ATE375156T1 - Benzimidazol-derivate als menschliche chymase - inhibitoren - Google Patents

Benzimidazol-derivate als menschliche chymase - inhibitoren

Info

Publication number: ATE375156T1
Authority: AT; Austria
Prior art keywords: halo; optionally substituted; oxo; trihalomethyl; alk
Prior art date: 2000-01-17

Application number

AT01901397T

Other languages

English (en)

Inventor

Naoki Tsuchiya

Yoshiyuki Matsumoto

Hiroshi Saitou

Tsuyoshi Mizuno

Original Assignee

Teijin Pharma Ltd

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.)

2000-01-17

Filing date

2001-01-17

Publication date

2007-10-15

2001-01-17 Application filed by Teijin Pharma Ltd filed Critical Teijin Pharma Ltd

2007-10-15 Application granted granted Critical

2007-10-15 Publication of ATE375156T1 publication Critical patent/ATE375156T1/de

Links

229940058303 antinematodal benzimidazole derivative Drugs 0.000 title abstract 3
150000001556 benzimidazoles Chemical class 0.000 title abstract 3
101000909983 Homo sapiens Chymase Proteins 0.000 title abstract 2
239000003601 chymase inhibitor Substances 0.000 title abstract 2
125000001475 halogen functional group Chemical group 0.000 abstract 6
125000004953 trihalomethyl group Chemical group 0.000 abstract 4
DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 abstract 3
125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 abstract 3
125000000217 alkyl group Chemical group 0.000 abstract 3
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 3
125000004043 oxo group Chemical group O=* 0.000 abstract 3
125000004951 trihalomethoxy group Chemical group 0.000 abstract 3
WMNWZTLQAKKZDD-UHFFFAOYSA-N 4-[1-[(1,4-dimethylindol-3-yl)methyl]benzimidazol-2-yl]sulfanylbutanoic acid Chemical compound OC(=O)CCCSC1=NC2=CC=CC=C2N1CC1=CN(C)C2=C1C(C)=CC=C2 WMNWZTLQAKKZDD-UHFFFAOYSA-N 0.000 abstract 2
-1 5-oxo-1,2,4-thiadiazol-3-yl Chemical group 0.000 abstract 2
125000002252 acyl group Chemical group 0.000 abstract 2
125000004442 acylamino group Chemical group 0.000 abstract 2
125000002947 alkylene group Chemical group 0.000 abstract 2
125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 2
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
229940119334 Chymase inhibitor Drugs 0.000 abstract 1
241000700159 Rattus Species 0.000 abstract 1
125000003545 alkoxy group Chemical group 0.000 abstract 1
230000003266 anti-allergic effect Effects 0.000 abstract 1
230000003110 anti-inflammatory effect Effects 0.000 abstract 1
238000003556 assay Methods 0.000 abstract 1
239000008280 blood Substances 0.000 abstract 1
210000004369 blood Anatomy 0.000 abstract 1
230000000694 effects Effects 0.000 abstract 1
125000001072 heteroaryl group Chemical group 0.000 abstract 1
230000010534 mechanism of action Effects 0.000 abstract 1
230000000241 respiratory effect Effects 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1
125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Physical Education & Sports Medicine (AREA)
Rheumatology (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Immunology (AREA)
Pulmonology (AREA)
Dermatology (AREA)
Hematology (AREA)
Obesity (AREA)
Orthopedic Medicine & Surgery (AREA)
Diabetes (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Pain & Pain Management (AREA)
Endocrinology (AREA)
Otolaryngology (AREA)
Hospice & Palliative Care (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Medicinal Preparation (AREA)

AT01901397T 2000-01-17 2001-01-17 Benzimidazol-derivate als menschliche chymase - inhibitoren ATE375156T1 (de)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
JP2000007533		2000-01-17
JP2000392303		2000-12-25

Publications (1)

Publication Number	Publication Date
ATE375156T1 true ATE375156T1 (de)	2007-10-15

Family

ID=26583615

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT01901397T ATE375156T1 (de)	2000-01-17	2001-01-17	Benzimidazol-derivate als menschliche chymase - inhibitoren

Country Status (18)

Country	Link
EP (1)	EP1249450B1 (de)
JP (1)	JP4059671B2 (de)
KR (2)	KR100763779B1 (de)
CN (2)	CN100415723C (de)
AT (1)	ATE375156T1 (de)
AU (2)	AU777813B2 (de)
CA (1)	CA2396908A1 (de)
CZ (1)	CZ301504B6 (de)
DE (1)	DE60130865T2 (de)
DK (1)	DK1249450T3 (de)
ES (1)	ES2295128T3 (de)
IL (1)	IL150565A0 (de)
NO (1)	NO324049B1 (de)
NZ (1)	NZ520028A (de)
PT (1)	PT1249450E (de)
RU (1)	RU2263674C2 (de)
SI (1)	SI1249450T1 (de)
WO (1)	WO2001053291A1 (de)

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ATE404551T1 (de) *	2001-05-07	2008-08-15	Teijin Pharma Ltd	3-hydroxymethylbenzo b thiophen-derivate und verfahren zu deren herstellung
KR100902799B1 (ko) *	2001-08-24	2009-06-12	데이진 가부시키가이샤	키마제 저해제 및 ａｃｅ 저해제를 유효성분으로 함유하는약제
CL2004001034A1 (es) *	2003-05-14	2005-03-28	Teijin Pharma Ltd	Formas cristalinas de acido 4-(1-((,etilbenzotiofen-3-il)me til)benzimidazol-2-iltio)butanoico; procedimiento de preparacion de las formas cristalinas; composicion farmaceutica; y su uso para el tratamiento de enfermedades inflamatorias, alergicas, r
AU2004266536A1 (en) *	2003-08-22	2005-03-03	Teijin Pharma Limited	Drug containing chymase inhibitor as the active ingredient
US20080015240A1 (en) *	2004-11-12	2008-01-17	Mitsuru Teramoto	Acid Salt of Benzimidazole Derivative and Crystal Thereof
US20090155361A1 (en)	2005-08-18	2009-06-18	Masahiko Narasaki	Tablet with multiple drug-containing sections
JP5059611B2 (ja)	2005-08-18	2012-10-24	帝人ファーマ株式会社	正確な用量分割機能を有する製剤
JPWO2007049812A1 (ja)	2005-10-27	2009-04-30	帝人ファーマ株式会社	３−ヒドロキシメチルベンゾ［ｂ］チオフェン誘導体およびその製造方法
JP2007145827A (ja)	2005-10-27	2007-06-14	Teijin Pharma Ltd	ベンゾ［ｂ］チオフェン誘導体およびその製造方法
PE20070698A1 (es)	2005-11-14	2007-08-17	Teijin Pharma Ltd	Comprimido de disgregacion rapida intraoral que contiene hidrocloruro de ambroxol
UA95788C2 (en) *	2005-12-15	2011-09-12	Ф. Хоффманн-Ля Рош Аг	Fused pyrrole derivatives
CA2687821C (en)	2007-05-22	2015-04-14	Boehringer Ingelheim International Gmbh	Benzimidazolone chymase inhibitors
US9242933B2 (en) *	2007-05-25	2016-01-26	AbbVie Deutschland GmbH & Co. KG	Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mGlu2 receptor)
WO2008153129A1 (ja) *	2007-06-14	2008-12-18	Teijin Pharma Limited	尿酸値低下剤
WO2009133964A1 (ja) *	2008-04-28	2009-11-05	国立大学法人九州大学	酸化ストレス抑制剤
JP5662319B2 (ja) *	2008-09-09	2015-01-28	ベーリンガーインゲルハイムインターナショナルゲゼルシャフトミットベシュレンクテルハフツング	アザ−ベンゾイミダゾロンキマーゼ阻害剤
CN102361857B (zh)	2008-09-26	2015-09-16	默沙东公司	可用作抗糖尿病剂的环状苯并咪唑衍生物
EP2348857B1 (de)	2008-10-22	2016-02-24	Merck Sharp & Dohme Corp.	Neue cyclische benzimidazolderivate als antidiabetika
CN102271511A (zh)	2008-10-29	2011-12-07	默沙东公司	可用作抗糖尿病剂的新颖的环状苯并咪唑衍生物
JP5557845B2 (ja)	2008-10-31	2014-07-23	メルク・シャープ・アンド・ドーム・コーポレーション	糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体
TW201121957A (en) *	2009-11-18	2011-07-01	Astrazeneca Ab	Benzoimidazole compounds and uses thereof
AU2011218830B2 (en)	2010-02-25	2014-07-24	Merck Sharp & Dohme Corp.	Novel cyclic benzimidazole derivatives useful anti-diabetic agents
MX348131B (es)	2011-02-25	2017-05-26	Merck Sharp & Dohme	Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos.
JP6180514B2 (ja) *	2012-05-04	2017-08-16	ノバルティスアーゲー	補体経路モジュレーターおよびその使用
WO2014022528A1 (en)	2012-08-02	2014-02-06	Merck Sharp & Dohme Corp.	Antidiabetic tricyclic compounds
US9382243B2 (en)	2012-08-22	2016-07-05	Merck Sharp & Dohme Corp.	Azabenzimidazole tetrahydropyran derivatives
EP2888008B1 (de)	2012-08-22	2018-12-26	Merck Sharp & Dohme Corp.	Neuartige azabenzimidazol-tetrahydrofuranderivate
WO2014031441A1 (en)	2012-08-22	2014-02-27	Merck Sharp & Dohme Corp.	Novel benzimidazole tetrahydrofuran derivatives
JP2015526468A (ja)	2012-08-22	2015-09-10	メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋＳｈａｒｐ＆ＤｏｈｍｅＣｏｒｐ．	新規なアザベンズイミダゾールヘキサヒドロフロ［３，２−ｂ］フラン誘導体
WO2014031445A1 (en)	2012-08-22	2014-02-27	Merck Sharp & Dohme Corp.	Novel benzimidazole tetrahydropyran derivatives
ES2755087T3 (es)	2012-08-22	2020-04-21	Merck Sharp & Dohme	Derivados de benzimidazol hexahidrofuro[3,2-b]furano útiles como activadores de proteína cinasa activada por AMP
WO2014139388A1 (en)	2013-03-14	2014-09-18	Merck Sharp & Dohme Corp.	Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en)	2013-10-08	2015-04-16	Merck Sharp & Dohme Corp.	Antidiabetic tricyclic compounds
US10519115B2 (en)	2013-11-15	2019-12-31	Merck Sharp & Dohme Corp.	Antidiabetic tricyclic compounds
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CN111004125B (zh) *	2019-12-24	2022-11-22	东华理工大学	一种缩醛或缩酮化合物的制备方法
CN116903541B (zh) *	2023-08-14	2023-12-08	中国环境科学研究院	用于酚类污染物检测的酰基咪唑类化合物、制备方法及应用

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2001
- 2001-01-17 PT PT01901397T patent/PT1249450E/pt unknown
- 2001-01-17 EP EP01901397A patent/EP1249450B1/de not_active Expired - Lifetime
- 2001-01-17 AU AU27049/01A patent/AU777813B2/en not_active Ceased
- 2001-01-17 JP JP2001553765A patent/JP4059671B2/ja not_active Expired - Fee Related
- 2001-01-17 CZ CZ20022442A patent/CZ301504B6/cs not_active IP Right Cessation
- 2001-01-17 IL IL15056501A patent/IL150565A0/xx not_active IP Right Cessation
- 2001-01-17 WO PCT/JP2001/000271 patent/WO2001053291A1/ja not_active Ceased
- 2001-01-17 ES ES01901397T patent/ES2295128T3/es not_active Expired - Lifetime
- 2001-01-17 DK DK01901397T patent/DK1249450T3/da active
- 2001-01-17 KR KR1020027009200A patent/KR100763779B1/ko not_active Expired - Fee Related
- 2001-01-17 CN CNB2005100526041A patent/CN100415723C/zh not_active Expired - Fee Related
- 2001-01-17 CA CA002396908A patent/CA2396908A1/en not_active Abandoned
- 2001-01-17 DE DE60130865T patent/DE60130865T2/de not_active Expired - Lifetime
- 2001-01-17 KR KR1020077010650A patent/KR20070057276A/ko not_active Abandoned
- 2001-01-17 AT AT01901397T patent/ATE375156T1/de not_active IP Right Cessation
- 2001-01-17 CN CNB018066623A patent/CN1198819C/zh not_active Expired - Fee Related
- 2001-01-17 NZ NZ520028A patent/NZ520028A/en unknown
- 2001-01-17 RU RU2002122105/04A patent/RU2263674C2/ru not_active IP Right Cessation
- 2001-01-17 SI SI200130792T patent/SI1249450T1/sl unknown
2002
- 2002-07-16 NO NO20023415A patent/NO324049B1/no not_active IP Right Cessation
2005
- 2005-01-14 AU AU2005200172A patent/AU2005200172B2/en not_active Ceased

Also Published As

Publication number	Publication date
CN1680339A (zh)	2005-10-12
CN100415723C (zh)	2008-09-03
RU2263674C2 (ru)	2005-11-10
IL150565A0 (en)	2003-02-12
ES2295128T3 (es)	2008-04-16
HK1050009A1 (en)	2003-06-06
JP4059671B2 (ja)	2008-03-12
EP1249450A1 (de)	2002-10-16
DE60130865D1 (de)	2007-11-22
CN1418211A (zh)	2003-05-14
KR100763779B1 (ko)	2007-10-05
EP1249450B1 (de)	2007-10-10
EP1249450A4 (de)	2003-04-09
CA2396908A1 (en)	2001-07-26
AU2005200172A1 (en)	2005-02-10
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