CN1500089A - 作为辣椒素受体拮抗剂用于治疗疼痛的稠合吡啶衍生物 - Google Patents

作为辣椒素受体拮抗剂用于治疗疼痛的稠合吡啶衍生物 Download PDF

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Publication number
CN1500089A
CN1500089A CNA028073495A CN02807349A CN1500089A CN 1500089 A CN1500089 A CN 1500089A CN A028073495 A CNA028073495 A CN A028073495A CN 02807349 A CN02807349 A CN 02807349A CN 1500089 A CN1500089 A CN 1500089A
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China
Prior art keywords
alkyl
compound
treatment
hydrogen
free alkali
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Pending
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CNA028073495A
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English (en)
Chinese (zh)
Inventor
A��J���Ϳ�
A·J·卡尚
P·格尔
A·哈利特
H-Y·金
M·P塞勒
K·齐默尔曼
�ɳ��
Y·刘
M·普拉沙德
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Novartis AG
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Novartis AG
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Priority claimed from GB0107505A external-priority patent/GB0107505D0/en
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN1500089A publication Critical patent/CN1500089A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • A61P11/14—Antitussive agents
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CNA028073495A 2001-03-26 2002-03-25 作为辣椒素受体拮抗剂用于治疗疼痛的稠合吡啶衍生物 Pending CN1500089A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0107505A GB0107505D0 (en) 2001-03-26 2001-03-26 Organic compounds
GB0107505.0 2001-03-26
US33828101P 2001-12-06 2001-12-06
US60/338,281 2001-12-06

Publications (1)

Publication Number Publication Date
CN1500089A true CN1500089A (zh) 2004-05-26

Family

ID=26245894

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA028073495A Pending CN1500089A (zh) 2001-03-26 2002-03-25 作为辣椒素受体拮抗剂用于治疗疼痛的稠合吡啶衍生物

Country Status (17)

Country Link
US (1) US7915264B2 (enExample)
EP (1) EP1377576A2 (enExample)
JP (1) JP4205430B2 (enExample)
KR (1) KR20030083755A (enExample)
CN (1) CN1500089A (enExample)
BR (1) BR0208338A (enExample)
CA (1) CA2441599A1 (enExample)
CZ (1) CZ20032561A3 (enExample)
HU (1) HUP0303623A2 (enExample)
IL (1) IL157815A0 (enExample)
MX (1) MXPA03008754A (enExample)
NO (1) NO326546B1 (enExample)
PE (1) PE20021161A1 (enExample)
PL (1) PL363907A1 (enExample)
RU (1) RU2003130221A (enExample)
SK (1) SK11952003A3 (enExample)
WO (1) WO2002076946A2 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101754774B (zh) * 2007-07-18 2013-08-21 诺瓦提斯公司 Vr-1拮抗剂和cox-2抑制剂的协同组合
CN103382176A (zh) * 2005-10-19 2013-11-06 格吕伦塔尔有限公司 新颖的辣椒素受体配体和它们用于生产药物的用途
CN108863949A (zh) * 2018-07-09 2018-11-23 湖南博隽生物医药有限公司 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法
CN114605408A (zh) * 2022-03-30 2022-06-10 沈阳药科大学 5-羟基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制法和应用

Families Citing this family (37)

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NZ523882A (en) 2000-08-21 2004-11-26 Pacific Corp Novel thiourea derivatives and the pharmaceutical compositions containing the same
EP1311478B1 (en) 2000-08-21 2006-06-07 Pacific Corporation Novel (thio)urea compounds and the pharmaceutical compositions containing the same
RS63204A (sr) 2002-01-17 2006-10-27 Neurogen Corporation Supstituisani analozi hinazolin-4-ilamina kao modulatori kapsaicina
AU2003212882A1 (en) 2002-02-01 2003-09-02 Euro-Celtique S.A. 2 - piperazine - pyridines useful for treating pain
US6864261B2 (en) 2002-05-02 2005-03-08 Euro-Celtique S.A. Therapeutic agents useful for treating pain
GB0229808D0 (en) 2002-12-20 2003-01-29 Glaxo Group Ltd Novel compositions
US7531558B2 (en) 2003-02-14 2009-05-12 Glaxo Group Limited Carboxamide derivatives
ATE556067T1 (de) 2003-05-20 2012-05-15 Ajinomoto Kk Modulatoren des vanilloid rezeptors
GB0319150D0 (en) 2003-08-14 2003-09-17 Glaxo Group Ltd Novel compounds
EP1687306A1 (en) 2003-11-14 2006-08-09 MERCK SHARP & DOHME LTD. Bicyclic pyrimidin-4-(3h)-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (vr1)
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
WO2006019965A2 (en) * 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
JP2008508190A (ja) 2004-07-19 2008-03-21 ノボ ノルディスク アクティーゼルスカブ 肥満または肥満に関連する疾患および障害の治療におけるカプサイシン受容体の活性の阻害
DE102004039373A1 (de) * 2004-08-12 2006-02-23 Grünenthal GmbH Para-Alkyl-substituierte N-(4-Hydroxy-3-methoxy-benzyl)-zimtsäureamide und deren Verwendung zur Herstellung von Arzneimitteln
KR20060087386A (ko) 2005-01-28 2006-08-02 주식회사 대웅제약 신규 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물
WO2006098554A1 (en) * 2005-03-16 2006-09-21 Amorepacific Corporation Novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and a pharmaceutical composition containing the same
GB0506147D0 (en) * 2005-03-24 2005-05-04 Merck Sharp & Dohme Therapeutic agents
GB0509573D0 (en) * 2005-05-11 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
AU2006244027A1 (en) * 2005-05-11 2006-11-16 Merck Sharp & Dohme Limited 2,3-substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilloid-1 receptor (VR1)
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
KR100761222B1 (ko) * 2006-03-08 2007-10-04 성균관대학교산학협력단 약물의존중독을 예방 및 치료하기 위한 바닐로이드 수용체길항제
GB0614471D0 (en) 2006-07-20 2006-08-30 Syngenta Ltd Herbicidal Compounds
EA200900330A1 (ru) 2006-08-23 2009-08-28 Ньюроджен Корпорейшн Аналоги 2-феноксипиримидинона
EP1958947A1 (en) 2007-02-15 2008-08-20 Ranbaxy Laboratories Limited Inhibitors of phosphodiesterase type 4
CL2008001112A1 (es) * 2007-04-20 2008-12-19 Novartis Ag Usos de compuestos derivados de pirido[2,3-d]pirimidin-4-ona para tratar comezon o un trastorno relacionado con comezon; combinacion de los compuestos con otro farmaco; y uso de la combinacion para tratar la comezon o un trastorno relacionado con comezon.
GEP20125574B (en) * 2008-01-11 2012-07-10 Glenmark Pharmaceuticals Sa Fused pyrimidine derivatives as trpv3 modulators
WO2009121036A2 (en) * 2008-03-27 2009-10-01 Neurogen Corporation Substituted aryl pyrimidinone derivatives
CN101983197B (zh) 2008-04-18 2015-04-22 大熊制药株式会社 新型苯并噁嗪苯并咪唑衍生物、含有该衍生物的药物组合物及其用途
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
CN102762572A (zh) 2010-02-01 2012-10-31 诺瓦提斯公司 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
EP2531490B1 (en) 2010-02-02 2014-10-15 Novartis AG Cyclohexyl amide derivatives as crf receptor antagonists
KR101293384B1 (ko) 2010-10-13 2013-08-05 주식회사 대웅제약 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도
UY34094A (es) 2011-05-27 2013-01-03 Novartis Ag Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina
WO2013164790A1 (en) 2012-05-03 2013-11-07 Novartis Ag L-malate salt of 2, 7 - diaza - spiro [4.5 ] dec- 7 - yle derivatives and crystalline forms thereof as ghrelin receptor agonists
CN107108429B (zh) 2015-12-23 2022-08-19 联邦科学与工业研究组织 化合物
DE102022104759A1 (de) 2022-02-28 2023-08-31 SCi Kontor GmbH Co-Kristall-Screening Verfahren, insbesondere zur Herstellung von Co-Kristallen

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US2749344A (en) * 1953-01-02 1956-06-05 Burroughs Wellcome Co Pyrimidine compounds
US5958930A (en) 1991-04-08 1999-09-28 Duquesne University Of The Holy Ghost Pyrrolo pyrimidine and furo pyrimidine derivatives
IL112235A (en) 1994-01-03 2000-06-29 Acea Pharm Inc 1,4-dihydro-pyrido¬2,3-b¾pyrazine-2,3-dione (5 or 8) oxide derivatives and pharmaceutical compositions containing them
FR2750862B1 (fr) 1996-07-12 1998-10-16 Dupin Jean Pierre Utilisation d'heterocycles diazotes fusionnes avec un systeme aromatique ou heteroaromatique pour le traitement des maladies thrombo-emboliques

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103382176A (zh) * 2005-10-19 2013-11-06 格吕伦塔尔有限公司 新颖的辣椒素受体配体和它们用于生产药物的用途
CN101754774B (zh) * 2007-07-18 2013-08-21 诺瓦提斯公司 Vr-1拮抗剂和cox-2抑制剂的协同组合
CN108863949A (zh) * 2018-07-09 2018-11-23 湖南博隽生物医药有限公司 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法
CN108863949B (zh) * 2018-07-09 2021-01-15 湖南博隽生物医药有限公司 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法
CN114605408A (zh) * 2022-03-30 2022-06-10 沈阳药科大学 5-羟基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制法和应用

Also Published As

Publication number Publication date
KR20030083755A (ko) 2003-10-30
CA2441599A1 (en) 2002-10-03
PL363907A1 (en) 2004-11-29
SK11952003A3 (sk) 2004-03-02
JP2004528312A (ja) 2004-09-16
HUP0303623A2 (hu) 2004-03-01
RU2003130221A (ru) 2005-04-10
US7915264B2 (en) 2011-03-29
NO20034122D0 (no) 2003-09-16
BR0208338A (pt) 2004-03-09
US20040138454A1 (en) 2004-07-15
JP4205430B2 (ja) 2009-01-07
WO2002076946A3 (en) 2002-12-27
EP1377576A2 (en) 2004-01-07
NO326546B1 (no) 2009-01-05
IL157815A0 (en) 2004-03-28
PE20021161A1 (es) 2003-02-21
CZ20032561A3 (cs) 2003-12-17
MXPA03008754A (es) 2004-02-18
WO2002076946A2 (en) 2002-10-03
NO20034122L (no) 2003-09-16

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