CA2129689A1 - Identification and use of protease inhibitors - Google Patents

Identification and use of protease inhibitors

Info

Publication number
CA2129689A1
CA2129689A1 CA002129689A CA2129689A CA2129689A1 CA 2129689 A1 CA2129689 A1 CA 2129689A1 CA 002129689 A CA002129689 A CA 002129689A CA 2129689 A CA2129689 A CA 2129689A CA 2129689 A1 CA2129689 A1 CA 2129689A1
Authority
CA
Canada
Prior art keywords
alkyl
reaction
aspartyl protease
amino
aryl
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
CA002129689A
Other languages
English (en)
French (fr)
Inventor
Harry F. Dovey
Varghese John
Bennett C. Laguzza
Ivan M. Lieberberg
Sheila P. Little
Sukanto Sinha
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.)
Athena Neurosciences Inc
Eli Lilly and Co
Original Assignee
Athena Neurosciences Inc
Eli Lilly and Co
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 Athena Neurosciences Inc, Eli Lilly and Co filed Critical Athena Neurosciences Inc
Publication of CA2129689A1 publication Critical patent/CA2129689A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
CA002129689A 1993-08-09 1994-08-08 Identification and use of protease inhibitors Abandoned CA2129689A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10429393A 1993-08-09 1993-08-09
US08/104,293 1993-08-09

Publications (1)

Publication Number Publication Date
CA2129689A1 true CA2129689A1 (en) 1995-02-10

Family

ID=22299686

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002129689A Abandoned CA2129689A1 (en) 1993-08-09 1994-08-08 Identification and use of protease inhibitors

Country Status (12)

Country Link
EP (1) EP0652009A1 (forum.php)
JP (1) JPH07165606A (forum.php)
KR (1) KR950005321A (forum.php)
CN (1) CN1120040A (forum.php)
AU (1) AU6897094A (forum.php)
CA (1) CA2129689A1 (forum.php)
CZ (1) CZ184194A3 (forum.php)
IL (1) IL110525A0 (forum.php)
NO (1) NO942883L (forum.php)
NZ (1) NZ264143A (forum.php)
RU (1) RU94028644A (forum.php)
ZA (1) ZA945719B (forum.php)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262302B1 (en) 1996-11-22 2001-07-17 Elan Pharmaceuticals, Inc. N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds

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* Cited by examiner, † Cited by third party
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US5804560A (en) * 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
JPH11506923A (ja) * 1995-06-06 1999-06-22 アセナ ニューロサイエンシーズ，インコーポレイテッド 新しいカテプシンならびにその阻害のための方法および組成物
CA2191924A1 (en) 1995-12-05 1997-06-06 Kevin Felsenstein 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of .beta.-amyloid protein production
US5849691A (en) * 1996-02-20 1998-12-15 The United States Of America As Represented By The Department Of Health And Human Services Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II
US6245751B1 (en) * 1996-07-09 2001-06-12 University Of Cincinnati Methods for the treatment of apolipoprotein E related diseases
US5703129A (en) * 1996-09-30 1997-12-30 Bristol-Myers Squibb Company 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production
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
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6642261B2 (en) 1997-11-21 2003-11-04 Athena Neurosciences, Inc. N-(aryl/heteroarylacety) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
WO1998022430A1 (en) * 1996-11-22 1998-05-28 Elan Pharmaceuticals, Inc. N-(ARYL/HETEROARYLACETYL) AMINO ACID ESTERS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING b-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS
US6211235B1 (en) 1996-11-22 2001-04-03 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6117901A (en) 1996-11-22 2000-09-12 Athena Neurosciences, Inc. N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for use
US6207710B1 (en) 1996-11-22 2001-03-27 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
TR199901343T2 (xx) * 1996-12-23 1999-09-21 Elan Pharmaceuticals, Inc. Sikloalkil, laktam, lakton ve ilgili bile�ikler, bunlar� i�eren farmas�tik bile�imler ve b�yle bile�ikler kullan�larak �-amiloid peptidinin sal�nmas�n� ve/veya sentezini inhibe etmek i�in y�ntemler.
US6683075B1 (en) 1996-12-23 2004-01-27 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use
US6635632B1 (en) 1996-12-23 2003-10-21 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
WO1999032453A1 (en) * 1997-12-22 1999-07-01 Elan Pharmaceuticals, Inc. POLYCYCLIC α-AMINO-⊂-CAPROLACTAMS AND RELATED COMPOUNDS
US6506782B1 (en) 1998-02-27 2003-01-14 Athena Neurosciences, Inc. Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6774125B2 (en) 1998-06-22 2004-08-10 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6958330B1 (en) 1998-06-22 2005-10-25 Elan Pharmaceuticals, Inc. Polycyclic α-amino-ε-caprolactams and related compounds
US6528505B1 (en) 1998-06-22 2003-03-04 Elan Pharmaceuticals, Inc. Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6509331B1 (en) 1998-06-22 2003-01-21 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6569851B1 (en) 1998-06-22 2003-05-27 Elan Pharmaceutials, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6552013B1 (en) 1998-06-22 2003-04-22 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
NZ525513A (en) 1998-08-07 2004-09-24 Pont Pharmaceuticals Du Succinoylamino lactams as inhibitors of Abeta protein production
WO2000028331A1 (en) * 1998-11-12 2000-05-18 Du Pont Pharmaceuticals Company Use of radioligands to screen inhibitors of amyloid-beta peptide production
US6737038B1 (en) 1998-11-12 2004-05-18 Bristol-Myers Squibb Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
AU7490900A (en) * 1999-09-16 2001-04-17 Axys Pharmaceuticals, Inc. Chemical compounds and compositions and their use as cathepsin s inhibitors
JP2003528071A (ja) 2000-03-23 2003-09-24 エラン ファーマスーティカルズ インコーポレイテッド アルツハイマー病治療用組成物および方法
WO2001074796A1 (en) * 2000-03-31 2001-10-11 Bristol-Myers Squibb Pharma Company SUCCINOYLAMINO HETEROCYCLES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
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CA2404273A1 (en) 2000-04-11 2001-10-18 Bristol-Myers Squibb Pharma Company Substituted lactams as inhibitors of a.beta. protein production
WO2001087354A2 (en) 2000-05-17 2001-11-22 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands for diagnostic imaging
CN1386118A (zh) 2000-06-01 2002-12-18 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物
EP1666452A2 (en) 2000-06-30 2006-06-07 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
JP2004502665A (ja) 2000-06-30 2004-01-29 イーラン　ファーマスーティカルズ、インコーポレイテッド アルツハイマー病を治療する化合物
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US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
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US6432944B1 (en) 2000-07-06 2002-08-13 Bristol-Myers Squibb Company Benzodiazepinone β-amyloid inhibitors: arylacetamidoalanyl derivatives
FR2817867B1 (fr) * 2000-12-11 2006-06-30 Trophos Isocoumarines inhibitrices de la production de peptide amyloide, preparation, compositions les contenant et utilisations
ES2267853T3 (es) 2000-12-13 2007-03-16 Wyeth Inhibidroes de sulfonamida heteriociclicos de la produccion de beta amiloides.
US6657070B2 (en) 2000-12-13 2003-12-02 Wyeth Production of chirally pure α-amino acids and N-sulfonyl α-amino acids
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RS50504A (sr) * 2001-11-08 2007-04-10 Elan Pharmaceuticals Inc., Derivati n,n'-supstituisanog-1,3- diamino-2-hidroksipropana
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CN103788178A (zh) * 2014-02-14 2014-05-14 国家纳米科学中心 一种短肽抑制剂及其用途

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CN1071930A (zh) * 1991-07-10 1993-05-12 伊莱利利公司 用作治疗艾滋病的人免疫缺陷病毒蛋白酶的抑制剂
GB9122051D0 (en) * 1991-10-17 1991-11-27 Univ Nottingham Medicines
US5538845A (en) * 1992-02-05 1996-07-23 Athena Neurosciences, Inc. Beta-amyloid peptide production inhibitors and methods for their identification
AU679675B2 (en) * 1992-05-11 1997-07-10 Bayer Corporation Methods for detecting beta amyloid precursor protein processing enzymes
NZ247837A (en) * 1992-06-19 1995-04-27 Lilly Co Eli Cyclic oxirane derivatives, medicaments and precursors
US5554653A (en) * 1992-12-22 1996-09-10 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of AIDS
US5491166A (en) * 1992-12-22 1996-02-13 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of AIDS

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262302B1 (en) 1996-11-22 2001-07-17 Elan Pharmaceuticals, Inc. N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds

Also Published As

Publication number Publication date
RU94028644A (ru) 1996-11-10
ZA945719B (en) 1996-02-01
CZ184194A3 (en) 1995-03-15
KR950005321A (ko) 1995-03-20
NO942883D0 (forum.php) 1994-08-03
AU6897094A (en) 1995-02-16
EP0652009A1 (en) 1995-05-10
NO942883L (no) 1995-02-10
IL110525A0 (en) 1994-11-11
NZ264143A (en) 1996-11-26
JPH07165606A (ja) 1995-06-27
CN1120040A (zh) 1996-04-10

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