AR046643A1 - Derivados de pirrol - Google Patents

Derivados de pirrol

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Publication number
AR046643A1
AR046643A1 ARP040104272A ARP040104272A AR046643A1 AR 046643 A1 AR046643 A1 AR 046643A1 AR P040104272 A ARP040104272 A AR P040104272A AR P040104272 A ARP040104272 A AR P040104272A AR 046643 A1 AR046643 A1 AR 046643A1
Authority
AR
Argentina
Prior art keywords
hal
mono
nha
unsubstituted
het1
Prior art date
Application number
ARP040104272A
Other languages
English (en)
Inventor
Finsinger Dirk Dr
Buchstaller Hans-Peter Dr
Burgdorf Lars Dr
Wiesner Matthias Dr
Amendt Christiane Dr
Matthias Drgrell
Zenke Frank Dr
Sirrenberg Christian Dr
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR046643A1 publication Critical patent/AR046643A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • 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
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    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/00Drugs for dermatological disorders
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
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    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
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    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Los compuestos de la fórmula (1), en donde: Ar es fenilo, naftilo, bifenilo o Het insustituido o mono, di, tri o tetrasustituido con R1; X es -O-, -S-, -(CH2)n-, -C(=O)-, -CH(OH)-, -(CH2)nO-, -O(CH2)n-, -(CH2)nS-, -S(CH2)n-, -(CH2)nNH-, -NH(CH2)n-, - (CH2)nNA-, -NA(CH2)n-, -CHHal- o -C(Hal)2-; Y es O, S, CH-NO2, C(CN)2 o N-R4; Z es -Ar, -Ar-X-Ar, -CH2-Ar o -CH2-Ar-X-Ar; Het es un heterociclo aromático mono o bicíclico con 1 a 4 átomos de N, O y/o S; R1 es A, Ar', OR3, SR3, OAr', SAr', N(R3)2, NHAr', Hal, NO2, CN, (CH2)mCOOR3, (CH2)mCON(R3)2, COR3, S(O)mA, S(O)mAr', NHCOA, NHCOAr', NHSO2A, NHSO2Ar', SO2N(R3)2, -O-(CH2)p-NH2, -O-(CH2)p-NHA, -O-(CH2)p-NA2, -NH-(CH2)p-NH2, -NH-(CH2)-NHA, -NH-(CH2)p-NA2, -NA-(CH2)p-NH2, -NA-(CH2)p-NHA, -NA- (CH2)p-NA2, -O-(CH2)n-Het1 o Het1; R3 es H, A o -(CH2)nAr'; R4 es H, CN, OH, A, (CH2)mAr', COR3, COAr', S(O)mA o S(O)mAr'; Ar' es fenilo insustituido o mono, di, tri, tetra o pentasustituido con A, Ph, OH, OA, SH, SA, OPh, SPh, NH2, NHA, NA2, NHPh, Hal, NO2, CN, (CH2)mCOOH, (CH2)mCOOA, (CH2)mCONH2, (CH2)mCONHA, CHO, COA, S(O)mA, S(O)mPh, NHCOA, NHCOPh, NHSO2A, NHSO2Ph o SO2NH2; Ph es fenilo insustituido o mono, di o trisustituido con A, Hal, CN, CO-OR, COOH, NH2, NO2, OH u OA; Het1 es un heterociclo saturado monocíclico con 1 a 4 átomos de N, O y/o S, que puede estar insustituido, o mono, di o trisustituido con Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NH2, =NH, =N-OH, =N-OA y/o el oxígeno del carbonilo (=O); A es alquilo C1-10, en donde también 1-7 átomos de H pueden estar reemplazados por F y/o cloro; Hal es F, Cl, Br o I; n es 0, 1, 2 ó 3; m es 0, 1 ó 2; p es 1, 2, 3 ó 4; así como sus derivados, solvatos, sales y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidoras de la Raf-quinasa y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
ARP040104272A 2003-11-19 2004-11-19 Derivados de pirrol AR046643A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10354060A DE10354060A1 (de) 2003-11-19 2003-11-19 Pyrrolderivate

Publications (1)

Publication Number Publication Date
AR046643A1 true AR046643A1 (es) 2005-12-14

Family

ID=34530259

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040104272A AR046643A1 (es) 2003-11-19 2004-11-19 Derivados de pirrol

Country Status (19)

Country Link
US (1) US7598274B2 (es)
EP (1) EP1685125B1 (es)
JP (1) JP4805839B2 (es)
KR (1) KR20060118492A (es)
CN (1) CN1882571A (es)
AR (1) AR046643A1 (es)
AU (1) AU2004291255B2 (es)
BR (1) BRPI0416690A (es)
CA (1) CA2546334C (es)
CY (1) CY1112947T1 (es)
DE (1) DE10354060A1 (es)
DK (1) DK1685125T3 (es)
ES (1) ES2385329T3 (es)
MX (1) MXPA06005478A (es)
PL (1) PL1685125T3 (es)
PT (1) PT1685125E (es)
SI (1) SI1685125T1 (es)
WO (1) WO2005049603A1 (es)
ZA (1) ZA200604968B (es)

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PT1478358E (pt) 2002-02-11 2013-09-11 Bayer Healthcare Llc Tosilato de sorafenib para o tratamento de doenças caracterizadas por angiogénese anormal
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
JP2007511203A (ja) 2003-05-20 2007-05-10 バイエル、ファーマシューテイカルズ、コーポレイション キナーゼ阻害活性を有するジアリール尿素
DE602004010407T2 (de) 2003-07-23 2008-10-16 Bayer Pharmaceuticals Corp., West Haven Fluorsubstituierter omega-carboxyaryldiphenylharnstoff zur behandlung und prävention von krankheiten und leiden
US7459562B2 (en) 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
FR2881426B1 (fr) * 2005-02-03 2007-03-30 Aventis Pharma Sa Pyrolles et imidazoles substitues, compositions les contenant, procede de frabrication et utilisation
FR2881742B1 (fr) 2005-02-10 2007-09-07 Aventis Pharma Sa Pyrroles substitues, compositions les contenant, procede de fabrication et utilisation
CN101679243B (zh) * 2007-04-09 2012-09-26 第一三共株式会社 吡咯衍生物的阻转异构体
PT2424843E (pt) 2009-04-30 2014-06-02 Novartis Ag Derivados de imidazol e seu uso como moduladores de quinases dependentes de ciclina
JP5620979B2 (ja) * 2009-05-05 2014-11-05 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. P38キナーゼ阻害剤
CN102146074B (zh) * 2011-01-26 2013-02-06 江苏先声药物研究有限公司 吡咯衍生物的制备方法及应用
US9199975B2 (en) 2011-09-30 2015-12-01 Asana Biosciences, Llc Biaryl imidazole derivatives for regulating CYP17
US8809372B2 (en) 2011-09-30 2014-08-19 Asana Biosciences, Llc Pyridine derivatives
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
US20180251425A1 (en) * 2015-08-17 2018-09-06 University Of Mysore 2,3,5 trisubstituted pyrrole derivatives as topoisomerase inhibitors and therapeutic uses thereof
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JP7416716B2 (ja) 2017-12-28 2024-01-17 トラクト ファーマシューティカルズ インコーポレイテッド 円柱上皮幹細胞のための幹細胞培養系およびそれに関連した使用法
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BRPI0416690A (pt) 2007-01-30
CA2546334A1 (en) 2005-06-02
PT1685125E (pt) 2012-09-12
EP1685125A1 (de) 2006-08-02
PL1685125T3 (pl) 2012-10-31
WO2005049603A1 (de) 2005-06-02
JP2007511553A (ja) 2007-05-10
KR20060118492A (ko) 2006-11-23
AU2004291255A1 (en) 2005-06-02
DK1685125T3 (da) 2012-07-23
ZA200604968B (en) 2007-10-31
SI1685125T1 (sl) 2012-08-31
US7598274B2 (en) 2009-10-06
CY1112947T1 (el) 2016-04-13
MXPA06005478A (es) 2006-08-11
DE10354060A1 (de) 2005-06-02
JP4805839B2 (ja) 2011-11-02
CN1882571A (zh) 2006-12-20
AU2004291255B2 (en) 2011-02-03
US20070149594A1 (en) 2007-06-28
ES2385329T3 (es) 2012-07-23
CA2546334C (en) 2012-06-19
EP1685125B1 (de) 2012-06-06

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