CN100577162C - 用于联合治疗的取代的唑烷酮类化合物 - Google Patents
用于联合治疗的取代的唑烷酮类化合物 Download PDFInfo
- Publication number
- CN100577162C CN100577162C CN02812411A CN02812411A CN100577162C CN 100577162 C CN100577162 C CN 100577162C CN 02812411 A CN02812411 A CN 02812411A CN 02812411 A CN02812411 A CN 02812411A CN 100577162 C CN100577162 C CN 100577162C
- Authority
- CN
- China
- Prior art keywords
- methyl
- oxo
- chloro
- phenyl
- oxazolidine
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
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Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
Abstract
Description
实施例 | ED<sub>50</sub>[mg/kg]p.o. | ED<sub>50</sub>[mg/kg]i.v. |
1 | 10 | |
17 | 6 | |
44 | 3 | |
95 | 3 | |
114 | 3 | |
115 | 3 | |
123 | 3 | |
162 | 3 |
时间 | A:% | B:% | 流速 |
0.00 | 10.0 | 90.0 | 0.50 |
4.00 | 90.0 | 10.0 | 0.50 |
6.00 | 90.0 | 10.0 | 0.50 |
6.10 | 10.0 | 90.0 | 1.00 |
7.50 | 10.0 | 90.0 | 0.50 |
Claims (7)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10129725A DE10129725A1 (de) | 2001-06-20 | 2001-06-20 | Kombinationstherapie substituierter Oxazolidinone |
DE10129725.4 | 2001-06-20 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1523986A CN1523986A (zh) | 2004-08-25 |
CN100577162C true CN100577162C (zh) | 2010-01-06 |
Family
ID=7688824
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN02812411A Expired - Lifetime CN100577162C (zh) | 2001-06-20 | 2002-06-07 | 用于联合治疗的取代的唑烷酮类化合物 |
Country Status (33)
Country | Link |
---|---|
US (2) | US7767702B2 (zh) |
EP (1) | EP1411932B1 (zh) |
JP (1) | JP4667744B2 (zh) |
KR (1) | KR100904138B1 (zh) |
CN (1) | CN100577162C (zh) |
AT (1) | ATE457171T1 (zh) |
AU (1) | AU2002312982B2 (zh) |
BG (1) | BG66354B1 (zh) |
BR (1) | BRPI0210941B8 (zh) |
CA (1) | CA2451258C (zh) |
CO (1) | CO5550434A2 (zh) |
CU (1) | CU23366B7 (zh) |
CY (1) | CY1110019T1 (zh) |
CZ (1) | CZ303715B6 (zh) |
DE (2) | DE10129725A1 (zh) |
DK (1) | DK1411932T3 (zh) |
EC (1) | ECSP034916A (zh) |
EE (1) | EE05419B1 (zh) |
ES (1) | ES2338997T3 (zh) |
HK (1) | HK1068811A1 (zh) |
HR (1) | HRP20040042B1 (zh) |
HU (1) | HU230120B1 (zh) |
IL (2) | IL159257A0 (zh) |
MX (1) | MXPA03011519A (zh) |
NO (1) | NO334821B1 (zh) |
NZ (1) | NZ530223A (zh) |
PL (1) | PL206803B1 (zh) |
PT (1) | PT1411932E (zh) |
RU (1) | RU2321407C9 (zh) |
SI (1) | SI1411932T1 (zh) |
SK (1) | SK287904B6 (zh) |
UA (1) | UA82986C2 (zh) |
WO (1) | WO2003000256A1 (zh) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104447729A (zh) * | 2014-12-05 | 2015-03-25 | 广东东阳光药业有限公司 | 噁唑烷酮类化合物及其在药物中的应用 |
CN111253383A (zh) * | 2020-03-27 | 2020-06-09 | 南京国星生物技术研究院有限公司 | 一种利伐沙班的合成方法 |
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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 |
EP1631560A2 (en) * | 2003-04-25 | 2006-03-08 | 3-Dimensional Pharmaceuticals, Inc. | C-fms kinase inhibitors |
WO2004101552A1 (en) * | 2003-05-14 | 2004-11-25 | Orchid Chemicals & Pharmaceuticals Ltd | Oxazolidinone derivatives as antibacterial agents |
DE10336716A1 (de) | 2003-08-11 | 2005-03-10 | Merck Patent Gmbh | Verfahren zur Herstellung von N-Aryl-morpholinonen |
US7687627B2 (en) * | 2003-09-08 | 2010-03-30 | Wockhardt Limited | Substituted piperidino phenyloxazolidinones having antimicrobial activity with improved in vivo efficacy |
DE10342570A1 (de) * | 2003-09-15 | 2005-04-14 | Bayer Healthcare Ag | Verfahren zur Herstellung von 4-(4-Aminophenyl)-3-morpholinon |
WO2005027896A1 (ja) * | 2003-09-19 | 2005-03-31 | Kissei Pharmaceutical Co., Ltd. | 併用医薬 |
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 |
US7371743B2 (en) * | 2004-02-28 | 2008-05-13 | Boehringer Ingelheim International Gmbh | Carboxylic acid amides, the preparation thereof and their use as medicaments |
US7521470B2 (en) | 2004-06-18 | 2009-04-21 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
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 |
DE102005018690A1 (de) * | 2005-04-22 | 2006-10-26 | Bayer Healthcare Ag | Imino-oxazolidine und ihre Verwendung |
JP5214096B2 (ja) * | 2005-06-17 | 2013-06-19 | 富士フイルムファインケミカルズ株式会社 | 新規なビピリジン誘導体 |
DE102005045518A1 (de) | 2005-09-23 | 2007-03-29 | Bayer Healthcare Ag | 2-Aminoethoxyessigsäure-Derivate und ihre Verwendung |
PL1934208T3 (pl) * | 2005-10-04 | 2011-09-30 | Bayer Ip Gmbh | Nowa polimorficzna postać 5-chloro-N-({ (5S)-2-okso-3-[4-( 3-okso-4-morfolinylo)-fenylo]-1,3-oksazolidyn-5-ylo}-metylo)-2-tiofenokarboksamidu |
DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
DE102005047558A1 (de) * | 2005-10-04 | 2008-02-07 | Bayer Healthcare Ag | Kombinationstherapie substituierter Oxazolidinone zur Prophylaxe und Behandlung von cerebralen Durchblutungsstörungen |
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 |
DE102005052174A1 (de) | 2005-11-02 | 2007-06-06 | Bayer Healthcare Ag | Phenylen-bis-oxazolidin-Derivate und ihre Verwendung |
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DE102006007146A1 (de) * | 2006-02-16 | 2007-08-23 | Bayer Healthcare Ag | Aminoacyl-Prodrugs |
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2001
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- 2002-06-07 RU RU2004101404/15A patent/RU2321407C9/ru active
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- 2002-06-07 WO PCT/EP2002/006237 patent/WO2003000256A1/de active IP Right Grant
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- 2002-06-07 KR KR1020037016596A patent/KR100904138B1/ko active IP Right Grant
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- 2002-06-07 HU HU0400240A patent/HU230120B1/hu unknown
- 2002-06-07 DK DK02738154.0T patent/DK1411932T3/da active
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- 2002-06-07 DE DE50214206T patent/DE50214206D1/de not_active Expired - Lifetime
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- 2002-06-07 PT PT02738154T patent/PT1411932E/pt unknown
- 2002-06-07 MX MXPA03011519A patent/MXPA03011519A/es active IP Right Grant
- 2002-06-07 AT AT02738154T patent/ATE457171T1/de active
- 2002-06-07 PL PL368079A patent/PL206803B1/pl unknown
- 2002-07-06 UA UA2004010387A patent/UA82986C2/uk unknown
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- 2003-11-26 CU CU20030276A patent/CU23366B7/es unknown
- 2003-12-09 IL IL159257A patent/IL159257A/en active IP Right Grant
- 2003-12-12 BG BG108443A patent/BG66354B1/bg unknown
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- 2003-12-19 NO NO20035743A patent/NO334821B1/no not_active IP Right Cessation
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- 2004-01-19 HR HRP20040042AA patent/HRP20040042B1/hr not_active IP Right Cessation
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2005
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104447729A (zh) * | 2014-12-05 | 2015-03-25 | 广东东阳光药业有限公司 | 噁唑烷酮类化合物及其在药物中的应用 |
CN111253383A (zh) * | 2020-03-27 | 2020-06-09 | 南京国星生物技术研究院有限公司 | 一种利伐沙班的合成方法 |
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