CY1112597T1 - Νεες κρυσταλλικες μορφες της ερβουμινικης περινδοπριλης - Google Patents

Νεες κρυσταλλικες μορφες της ερβουμινικης περινδοπριλης

Info

Publication number
CY1112597T1
CY1112597T1 CY20121100334T CY121100334T CY1112597T1 CY 1112597 T1 CY1112597 T1 CY 1112597T1 CY 20121100334 T CY20121100334 T CY 20121100334T CY 121100334 T CY121100334 T CY 121100334T CY 1112597 T1 CY1112597 T1 CY 1112597T1
Authority
CY
Cyprus
Prior art keywords
crystalline form
stirring
water
tert
methyl ether
Prior art date
Application number
CY20121100334T
Other languages
English (en)
Inventor
Christoph Strässler
Vit Lellek
Roger Fässler
Original Assignee
Les Laboratoires Servier
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Les Laboratoires Servier filed Critical Les Laboratoires Servier
Publication of CY1112597T1 publication Critical patent/CY1112597T1/el

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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)
  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (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

Περιγράφονται δύο νέες κρυσταλλικές μορφές δ και ε της ερβουμινικής περινδοπρίλης. Αυτές είναι κατάλληλες ως θεραπευτικές δραστικές ουσίες για φάρμακα προοριζόμενα για αγωγή καρδιαγγειακών παθήσεων, ιδίως υπέρτασης ή καρδιακής ανεπάρκειας. Η κρυσταλλική μορφή ε λαμβάνεται κατά την κρυστάλλωση της ερβουμινικής περινδοπρίλης από ΜΤΒΕ ο οποίος περιέχει 1,5 - 2,5 % (v/v) ύδωρ, στους 30-45°C, κατά προτίμηση 34-45°C• αυτή η κρυστάλλωση πραγματοποιείται σκοπίμως υπό ανάδευση. Όταν στη συνέχεια το ύδωρ απομακρυνθεί, σκοπίμως μέσω αζεοτροπικής απόσταξης, κατά προτίμηση στους 35-37°C, και στη συνέχεια γίνει περαιτέρω ανάδευση για τουλάχιστον 15 h στους 30-45°C, κατά προτίμηση 35-37°C, η κρυσταλλική μορφή ε μετατρέπεται στην κρυσταλλική μορφή δ. Η κρυσταλλική μορφή δ μπορεί να ληφθεί και μέσω ανάδευσης της κρυσταλλικής μορφής α ή β εντός τριτ.βουτυλομεθυλαιθέρα ο οποίος περιέχει 0,9-1,4 % (v/v) ύδωρ, στους 33-38°C με ταυτόχρονο εμβολιασμό με την κρυσταλλική μορφή δ. Η κρυσταλλική μορφή ε μπορεί να ληφθεί και μέσω ανάδευσης της κρυσταλλικής μορφής α ή β εντός τριτ.βουτυλομεθυλαιθέρα ο οποίος περιέχει 0,9-1,4 % (v/v) ύδωρ, στους 28-35°C με ταυτόχρονο εμβολιασμό με την κρυσταλλική μορφή ε· ή μέσω ανάδευσης της κρυσταλλικής μορφής α ή β εντός τριτ.βουτυλομεθυλαιθέρα ο οποίος περιέχει 1,5-2,0 % (v/v) ύδωρ, στους 35-38°C.
CY20121100334T 2003-06-24 2012-04-04 Νεες κρυσταλλικες μορφες της ερβουμινικης περινδοπριλης CY1112597T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH11092003 2003-06-24
EP04737029A EP1636185B1 (de) 2003-06-24 2004-06-18 Neue kristalline formen von perindopril erbumine

Publications (1)

Publication Number Publication Date
CY1112597T1 true CY1112597T1 (el) 2016-02-10

Family

ID=33520350

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20121100334T CY1112597T1 (el) 2003-06-24 2012-04-04 Νεες κρυσταλλικες μορφες της ερβουμινικης περινδοπριλης

Country Status (22)

Country Link
US (2) US7705046B2 (el)
EP (1) EP1636185B1 (el)
JP (1) JP2007507418A (el)
KR (1) KR20060035636A (el)
CN (2) CN101333181A (el)
AT (1) ATE540924T1 (el)
AU (1) AU2004249345B8 (el)
BR (1) BRPI0411966A (el)
CA (1) CA2530550C (el)
CY (1) CY1112597T1 (el)
DK (1) DK1636185T3 (el)
EA (1) EA008603B1 (el)
ES (1) ES2382171T3 (el)
HK (1) HK1093984A1 (el)
MX (1) MXPA05013811A (el)
NO (1) NO333128B1 (el)
NZ (1) NZ544160A (el)
PL (1) PL1636185T3 (el)
PT (1) PT1636185E (el)
SI (1) SI1636185T1 (el)
WO (1) WO2004113293A1 (el)
ZA (1) ZA200600655B (el)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
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
WO2007017893A2 (en) * 2005-05-05 2007-02-15 Arch Pharmalabs Limited Preparation of novel crystalline form of perindopril erbumine monohydrate
WO2007017894A2 (en) * 2005-05-05 2007-02-15 Arch Pharmalabs Limited PREPARATION OF NOVEL CRYSTALLINE η(ETA) FORM OF PERINDOPRIL ERBUMINE
AU2006281684B2 (en) * 2005-08-12 2012-08-02 Lek Pharmaceuticals D.D. A process for the preparation of perindopril erbumine
MX2008002066A (es) * 2005-08-12 2008-04-16 Sandoz Ag Neuva forma cristalina de perindopril-erbumina.
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
EA200600630A1 (ru) * 2006-04-20 2007-02-27 ИСМАГИЛОВ, Искандар Халиуллович ζ-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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4508729A (en) 1979-12-07 1985-04-02 Adir Substituted iminodiacids, their preparation and pharmaceutical compositions containing them
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
FR2620709B1 (fr) 1987-09-17 1990-09-07 Adir Procede de synthese industrielle du perindopril et de ses principaux intermediaires de synthese
EP1243594B1 (en) * 1993-01-08 2004-05-12 Kanegafuchi Kagaku Kogyo Kabushiki Kaisha Process for crystallizing N2-((S)-1-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysyl-L-proline
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
US20070178166A1 (en) * 2005-12-15 2007-08-02 Acusphere, Inc. Processes for making particle-based pharmaceutical formulations for pulmonary or nasal administration

Also Published As

Publication number Publication date
NZ544160A (en) 2008-07-31
PT1636185E (pt) 2012-04-16
EA200501859A1 (ru) 2006-06-30
US7705046B2 (en) 2010-04-27
EP1636185B1 (de) 2012-01-11
NO20060256L (no) 2006-01-18
WO2004113293A1 (de) 2004-12-29
NO333128B1 (no) 2013-03-11
ES2382171T3 (es) 2012-06-06
AU2004249345B2 (en) 2009-02-26
CN101333181A (zh) 2008-12-31
AU2004249345A1 (en) 2004-12-29
US20070135512A1 (en) 2007-06-14
US7981921B2 (en) 2011-07-19
EA008603B1 (ru) 2007-06-29
CN100395235C (zh) 2008-06-18
EP1636185A1 (de) 2006-03-22
CA2530550C (en) 2017-04-04
CA2530550A1 (en) 2004-12-08
AU2004249345B8 (en) 2009-06-25
US20100160404A1 (en) 2010-06-24
JP2007507418A (ja) 2007-03-29
PL1636185T3 (pl) 2012-12-31
ATE540924T1 (de) 2012-01-15
CN1812971A (zh) 2006-08-02
HK1093984A1 (en) 2007-03-16
MXPA05013811A (es) 2006-06-27
SI1636185T1 (sl) 2012-06-29
BRPI0411966A (pt) 2006-08-29
DK1636185T3 (da) 2012-05-07
ZA200600655B (en) 2007-05-30
KR20060035636A (ko) 2006-04-26

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