SG166126A1 - Novel polymorphous form and the amorphous form of 5-chloro-n-({(5s)-2-oxo- 3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide - Google Patents
Novel polymorphous form and the amorphous form of 5-chloro-n-({(5s)-2-oxo- 3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamideInfo
- Publication number
- SG166126A1 SG166126A1 SG201007274-2A SG2010072742A SG166126A1 SG 166126 A1 SG166126 A1 SG 166126A1 SG 2010072742 A SG2010072742 A SG 2010072742A SG 166126 A1 SG166126 A1 SG 166126A1
- Authority
- SG
- Singapore
- Prior art keywords
- oxo
- morpholinyl
- chloro
- phenyl
- methyl
- Prior art date
Links
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 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 abstract 1
Classifications
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- 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
- 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
- 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
- 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
- C07D333/28—Halogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (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)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005047564A DE102005047564A1 (de) | 2005-10-04 | 2005-10-04 | Amorphe Form von 5-Chlor-N-({(5S)2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl)-methyl)-2-thiophencarboxamid |
| DE102005047563A DE102005047563A1 (de) | 2005-10-04 | 2005-10-04 | Neue polymorphe Form von 5-Chlor-N-{(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl)-methyl)-2-thiophencarboxamid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG166126A1 true SG166126A1 (en) | 2010-11-29 |
Family
ID=37691766
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG201007274-2A SG166126A1 (en) | 2005-10-04 | 2006-09-22 | Novel polymorphous form and the amorphous form of 5-chloro-n-({(5s)-2-oxo- 3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8188270B2 (fr) |
| EP (1) | EP1934208B1 (fr) |
| JP (1) | JP5416408B2 (fr) |
| KR (1) | KR101364400B1 (fr) |
| AT (1) | ATE502937T1 (fr) |
| AU (1) | AU2006299126B2 (fr) |
| BR (1) | BRPI0616801B8 (fr) |
| CA (2) | CA2624310C (fr) |
| CR (1) | CR9863A (fr) |
| DE (1) | DE502006009169D1 (fr) |
| DK (1) | DK1934208T3 (fr) |
| EC (1) | ECSP088341A (fr) |
| IL (1) | IL190204A (fr) |
| MY (1) | MY145616A (fr) |
| NO (1) | NO341632B1 (fr) |
| NZ (1) | NZ567092A (fr) |
| PL (1) | PL1934208T3 (fr) |
| PT (1) | PT1934208E (fr) |
| RU (2) | RU2578602C2 (fr) |
| SG (1) | SG166126A1 (fr) |
| SV (1) | SV2009002858A (fr) |
| WO (1) | WO2007039132A1 (fr) |
Families Citing this family (38)
| 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 |
| DE10355461A1 (de) | 2003-11-27 | 2005-06-23 | Bayer Healthcare Ag | Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung |
| 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 |
| DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
| RU2578602C2 (ru) | 2005-10-04 | 2016-03-27 | Байер Интеллектуэль Проперти Гмбх | Способ получения 5-хлор-n-(5s)-2-оксо-3-[4-(3-оксо-морфолинил)-фенил]-1,3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида в модификации ii (варианты) |
| DE102007028318A1 (de) * | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Oxazolidinone zur Behandlung und Prophylaxe von Sepsis |
| CN101821260B (zh) * | 2007-08-14 | 2013-07-31 | 康塞特医药品有限公司 | 取代的噁唑烷酮衍生物 |
| JP5524852B2 (ja) * | 2007-11-15 | 2014-06-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換アミド、それらの製造及び医薬品としての使用 |
| DE102008028071A1 (de) | 2008-06-12 | 2009-12-17 | Bayer Schering Pharma Aktiengesellschaft | Neue Cokristall-Verbindung von Rivaroxaban und Malonsäure |
| EP2303240A1 (fr) | 2008-07-08 | 2011-04-06 | Ratiopharm GmbH | Compositions pharmaceutiques comprenant du 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phényl]-1,3-oxazolidin-5-yl}-méthyl)-2-thiophènecarboxamide |
| 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 |
| US7816355B1 (en) * | 2009-04-28 | 2010-10-19 | Apotex Pharmachem Inc | Processes for the preparation of rivaroxaban and intermediates thereof |
| EP2266541A1 (fr) | 2009-06-18 | 2010-12-29 | Krka Tovarna Zdravil, D.D., Novo Mesto | Composition pharmaceutique solide comprenant du rivaroxaban |
| HRP20161617T4 (hr) | 2009-06-18 | 2019-06-28 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Čvrsti farmaceutski sastav koji sadrži rivaroksaban |
| HUE057769T2 (hu) * | 2009-07-31 | 2022-06-28 | Krka D D Novo Mesto | Eljárás rivaroxaban kristályosítására |
| US20120231076A1 (en) | 2009-10-06 | 2012-09-13 | Ratiopharm Gmbh | Pharmaceutical compositions comprising rivaroxaban |
| EP2308472A1 (fr) | 2009-10-06 | 2011-04-13 | ratiopharm GmbH | Compositions pharmaceutiques comportant du rivaroxaban |
| 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 |
| AT511045A1 (de) | 2011-01-28 | 2012-08-15 | Blum Gmbh Julius | Möbelteil mit einer drehmomentübertragenden welle |
| WO2013098833A2 (fr) | 2011-09-08 | 2013-07-04 | Cadila Healthcare Limited | Procédés et intermédiaires destinés à la préparation de rivaroxaban |
| EP2573084A1 (fr) | 2011-09-22 | 2013-03-27 | Enantia, S.L. | Nouvelles formes cristallines de rivaroxaban et leurs procédés de préparation |
| HU230734B1 (hu) | 2011-10-10 | 2017-12-28 | EGIS Gyógyszergyár Nyrt | Gyógyászati készítmény előállítására alkalmazható rivaroxaban kokristályok |
| WO2014016842A1 (fr) * | 2012-07-23 | 2014-01-30 | Symed Labs Limited | Coprécipités amorphes du rivaroxaban |
| PT2935255T (pt) | 2012-12-21 | 2017-11-21 | D O O Farma Grs | Processo para a preparação de rivaroxaban |
| ES2610020T3 (es) | 2012-12-26 | 2017-04-25 | Wanbury Limited | Producto intermedio de rivaroxabán y preparación del mismo |
| EP2897619A4 (fr) | 2012-12-26 | 2016-08-17 | Wanbury Ltd | Dérivé aldéhyde d'oxalidinones substituées |
| IN2014CH00290A (fr) * | 2014-01-23 | 2015-08-14 | Symed Labs Ltd | |
| WO2015176677A1 (fr) * | 2014-05-22 | 2015-11-26 | Sunshine Lake Pharma Co., Ltd. | Formes cristallines et amorphisme de composé d'oxazolidinone |
| EA034656B1 (ru) * | 2014-10-22 | 2020-03-03 | Закляды Фармацеутычне Польфарма С.А | Способ получения полиморфа ривароксабана |
| WO2020101587A1 (fr) | 2018-11-16 | 2020-05-22 | Santa Farma İlaç Sanayi̇ A.Ş. | Formulations orales comprenant du rivaroxaban |
| RU2020103395A (ru) * | 2020-01-28 | 2021-07-28 | Закрытое Акционерное Общество "Алмаз Фарм" | L-, U-модификации 5-хлор-N-({ 5S)-2-оксо-3-[4-3-оксо-4-морфолинил)-фенил]-1,3-оксазолидин-5-ил} -метил)-2-тиофенкарбоксамида, сольват с диметилсульфоксидом, способы их получения, фармацевтические композиции на их основе, ингибирующие фактор Ха |
| GB202102575D0 (en) | 2021-02-23 | 2021-04-07 | Teva Pharmaceutical Industries Ltd | Fixed-dose pharmaceutical compositions |
| GR1010231B (el) | 2021-03-24 | 2022-05-10 | Φαρματεν Α.Β.Ε.Ε., | Φαρμακευτικο σκευασμα που περιλαμβανει ριβαροξαμπανη και μεθοδος παρασκευης αυτου |
| EP4201933A1 (fr) | 2021-12-23 | 2023-06-28 | Zaklady Farmaceutyczne Polpharma S.A. | Processus de cristallisation de rivaroxaban |
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| US6474231B1 (en) * | 2000-07-26 | 2002-11-05 | Heidelberger Druckmaschinen Ag | Multi-color printing press with common blanket cylinder |
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| DE10110438A1 (de) | 2001-03-05 | 2002-09-19 | Bayer Ag | Substituierte 2-Oxy-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung |
| DE10110747A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Substituierte 2,6-Diamino-3,5-dicyano-4-aryl-pyridine und ihre Verwendung |
| DE10110754A1 (de) | 2001-03-07 | 2002-09-19 | Bayer Ag | Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung |
| DE10115922A1 (de) | 2001-03-30 | 2002-10-10 | Bayer Ag | Cyclisch substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung |
| DE10115945A1 (de) | 2001-03-30 | 2002-10-02 | Bayer Ag | Substituierte 2-Carba-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung |
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| DE10134481A1 (de) | 2001-07-16 | 2003-01-30 | Bayer Ag | Substituierte 2-Thio-3,5-dicyano-4-phenyl-6-aminopyridine und ihre Verwendung |
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| 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 |
| 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 (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 |
| DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
| RU2578602C2 (ru) | 2005-10-04 | 2016-03-27 | Байер Интеллектуэль Проперти Гмбх | Способ получения 5-хлор-n-(5s)-2-оксо-3-[4-(3-оксо-морфолинил)-фенил]-1,3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида в модификации ii (варианты) |
| DE102005047558A1 (de) | 2005-10-04 | 2008-02-07 | Bayer Healthcare Ag | Kombinationstherapie substituierter Oxazolidinone zur Prophylaxe und Behandlung von cerebralen Durchblutungsstörungen |
| DE102005048824A1 (de) | 2005-10-10 | 2007-04-12 | Bayer Healthcare Ag | Behandlung und Prophylaxe von Mikroangiopathien |
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2006
- 2006-09-22 RU RU2011115874/04A patent/RU2578602C2/ru active
- 2006-09-22 DK DK06792210.4T patent/DK1934208T3/da active
- 2006-09-22 KR KR1020087008058A patent/KR101364400B1/ko not_active Expired - Fee Related
- 2006-09-22 SG SG201007274-2A patent/SG166126A1/en unknown
- 2006-09-22 AU AU2006299126A patent/AU2006299126B2/en not_active Ceased
- 2006-09-22 EP EP06792210A patent/EP1934208B1/fr active Active
- 2006-09-22 AT AT06792210T patent/ATE502937T1/de active
- 2006-09-22 US US12/089,095 patent/US8188270B2/en active Active
- 2006-09-22 CA CA2624310A patent/CA2624310C/fr active Active
- 2006-09-22 BR BRPI0616801A patent/BRPI0616801B8/pt not_active IP Right Cessation
- 2006-09-22 WO PCT/EP2006/009202 patent/WO2007039132A1/fr not_active Ceased
- 2006-09-22 DE DE502006009169T patent/DE502006009169D1/de active Active
- 2006-09-22 NZ NZ567092A patent/NZ567092A/en not_active IP Right Cessation
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- 2006-09-22 CA CA2823159A patent/CA2823159C/fr active Active
- 2006-09-22 RU RU2008116834/04A patent/RU2429236C2/ru active
- 2006-09-22 JP JP2008533895A patent/JP5416408B2/ja not_active Expired - Fee Related
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- 2008-04-30 NO NO20082059A patent/NO341632B1/no unknown
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