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
- Publication number
- 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
- Authority
- RU
- Russia
- Prior art keywords
- modification
- formula
- compound
- oxo
- obtaining
- Prior art date
Links
- 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
-
- 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)
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 |
|---|---|---|---|
| DE102005047564.7 | 2005-10-04 | ||
| 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 |
| DE102005047563.9 | 2005-10-04 | ||
| 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 |
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 (23)
| 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) |
| HK (1) | HK1125103A1 (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) |
Families Citing this family (37)
| 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 (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 |
| AU2006299126B2 (en) | 2005-10-04 | 2012-06-28 | Bayer Intellectual Property Gmbh | 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 |
| DE102007028318A1 (de) * | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Oxazolidinone zur Behandlung und Prophylaxe von Sepsis |
| WO2009023233A1 (en) * | 2007-08-14 | 2009-02-19 | Concert Pharmaceuticals, Inc. | Substituted oxazolidinone derivatives |
| EP2220079A2 (en) * | 2007-11-15 | 2010-08-25 | Boehringer Ingelheim International GmbH | Substituted amides, manufacturing and use thereof as medicaments |
| DE102008028071A1 (de) * | 2008-06-12 | 2009-12-17 | Bayer Schering Pharma Aktiengesellschaft | Neue Cokristall-Verbindung von Rivaroxaban und Malonsäure |
| CN102105138A (zh) | 2008-07-08 | 2011-06-22 | 德国通益药业有限公司 | 包含5-氯-n-({(5s)-2-氧代-3-[4-(3-氧代-4-吗啉基)-苯基]-1,3-噁唑烷-5-基}-甲基)-2-噻吩羧酰胺的药物组合物 |
| 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 (en) | 2009-06-18 | 2010-12-29 | Krka Tovarna Zdravil, D.D., Novo Mesto | Solid pharmaceutical composition comprising rivaroxaban |
| LT2442799T (lt) | 2009-06-18 | 2016-12-27 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Kieta farmacinė kompozicija, apimanti rivaroksabaną |
| SI2459555T1 (sl) * | 2009-07-31 | 2022-03-31 | Krka, D.D., Novo Mesto | Postopek kristalizacije rivaroksabana |
| US20120231076A1 (en) | 2009-10-06 | 2012-09-13 | Ratiopharm Gmbh | Pharmaceutical compositions comprising rivaroxaban |
| EP2308472A1 (en) | 2009-10-06 | 2011-04-13 | ratiopharm GmbH | Pharmaceutical compositions comprising rivaroxaban |
| 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 |
| US20140378682A1 (en) | 2011-09-08 | 2014-12-25 | 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 |
| HU230734B1 (hu) | 2011-10-10 | 2017-12-28 | EGIS Gyógyszergyár Nyrt | Gyógyászati készítmény előállítására alkalmazható rivaroxaban kokristályok |
| WO2014016842A1 (en) * | 2012-07-23 | 2014-01-30 | Symed Labs Limited | Amorphous coprecipitates of rivaroxaban |
| PL2935255T3 (pl) | 2012-12-21 | 2018-01-31 | Farma Grs D O O | Sposób wytwarzania rywaroksabanu |
| BR112015011033A2 (pt) | 2012-12-26 | 2017-07-11 | Wanbury Ltd | derivado aldeído de oxazolidinonas substituídas |
| ES2610020T3 (es) | 2012-12-26 | 2017-04-25 | Wanbury Limited | Producto intermedio de rivaroxabán y preparación del mismo |
| IN2014CH00290A (ru) * | 2014-01-23 | 2015-08-14 | Symed Labs Ltd | |
| WO2015176677A1 (en) * | 2014-05-22 | 2015-11-26 | Sunshine Lake Pharma Co., Ltd. | Crystalline forms and amorphism of oxazolidinone compound |
| WO2016062828A1 (en) | 2014-10-22 | 2016-04-28 | Zaklady Farmaceutyczne Polpharma S.A | Process for preparing a polymorph of 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 (en) | 2021-12-23 | 2023-06-28 | Zaklady Farmaceutyczne Polpharma S.A. | Crystallisation process for rivaroxaban |
Family Cites Families (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2811555A (en) | 1955-05-02 | 1957-10-29 | Eastman Kodak Co | Reduction of 2-nitroso-5-diethylaminotoluene |
| US3279880A (en) | 1965-07-12 | 1966-10-18 | Eastman Kodak Co | Polyester textile material dyed with 1-hydroxy-4-n-p-(2'-pyrrolidonyl-1-) phenyl-amino anthraquinones |
| LU80081A1 (fr) | 1977-08-26 | 1979-05-15 | Delalande Sa | Nouvelles hydroxymethyl-5 oxazolidinones-2,leur procede de preparation et leur application therapeutique |
| US4128654A (en) | 1978-02-10 | 1978-12-05 | E. I. Du Pont De Nemours And Company | 5-Halomethyl-3-phenyl-2-oxazolidinones |
| US4500519A (en) | 1978-11-06 | 1985-02-19 | Choay S.A. | Mucopolysaccharides having biological properties, preparation and method of use |
| US4327725A (en) | 1980-11-25 | 1982-05-04 | Alza Corporation | Osmotic device with hydrogel driving member |
| HU190072B (en) | 1983-03-11 | 1986-08-28 | Biogal Gyogyszergyar,Hu | Process for production of medical preparatives with sinergetic influence |
| NZ206600A (en) | 1983-05-11 | 1987-01-23 | Alza Corp | Osmotic drug delivery device |
| US4765989A (en) | 1983-05-11 | 1988-08-23 | Alza Corporation | Osmotic device for administering certain drugs |
| ES533097A0 (es) | 1983-06-07 | 1985-08-01 | Du Pont | Un procedimiento para la preparacion de nuevos derivados del amino-metil-oxooxazolidinil-benzeno. |
| DE3884563T2 (de) | 1987-10-21 | 1994-02-17 | Du Pont Merck Pharma | Aminomethyl-oxo-oxazolidinyl-ethenylbenzen-Derivate, nützlich als antibakterielles Mittel. |
| US4977173A (en) | 1987-10-21 | 1990-12-11 | E. I. Du Pont De Nemours And Company | Aminomethyl oxooxazolidinyl ethenylbenzene derivatives useful as antibacterial agents |
| DE3822650A1 (de) | 1988-07-05 | 1990-02-01 | Boehringer Mannheim Gmbh | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
| US4948801A (en) | 1988-07-29 | 1990-08-14 | E. I. Du Pont De Nemours And Company | Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents |
| US5254577A (en) | 1988-07-29 | 1993-10-19 | The Du Pont Merck Pharmaceutical Company | Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents |
| DE69216251T2 (de) | 1991-11-01 | 1997-05-15 | Pharmacia & Upjohn Co., Kalamazoo, Mich. | Substituierte aryl- und heteroaryl-phenyloxazolidinone |
| SK283420B6 (sk) | 1992-05-08 | 2003-07-01 | Pharmacia & Upjohn Company | Antimikrobiálne oxazolidinóny obsahujúce substituované diazínové skupiny |
| US5349045A (en) | 1993-01-26 | 1994-09-20 | United States Surgical Corporation | Polymer derived from cyclic amide and medical devices manufactured therefrom |
| ATE181735T1 (de) | 1993-05-01 | 1999-07-15 | Merck Patent Gmbh | Substituierte 1-phenyl-oxazolidin-2-on derivate, deren herstellung und deren verwendung als adhäsionsrezeptor-antagonisten |
| US5688792A (en) | 1994-08-16 | 1997-11-18 | Pharmacia & Upjohn Company | Substituted oxazine and thiazine oxazolidinone antimicrobials |
| DE4332384A1 (de) | 1993-09-23 | 1995-03-30 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten III |
| RU2154645C2 (ru) | 1995-02-03 | 2000-08-20 | Фармация Энд Апджон Компани | Фенилоксазолидиноны, замещенные в кольце гетероароматическими кольцами, в качестве антимикробных агентов |
| HRP960159A2 (en) | 1995-04-21 | 1997-08-31 | Bayer Ag | Benzocyclopentane oxazolidinones containing heteroatoms |
| DE19524765A1 (de) | 1995-07-07 | 1997-01-09 | Boehringer Mannheim Gmbh | Neue Oxazolidinonderivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DK0856002T3 (da) | 1995-09-01 | 2002-02-11 | Upjohn Co | Phenyloxazolidinoner med en C-C-binding til 4-8 ledede heterocycliske ringe |
| ES2214546T3 (es) | 1995-09-15 | 2004-09-16 | PHARMACIA & UPJOHN COMPANY | N-oxidos de aminoariloxazolidinona. |
| DE19601264A1 (de) | 1996-01-16 | 1997-07-17 | Bayer Ag | Pyrido-annellierte Thienyl- und Furanyl-Oxazolidinone |
| HRP970049A2 (en) | 1996-02-06 | 1998-04-30 | Bayer Ag | New heteroaryl oxazolidinones |
| DE19604223A1 (de) | 1996-02-06 | 1997-08-07 | Bayer Ag | Neue substituierte Oxazolidinone |
| GB9614238D0 (en) | 1996-07-06 | 1996-09-04 | Zeneca Ltd | Chemical compounds |
| HU225415B1 (en) | 1996-07-15 | 2006-11-28 | Sankyo Co | Medicinal compositions comprising cs-866 and insulin resistance improving agents and their use for the treatment of arteriosclerosis and xanthoma |
| US5935724A (en) | 1997-04-04 | 1999-08-10 | Wilson Greatbatch Ltd. | Electrochemical cell having multiplate electrodes with differing discharge rate regions |
| US6273913B1 (en) | 1997-04-18 | 2001-08-14 | Cordis Corporation | Modified stent useful for delivery of drugs along stent strut |
| NZ501412A (en) | 1997-05-30 | 2001-11-30 | Upjohn Co | Oxazolidinone antibacterial agents having a thiocarbonyl functionality |
| AU729745B2 (en) | 1997-07-11 | 2001-02-08 | Pharmacia & Upjohn Company | Thiadiazolyl and oxadiazolyl phenyl oxazolidinone antibacterial agents |
| DE19730847A1 (de) | 1997-07-18 | 1999-01-28 | Bayer Ag | Tricyclisch substituierte Oxazolidinone |
| GB9715894D0 (en) | 1997-07-29 | 1997-10-01 | Zeneca Ltd | Heterocyclic derivatives |
| DE19747261A1 (de) | 1997-10-25 | 1999-04-29 | Bayer Ag | Osmotisches Arzneimittelfreisetzungssystem |
| KR20010031953A (ko) | 1997-11-12 | 2001-04-16 | 로렌스 티. 마이젠헬더 | 옥사졸리디논 유도체 및 제약 조성물 |
| US6083967A (en) | 1997-12-05 | 2000-07-04 | Pharmacia & Upjohn Company | S-oxide and S,S-dioxide tetrahydrothiopyran phenyloxazolidinones |
| DE19755268A1 (de) | 1997-12-12 | 1999-06-17 | Merck Patent Gmbh | Benzamidinderivate |
| BR9907183A (pt) | 1998-01-23 | 2003-06-10 | Versicor Inc | Colet neas combinatórias de oxazolidinona, composições e processos de preparação |
| UA59433C2 (ru) | 1998-01-27 | 2003-09-15 | Авентіс Фармасьютікалс Продактс Інк. | Замещенные оксоазагетероциклические ингибиторы фактора ха |
| US20010029351A1 (en) | 1998-04-16 | 2001-10-11 | Robert Falotico | Drug combinations and delivery devices for the prevention and treatment of vascular disease |
| AU746606B2 (en) | 1998-05-18 | 2002-05-02 | Pharmacia & Upjohn Company | Enhancement of oxazolidinone antibacterial agents activity by using arginine derivatives |
| DE19842753A1 (de) | 1998-09-18 | 2000-03-23 | Bayer Ag | Agitationsunabhängige pharmazeutische Retardzubereitungen und Verfahren zu ihrer Herstellung |
| US6413981B1 (en) | 1999-08-12 | 2002-07-02 | Ortho-Mcneil Pharamceutical, Inc. | Bicyclic heterocyclic substituted phenyl oxazolidinone antibacterials, and related compositions and methods |
| PE20010851A1 (es) | 1999-12-14 | 2001-08-17 | Upjohn Co | Esteres del acido benzoico de oxazolidinonas que tienen un substituyente hidroxiacetilpiperazina |
| JP2003518117A (ja) | 1999-12-21 | 2003-06-03 | ファルマシア・アンド・アップジョン・カンパニー | スルホキシミン官能基を有するオキサゾリジノンおよび抗微生物剤としてのその使用 |
| DE19962924A1 (de) * | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| CA2395948A1 (en) * | 1999-12-28 | 2001-07-05 | Ajinomoto Co., Inc. | Crystal of aspartame derivative |
| DE10105989A1 (de) | 2001-02-09 | 2002-08-14 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| DE10110438A1 (de) | 2001-03-05 | 2002-09-19 | Bayer Ag | Substituierte 2-Oxy-3,5-dicyano-4-aryl-6-aminopyridine 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 |
| DE10110747A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Substituierte 2,6-Diamino-3,5-dicyano-4-aryl-pyridine 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 |
| DE10129725A1 (de) * | 2001-06-20 | 2003-01-02 | Bayer Ag | Kombinationstherapie substituierter Oxazolidinone |
| DE10134481A1 (de) | 2001-07-16 | 2003-01-30 | Bayer Ag | Substituierte 2-Thio-3,5-dicyano-4-phenyl-6-aminopyridine und ihre Verwendung |
| DE10152460A1 (de) | 2001-10-24 | 2003-05-08 | Bayer Ag | Stents |
| DE10238113A1 (de) | 2001-12-11 | 2003-06-18 | Bayer Ag | Substituierte 2-Thio-3,5-dicyano-4-phenyl-6-aminopyridine und ihre Verwendung |
| US20030161882A1 (en) | 2002-02-01 | 2003-08-28 | Waterman Kenneth C. | Osmotic delivery system |
| US20040024660A1 (en) | 2002-08-05 | 2004-02-05 | General Electric Company | System and method for providing asset management and tracking capabilities |
| 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 (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 |
| 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 |
| AU2006299126B2 (en) | 2005-10-04 | 2012-06-28 | Bayer Intellectual Property Gmbh | 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 |
| DE102005048824A1 (de) | 2005-10-10 | 2007-04-12 | Bayer Healthcare Ag | Behandlung und Prophylaxe von Mikroangiopathien |
-
2006
- 2006-09-22 AU AU2006299126A patent/AU2006299126B2/en active Active
- 2006-09-22 DK DK06792210.4T patent/DK1934208T3/da active
- 2006-09-22 CA CA2624310A patent/CA2624310C/en active Active
- 2006-09-22 NZ NZ567092A patent/NZ567092A/en unknown
- 2006-09-22 JP JP2008533895A patent/JP5416408B2/ja active Active
- 2006-09-22 RU RU2011115874/04A patent/RU2578602C2/ru active
- 2006-09-22 US US12/089,095 patent/US8188270B2/en active Active
- 2006-09-22 AT AT06792210T patent/ATE502937T1/de active
- 2006-09-22 SG SG201007274-2A patent/SG166126A1/en unknown
- 2006-09-22 RU RU2008116834/04A patent/RU2429236C2/ru active
- 2006-09-22 PL PL06792210T patent/PL1934208T3/pl unknown
- 2006-09-22 CA CA2823159A patent/CA2823159C/en active Active
- 2006-09-22 DE DE502006009169T patent/DE502006009169D1/de active Active
- 2006-09-22 MY MYPI20080967A patent/MY145616A/en unknown
- 2006-09-22 BR BRPI0616801A patent/BRPI0616801B8/pt active IP Right Grant
- 2006-09-22 EP EP06792210A patent/EP1934208B1/de active Active
- 2006-09-22 WO PCT/EP2006/009202 patent/WO2007039132A1/de active Application Filing
- 2006-09-22 KR KR1020087008058A patent/KR101364400B1/ko active IP Right Grant
- 2006-09-22 PT PT06792210T patent/PT1934208E/pt unknown
-
2008
- 2008-03-17 IL IL190204A patent/IL190204A/en active IP Right Grant
- 2008-04-02 EC EC2008008341A patent/ECSP088341A/es unknown
- 2008-04-02 SV SV2008002858A patent/SV2009002858A/es unknown
- 2008-04-03 CR CR9863A patent/CR9863A/es unknown
- 2008-04-30 NO NO20082059A patent/NO341632B1/no unknown
-
2009
- 2009-03-31 HK HK09103051.1A patent/HK1125103A1/xx unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2011115874A (ru) | 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 | |
| RU2379289C2 (ru) | Соединение индолина и способ его получения | |
| RU2010145171A (ru) | Аналоги галихондрина в | |
| RU2009141611A (ru) | Способ получения амидного соединения | |
| RU2006129341A (ru) | Способ получения 5-хлор-n-(5s)-2-оксо-3-{4-(3-оксо-4-морфолинил)-фенил}-1, 3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида | |
| CA2727378A1 (en) | New co-crystal compound of rivaroxaban and malonic acid | |
| KR20120104077A (ko) | 리바록사반 및 그 중간생성물의 제조방법 | |
| EA200701470A1 (ru) | Способы получения производных 4-(фенокси-5-метилпиримидин-4-илокси)пиперидин-1-карбоновой кислоты и родственных соединений | |
| JP2016511269A (ja) | （２ｓ，５ｒ）−６−ベンジルオキシ−７−オキソ−１，６−ジアザ−ビシクロ［３．２．１］オクタン−２−カルボン酸のナトリウム塩およびその調製 | |
| RU2012131341A (ru) | Индол-пиперидинилбензиламины как ингибиторы бета-триптазы | |
| JP2016155863A (ja) | （＋）および（−）−１−（３，４−ジクロロフェニル）−３−アザビシクロ［３．１．０］ヘキサンの合成のための方法 | |
| TWI714702B (zh) | 一種吡啶衍生物類化合物的製備方法及其中間體和晶型 | |
| ATE418541T1 (de) | Verfahren zur herstellung von carvedilol | |
| JP2015514114A (ja) | リバーロキサバンを調製するためのプロセス | |
| RU2011143166A (ru) | Новые кристаллические формы адефовира дипивоксила и способы его получения | |
| JP6248202B2 (ja) | シロドシン及びその中間体の製造方法 | |
| WO2012041263A2 (en) | A method of manufacturing 2-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]- l,3-oxazolidin-5-yl}methyl)-lh-isoindol-l,3(2h)-dione with a high optical purity | |
| TW201041855A (en) | New process for preparing | |
| CN103113408A (zh) | 一种制备磷霉素左磷右胺盐的新方法 | |
| JP2011506323A5 (ru) | ||
| CN101668736A (zh) | 用于制备组织蛋白酶k抑制剂的酰胺化反应 | |
| JP2011529942A5 (ru) | ||
| JP2008517967A5 (ru) | ||
| RU2010147864A (ru) | Способы получения замещенных гетероциклов -149 | |
| CN104230955A (zh) | 一种对羟基青霉素v酸及其盐的制备方法 |