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ME02689B - Novi kristalni oblik iii agomelatina, postupak za njegovu pripremu i farmaceutski preparati istog - Google Patents

Novi kristalni oblik iii agomelatina, postupak za njegovu pripremu i farmaceutski preparati istog

Info

Publication number
ME02689B
ME02689B MEP-2017-33A MEP3317A ME02689B ME 02689 B ME02689 B ME 02689B ME P3317 A MEP3317 A ME P3317A ME 02689 B ME02689 B ME 02689B
Authority
ME
Montenegro
Prior art keywords
disorders
form iii
accordance
production
agomelatine
Prior art date
Application number
MEP-2017-33A
Other languages
German (de)
English (en)
French (fr)
Inventor
Gérard Coquerel
Julie Linol
Jean-Claude Souvie
Original Assignee
Servier Lab
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 Servier Lab filed Critical Servier Lab
Publication of ME02689B publication Critical patent/ME02689B/me

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/22Separation; Purification; Stabilisation; Use of additives
    • C07C231/24Separation; Purification
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/18Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
    • C07C2602/02Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (5)

1. Kristalni oblik III agomelatina formule (I): naznačen time, da je praćen dijagramom rendgenske difrakcijske zraka, mjeren uporabom Siemens D5005matik difraktometra (bakarna antikatoda) i izražen interplanarnom razdaljinom d, Braggovog kuta 2 teta i relativnim intenzitetom (izraženim u postocima u odnosu na najintenzivniju crtu): 2-Teta (°) izr. d (Å) izr. Intenzitet (%) 10.52 12.92 16.15 17.38 17. 84 18.55 19.20 19.89 20.32 21.15 22.08 22.96 23.33 23.84 24.52 24.88 25.07 26.27 26.86 27.97 29.51 8.405 6.848 5.482 5.097 4.968 4.779 4.619 4.460 4.366 4.197 4.022 3.870 3.810 3.730 3.628 3.576 3.550 3.390 3.316 3.187 3.024 100 40 53 69 96 22 97 30 24 26 16 23 95 33 25 59 90 61 22 20 43
2. Postupak za pripravu kristalnog oblika III spoja formule (I) u skladu s patentnim zahtjevom 1, naznačen time, da se agomelatin izlaže temperature do 110°C dok se potpuno ne rastopi, nakon čega se polagano hladi dok se ponovo ne kristalizira.
3. Farmaceutski pripravci koji sadrže djelatni sastojak kristalnog oblika III agomelatina u skladu s patentnim zahtjevom 1, naznačeno time, da je u kombinaciji s jednim ili više intertnih, netoksičnih, farmaceutski prihvatljivih nosača.
4. Farmaceutski pripravci u skladu s patentnim zahtjevom 3, naznačeni time, da se koriste u proizvodnji lijekova za liječenje poremećaja melatoninergičkog sustava.
5. Farmaceutski pripravci u skladu s patentnim zahtjevom 3, naznačeni time, da se koriste u proizvodnji lijekova za liječenje poremećaja spavanja, stresa, anksioznosti, sezonskih depresija ili teške depresije, kardiovaskularnih patologija, patologija probavnog sustava, nesanice i umora uslijed vremenske razlike nakon letenja (jet-lag), shizofrenije, napadaja panike, melankolije, poremećaja apetita, pretilosti, nesanice, psihotičkih poremećaja, epilepsije, dijabetesa, Parkinsonove bolesti, senilne demencija, raznih poremećaja povezanih s uobičajenim ili patološkim starenjem, migrene, gubitka pamćenja, Alzheimerove bolesti, poremećaja moždane cirkulacije, također i seksualne disfunkcije, kao inhibitori ovulacije i imunomodulatori i u liječenju karcinoma.
MEP-2017-33A 2005-08-03 2006-08-02 Novi kristalni oblik iii agomelatina, postupak za njegovu pripremu i farmaceutski preparati istog ME02689B (me)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0508276A FR2889521B1 (fr) 2005-08-03 2005-08-03 Nouvelle forme cristalline iii de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent
EP10003436.2A EP2210872B1 (fr) 2005-08-03 2006-08-02 Nouvelle forme cristalline iii de l'agomélatine, son procédé de préparation et les compositions pharmaceutiques qui la contiennent

Publications (1)

Publication Number Publication Date
ME02689B true ME02689B (me) 2017-10-20

Family

ID=36587257

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2017-33A ME02689B (me) 2005-08-03 2006-08-02 Novi kristalni oblik iii agomelatina, postupak za njegovu pripremu i farmaceutski preparati istog

Country Status (35)

Country Link
EP (3) EP1752445A1 (me)
JP (1) JP4580370B2 (me)
CN (1) CN100450995C (me)
AR (1) AR057713A1 (me)
AU (1) AU2006203336B2 (me)
BR (1) BRPI0603074A (me)
CA (1) CA2555117A1 (me)
CY (1) CY1118637T1 (me)
DK (1) DK2210872T3 (me)
EA (1) EA011031B1 (me)
ES (1) ES2614934T3 (me)
FR (1) FR2889521B1 (me)
GE (1) GEP20094576B (me)
GT (1) GT200600347A (me)
HR (1) HRP20170095T1 (me)
HU (1) HUE030506T2 (me)
JO (1) JO3360B1 (me)
LT (1) LT2210872T (me)
MA (1) MA28449B1 (me)
ME (1) ME02689B (me)
MX (1) MXPA06008790A (me)
MY (1) MY142856A (me)
NO (1) NO337010B1 (me)
NZ (1) NZ548862A (me)
PE (1) PE20070213A1 (me)
PL (1) PL2210872T3 (me)
PT (1) PT2210872T (me)
RS (1) RS55499B1 (me)
SA (1) SA06270253B1 (me)
SG (1) SG130112A1 (me)
SI (1) SI2210872T1 (me)
TW (1) TWI389873B (me)
UA (1) UA83719C2 (me)
WO (1) WO2007015003A2 (me)
ZA (1) ZA200606454B (me)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2934856B1 (fr) * 2008-08-05 2010-08-13 Servier Lab Nouveau procede d'obtention de la forme cristalline v de l'agomelatine
CN101585779B (zh) * 2009-03-10 2014-04-02 上海医药工业研究院 阿戈美拉汀的晶型vi及其制备方法和应用
WO2011006387A1 (zh) * 2009-07-11 2011-01-20 浙江华海药业股份有限公司 阿戈美拉汀的制备方法、阿戈美拉汀晶形及其制备方法
CN102001959B (zh) * 2009-09-01 2014-07-02 北京本草天源药物研究院 一种药物晶体及其制备方法和用途
CN102050755B (zh) * 2009-10-29 2014-11-05 重庆医药工业研究院有限责任公司 阿戈美拉汀的晶型及其制备方法
CN101709036B (zh) * 2009-12-17 2012-07-04 天津药物研究院 阿戈美拉汀中间体2-(7-甲氧基-1-萘基)乙胺的制备
CN101781226B (zh) 2009-12-23 2012-03-28 天津泰普药品科技发展有限公司 阿戈美拉汀及其药物组合物
CN101774937B (zh) * 2010-02-05 2014-01-08 天津市汉康医药生物技术有限公司 N-[2-(7-甲氧基-1-萘基)乙基]乙酰胺及其组合物
CL2011001405A1 (es) 2010-06-10 2012-03-30 Gador S A Conicet Procedimiento para la preparacion de n-[2-(7-metoxi-1-naftil)etil]acetamida, agometalina.
CZ303787B6 (cs) * 2011-01-21 2013-05-02 Zentiva, K.S. Metastabilní krystalové formy agomelatinu a jejich farmaceutické kompozice
CN102690210A (zh) * 2011-03-23 2012-09-26 上海医药工业研究院 阿戈美拉汀的新晶型ⅶ、其制备方法、应用和包含其的药物组合物
CN102690209A (zh) * 2011-03-23 2012-09-26 上海医药工业研究院 阿戈美拉汀的混晶(形式-ⅷ)、其制备方法、应用和包含其的药物组合物
FR2978916B1 (fr) 2011-08-10 2013-07-26 Servier Lab Composition pharmaceutique solide pour administration buccale d'agomelatine
WO2013082302A1 (en) 2011-11-30 2013-06-06 Ratiopharm Gmbh Agomelatine-urea complex and crystalline forms thereof
CZ2012108A3 (en) 2012-02-15 2013-02-27 Zentiva Ks A method for the manufacture of a polymorphously stable pharmaceutical composition containing agomelatine
WO2014096373A1 (en) 2012-12-21 2014-06-26 Laboratorios Lesvi, S. L. Process for prepararing n-(2-(7-methoxy-1-naphthalenyl)ethyl) acetamide and solid forms thereof
FR3001894A1 (fr) 2013-02-08 2014-08-15 Servier Lab Composition pharmaceutique solide pour administration buccale d'agomelatine
EP2810647A1 (en) 2013-06-06 2014-12-10 Zentiva, a.s. Pharmaceutical formulations comprising agomelatine in the form of agomelatine co-crystal with an organic acid
ES2645223T3 (es) 2013-06-06 2017-12-04 Zentiva, K.S. Formulaciones de agomelatina que comprenden agomelatina en forma de co-cristales
CZ2013621A3 (cs) 2013-08-13 2015-02-25 Zentiva, K.S. Termodynamicky stabilní tuhý roztok agomelatinu pro použití ve farmaceutické formulaci
WO2015124496A1 (en) 2014-02-19 2015-08-27 Synthon B.V. Pharmaceutical composition comprising amorphous agomelatine
PL3075724T3 (pl) 2015-03-31 2023-12-27 F.I.S.- Fabbrica Italiana Sintetici S.P.A. Stała postać agomelatyny

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2658818B1 (fr) * 1990-02-27 1993-12-31 Adir Cie Nouveaux derives a structure naphtalenique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
FR2866335B1 (fr) * 2004-02-13 2006-05-26 Servier Lab Nouveau procede de synthese de l'agomelatine
FR2866336B1 (fr) * 2004-02-13 2006-03-24 Servier Lab Nouveau procede de synthese du (7-methoxy-3,4-dihydro-1-naphtalenyl) acetonitrile et application a la synthese de l'agomelatine

Also Published As

Publication number Publication date
EA011031B1 (ru) 2008-12-30
HRP20170095T1 (hr) 2017-03-24
FR2889521A1 (fr) 2007-02-09
PT2210872T (pt) 2016-12-01
SA06270253B1 (ar) 2011-05-14
ES2614934T3 (es) 2017-06-02
NO337010B1 (no) 2015-12-21
JO3360B1 (ar) 2019-03-13
GT200600347A (es) 2007-02-28
HUE030506T2 (en) 2017-05-29
WO2007015003A2 (fr) 2007-02-08
UA83719C2 (ru) 2008-08-11
CA2555117A1 (fr) 2007-02-03
LT2210872T (lt) 2017-01-10
RS55499B1 (sr) 2017-05-31
DK2210872T3 (en) 2017-02-20
JP2007051140A (ja) 2007-03-01
EA200601274A1 (ru) 2007-02-27
AR057713A1 (es) 2007-12-12
MY142856A (en) 2011-01-14
NZ548862A (en) 2008-03-28
PE20070213A1 (es) 2007-05-06
MXPA06008790A (es) 2008-02-04
EP2210872B1 (fr) 2016-11-16
SG130112A1 (en) 2007-03-20
ZA200606454B (en) 2007-12-27
EP2210872A1 (fr) 2010-07-28
PL2210872T3 (pl) 2017-07-31
CN1907959A (zh) 2007-02-07
BRPI0603074A (pt) 2007-08-14
GEP20094576B (en) 2009-01-12
NO20063516L (no) 2007-02-05
SI2210872T1 (sl) 2017-03-31
EP2008993A1 (fr) 2008-12-31
TWI389873B (zh) 2013-03-21
AU2006203336A1 (en) 2007-02-22
CN100450995C (zh) 2009-01-14
WO2007015003A3 (fr) 2007-04-05
CY1118637T1 (el) 2017-07-12
EP1752445A1 (fr) 2007-02-14
JP4580370B2 (ja) 2010-11-10
HK1098130A1 (zh) 2007-07-13
AU2006203336B2 (en) 2012-07-12
FR2889521B1 (fr) 2007-12-28
MA28449B1 (fr) 2007-03-01
TW200736197A (en) 2007-10-01

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