ltd | |
US20170267669A1 (en) * | 2014-08-25 | 2017-09-21 | Cipla Limited | Process for the Preparation of Rivaroxaban |
CN104311545B (zh) * | 2014-09-29 | 2017-03-22 | 哈药集团制药总厂 | 一种利伐沙班关键中间体的制备方法 |
KR101811123B1 (ko) * | 2016-02-19 | 2017-12-20 | 일동제약(주) | 신규의 모르폴린 이인산염 및 이를 이용한 고순도 리바록사반의 제조방법 |
PL4073051T3 (pl) * | 2019-12-10 | 2024-05-20 | Eli Lilly And Company | Sposób i związek pośredni do wytwarzania oksetan-2-ylometanoaminy |
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DE3408327A1 (de) | 1984-03-07 | 1985-09-12 | Ludwig Heumann & Co GmbH, 8500 Nürnberg | Diaminderivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
ATE252543T1 (de) * | 1998-04-14 | 2003-11-15 | Samsung Fine Chemicals Co Ltd | Verfahren zur herstellung chiraler (s)-2,3- disubstituierter 1-propylamin-derivate |
AU764980B2 (en) * | 1998-11-27 | 2003-09-04 | Pharmacia & Upjohn Company | Oxazolidinone antibacterial agents having a thiocarbonyl functionality |
DE19962924A1 (de) * | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
GB0016877D0 (en) * | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
MXPA03003473A (es) * | 2000-10-17 | 2003-08-19 | Upjohn Co | Metodos para producir compuestos de oxazolidinona. |
DE10105989A1 (de) * | 2001-02-09 | 2002-08-14 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
DE10129725A1 (de) | 2001-06-20 | 2003-01-02 | Bayer Ag | Kombinationstherapie substituierter Oxazolidinone |
JP2003206282A (ja) * | 2002-01-07 | 2003-07-22 | Daiso Co Ltd | オキサゾリジン−2−オン誘導体の製造法 |
WO2004002973A1 (ja) * | 2002-06-28 | 2004-01-08 | Kaneka Corporation | 光学活性1−置換アミノー2,3−エポキシプロパンの製造方法並びにその合成中間体およびそれらの製造方法 |
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 |
EP1479675A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Indazole-derivatives as factor Xa inhibitors |
WO2005006845A2 (en) | 2003-07-14 | 2005-01-27 | Agrinomics Llc | Generation of plants with altered oil content |
JP2007505050A (ja) | 2003-09-12 | 2007-03-08 | アルピダ エー/エス | ペプチドデホルミラーゼ阻害剤としてのイソキサゾール類 |
DE10342570A1 (de) * | 2003-09-15 | 2005-04-14 | Bayer Healthcare Ag | Verfahren zur Herstellung von 4-(4-Aminophenyl)-3-morpholinon |
DE102004002044A1 (de) * | 2004-01-15 | 2005-08-04 | Bayer Healthcare Ag | Herstellverfahren |
EP1835818B1 (en) | 2004-12-09 | 2011-08-10 | Eurark, LLC | Product and method for producing a vehicle for oral administration of nutraceuticals |
EP1985620A4 (en) * | 2006-02-07 | 2012-08-15 | Taisho Pharmaceutical Co Ltd | COMPOUND 10a-AZALIDE |
DE102006051625A1 (de) * | 2006-11-02 | 2008-05-08 | Bayer Materialscience Ag | Kombinationstherapie substituierter Oxazolidinone |
KR100898361B1 (ko) | 2008-07-03 | 2009-05-20 | 주식회사 레고켐 바이오사이언스 | P4 위치에 사이클릭 아미독심 또는 사이클릭 아미드라존기를 가지는 FXa 저해제, 이의 유도체, 제조방법 및이를 함유하는 의약 조성물 |
CN101774978B (zh) | 2009-01-13 | 2011-09-21 | 联化科技股份有限公司 | 一种利奈唑胺的制备方法及其中间体 |
US7816355B1 (en) * | 2009-04-28 | 2010-10-19 | Apotex Pharmachem Inc | Processes for the preparation of rivaroxaban and intermediates thereof |
PL2459555T3 (pl) | 2009-07-31 | 2022-03-28 | Krka, D.D., Novo Mesto | Sposoby krystalizacji rywaroksabanu |
EP2388260A1 (de) * | 2010-05-21 | 2011-11-23 | Archimica GmbH | Herstellungsverfahren für einen Inhibitor eines Blutgerinnungsfaktors |
CN107021932A (zh) * | 2010-06-29 | 2017-08-08 | 欧美嘉股份有限公司 | 制备5‑左旋‑氨甲基‑3‑芳基‑2‑恶唑烷酮类的方法 |
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 |
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 |
WO2013053739A1 (en) * | 2011-10-10 | 2013-04-18 | Laboratorios Lesvi, S. L. | Process for preparing factor xa inhibitors |
CN102408420B (zh) * | 2011-10-19 | 2014-10-22 | 汕头经济特区鮀滨制药厂 | 一种利伐沙班及其中间体的制备方法以及中间体化合物 |
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 |
-
2012
- 2012-05-04 UA UAA201314292A patent/UA114601C2/uk unknown
- 2012-05-04 MD MDA20130094A patent/MD4557C1/ro not_active IP Right Cessation
- 2012-05-04 EA EA201391647A patent/EA024685B1/ru not_active IP Right Cessation
- 2012-05-04 GE GEAP201213310A patent/GEP20156397B/en unknown
- 2012-05-04 WO PCT/HU2012/000033 patent/WO2012153155A1/en active Application Filing
- 2012-05-04 EP EP12731645.3A patent/EP2705028B1/en active Active
- 2012-05-04 US US14/115,359 patent/US9556163B2/en active Active
- 2012-05-04 JP JP2014508876A patent/JP6325978B2/ja not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
EP2705028A1 (en) | 2014-03-12 |
MD20130094A2 (ro) | 2014-04-30 |
JP6325978B2 (ja) | 2018-05-16 |
EP2705028B1 (en) | 2019-08-21 |
US20140142303A1 (en) | 2014-05-22 |
GEP20156397B (en) | 2015-11-10 |
UA114601C2 (uk) | 2017-07-10 |
EA024685B1 (ru) | 2016-10-31 |
JP2014513115A (ja) | 2014-05-29 |
WO2012153155A1 (en) | 2012-11-15 |
EA201391647A1 (ru) | 2014-02-28 |
MD4557B1 (ro) | 2018-03-31 |
US9556163B2 (en) | 2017-01-31 |
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Legal Events
Date | Code | Title | Description |
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HC9A | Name of applicant changed (patent for invention) |
Owner name: EGIS GYOGYSZERGYAR ZARTKOERUEN MUKOEDO RESZVENYTAR Free format text: PREVIOUS NAME OF APPLICANT: EGIS GYOGYSZERGYAR NYILVANOSAN MUKOEDO RESZVENYTARSASAG, HU |
|
TK4A | Erratum in official gazette in regard to patent for invention |
Free format text: RECTIFICATION IN INID 72 |
|
FG4A | Patent for invention issued | ||
KA4A | Patent for invention lapsed due to non-payment of fees (with right of restoration) | ||
MM4A | Patent for invention definitely lapsed due to non-payment of fees |