RU2011115874A - 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) и способ его получения в аморфной форме - Google Patents
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) и способ его получения в аморфной форме Download PDFInfo
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- RU2011115874A RU2011115874A RU2011115874/04A RU2011115874A RU2011115874A RU 2011115874 A RU2011115874 A RU 2011115874A RU 2011115874/04 A RU2011115874/04 A RU 2011115874/04A RU 2011115874 A RU2011115874 A RU 2011115874A RU 2011115874 A RU2011115874 A RU 2011115874A
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- 238000012986 modification Methods 0.000 title claims abstract 15
- 230000004048 modification Effects 0.000 title claims abstract 15
- 238000000034 method Methods 0.000 title claims abstract 11
- 238000004519 manufacturing process Methods 0.000 title 2
- -1 3-OXO-MORPHOLINYL Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 239000012442 inert solvent Substances 0.000 claims abstract 6
- 238000006243 chemical reaction Methods 0.000 claims abstract 4
- 239000000725 suspension Substances 0.000 claims abstract 4
- 239000003795 chemical substances by application Substances 0.000 claims abstract 2
- 230000001376 precipitating effect Effects 0.000 claims abstract 2
- 239000002904 solvent Substances 0.000 claims abstract 2
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
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- 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
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- 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
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- 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
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- 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
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- 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)
Abstract
1. Способ получения соединения формулы (I) ! ! в модификации II, отличающийся тем, что соединение формулы (I) в модификации I растворяют в инертном растворителе и осаждают соединение путем добавки осаждающего средства. !2. Способ получения соединения формулы (I) ! ! в модификации II, отличающийся тем, что соединение формулы (I) в модификации I растворяют в инертном растворителе и раствор выдерживают при повышенной температуре до полного испарения растворителя. ! 3. Способ получения соединения формулы (I) ! ! в модификации II, отличающийся тем, что соединение формулы (I) в аморфной форме суспендируют в безводном инертном растворителе и перемешивают или встряхивают суспензию до преобразования в модификацию II. ! 4. Способ по п.3, отличающийся тем, что перемешивают или встряхивают суспензию до количественного преобразования в модификацию II. ! 5. Способ получения соединения формулы (I) ! ! в аморфной форме, отличающийся тем, что соединение формулы (I) в кристаллической форме полностью расплавляют и затем быстро охлаждают.
Claims (5)
1. Способ получения соединения формулы (I)
в модификации II, отличающийся тем, что соединение формулы (I) в модификации I растворяют в инертном растворителе и осаждают соединение путем добавки осаждающего средства.
2. Способ получения соединения формулы (I)
в модификации II, отличающийся тем, что соединение формулы (I) в модификации I растворяют в инертном растворителе и раствор выдерживают при повышенной температуре до полного испарения растворителя.
3. Способ получения соединения формулы (I)
в модификации II, отличающийся тем, что соединение формулы (I) в аморфной форме суспендируют в безводном инертном растворителе и перемешивают или встряхивают суспензию до преобразования в модификацию II.
4. Способ по п.3, отличающийся тем, что перемешивают или встряхивают суспензию до количественного преобразования в модификацию II.
5. Способ получения соединения формулы (I)
в аморфной форме, отличающийся тем, что соединение формулы (I) в кристаллической форме полностью расплавляют и затем быстро охлаждают.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
| 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 |
| DE102005047564.7 | 2005-10-04 | ||
| DE102005047563.9 | 2005-10-04 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008116834/04A Division RU2429236C2 (ru) | 2005-10-04 | 2006-09-22 | Новая полиморфная форма и аморфная форма 5-хлор-n-({(5s)-2-оксо-3-[4-(3-оксо-4-морфолинил)-фенил]-1, 3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2011115874A true RU2011115874A (ru) | 2012-10-27 |
| RU2578602C2 RU2578602C2 (ru) | 2016-03-27 |
Family
ID=37691766
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011115874/04A RU2578602C2 (ru) | 2005-10-04 | 2006-09-22 | 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) |
| RU2008116834/04A RU2429236C2 (ru) | 2005-10-04 | 2006-09-22 | Новая полиморфная форма и аморфная форма 5-хлор-n-({(5s)-2-оксо-3-[4-(3-оксо-4-морфолинил)-фенил]-1, 3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008116834/04A RU2429236C2 (ru) | 2005-10-04 | 2006-09-22 | Новая полиморфная форма и аморфная форма 5-хлор-n-({(5s)-2-оксо-3-[4-(3-оксо-4-морфолинил)-фенил]-1, 3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8188270B2 (ru) |
| EP (1) | EP1934208B1 (ru) |
| JP (1) | JP5416408B2 (ru) |
| KR (1) | KR101364400B1 (ru) |
| AT (1) | ATE502937T1 (ru) |
| AU (1) | AU2006299126B2 (ru) |
| BR (1) | BRPI0616801B8 (ru) |
| CA (2) | CA2624310C (ru) |
| CR (1) | CR9863A (ru) |
| DE (1) | DE502006009169D1 (ru) |
| DK (1) | DK1934208T3 (ru) |
| EC (1) | ECSP088341A (ru) |
| IL (1) | IL190204A (ru) |
| MY (1) | MY145616A (ru) |
| NO (1) | NO341632B1 (ru) |
| NZ (1) | NZ567092A (ru) |
| PL (1) | PL1934208T3 (ru) |
| PT (1) | PT1934208E (ru) |
| RU (2) | RU2578602C2 (ru) |
| SG (1) | SG166126A1 (ru) |
| SV (1) | SV2009002858A (ru) |
| WO (1) | WO2007039132A1 (ru) |
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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 |
| EP1685841A1 (en) | 2005-01-31 | 2006-08-02 | Bayer Health Care Aktiengesellschaft | Prevention and treatment of thromboembolic disorders |
| 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 |
| EP1934208B1 (de) | 2005-10-04 | 2011-03-23 | Bayer Schering Pharma Aktiengesellschaft | Neue polymorphe form von 5-chlor-n-({ ( 5s )-2-0x0-3-[4-( 3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl} -methyl)-2-thiophencarboxamid |
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| WO2010003641A1 (en) | 2008-07-08 | 2010-01-14 | Ratiopharm Gmbh | Pharmaceutical compositions comprising 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid |
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| US7816355B1 (en) * | 2009-04-28 | 2010-10-19 | Apotex Pharmachem Inc | Processes for the preparation of rivaroxaban and intermediates thereof |
| EA035562B1 (ru) | 2009-06-18 | 2020-07-08 | Крка, Товарна Здравил, Д. Д., Ново Место | Способ получения твердой фармацевтической композиции, содержащей ривароксабан |
| EP2266541A1 (en) | 2009-06-18 | 2010-12-29 | Krka Tovarna Zdravil, D.D., Novo Mesto | Solid pharmaceutical composition comprising rivaroxaban |
| EP2459555B1 (en) | 2009-07-31 | 2021-11-03 | KRKA, D.D., Novo Mesto | Processes for crystallization of rivaroxaban |
| EP2308472A1 (en) | 2009-10-06 | 2011-04-13 | ratiopharm GmbH | Pharmaceutical compositions comprising rivaroxaban |
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| EP2404920A1 (en) | 2010-07-06 | 2012-01-11 | Sandoz AG | Crystalline form of 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 |
| EP2753619A2 (en) | 2011-09-08 | 2014-07-16 | Cadila Healthcare Limited | Processes and intermediates for preparing rivaroxaban |
| EP2573084A1 (en) | 2011-09-22 | 2013-03-27 | Enantia, S.L. | Novel crystalline forms of rivaroxaban and processes for their preparation |
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| WO2014102820A2 (en) | 2012-12-26 | 2014-07-03 | Wanbury Ltd. | Rivaroxaban intermediate and preparation thereof |
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| WO2015176677A1 (en) * | 2014-05-22 | 2015-11-26 | Sunshine Lake Pharma Co., Ltd. | Crystalline forms and amorphism of oxazolidinone compound |
| EA034656B1 (ru) * | 2014-10-22 | 2020-03-03 | Закляды Фармацеутычне Польфарма С.А | Способ получения полиморфа ривароксабана |
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| 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 |
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-
2006
- 2006-09-22 EP EP06792210A patent/EP1934208B1/de active Active
- 2006-09-22 SG SG201007274-2A patent/SG166126A1/en unknown
- 2006-09-22 MY MYPI20080967A patent/MY145616A/en unknown
- 2006-09-22 CA CA2624310A patent/CA2624310C/en active Active
- 2006-09-22 DE DE502006009169T patent/DE502006009169D1/de active Active
- 2006-09-22 PT PT06792210T patent/PT1934208E/pt unknown
- 2006-09-22 US US12/089,095 patent/US8188270B2/en active Active
- 2006-09-22 PL PL06792210T patent/PL1934208T3/pl unknown
- 2006-09-22 BR BRPI0616801A patent/BRPI0616801B8/pt not_active IP Right Cessation
- 2006-09-22 DK DK06792210.4T patent/DK1934208T3/da active
- 2006-09-22 RU RU2011115874/04A patent/RU2578602C2/ru active
- 2006-09-22 JP JP2008533895A patent/JP5416408B2/ja not_active Expired - Fee Related
- 2006-09-22 AU AU2006299126A patent/AU2006299126B2/en not_active Ceased
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- 2006-09-22 WO PCT/EP2006/009202 patent/WO2007039132A1/de not_active Ceased
- 2006-09-22 KR KR1020087008058A patent/KR101364400B1/ko not_active Expired - Fee Related
- 2006-09-22 AT AT06792210T patent/ATE502937T1/de active
- 2006-09-22 RU RU2008116834/04A patent/RU2429236C2/ru active
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