CN100360499C - 抑制整联蛋白与其受体结合的丙酸衍生物 - Google Patents

抑制整联蛋白与其受体结合的丙酸衍生物 Download PDF

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Publication number
CN100360499C
CN100360499C CNB00809957XA CN00809957A CN100360499C CN 100360499 C CN100360499 C CN 100360499C CN B00809957X A CNB00809957X A CN B00809957XA CN 00809957 A CN00809957 A CN 00809957A CN 100360499 C CN100360499 C CN 100360499C
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alkyl
amino
group
aryl
compound
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Chinese (zh)
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CN1370143A (zh
Inventor
R·J·比迪格
G·W·霍兰德
J·M·卡斯尔
W·李
R·V·马克特
I·L·斯科特
C·吴
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Texas Biotechnology Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CNB00809957XA 1999-05-07 2000-05-05 抑制整联蛋白与其受体结合的丙酸衍生物 Expired - Fee Related CN100360499C (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13296799P 1999-05-07 1999-05-07
US60/132967 1999-05-07
US17044199P 1999-12-10 1999-12-10
US60/170441 1999-12-10
PCT/US2000/012464 WO2000068188A1 (en) 1999-05-07 2000-05-05 Propanoic acid derivatives that inhibit the binding of integrins to their receptors

Publications (2)

Publication Number Publication Date
CN1370143A CN1370143A (zh) 2002-09-18
CN100360499C true CN100360499C (zh) 2008-01-09

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CNB00809957XA Expired - Fee Related CN100360499C (zh) 1999-05-07 2000-05-05 抑制整联蛋白与其受体结合的丙酸衍生物

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Country Link
EP (1) EP1189881B2 (enExample)
JP (2) JP4841729B2 (enExample)
KR (1) KR100767199B1 (enExample)
CN (1) CN100360499C (enExample)
AT (1) ATE277923T1 (enExample)
AU (1) AU4826900A (enExample)
BR (1) BR0010349B1 (enExample)
CA (1) CA2373180C (enExample)
CZ (1) CZ304225B6 (enExample)
DE (1) DE60014369T3 (enExample)
ES (1) ES2228527T5 (enExample)
HK (1) HK1044533A1 (enExample)
HU (1) HU229155B1 (enExample)
IL (2) IL146312A0 (enExample)
MX (1) MXPA01011341A (enExample)
NO (1) NO329899B1 (enExample)
NZ (1) NZ515249A (enExample)
RO (1) RO121640B1 (enExample)
RU (1) RU2255933C9 (enExample)
SI (1) SI20876B (enExample)
SK (1) SK288186B6 (enExample)
TR (1) TR200103427T2 (enExample)
WO (1) WO2000068188A1 (enExample)

Families Citing this family (24)

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US6723711B2 (en) * 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
US6972296B2 (en) 1999-05-07 2005-12-06 Encysive Pharmaceuticals Inc. Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
AR026748A1 (es) * 1999-12-08 2003-02-26 Vertex Pharma Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis
AR030817A1 (es) 2000-10-02 2003-09-03 Novartis Ag Derivados de diazacicloalcanodiona
FR2834212B1 (fr) * 2001-12-27 2004-07-09 Besins Int Belgique Utilisation d'une poudre a liberation immediate dans des compositions pharmaceutiques et nutraceutiques
PE20040728A1 (es) 2002-06-28 2004-10-23 Vertex Pharma Inhibidores de caspasa
US7122580B2 (en) 2002-08-09 2006-10-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds and methods to modulate coagulation
US7612091B2 (en) 2002-12-20 2009-11-03 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
PE20050159A1 (es) 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
WO2005014532A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
US7544699B2 (en) 2003-08-08 2009-06-09 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
WO2006053342A2 (en) * 2004-11-12 2006-05-18 Osi Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
AP2007004244A0 (en) 2005-05-10 2007-12-31 Intermune Inc Method of modulating stress-activated protein kinase system
MY144590A (en) 2005-07-11 2011-10-14 Wyeth Corp Glutamate aggrecanase inhibitors
KR20080058436A (ko) 2005-10-13 2008-06-25 와이어쓰 글루탐산 유도체의 제조 방법
EP2296653B1 (en) 2008-06-03 2016-01-27 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
RU2692485C2 (ru) 2014-04-02 2019-06-25 Интермьюн, Инк. Противофиброзные пиридиноны
US10875875B2 (en) * 2017-04-26 2020-12-29 Aviara Pharmaceuticals, Inc. Propionic acid derivatives and methods of use thereof
TW202528300A (zh) 2018-04-12 2025-07-16 美商莫菲克醫療股份有限公司 人類整合素α4β7拮抗劑
BR112022007284A2 (pt) * 2019-10-16 2022-07-05 Morphic Therapeutic Inc Inibição de integrina humana alpha-4 beta-7
WO2023134698A1 (zh) * 2022-01-11 2023-07-20 深圳信立泰药业股份有限公司 一种哒嗪-1(6h)-6-氧代类化合物及其制备方法与应用
WO2024235299A1 (zh) * 2023-05-17 2024-11-21 西藏海思科制药有限公司 一种羧基衍生物及其在医药上的应用

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US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme

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US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
GR851819B (enExample) * 1984-08-17 1985-11-26 Wyeth John & Brother Ltd
FI934894L (fi) * 1991-05-07 1993-11-05 Merck & Co Inc Fibrinogenreceptorantagonister
EP0761680A3 (en) * 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
JP2000516596A (ja) * 1996-07-25 2000-12-12 バイオジェン，インコーポレイテッド 細胞接着インヒビター
JP2002511052A (ja) * 1996-08-29 2002-04-09 メルク エンド カンパニー インコーポレーテッド インテグリンアンタゴニスト
CA2268098A1 (en) * 1996-10-11 1998-04-23 Warner-Lambert Company Aspartate ester inhibitors of interleukin-1.beta. converting enzyme
DE19647380A1 (de) * 1996-11-15 1998-05-20 Hoechst Ag 5-Ring-Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
AR016751A1 (es) * 1996-11-22 2001-08-01 Athena Neurosciences Inc Metodo para inhibir la liberacion del peptido beta-amiloide en una celula, composicion farmaceutica y compuestos utiles en dicho metodo
TR199902692T2 (xx) * 1997-05-02 2000-07-21 Akzo Nobel N.V. Serin proteaz inhibit�rleri.
DE19741235A1 (de) * 1997-09-18 1999-03-25 Hoechst Marion Roussel De Gmbh Neue Imidazolidinderivate, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
US6331640B1 (en) * 1998-10-13 2001-12-18 Hoffmann-La Roche Inc. Diaminopropionic acid derivatives
WO2000061631A1 (en) * 1999-04-12 2000-10-19 Astrazeneca Ab Modified pentapeptide antagonists of the atrial natriuretic peptide clearance receptor

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Publication number Priority date Publication date Assignee Title
US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme

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ES2228527T5 (es) 2013-05-23
TR200103427T2 (tr) 2002-10-21
JP2012006932A (ja) 2012-01-12
BR0010349A (pt) 2003-07-08
JP2002544187A (ja) 2002-12-24
WO2000068188A9 (en) 2002-08-29
AU4826900A (en) 2000-11-21
CA2373180C (en) 2009-12-15
ATE277923T1 (de) 2004-10-15
CN1370143A (zh) 2002-09-18
KR100767199B1 (ko) 2007-10-17
DE60014369T2 (de) 2005-11-24
EP1189881A4 (en) 2002-11-27
BR0010349C1 (pt) 2003-11-04
NZ515249A (en) 2004-07-30
JP4841729B2 (ja) 2011-12-21
NO20015419L (no) 2001-12-20
CA2373180A1 (en) 2000-11-16
EP1189881B1 (en) 2004-09-29
BR0010349B1 (pt) 2011-10-04
CZ304225B6 (cs) 2014-01-15
EP1189881B2 (en) 2013-01-23
MXPA01011341A (es) 2002-06-21
KR20020009608A (ko) 2002-02-01
JP5468578B2 (ja) 2014-04-09
RO121640B1 (ro) 2008-01-30
HK1044533A1 (zh) 2002-10-25
EP1189881A1 (en) 2002-03-27
IL146312A (en) 2010-12-30
HU229155B1 (en) 2013-09-30
RU2255933C9 (ru) 2005-11-20
SI20876A (sl) 2002-10-31
SI20876B (sl) 2009-08-31
HUP0202184A3 (en) 2003-03-28
WO2000068188A1 (en) 2000-11-16
CZ20013983A3 (cs) 2002-04-17
DE60014369D1 (de) 2004-11-04
SK288186B6 (sk) 2014-05-06
DE60014369T3 (de) 2013-06-27
NO329899B1 (no) 2011-01-24
NO20015419D0 (no) 2001-11-06
ES2228527T3 (es) 2005-04-16
PL354957A1 (en) 2004-03-22
SK16092001A3 (sk) 2002-04-04
IL146312A0 (en) 2002-07-25
HUP0202184A2 (hu) 2002-12-28
RU2255933C2 (ru) 2005-07-10

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