RU2000103033A - Термодинамически стабильная модификация 1-(4-карбазолилокси)-3-[2-(2-метоксифенокси)этиламино]-2-пропанола, способ ее получения и содержащие ее фармацевтические композиции - Google Patents
Термодинамически стабильная модификация 1-(4-карбазолилокси)-3-[2-(2-метоксифенокси)этиламино]-2-пропанола, способ ее получения и содержащие ее фармацевтические композицииInfo
- Publication number
- RU2000103033A RU2000103033A RU2000103033/04A RU2000103033A RU2000103033A RU 2000103033 A RU2000103033 A RU 2000103033A RU 2000103033/04 A RU2000103033/04 A RU 2000103033/04A RU 2000103033 A RU2000103033 A RU 2000103033A RU 2000103033 A RU2000103033 A RU 2000103033A
- Authority
- RU
- Russia
- Prior art keywords
- carbazolyloxy
- methoxyphenoxy
- ethylamino
- propanol
- modification
- Prior art date
Links
- OGHNVEJMJSYVRP-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=C1C1=CC=CC=C1N2 OGHNVEJMJSYVRP-UHFFFAOYSA-N 0.000 title claims 5
- 230000004048 modification Effects 0.000 title claims 4
- 238000006011 modification reaction Methods 0.000 title claims 4
- 238000004519 manufacturing process Methods 0.000 title claims 2
- 239000003814 drug Substances 0.000 title 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 4
- 229960004195 carvedilol Drugs 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000240 adjuvant Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000010238 heart disease Diseases 0.000 claims 1
- 238000002329 infrared spectrum Methods 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N iso-propanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000002285 radioactive Effects 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
Claims (7)
1. Модификация (±)1-(4-карбазолилокси)-3-[2-(2-метоксифенокси)этиламино] -2-пропанола, на рентгенограмме которой, полученной с использованием радиоактивного источника CuKα, угол 2θ имеет следующие значения: 9,5, 10,8, 12,0, 14,5, 19,6, 21,5, 22,3, в инфракрасном спектре которой имеется острый пик при 3451 см-1 и температура плавления которой составляет приблизительно 123-126o С.
2. Фармакологически приемлемые соли или оптически активные формы соединения по п.1.
3. Способ получения и выделения практически чистой формы соединения по п.1, отличающийся тем, что неочищенный карведилол подвергают перегруппировке в метаноле или изопропаноле.
4. Способ по п.3, где перегруппировку осуществляют в метаноле при температуре от 25 до 35oС в течение 3-22 ч.
5. Способ по п.3 или 4, где модификацию карведилола с более высокой температурой плавления выделяют из реакционной смеси, предназначенной для перегруппировки, при температуре 0oС.
6. Фармацевтическая композиция, включающая в качестве действующего вещества практически чистую форму стабильной модификации 1-(4-карбазолилокси)-3[2-(2-метоксифенокси)этиламино] -2-пропанола по п. 1 вместе с одним или несколькими фармацевтически приемлемыми носителями или адъювантами.
7. Применение фармацевтической композиции по п.5 для приготовления лекарственного средства, предназначенного для профилактики или лечения болезней сердца.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE97112491.2 | 1997-07-22 | ||
| EP97112491A EP0893440A1 (en) | 1997-07-22 | 1997-07-22 | Thermodynamically stable modification of 1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole, process for its preparation and pharmaceutical compositions containing it |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2000103033A true RU2000103033A (ru) | 2001-12-10 |
| RU2202542C2 RU2202542C2 (ru) | 2003-04-20 |
Family
ID=8227094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2000103033/04A RU2202542C2 (ru) | 1997-07-22 | 1998-07-18 | Термодинамически стабильная модификация (±)1-(4-карбазолилокси)-3-[2-(2-метоксифенокси)этиламино]-2-пропанола , способ ее получения и содержащая ее фармацевтическая композиция |
Country Status (32)
| Country | Link |
|---|---|
| EP (2) | EP0893440A1 (ru) |
| JP (1) | JP2001510824A (ru) |
| KR (1) | KR100336229B1 (ru) |
| CN (1) | CN1125047C (ru) |
| AR (1) | AR015133A1 (ru) |
| AT (1) | ATE236123T1 (ru) |
| AU (1) | AU740453B2 (ru) |
| BR (1) | BR9810776A (ru) |
| CA (1) | CA2296637C (ru) |
| CZ (1) | CZ296947B6 (ru) |
| DE (1) | DE69812964T2 (ru) |
| DK (1) | DK1000027T3 (ru) |
| ES (1) | ES2195366T3 (ru) |
| HK (1) | HK1029339A1 (ru) |
| HR (1) | HRP980406A2 (ru) |
| HU (1) | HUP0003198A3 (ru) |
| IL (1) | IL133677A (ru) |
| MA (1) | MA26523A1 (ru) |
| MY (1) | MY117734A (ru) |
| NO (1) | NO313588B1 (ru) |
| NZ (1) | NZ502136A (ru) |
| PE (1) | PE96999A1 (ru) |
| PL (1) | PL191602B1 (ru) |
| PT (1) | PT1000027E (ru) |
| RU (1) | RU2202542C2 (ru) |
| SI (1) | SI1000027T1 (ru) |
| TR (1) | TR200000148T2 (ru) |
| TW (1) | TW505631B (ru) |
| UY (1) | UY25108A1 (ru) |
| WO (1) | WO1999005105A1 (ru) |
| YU (1) | YU2200A (ru) |
| ZA (1) | ZA986475B (ru) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001074356A1 (en) * | 2000-04-03 | 2001-10-11 | F. Hoffmann-La Roche Ag | Concentrated solutions of carvedilol |
| EP1655285A1 (en) * | 2000-06-28 | 2006-05-10 | Teva Pharmaceutical Industries Ltd. | Method for preparation of a crystalline form of carvedilol (form II) |
| CN1245974C (zh) * | 2000-06-28 | 2006-03-22 | 特瓦制药工业有限公司 | 卡维地洛 |
| ATE328595T1 (de) * | 2001-07-13 | 2006-06-15 | Smithkline Beecham Corp | Carvedilolpolymorph |
| ATE381924T1 (de) | 2001-09-21 | 2008-01-15 | Egalet As | Feste dispersionen mit kontrollierter freisetzung von carvedilol |
| BR0212927A (pt) * | 2001-09-28 | 2004-10-13 | Hoffmann La Roche | Formas pseudopolimórficas de carvedilol |
| CA2472377A1 (en) * | 2002-01-15 | 2003-07-24 | Teva Pharmaceutical Industries Ltd. | Crystalline solids of carvedilol and processes for their preparation |
| WO2003092622A2 (en) * | 2002-04-30 | 2003-11-13 | Sb Pharmco Puerto Rico Inc. | Carvedilol monocitrate monohydrate |
| EP1539140A4 (en) | 2002-06-27 | 2005-12-07 | Sb Pharmco Inc | CARVEDILOLHYDOBROMID |
| CN103288714A (zh) * | 2002-06-27 | 2013-09-11 | 史密斯克莱.比奇曼（科克）有限公司 | 卡维地洛磷酸盐和/或其溶剂合物相应的组合物和/或治疗方法 |
| EP1562552A1 (en) | 2002-11-08 | 2005-08-17 | Egalet A/S | Controlled release carvedilol compositions |
| WO2004084868A1 (en) | 2003-03-26 | 2004-10-07 | Egalet A/S | Morphine controlled release system |
| EP1615888A1 (en) | 2003-04-21 | 2006-01-18 | Matrix Laboratories Ltd | Process for the preparation of carvedilol form-ii |
| SI21616A (sl) * | 2003-09-02 | 2005-04-30 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Nove kristalne oblike karvedilola |
| US7750036B2 (en) | 2003-11-25 | 2010-07-06 | Sb Pharmco Puerto Rico Inc. | Carvedilol salts, corresponding compositions, methods of delivery and/or treatment |
| ATE445601T1 (de) * | 2004-12-09 | 2009-10-15 | Zach System Spa | Verfahren zur herstellung von carvedilol und seinen enantiomeren |
| US20070043099A1 (en) * | 2005-06-09 | 2007-02-22 | Igor Lifshitz | Crystalline forms of carvedilol and processes for their preparation |
| WO2008002683A2 (en) | 2006-06-28 | 2008-01-03 | Teva Pharmaceutical Industries Ltd. | Polymorphous forms of carvedilol phosphate |
| US20080249317A1 (en) * | 2007-04-04 | 2008-10-09 | Apotex Inc. | Novel amorphous form of carvedilol phosphate and processes for the preparation thereof |
| WO2008148798A2 (en) | 2007-06-04 | 2008-12-11 | Egalet A/S | Controlled release pharmaceutical compositions for prolonged effect |
| US9005660B2 (en) | 2009-02-06 | 2015-04-14 | Egalet Ltd. | Immediate release composition resistant to abuse by intake of alcohol |
| CA2766179A1 (en) | 2009-06-24 | 2010-12-29 | Egalet Ltd. | Controlled release formulations |
Family Cites Families (2)
| 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 |
-
1997
- 1997-07-22 EP EP97112491A patent/EP0893440A1/en not_active Withdrawn
-
1998
- 1998-07-15 MY MYPI98003245A patent/MY117734A/en unknown
- 1998-07-15 PE PE1998000626A patent/PE96999A1/es not_active Application Discontinuation
- 1998-07-18 CN CN98807436A patent/CN1125047C/zh not_active Expired - Fee Related
- 1998-07-18 BR BR9810776-3A patent/BR9810776A/pt not_active Application Discontinuation
- 1998-07-18 TR TR2000/00148T patent/TR200000148T2/xx unknown
- 1998-07-18 WO PCT/EP1998/004475 patent/WO1999005105A1/en active IP Right Grant
- 1998-07-18 JP JP2000504104A patent/JP2001510824A/ja active Pending
- 1998-07-18 CA CA002296637A patent/CA2296637C/en not_active Expired - Fee Related
- 1998-07-18 KR KR1020007000667A patent/KR100336229B1/ko not_active IP Right Cessation
- 1998-07-18 NZ NZ502136A patent/NZ502136A/en unknown
- 1998-07-18 PL PL338432A patent/PL191602B1/pl unknown
- 1998-07-18 DE DE69812964T patent/DE69812964T2/de not_active Expired - Fee Related
- 1998-07-18 DK DK98937576T patent/DK1000027T3/da active
- 1998-07-18 IL IL13367798A patent/IL133677A/en not_active IP Right Cessation
- 1998-07-18 SI SI9830442T patent/SI1000027T1/xx unknown
- 1998-07-18 EP EP98937576A patent/EP1000027B1/en not_active Expired - Lifetime
- 1998-07-18 YU YU2200A patent/YU2200A/sh unknown
- 1998-07-18 AT AT98937576T patent/ATE236123T1/de not_active IP Right Cessation
- 1998-07-18 HU HU0003198A patent/HUP0003198A3/hu unknown
- 1998-07-18 PT PT98937576T patent/PT1000027E/pt unknown
- 1998-07-18 CZ CZ20000221A patent/CZ296947B6/cs not_active IP Right Cessation
- 1998-07-18 AU AU86319/98A patent/AU740453B2/en not_active Ceased
- 1998-07-18 TW TW087111738A patent/TW505631B/zh not_active IP Right Cessation
- 1998-07-18 ES ES98937576T patent/ES2195366T3/es not_active Expired - Lifetime
- 1998-07-18 RU RU2000103033/04A patent/RU2202542C2/ru not_active IP Right Cessation
- 1998-07-20 MA MA25178A patent/MA26523A1/fr unknown
- 1998-07-21 ZA ZA9806475A patent/ZA986475B/xx unknown
- 1998-07-21 AR ARP980103547A patent/AR015133A1/es unknown
- 1998-07-22 HR HR97112491.2A patent/HRP980406A2/hr not_active Application Discontinuation
- 1998-07-22 UY UY25108A patent/UY25108A1/es not_active IP Right Cessation
-
2000
- 2000-01-21 NO NO20000301A patent/NO313588B1/no unknown
-
2001
- 2001-01-02 HK HK01100012A patent/HK1029339A1/xx not_active IP Right Cessation
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