ES2188194T3 - 1,8-naftiridin-4(1h)-onas sustituidas como inhibidores de la fosfodiesterasa 4. - Google Patents
1,8-naftiridin-4(1h)-onas sustituidas como inhibidores de la fosfodiesterasa 4.Info
- Publication number
- ES2188194T3 ES2188194T3 ES99933078T ES99933078T ES2188194T3 ES 2188194 T3 ES2188194 T3 ES 2188194T3 ES 99933078 T ES99933078 T ES 99933078T ES 99933078 T ES99933078 T ES 99933078T ES 2188194 T3 ES2188194 T3 ES 2188194T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- aminosulfonyl
- amino
- uncle
- phosphodesterase
- 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 - Lifetime
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 229960004583 pranlukast Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- -1 chlocloalkyl (C3-C7) Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000006823 (C1-C6) acyl group Chemical group 0.000 abstract 1
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto de fórmula**(Fórmula)** o una sal farmacéuticamente aceptable del mismo, en la que R1 se selecciona del grupo constituido por hidrógeno, alquilo(C1-C6), clocloalquilo(C3-C7), arilo(C6-C10), heteroarilo(C5-C9) y heterocicloalquilo(C2-C9), en la que los grupos alquilo, cicloalquilo, arilo, heteroarilo o heterocicloalquilo están opcionalmente sustituidos por halo, hidroxilo, alquilo(C1-C6), alcoxilo(C1-C6), amino, alquil(C1-C6)amino, (alquil(C1-C6))2-amino, tío, alquil(C1-C6)tío, ciano, carboxilo, carboxialquilo(C1-C6), hidroxialquilo(C1-C6), acilo(C1-C6), aminosulfonilo, alquil(C1-C6)aminosulfonilo o (alquil(C1-C6)2-aminosulfonilo. R2 es arilo(C6-C10) o heteroarilo(C5-C9); y R3 es hidrógeno, halo, hidroxilo, alquilo(C1-C6), alcoxilo(C1-C6), amino, alquil(C1-C6)amino, (alquil(C1-C6))2-amino, tío, alquil(C1-C6)tío, carboxilo, carboxialquilo(C1-C6), hidroxialquilo(C1-C6), acilo(C1-C6), aminosulfonilo, alquil(C1-C6)-aminosulfonilo o (alquil(C1-C6)2-aminosulfonilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9617698P | 1998-08-11 | 1998-08-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2188194T3 true ES2188194T3 (es) | 2003-06-16 |
Family
ID=22256080
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES99933078T Expired - Lifetime ES2188194T3 (es) | 1998-08-11 | 1999-08-05 | 1,8-naftiridin-4(1h)-onas sustituidas como inhibidores de la fosfodiesterasa 4. |
Country Status (44)
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8815951B2 (en) | 1996-08-13 | 2014-08-26 | The Regents Of The University Of California | Inhibitors of epoxide hydrolases for the treatment of inflammation |
CA2427430A1 (en) * | 2000-11-02 | 2002-06-13 | Research Foundation Of City University Of New York | Methods for stimulating nervous system regeneration and repair by inhibition phosphodiesterase type 4 |
WO2002088079A2 (en) * | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
JO2311B1 (en) * | 2001-08-29 | 2005-09-12 | ميرك فروست كندا ليمتد | Alkyl inhibitors Ariel phosphodiesterase-4 |
CA2478310A1 (en) * | 2002-03-15 | 2003-09-25 | Merck & Co., Inc. | N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as hiv integrase inhibitors |
KR100454750B1 (ko) * | 2002-06-20 | 2004-11-03 | 삼성에스디아이 주식회사 | 유기 전계 발광 소자용 청색 발광 화합물 및 이를 사용한유기 전계 발광 소자 |
AU2003289898A1 (en) * | 2002-11-27 | 2004-06-18 | Altana Pharma Ag | Pde4 and pde3/4 inhibitors for use in the treatment of cachexia |
US6861422B2 (en) * | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
DE10349497A1 (de) * | 2003-10-23 | 2005-05-25 | Bayer Cropscience Ag | N-substituierte Pyrazolylcarboxanilide |
DE102004002557A1 (de) * | 2004-01-17 | 2005-08-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verwendung von substituierten Pyrimido(5,4-d)pyrimidinen zur Behandlung von Atemwegserkrankungen |
CA2552540A1 (en) * | 2004-01-17 | 2005-07-28 | Boehringer Ingelheim International Gmbh | Use of substituted pteridines for the treatment of diseases of the respiratory tract |
DE102004029784A1 (de) * | 2004-06-21 | 2006-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel |
DE102004033670A1 (de) * | 2004-07-09 | 2006-02-02 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel |
US7728134B2 (en) * | 2004-08-14 | 2010-06-01 | Boehringer Ingelheim International Gmbh | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament |
US7759485B2 (en) * | 2004-08-14 | 2010-07-20 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dihydropteridinones |
US20060074088A1 (en) * | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
US20060035903A1 (en) * | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
US20060058311A1 (en) * | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
EP1632493A1 (de) * | 2004-08-25 | 2006-03-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
EP1630163A1 (de) * | 2004-08-25 | 2006-03-01 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
DE102004058337A1 (de) * | 2004-12-02 | 2006-06-14 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten |
WO2007014838A1 (en) * | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Dihydropteridinones in the treatment of respiratory diseases |
US7439358B2 (en) * | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
WO2009019205A1 (en) * | 2007-08-03 | 2009-02-12 | Boehringer Ingelheim International Gmbh | Crystalline form of a dihydropteridione derivative |
US8546566B2 (en) | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
RS59921B1 (sr) * | 2012-08-08 | 2020-03-31 | Merck Patent Gmbh | (aza-)izohinolinon derivati |
JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
WO2015011236A1 (en) | 2013-07-26 | 2015-01-29 | Boehringer Ingelheim International Gmbh | Treatment of myelodysplastic syndrome |
US9867831B2 (en) | 2014-10-01 | 2018-01-16 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia and myelodysplastic syndrome |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HU165405B (es) * | 1972-06-29 | 1974-08-28 | ||
US3856800A (en) * | 1973-02-26 | 1974-12-24 | Sterling Drug Inc | Process of preparing 1,4-dihydro-4-oxo-7-q-3-unsubstituted-1,8-naphthyridines from cyclic alkylidenyl n-(6-q-2-pyridyl) aminomethylenemalonates |
US3882132A (en) * | 1973-03-08 | 1975-05-06 | Sterling Drug Inc | Preparation of 1-alkyl-1,4-dihydro-7-substituted-4-oxo-1,8-naphthyridine-3-carboxylic acids via the 3-aminomethyl analogs |
NZ291507A (en) * | 1994-08-29 | 1997-12-19 | Yamanouchi Pharma Co Ltd | 1,8-naphthyridine derivatives; medicaments |
JP4323574B2 (ja) * | 1995-12-13 | 2009-09-02 | 大日本住友製薬株式会社 | 抗腫瘍剤 |
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1999
- 1999-08-05 AP APAP/P/2001/002068A patent/AP2001002068A0/en unknown
- 1999-08-05 DK DK99933078T patent/DK1104420T3/da active
- 1999-08-05 TR TR2001/00433T patent/TR200100433T2/xx unknown
- 1999-08-05 WO PCT/IB1999/001390 patent/WO2000009504A1/en not_active Application Discontinuation
- 1999-08-05 EP EP99933078A patent/EP1104420B1/en not_active Expired - Lifetime
- 1999-08-05 CA CA002340180A patent/CA2340180A1/en not_active Abandoned
- 1999-08-05 AT AT99933078T patent/ATE229955T1/de not_active IP Right Cessation
- 1999-08-05 JP JP2000564956A patent/JP2002522541A/ja active Pending
- 1999-08-05 ES ES99933078T patent/ES2188194T3/es not_active Expired - Lifetime
- 1999-08-05 DE DE69904602T patent/DE69904602T2/de not_active Expired - Fee Related
- 1999-08-05 HK HK02100400.2A patent/HK1038917A1/zh unknown
- 1999-08-05 KR KR1020017001718A patent/KR20010072368A/ko not_active Ceased
- 1999-08-05 GE GEAP19995743A patent/GEP20033029B/en unknown
- 1999-08-05 IL IL14086899A patent/IL140868A0/xx unknown
- 1999-08-05 PL PL99346005A patent/PL346005A1/xx not_active Application Discontinuation
- 1999-08-05 PT PT99933078T patent/PT1104420E/pt unknown
- 1999-08-05 HU HU0103466A patent/HUP0103466A3/hu unknown
- 1999-08-05 ID IDW20010315A patent/ID27843A/id unknown
- 1999-08-05 BR BR9912902-7A patent/BR9912902A/pt not_active Application Discontinuation
- 1999-08-05 EE EEP200100085A patent/EE200100085A/xx unknown
- 1999-08-05 EA EA200100124A patent/EA200100124A1/ru unknown
- 1999-08-05 SK SK182-2001A patent/SK1822001A3/sk unknown
- 1999-08-05 NZ NZ509297A patent/NZ509297A/en not_active Application Discontinuation
- 1999-08-05 CZ CZ2001485A patent/CZ2001485A3/cs unknown
- 1999-08-05 CN CN99809505A patent/CN1312810A/zh active Pending
- 1999-08-05 HR HR20010107A patent/HRP20010107A2/hr not_active Application Discontinuation
- 1999-08-05 AU AU49249/99A patent/AU4924999A/en not_active Abandoned
- 1999-08-05 OA OA1200100032A patent/OA11591A/en unknown
- 1999-08-06 TW TW088113482A patent/TW542835B/zh active
- 1999-08-09 HN HN1999000130A patent/HN1999000130A/es unknown
- 1999-08-09 GT GT199900128A patent/GT199900128A/es unknown
- 1999-08-09 PE PE1999000802A patent/PE20000950A1/es not_active Application Discontinuation
- 1999-08-10 MA MA25723A patent/MA26669A1/fr unknown
- 1999-08-10 DZ DZ990166A patent/DZ2866A1/xx active
- 1999-08-10 PA PA19998480001A patent/PA8480001A1/es unknown
- 1999-08-10 AR ARP990103992A patent/AR015557A1/es not_active Application Discontinuation
- 1999-08-10 SV SV1999000120A patent/SV1999000120A/es not_active Application Discontinuation
- 1999-08-10 TN TNTNSN99155A patent/TNSN99155A1/fr unknown
- 1999-08-11 CO CO99051075A patent/CO5130004A1/es unknown
- 1999-08-11 US US09/372,735 patent/US6174895B1/en not_active Expired - Fee Related
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2001
- 2001-01-16 IS IS5815A patent/IS5815A/is unknown
- 2001-02-07 ZA ZA200101040A patent/ZA200101040B/en unknown
- 2001-02-09 NO NO20010684A patent/NO20010684L/no not_active Application Discontinuation
- 2001-03-09 BG BG105321A patent/BG105321A/xx unknown
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