CN1184204C - 用作ccr－3抑制剂的哌啶化合物 - Google Patents

用作ccr－3抑制剂的哌啶化合物 Download PDF

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Publication number
CN1184204C
CN1184204C CNB018126111A CN01812611A CN1184204C CN 1184204 C CN1184204 C CN 1184204C CN B018126111 A CNB018126111 A CN B018126111A CN 01812611 A CN01812611 A CN 01812611A CN 1184204 C CN1184204 C CN 1184204C
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CN
China
Prior art keywords
phenyl
substituted
alkyl
halogen
general formula
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Expired - Fee Related
Application number
CNB018126111A
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English (en)
Chinese (zh)
Other versions
CN1441780A (zh
Inventor
T·J·豪
G·巴莱
D·M·勒格兰德
T·施托尔茨
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Novartis AG
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Novartis AG
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Priority claimed from GB0017174A external-priority patent/GB0017174D0/en
Priority claimed from GB0023326A external-priority patent/GB0023326D0/en
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN1441780A publication Critical patent/CN1441780A/zh
Application granted granted Critical
Publication of CN1184204C publication Critical patent/CN1184204C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNB018126111A 2000-07-12 2001-07-10 用作ccr－3抑制剂的哌啶化合物 Expired - Fee Related CN1184204C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0017174.4 2000-07-12
GB0017174A GB0017174D0 (en) 2000-07-12 2000-07-12 Organic compounds
GB0023326.2 2000-09-22
GB0023326A GB0023326D0 (en) 2000-09-22 2000-09-22 Organic compounds

Publications (2)

Publication Number Publication Date
CN1441780A CN1441780A (zh) 2003-09-10
CN1184204C true CN1184204C (zh) 2005-01-12

Family

ID=26244644

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB018126111A Expired - Fee Related CN1184204C (zh) 2000-07-12 2001-07-10 用作ccr－3抑制剂的哌啶化合物

Country Status (25)

Country Link
US (1) US6670379B2 (cg-RX-API-DMAC7.html)
EP (1) EP1303488B1 (cg-RX-API-DMAC7.html)
JP (1) JP2004502756A (cg-RX-API-DMAC7.html)
KR (1) KR20030036603A (cg-RX-API-DMAC7.html)
CN (1) CN1184204C (cg-RX-API-DMAC7.html)
AR (1) AR031597A1 (cg-RX-API-DMAC7.html)
AT (1) ATE447553T1 (cg-RX-API-DMAC7.html)
AU (2) AU8197201A (cg-RX-API-DMAC7.html)
BR (1) BR0112456A (cg-RX-API-DMAC7.html)
CA (1) CA2412941C (cg-RX-API-DMAC7.html)
CZ (1) CZ200375A3 (cg-RX-API-DMAC7.html)
DE (1) DE60140366D1 (cg-RX-API-DMAC7.html)
ES (1) ES2334886T3 (cg-RX-API-DMAC7.html)
HU (1) HUP0301341A2 (cg-RX-API-DMAC7.html)
IL (1) IL153661A0 (cg-RX-API-DMAC7.html)
MX (1) MXPA02012848A (cg-RX-API-DMAC7.html)
MY (1) MY126139A (cg-RX-API-DMAC7.html)
NO (1) NO324760B1 (cg-RX-API-DMAC7.html)
NZ (1) NZ523414A (cg-RX-API-DMAC7.html)
PE (1) PE20020616A1 (cg-RX-API-DMAC7.html)
PL (1) PL358673A1 (cg-RX-API-DMAC7.html)
PT (1) PT1303488E (cg-RX-API-DMAC7.html)
SK (1) SK272003A3 (cg-RX-API-DMAC7.html)
TW (1) TWI227231B (cg-RX-API-DMAC7.html)
WO (1) WO2002004420A1 (cg-RX-API-DMAC7.html)

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DE19952147A1 (de) * 1999-10-29 2001-05-03 Boehringer Ingelheim Pharma Neue Cyclopropane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
BR0114485A (pt) * 2000-10-09 2003-11-18 Novartis Ag Amidas n-(4-ariloxipiperidin-1-ilalquil)cin micas como antagonistas de receptor de ccr33
GB0114699D0 (en) 2001-06-15 2001-08-08 Novartis Ag Organic compounds
JP5618452B2 (ja) 2003-09-16 2014-11-05 タケダ ゲゼルシャフト ミット ベシュレンクテル ハフツングＴａｋｅｄａ ＧｍｂＨ 呼吸器疾患の治療のためのシクレソニドの使用
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
MX364438B (es) * 2013-03-15 2019-04-26 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
CA2982360A1 (en) 2015-04-15 2016-10-20 Liansheng Li Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
MX2018005967A (es) 2015-11-16 2018-08-29 Araxes Pharma Llc Compuestos de quinazolina 2-sustituida que comprenden un grupo heterociclico sustituido y metodos de uso de los mismos.
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
CN110036010A (zh) 2016-09-29 2019-07-19 亚瑞克西斯制药公司 Kras g12c突变蛋白的抑制剂
WO2018068017A1 (en) 2016-10-07 2018-04-12 Araxes Pharma Llc Heterocyclic compounds as inhibitors of ras and methods of use thereof
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11059819B2 (en) 2017-01-26 2021-07-13 Janssen Biotech, Inc. Fused hetero-hetero bicyclic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
JP2020521740A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体ｋｒａｓ、ｈｒａｓまたはｎｒａｓの調節因子としてのキナゾリン誘導体
MX2019013954A (es) 2017-05-25 2020-08-31 Araxes Pharma Llc Inhibidores covalentes de kras.
KR20210045998A (ko) 2018-08-01 2021-04-27 아락세스 파마 엘엘씨 헤테로사이클릭 스피로 화합물 및 암 치료를 위한 그의 사용 방법

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IL125658A0 (en) 1997-08-18 1999-04-11 Hoffmann La Roche Ccr-3 receptor antagonists
ES2230899T3 (es) 1998-11-17 2005-05-01 F. Hoffmann-La Roche Ag Antagonistas iii receptores de 4-aroil-piperidin-ccr-3.
CA2348923A1 (en) * 1998-12-18 2000-06-22 Dean A. Wacker N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
EP1165545A1 (en) * 1999-03-26 2002-01-02 AstraZeneca AB Novel compounds

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Publication number Publication date
PL358673A1 (en) 2004-08-09
ES2334886T3 (es) 2010-03-17
MY126139A (en) 2006-09-29
NZ523414A (en) 2004-07-30
MXPA02012848A (es) 2003-05-15
PE20020616A1 (es) 2002-08-02
NO20030135D0 (no) 2003-01-10
PT1303488E (pt) 2010-01-19
IL153661A0 (en) 2003-07-06
CN1441780A (zh) 2003-09-10
KR20030036603A (ko) 2003-05-09
NO20030135L (no) 2003-02-19
TWI227231B (en) 2005-02-01
HUP0301341A2 (hu) 2003-08-28
CZ200375A3 (cs) 2003-04-16
AU2001281972B2 (en) 2004-06-03
US20030176460A1 (en) 2003-09-18
BR0112456A (pt) 2003-07-22
US6670379B2 (en) 2003-12-30
SK272003A3 (en) 2003-07-01
AU8197201A (en) 2002-01-21
EP1303488A1 (en) 2003-04-23
CA2412941A1 (en) 2002-01-17
CA2412941C (en) 2011-01-04
NO324760B1 (no) 2007-12-10
ATE447553T1 (de) 2009-11-15
WO2002004420A1 (en) 2002-01-17
EP1303488B1 (en) 2009-11-04
JP2004502756A (ja) 2004-01-29
DE60140366D1 (de) 2009-12-17
AR031597A1 (es) 2003-09-24

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