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
Prior art date
Legal status (The legal status 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 status listed.)
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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Publication date
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)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (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)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (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
GB0017174A GB0017174D0 (en) 2000-07-12 2000-07-12 Organic compounds
GB0017174.4 2000-07-12
GB0023326A GB0023326D0 (en) 2000-09-22 2000-09-22 Organic compounds
GB0023326.2 2000-09-22

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 (enExample)
EP (1) EP1303488B1 (enExample)
JP (1) JP2004502756A (enExample)
KR (1) KR20030036603A (enExample)
CN (1) CN1184204C (enExample)
AR (1) AR031597A1 (enExample)
AT (1) ATE447553T1 (enExample)
AU (2) AU2001281972B2 (enExample)
BR (1) BR0112456A (enExample)
CA (1) CA2412941C (enExample)
CZ (1) CZ200375A3 (enExample)
DE (1) DE60140366D1 (enExample)
ES (1) ES2334886T3 (enExample)
HU (1) HUP0301341A2 (enExample)
IL (1) IL153661A0 (enExample)
MX (1) MXPA02012848A (enExample)
MY (1) MY126139A (enExample)
NO (1) NO324760B1 (enExample)
NZ (1) NZ523414A (enExample)
PE (1) PE20020616A1 (enExample)
PL (1) PL358673A1 (enExample)
PT (1) PT1303488E (enExample)
SK (1) SK272003A3 (enExample)
TW (1) TWI227231B (enExample)
WO (1) WO2002004420A1 (enExample)

Families Citing this family (30)

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Publication number Priority date Publication date Assignee Title
DE19952147A1 (de) * 1999-10-29 2001-05-03 Boehringer Ingelheim Pharma Neue Cyclopropane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US7034042B2 (en) * 2000-10-09 2006-04-25 Novartis Ag N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as CCR33 receptor antagonists
GB0114699D0 (en) * 2001-06-15 2001-08-08 Novartis Ag Organic compounds
PL1670482T5 (pl) * 2003-09-16 2022-10-03 Covis Pharma Gmbh Zastosowanie cyklezonidu w leczeniu chorób układu oddechowego
AU2014239542A1 (en) * 2013-03-15 2015-10-01 Araxes Pharma Llc Covalent inhibitors of KRas G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC 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
EP3356339A1 (en) 2015-09-28 2018-08-08 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
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058915A1 (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
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
TW201726656A (zh) 2015-11-16 2017-08-01 亞瑞克西斯製藥公司 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法
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
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 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
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
WO2018218071A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
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
TW201900633A (zh) 2017-05-25 2019-01-01 美商亞瑞克西斯製藥公司 Kras之共價抑制劑
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer

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CA2296314A1 (en) * 1997-07-25 1999-02-04 Merck & Co., Inc. Cyclic amine modulators of chemokine receptor activity
IL125658A0 (en) * 1997-08-18 1999-04-11 Hoffmann La Roche Ccr-3 receptor antagonists
US6339087B1 (en) 1997-08-18 2002-01-15 Syntex (U.S.A.) Llc Cyclic amine derivatives-CCR-3 receptor antagonists
JP3475177B2 (ja) 1998-11-17 2003-12-08 エフ．ホフマン−ラ ロシュ アーゲー ４−アロイルピペリジンｃｃｒ−３受容体拮抗剤ｉｉｉ
WO2000035454A1 (en) 1998-12-18 2000-06-22 Du Pont Pharmaceuticals Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
EE200100502A (et) * 1999-03-26 2002-12-16 Astrazeneca Ab Ühendid

Also Published As

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

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