HRP20100023T1 - Postupak za pripremu karvedilola i njegovih enantiomera - Google Patents
Postupak za pripremu karvedilola i njegovih enantiomera Download PDFInfo
- Publication number
- HRP20100023T1 HRP20100023T1 HR20100023T HRP20100023T HRP20100023T1 HR P20100023 T1 HRP20100023 T1 HR P20100023T1 HR 20100023 T HR20100023 T HR 20100023T HR P20100023 T HRP20100023 T HR P20100023T HR P20100023 T1 HRP20100023 T1 HR P20100023T1
- Authority
- HR
- Croatia
- Prior art keywords
- enantiomers
- preparation
- carvedilol
- molar excess
- reaction solvent
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract 9
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 title claims abstract 6
- NPAKNKYSJIDKMW-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=NC3=CC=C[CH]C3=C12 NPAKNKYSJIDKMW-UHFFFAOYSA-N 0.000 title claims abstract 5
- 229960004195 carvedilol Drugs 0.000 title claims abstract 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims abstract 6
- 239000007810 chemical reaction solvent Substances 0.000 claims abstract 3
- CKJRKLKVCHMWLV-UHFFFAOYSA-N 2-(2-methoxyphenoxy)ethanamine Chemical compound COC1=CC=CC=C1OCCN CKJRKLKVCHMWLV-UHFFFAOYSA-N 0.000 claims 2
- SVWKIGRDISDRLO-UHFFFAOYSA-N 4-(oxiran-2-ylmethoxy)-9h-carbazole Chemical compound C=1C=CC=2NC3=CC=CC=C3C=2C=1OCC1CO1 SVWKIGRDISDRLO-UHFFFAOYSA-N 0.000 claims 1
- 150000002168 ethanoic acid esters Chemical group 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
-
- 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
- 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
- A61P9/10—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
-
- 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
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Postupak za pripremu karvedilola ili njegovih enantiomera reakcijom 4-(2,3-epoksipropoksi)karbazola ili njegovih enantiomera sa viškom 2-(2-metoksifenoksi)etilamina, naznačen time što je reakcijsko otapalo ester octene kiseline. Patent sadrži još 5 patentnih zahtjeva.
Claims (6)
1. Postupak za pripremu karvedilola ili njegovih enantiomera reakcijom 4-(2,3-epoksipropoksi)karbazola ili njegovih enantiomera sa viškom 2-(2-metoksifenoksi)etilamina, naznačen time što je reakcijsko otapalo ester octene kiseline.
2. Postupak prema patentnom zahtjevu 1, naznačen time što je reakcijsko otapalo etil acetat.
3. Postupak prema patentnom zahtjevu 1, naznačen time što je 2-(2-metoksifenoksi)etilamin korišten u molarnom višku od 1.5:1 do 2.5:1.
4. Postupak prema patentnom zahtjevu 3, naznačen time što je molarni višak od 1.8:1 do 2.2:1.
5. Postupak prema patentnom zahtjevu 4, naznačen time što je molarni višak 2:1.
6. Postupak prema patentnom zahtjevu 1 za pripremu karvedilola oblika II, naznačen time što je točka topljenja od 114 -115°C.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04106438 | 2004-12-09 | ||
| PCT/EP2005/056469 WO2006061364A1 (en) | 2004-12-09 | 2005-12-05 | Process for the preparation of carvedilol and its enantiomers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20100023T1 true HRP20100023T1 (hr) | 2010-02-28 |
Family
ID=35985349
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20100023T HRP20100023T1 (hr) | 2004-12-09 | 2010-01-13 | Postupak za pripremu karvedilola i njegovih enantiomera |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20090005429A1 (hr) |
| EP (1) | EP1838670B1 (hr) |
| JP (1) | JP2008523025A (hr) |
| CN (1) | CN100591668C (hr) |
| AT (1) | ATE445601T1 (hr) |
| CA (1) | CA2589699A1 (hr) |
| CY (1) | CY1110688T1 (hr) |
| DE (1) | DE602005017194D1 (hr) |
| DK (1) | DK1838670T3 (hr) |
| ES (1) | ES2333537T3 (hr) |
| HR (1) | HRP20100023T1 (hr) |
| IL (1) | IL183449A0 (hr) |
| PL (1) | PL1838670T3 (hr) |
| PT (1) | PT1838670E (hr) |
| SI (1) | SI1838670T1 (hr) |
| WO (1) | WO2006061364A1 (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6699997B2 (en) | 2000-06-28 | 2004-03-02 | Teva Pharmaceutical Industries Ltd. | Carvedilol |
| PL371409A1 (en) | 2002-01-15 | 2005-06-13 | Teva Pharmaceutical Industries Ltd. | Crystalline solids of carvedilol and processes for their preparation |
| KR100746455B1 (ko) * | 2006-02-23 | 2007-08-03 | 안국약품 주식회사 | 고광학순도의 키랄 카베딜롤의 제조방법 |
| EP1991527A2 (en) | 2006-06-28 | 2008-11-19 | Teva Pharmaceutical Industries Ltd | Polymorphous forms of carvedilol phosphate |
| CN102190613B (zh) * | 2010-03-14 | 2014-06-25 | 浙江华海药业股份有限公司 | 一种卡维地洛的制备方法 |
| KR20170102070A (ko) * | 2010-03-23 | 2017-09-06 | 시가 테크놀로지스, 인크. | 다형체 형태 ｓｔ―２４６ 및 제조방법 |
| WO2015031914A1 (en) * | 2013-08-30 | 2015-03-05 | Uti Limited Partnership | Store overload-induced calcium release inhibitors and methods for producing and using the same |
| CN104592096A (zh) * | 2014-12-24 | 2015-05-06 | 江苏苏南药业实业有限公司 | 一种s-卡维地洛的制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2815926A1 (de) * | 1978-04-13 | 1979-10-18 | Boehringer Mannheim Gmbh | Neue carbazolyl-(4)-oxy-propanolamin-derivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| DE3319027A1 (de) * | 1983-05-26 | 1984-11-29 | Boehringer Mannheim Gmbh, 6800 Mannheim | Verfahren zur herstellung von optisch aktiven carbazol-derivaten, neue r- und s-carbazol-derivate, sowie arzneimittel, die diese verbindungen enthalten |
| EP0893440A1 (en) * | 1997-07-22 | 1999-01-27 | Roche Diagnostics GmbH | Thermodynamically stable modification of 1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole, process for its preparation and pharmaceutical compositions containing it |
| US6699997B2 (en) * | 2000-06-28 | 2004-03-02 | Teva Pharmaceutical Industries Ltd. | Carvedilol |
-
2005
- 2005-12-05 JP JP2007544890A patent/JP2008523025A/ja active Pending
- 2005-12-05 SI SI200530863T patent/SI1838670T1/sl unknown
- 2005-12-05 US US11/720,110 patent/US20090005429A1/en not_active Abandoned
- 2005-12-05 CN CN200580042214A patent/CN100591668C/zh not_active Expired - Fee Related
- 2005-12-05 CA CA002589699A patent/CA2589699A1/en not_active Abandoned
- 2005-12-05 PL PL05815876T patent/PL1838670T3/pl unknown
- 2005-12-05 ES ES05815876T patent/ES2333537T3/es active Active
- 2005-12-05 DE DE602005017194T patent/DE602005017194D1/de active Active
- 2005-12-05 PT PT05815876T patent/PT1838670E/pt unknown
- 2005-12-05 WO PCT/EP2005/056469 patent/WO2006061364A1/en active Application Filing
- 2005-12-05 DK DK05815876.7T patent/DK1838670T3/da active
- 2005-12-05 AT AT05815876T patent/ATE445601T1/de active
- 2005-12-05 EP EP05815876A patent/EP1838670B1/en active Active
-
2007
- 2007-05-28 IL IL183449A patent/IL183449A0/en unknown
-
2009
- 2009-12-08 CY CY20091101281T patent/CY1110688T1/el unknown
-
2010
- 2010-01-13 HR HR20100023T patent/HRP20100023T1/hr unknown
-
2011
- 2011-10-27 US US13/282,868 patent/US20120041044A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CY1110688T1 (el) | 2015-06-10 |
| US20120041044A1 (en) | 2012-02-16 |
| CN100591668C (zh) | 2010-02-24 |
| PT1838670E (pt) | 2009-12-18 |
| DK1838670T3 (da) | 2010-03-01 |
| IL183449A0 (en) | 2007-09-20 |
| PL1838670T3 (pl) | 2010-03-31 |
| JP2008523025A (ja) | 2008-07-03 |
| US20090005429A1 (en) | 2009-01-01 |
| EP1838670B1 (en) | 2009-10-14 |
| ATE445601T1 (de) | 2009-10-15 |
| SI1838670T1 (sl) | 2010-04-30 |
| CN101072753A (zh) | 2007-11-14 |
| DE602005017194D1 (de) | 2009-11-26 |
| CA2589699A1 (en) | 2006-06-15 |
| WO2006061364A1 (en) | 2006-06-15 |
| EP1838670A1 (en) | 2007-10-03 |
| ES2333537T3 (es) | 2010-02-23 |
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