CA2241633A1 - Vitronectin receptor antagonists - Google Patents

Vitronectin receptor antagonists Download PDF

Info

Publication number
CA2241633A1
CA2241633A1 CA002241633A CA2241633A CA2241633A1 CA 2241633 A1 CA2241633 A1 CA 2241633A1 CA 002241633 A CA002241633 A CA 002241633A CA 2241633 A CA2241633 A CA 2241633A CA 2241633 A1 CA2241633 A1 CA 2241633A1
Authority
CA
Canada
Prior art keywords
methyl
oxo
carbonyl
tetrahydro
benzodiazepine
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.)
Abandoned
Application number
CA002241633A
Other languages
English (en)
French (fr)
Inventor
William Henry Miller
William Edward Bondinell
Thomas Wen-Fu Ku
Maria A. Lago
Fadia El-Fehail Ali
Richard Mcculloch Keenan
Chet Kwon
James Martin Samanen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
Individual
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.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2241633A1 publication Critical patent/CA2241633A1/en
Abandoned legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36Antigestagens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14Radicals substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CA002241633A 1995-12-29 1996-12-20 Vitronectin receptor antagonists Abandoned CA2241633A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US936695P 1995-12-29 1995-12-29
US60/009,366 1995-12-29

Publications (1)

Publication Number Publication Date
CA2241633A1 true CA2241633A1 (en) 1997-07-10

Family

ID=21737205

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002241633A Abandoned CA2241633A1 (en) 1995-12-29 1996-12-20 Vitronectin receptor antagonists

Country Status (16)

Country Link
EP (1) EP0869787A4 (hu)
JP (1) JP2000502354A (hu)
KR (1) KR19990076878A (hu)
CN (1) CN1209744A (hu)
AU (1) AU1354097A (hu)
BR (1) BR9612327A (hu)
CA (1) CA2241633A1 (hu)
CZ (1) CZ203698A3 (hu)
HU (1) HUP9900754A3 (hu)
IL (1) IL125033A0 (hu)
MX (1) MX9805255A (hu)
NO (1) NO983003L (hu)
PL (1) PL327694A1 (hu)
TR (1) TR199801253T2 (hu)
WO (1) WO1997024119A1 (hu)
ZA (1) ZA9610859B (hu)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
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US20030125317A1 (en) 1996-10-02 2003-07-03 Smithkline Beecham Corporation Vitronectin receptor antagonists
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US6218387B1 (en) * 1996-12-20 2001-04-17 Hoechst Aktiengesellschaft Vitronectin receptor anatagonists, their preparation and their use
DE19653645A1 (de) * 1996-12-20 1998-06-25 Hoechst Ag Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung
US6482821B2 (en) 1996-12-20 2002-11-19 Hoechst Aktiengellschaft Vitronectin receptor antagonists, their preparation and their use
EP1007051A4 (en) * 1997-08-04 2001-08-29 Smithkline Beecham Corp INTEGRIN RECEPTOR ANTAGONISTS
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RU2263111C2 (ru) 1998-06-12 2005-10-27 Сосьете Де Консей Де Решерш Э Д`Аппликасьон Сьентифик Сас Имидазольные производные
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US6339083B1 (en) * 1998-12-14 2002-01-15 Bayer Aktiengesellschaft Multiheterocyclic pharmAceuticals
CA2358855A1 (en) 1999-02-03 2000-08-10 Merck & Co., Inc. Benzazepine derivatives as alpha-v integrin receptor antagonists
ATE277927T1 (de) * 1999-04-02 2004-10-15 Neurogen Corp Aryl- und heteroaryl-kondensierte aminoalkyl- imidazol-derivate: selektive modulatoren der gabaa-rezeptoren
US6627624B1 (en) 1999-04-02 2003-09-30 Neurogen Corporation Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
US6358949B1 (en) 1999-04-02 2002-03-19 Neurogen Corporation Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors
US6281237B1 (en) 1999-04-02 2001-08-28 Neurogen Corporation N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives
US6380210B1 (en) 1999-04-02 2002-04-30 Neurogen Corporation Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
US6271241B1 (en) 1999-04-02 2001-08-07 Neurogen Corporation Cycloalkyl and aryl fused aminoalkyl-imidazole derivatives: modulators and GLP-1 receptors
GB9908355D0 (en) * 1999-04-12 1999-06-09 Rhone Poulenc Rorer Ltd Chemical compounds
AU5826100A (en) 1999-07-13 2001-01-30 F. Hoffmann-La Roche Ag Benzazepinones and quinazolines
AU6360200A (en) 1999-07-21 2001-02-13 American Home Products Corporation Bicyclic antagonists selective for the alphavbeta3 integrin
US6750219B1 (en) 1999-08-05 2004-06-15 Meiji Seika Kaisha, Ltd. Ω-amino-α-hydroxycarboxylic acid derivatives having integrin ανβ3 antagonistic activity
EP1208101A4 (en) * 1999-08-06 2003-03-19 Smithkline Beecham Corp VITRONECTIN RECEPTOR ANTAGONISTS USEFUL FOR THE TREATMENT OF VASCULAR ACCIDENTS
AU2001229580A1 (en) 2000-01-18 2001-08-14 Nuerogen Corporation Substituted imidazoles as selective modulators of bradykinin b2 receptors
US6545029B2 (en) 2000-06-12 2003-04-08 Bayer Aktiengesellschaft Phenylserine derivatives as integrin antagonists
ATE360620T1 (de) 2000-08-01 2007-05-15 Sod Conseils Rech Applic Imidazolderivate
JP4660067B2 (ja) 2001-04-24 2011-03-30 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 抗血管新生剤とTNFαとを用いる組合せ療法
US7030150B2 (en) 2001-05-11 2006-04-18 Trimeris, Inc. Benzimidazole compounds and antiviral uses thereof
KR20040058229A (ko) 2001-10-22 2004-07-03 더 스크립스 리서치 인스티튜트 항체 표적화 화합물
CN102174042B (zh) * 2003-05-19 2013-09-18 Irm有限责任公司 免疫抑制剂化合物和组合物
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
WO2005097766A1 (en) 2004-03-31 2005-10-20 Lexicon Genetics, Inc. 2-aminomethylthiazole-5-carboxamides as protein kinase modulators
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
MX2007001727A (es) 2004-08-13 2007-04-20 Genentech Inc Compuestos a base de 2-amido-tiazol que exhiben actividad inhibidora de enzima que utiliza atp y composiciones y usos de los mismos.
ES2521679T3 (es) 2006-01-18 2014-11-13 Merck Patent Gmbh Terapia específica usando ligandos de integrinas para el tratamiento del cáncer
DK2101805T3 (da) 2007-01-18 2013-01-21 Merck Patent Gmbh Integrinligander til anvendelse i behandling af cancer
EP2146722A4 (en) 2007-05-10 2011-08-03 Amr Technology Inc ARYL AND HETEROARYL SUBSTITUTED TETRAHYDROBENZO-1,4-DIAZEPINES AND THEIR USE FOR BLOCKING THE RECOVERY OF NOREPINEPHRIN, DOPAMINE AND SEROTONINE
US8518927B2 (en) 2009-02-10 2013-08-27 The Scripps Research Institute Chemically programmed vaccination
MX2011012491A (es) 2009-05-25 2011-12-14 Merck Patent Gmbh Administracion continua de cilengitida en tratamientos contra el cancer.
JP6649902B2 (ja) 2014-05-30 2020-02-19 ファイザー・インク 選択的アンドロゲン受容体モジュレーターとしてのカルボニトリル誘導体
CN111108105B (zh) 2017-09-22 2023-03-31 朱比兰特埃皮帕德有限公司 作为pad抑制剂的杂环化合物
WO2019077631A1 (en) 2017-10-18 2019-04-25 Jubilant Biosys Limited IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS
KR20200085836A (ko) 2017-11-06 2020-07-15 주빌런트 프로델 엘엘씨 Pd1/pd-l1 활성화 억제제로서의 피리미딘 유도체
BR112020010322A2 (pt) 2017-11-24 2020-11-17 Jubilant Episcribe Llc composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer
WO2019175897A1 (en) 2018-03-13 2019-09-19 Jubilant Biosys Limited Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

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US5250679A (en) * 1991-10-18 1993-10-05 Genentech, Inc. Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III.sub. receptor

Also Published As

Publication number Publication date
AU1354097A (en) 1997-07-28
CN1209744A (zh) 1999-03-03
NO983003D0 (no) 1998-06-26
PL327694A1 (en) 1998-12-21
NO983003L (no) 1998-08-26
TR199801253T2 (xx) 1998-12-21
MX9805255A (es) 1998-11-29
BR9612327A (pt) 1999-07-13
KR19990076878A (ko) 1999-10-25
CZ203698A3 (cs) 1999-05-12
EP0869787A1 (en) 1998-10-14
HUP9900754A2 (hu) 1999-07-28
IL125033A0 (en) 1999-01-26
WO1997024119A1 (en) 1997-07-10
EP0869787A4 (en) 1999-03-24
HUP9900754A3 (en) 1999-11-29
ZA9610859B (en) 1997-10-24
JP2000502354A (ja) 2000-02-29

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Legal Events

Date Code Title Description
FZDE Discontinued