NO20060256L - Nye krystallinske former av perindopril erbumin - Google Patents
Nye krystallinske former av perindopril erbuminInfo
- Publication number
- NO20060256L NO20060256L NO20060256A NO20060256A NO20060256L NO 20060256 L NO20060256 L NO 20060256L NO 20060256 A NO20060256 A NO 20060256A NO 20060256 A NO20060256 A NO 20060256A NO 20060256 L NO20060256 L NO 20060256L
- Authority
- NO
- Norway
- Prior art keywords
- crystalline form
- stirring
- water
- tert
- methyl ether
- Prior art date
Links
- IPVQLZZIHOAWMC-QXKUPLGCSA-N perindopril Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 title 1
- 229960002582 perindopril Drugs 0.000 title 1
- 238000003756 stirring Methods 0.000 abstract 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 5
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 abstract 4
- 238000002425 crystallisation Methods 0.000 abstract 2
- 230000008025 crystallization Effects 0.000 abstract 2
- 238000010899 nucleation Methods 0.000 abstract 2
- 229960003929 perindopril erbumine Drugs 0.000 abstract 2
- IYNMDWMQHSMDDE-MHXJNQAMSA-N perindopril erbumine Chemical compound CC(C)(C)N.C1CCC[C@@H]2N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H](C(O)=O)C[C@@H]21 IYNMDWMQHSMDDE-MHXJNQAMSA-N 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 238000010533 azeotropic distillation Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- 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
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Cardiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Indole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Det er beskrevet to nye krystallinske former, 5 og s av perindopril erbumin. Disse formene er egnet som terapeutisk aktive stoffer for medikamenter til behandling av kardiovaskulære sykdommer, spesielt høyt blodtrykk og hjertefeil. Den e krystallinske formen oppnås ved krystallisering av perindopril erbumin ved 30-45°C, fortrinnsvis 34-45°C, fra MTBE som inneholder 1,5-2,5 % (vol/vol) vann; hvor krystalliseringen fordelaktig utføres med omrøring. Hvis vannet deretter ^emes, fordelaktig ved azeotropisk destillasjon, fortrinnsvis ved 35-37°C, og omrøring deretter fortsettes i minst 15 timer ved 30-45°C, fortrinnsvis 35-37°C, blir den s krystallinske form konvertert til 5 krystallinsk form. Den 5 krystallinske form kan også oppnås ved omrøring av a eller p krystallinsk form ved 33-38°C i tert.-butylmetyleter som inneholder 0,9-1,4 % (vol/vol) vann med tilsetting av kim med 5 krystallinsk form. Den e krystallinske form kan også oppnås ved omrøring av a eller jJ krystallinske former ved 28-35°C i tert.-butylmety leter som inneholder 0,9-1,4 % (vol/vol) vann under tilsetting av kim med s krystallinske form; eller ved omrøring av a eller p krystallinsk form ved 35-38°C i tert.-butylmety leter som inneholder 1,5-2,0 % (vol/vol) vann.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH11092003 | 2003-06-24 | ||
| PCT/CH2004/000374 WO2004113293A1 (de) | 2003-06-24 | 2004-06-18 | Neue kristalline formen von perindopril erbumine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO20060256L true NO20060256L (no) | 2006-01-18 |
| NO333128B1 NO333128B1 (no) | 2013-03-11 |
Family
ID=33520350
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20060256A NO333128B1 (no) | 2003-06-24 | 2006-01-18 | Fremgangsmate for fremstilling av ¿ krystallinsk form av perindopril erbumin og fremgangsmate for fremstilling av et medikament inneholdende nevnte forbindelse |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US7705046B2 (no) |
| EP (1) | EP1636185B1 (no) |
| JP (1) | JP2007507418A (no) |
| KR (1) | KR20060035636A (no) |
| CN (2) | CN100395235C (no) |
| AT (1) | ATE540924T1 (no) |
| AU (1) | AU2004249345B8 (no) |
| BR (1) | BRPI0411966A (no) |
| CA (1) | CA2530550C (no) |
| CY (1) | CY1112597T1 (no) |
| DK (1) | DK1636185T3 (no) |
| EA (1) | EA008603B1 (no) |
| ES (1) | ES2382171T3 (no) |
| MX (1) | MXPA05013811A (no) |
| NO (1) | NO333128B1 (no) |
| NZ (1) | NZ544160A (no) |
| PL (1) | PL1636185T3 (no) |
| PT (1) | PT1636185E (no) |
| SI (1) | SI1636185T1 (no) |
| WO (1) | WO2004113293A1 (no) |
| ZA (1) | ZA200600655B (no) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG125976A1 (en) * | 2005-03-11 | 2006-10-30 | Servier Lab | New gama crystalline form of perindopril tert-butylamine salt, a process for its preparation and pharmaceutical compositions containing it |
| SG125975A1 (en) * | 2005-03-11 | 2006-10-30 | Servier Lab | New alpha crystalline form of perindopril tert-butylamine salt, a process for its preparation and pharmaceutical compositions containing it |
| WO2007017894A2 (en) * | 2005-05-05 | 2007-02-15 | Arch Pharmalabs Limited | PREPARATION OF NOVEL CRYSTALLINE η(ETA) FORM OF PERINDOPRIL ERBUMINE |
| WO2007017893A2 (en) * | 2005-05-05 | 2007-02-15 | Arch Pharmalabs Limited | Preparation of novel crystalline form of perindopril erbumine monohydrate |
| WO2007020009A1 (en) * | 2005-08-12 | 2007-02-22 | Sandoz Ag | New crystalline form of perindopril erbumine |
| WO2007020012A1 (en) * | 2005-08-12 | 2007-02-22 | Lek Pharmaceuticals D.D. | A process for the preparation of perindopril erbumine |
| EP1815857A1 (en) | 2006-02-02 | 2007-08-08 | LEK Pharmaceuticals D.D. | A pharmaceutical composition comprising perindopril |
| WO2007092758A2 (en) * | 2006-02-03 | 2007-08-16 | Dr. Reddy's Laboratories Ltd. | Crystalline forms of perindopril erbumine |
| EA007988B1 (ru) * | 2006-04-20 | 2007-02-27 | ИСМАГИЛОВ, Искандар Халиуллович | ξ-ЗЕТА ФОРМА ПЕРИНДОПРИЛ ЭРБУМИНА |
| WO2008050185A2 (en) * | 2006-10-26 | 2008-05-02 | Glenmark Pharmaceuticals Limited | Novel polymorphs of perindopril erbumine |
| EP2137148A1 (en) * | 2007-03-22 | 2009-12-30 | Aarti Healthcare Limited | Process for the preparation of perindopril erbumine salt and novel polymorph (s) thereof |
| SI22543A (sl) | 2007-06-27 | 2008-12-31 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Nove soli perindoprila |
| PT105315B (pt) | 2010-09-29 | 2013-01-16 | Inst Superior Tecnico | Uma nova forma cristalina hidratada de erbumina de perindopril, métodos para a sua preparação e sua utilização em preparações farmacêuticas |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2503155A2 (fr) | 1980-10-02 | 1982-10-08 | Science Union & Cie | Nouveaux imino diacides substitues, leurs procedes de preparation et leur emploi comme inhibiteur d'enzyme |
| US4508729A (en) * | 1979-12-07 | 1985-04-02 | Adir | Substituted iminodiacids, their preparation and pharmaceutical compositions containing them |
| FR2620709B1 (fr) | 1987-09-17 | 1990-09-07 | Adir | Procede de synthese industrielle du perindopril et de ses principaux intermediaires de synthese |
| DE69332738T2 (de) * | 1993-01-08 | 2003-10-02 | Kanegafuchi Kagaku Kogyo K.K., Osaka | Verfahren zur kristallisation von n2-((s)-1-ethoxycarbonyl-3-phenylpropyl)-n6-trifluoracetyl-l-lysyl-l-prolin |
| FR2807431B1 (fr) | 2000-04-06 | 2002-07-19 | Adir | Nouveau procede de synthese du perindopril et de ses sels pharmaceutiquement acceptables |
| FR2811320B1 (fr) * | 2000-07-06 | 2002-08-23 | Adir | Nouvelle forme cristalline alpha du sel de tert-butylamine du perindopril, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
| FR2811318B1 (fr) | 2000-07-06 | 2002-08-23 | Adir | Nouvelle forme cristalline gamma du sel de tert-butylamine du perindopril, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
| FR2811319B1 (fr) * | 2000-07-06 | 2002-08-23 | Adir | Nouvelle forme cristalline beta du sel de tert-butylamine du perindopril, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
| FR2827860B1 (fr) | 2001-07-24 | 2004-12-10 | Servier Lab | Nouveau procede de synthese de derives de l'acide (2s, 3as, 7as)-1-[(s)-alanyl]-octahydro-1h-indole-2-carboxyline et application a la synthese du perindopril |
| GB2395195A (en) | 2002-11-18 | 2004-05-19 | Cipla Ltd | Preparation of perindopril from carboxy-protected precursor, & perindopril monohydrates for use as angiotensin converting enzyme (ACE) inhibitors |
| CA2631493A1 (en) * | 2005-12-15 | 2007-06-21 | Acusphere, Inc. | Processes for making particle-based pharmaceutical formulations for pulmonary or nasal administration |
-
2004
- 2004-06-18 CN CNB2004800178672A patent/CN100395235C/zh not_active Expired - Fee Related
- 2004-06-18 SI SI200431851T patent/SI1636185T1/sl unknown
- 2004-06-18 PT PT04737029T patent/PT1636185E/pt unknown
- 2004-06-18 DK DK04737029.1T patent/DK1636185T3/da active
- 2004-06-18 AU AU2004249345A patent/AU2004249345B8/en not_active Ceased
- 2004-06-18 KR KR1020057024852A patent/KR20060035636A/ko not_active Ceased
- 2004-06-18 BR BRPI0411966-5A patent/BRPI0411966A/pt not_active Application Discontinuation
- 2004-06-18 PL PL04737029T patent/PL1636185T3/pl unknown
- 2004-06-18 CA CA2530550A patent/CA2530550C/en not_active Expired - Fee Related
- 2004-06-18 EA EA200501859A patent/EA008603B1/ru not_active IP Right Cessation
- 2004-06-18 ES ES04737029T patent/ES2382171T3/es not_active Expired - Lifetime
- 2004-06-18 US US10/560,464 patent/US7705046B2/en not_active Expired - Fee Related
- 2004-06-18 AT AT04737029T patent/ATE540924T1/de active
- 2004-06-18 WO PCT/CH2004/000374 patent/WO2004113293A1/de not_active Ceased
- 2004-06-18 JP JP2006515624A patent/JP2007507418A/ja active Pending
- 2004-06-18 CN CNA2008100912488A patent/CN101333181A/zh active Pending
- 2004-06-18 NZ NZ544160A patent/NZ544160A/en not_active IP Right Cessation
- 2004-06-18 EP EP04737029A patent/EP1636185B1/de not_active Expired - Lifetime
- 2004-06-18 MX MXPA05013811A patent/MXPA05013811A/es active IP Right Grant
-
2006
- 2006-01-18 NO NO20060256A patent/NO333128B1/no not_active IP Right Cessation
- 2006-01-23 ZA ZA200600655A patent/ZA200600655B/en unknown
-
2010
- 2010-03-09 US US12/720,250 patent/US7981921B2/en not_active Expired - Fee Related
-
2012
- 2012-04-04 CY CY20121100334T patent/CY1112597T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US7705046B2 (en) | 2010-04-27 |
| AU2004249345B8 (en) | 2009-06-25 |
| AU2004249345A1 (en) | 2004-12-29 |
| NO333128B1 (no) | 2013-03-11 |
| EA008603B1 (ru) | 2007-06-29 |
| NZ544160A (en) | 2008-07-31 |
| KR20060035636A (ko) | 2006-04-26 |
| US7981921B2 (en) | 2011-07-19 |
| CY1112597T1 (el) | 2016-02-10 |
| US20100160404A1 (en) | 2010-06-24 |
| PT1636185E (pt) | 2012-04-16 |
| ZA200600655B (en) | 2007-05-30 |
| EP1636185A1 (de) | 2006-03-22 |
| MXPA05013811A (es) | 2006-06-27 |
| ATE540924T1 (de) | 2012-01-15 |
| CN1812971A (zh) | 2006-08-02 |
| CA2530550C (en) | 2017-04-04 |
| SI1636185T1 (sl) | 2012-06-29 |
| EA200501859A1 (ru) | 2006-06-30 |
| ES2382171T3 (es) | 2012-06-06 |
| CN101333181A (zh) | 2008-12-31 |
| JP2007507418A (ja) | 2007-03-29 |
| CN100395235C (zh) | 2008-06-18 |
| AU2004249345B2 (en) | 2009-02-26 |
| BRPI0411966A (pt) | 2006-08-29 |
| CA2530550A1 (en) | 2004-12-08 |
| PL1636185T3 (pl) | 2012-12-31 |
| WO2004113293A1 (de) | 2004-12-29 |
| HK1093984A1 (zh) | 2007-03-16 |
| US20070135512A1 (en) | 2007-06-14 |
| DK1636185T3 (da) | 2012-05-07 |
| EP1636185B1 (de) | 2012-01-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CY1112597T1 (el) | Νεες κρυσταλλικες μορφες της ερβουμινικης περινδοπριλης | |
| NO134115B (no) | ||
| CN1284063A (zh) | 新化合物 | |
| US20070015779A1 (en) | Compositions and treatments for inhibiting kinase and/or hmg-coa reductase | |
| JPH02777A (ja) | 新規化合物、その製法及びそれを含む医薬組成物 | |
| KR980002029A (ko) | 에틸 3-(2-(4-(4-(아미노이미노메틸)페닐)-4-메틸-2.5-디옥소이미다졸리딘-1-일)아세틸아미노)-3-페닐프로피오네이트의 염 | |
| JP6178520B2 (ja) | 新規な抗ｈｐｖ医薬製剤の用途 | |
| JP6037969B2 (ja) | 子宮頸癌細胞増殖抑制剤 | |
| Goldstein et al. | Isosteres of natural phosphates. 2. Synthesis of the monosodium salt of 4-hydroxy-3-oxobutyl-l-phosphonic acid an isostere of dihydroxyacetone phosphate | |
| WO2008039087A3 (en) | Indoline derivatives and uses thereof | |
| US20050277653A1 (en) | Compositions and treatments for inhibiting kinase and/or HMG-CoA reductase | |
| JPH01125320A (ja) | テストステロン−５α−リダクターゼ阻害剤 | |
| JPS61275274A (ja) | １，３−ジチオ−ル−２−イリデン誘導体及びその用途 | |
| JP2754644B2 (ja) | 新規リグナン類およびリグナン類を有効成分とする５―リポキシゲナーゼ阻害剤およびアルドースリダクターゼ阻害剤 | |
| JPH04230628A (ja) | 脂質調節薬としての１０員環ラクトンの使用 | |
| CN108929320A (zh) | 3r-吲哚甲基-6r-恶唑烷酮修饰的哌嗪-2,5-二酮，其合成，活性和应用 | |
| GEP20043408B (en) | Process For Preparing 6-(4-Chlorophenyl)- 2,2-Dimethyl-7-Phenyl-2,3-Dihydro-1H-Pyrrolizin-5-YL-Acetic Acid, Pharmaceutical Composition Containing Them and Use Thereof for Treatment of Disorders of the Rheumatic Type | |
| CN101307080A (zh) | 具有镇静活性的5-(4-β-D-吡喃阿洛糖苷-苯基)-3-芳基-4,5-二氢吡唑-1-硫代酰胺类化合物的制备 | |
| CN109400562B (zh) | 一种含愈创兰烃薁结构的曲酸衍生物、制备方法及其应用 | |
| CN101775378A (zh) | 一种酶制剂的制备方法 | |
| WO2000006154A1 (en) | Urokinase production inhibitors, angiogenesis inhibitors and methods of prevention or treatment with both | |
| KR100355497B1 (ko) | 류코트리엔생성저해활성을가지는정유성분 | |
| Von Korff et al. | A DIFFERENCE IN BOVINE AND HUMAN FIBRINO-PEPTIDES WITH RESPECT TO THE OCCURRENCE OF TYROSINE-O-SULFATE | |
| JP2001151685A (ja) | 外用組成物 | |
| JPS61106564A (ja) | 不飽和脂肪酸アミド誘導体およびこれを含有する血小板凝集抑制剤 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| CHAD | Change of the owner's name or address (par. 44 patent law, par. patentforskriften) |
Owner name: LES LABORATOIRES SERVIER Free format text: NEW ADDRESS: 35 RUE DE VERDUN, FR-92284 SURESNES CEDEX, FR |
|
| MM1K | Lapsed by not paying the annual fees |