BG104391A - Therapeutically active compounds based on bioisosteric substitution of cathechol in pde4 inhibitors with indazole - Google Patents
Therapeutically active compounds based on bioisosteric substitution of cathechol in pde4 inhibitors with indazoleInfo
- Publication number
- BG104391A BG104391A BG104391A BG10439100A BG104391A BG 104391 A BG104391 A BG 104391A BG 104391 A BG104391 A BG 104391A BG 10439100 A BG10439100 A BG 10439100A BG 104391 A BG104391 A BG 104391A
- Authority
- BG
- Bulgaria
- Prior art keywords
- diseases
- group
- cathechol
- indazole
- therapeutically active
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title 1
- 238000006467 substitution reaction Methods 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 206010061218 Inflammation Diseases 0.000 abstract 2
- 206010040070 Septic Shock Diseases 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 230000004054 inflammatory process Effects 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 206010006458 Bronchitis chronic Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 208000011231 Crohn disease Diseases 0.000 abstract 1
- 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 abstract 1
- 206010014561 Emphysema Diseases 0.000 abstract 1
- 206010014824 Endotoxic shock Diseases 0.000 abstract 1
- 108010044467 Isoenzymes Proteins 0.000 abstract 1
- 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010044248 Toxic shock syndrome Diseases 0.000 abstract 1
- 231100000650 Toxic shock syndrome Toxicity 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 208000007451 chronic bronchitis Diseases 0.000 abstract 1
- 230000006378 damage Effects 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 230000000968 intestinal effect Effects 0.000 abstract 1
- 206010025135 lupus erythematosus Diseases 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000010410 reperfusion Effects 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- 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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6416097P | 1997-11-04 | 1997-11-04 | |
| PCT/IB1998/001579 WO1999023076A1 (en) | 1997-11-04 | 1998-10-09 | Therapeutically active compounds based on indazole bioisostere replacement of catechol in pde4 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BG104391A true BG104391A (en) | 2000-12-29 |
Family
ID=22053970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BG104391A BG104391A (en) | 1997-11-04 | 2000-04-28 | Therapeutically active compounds based on bioisosteric substitution of cathechol in pde4 inhibitors with indazole |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US6716978B2 (tr) |
| EP (1) | EP1040100A1 (tr) |
| JP (1) | JP2001521925A (tr) |
| KR (1) | KR20010031783A (tr) |
| CN (1) | CN1281441A (tr) |
| AP (1) | AP1122A (tr) |
| AR (1) | AR016413A1 (tr) |
| AU (1) | AU754184B2 (tr) |
| BG (1) | BG104391A (tr) |
| BR (1) | BR9813938A (tr) |
| CA (1) | CA2309175A1 (tr) |
| CZ (1) | CZ20001623A3 (tr) |
| DZ (1) | DZ2639A1 (tr) |
| EA (1) | EA200000385A1 (tr) |
| HN (1) | HN1998000172A (tr) |
| HR (1) | HRP20000262A2 (tr) |
| HU (1) | HUP0100330A3 (tr) |
| ID (1) | ID24942A (tr) |
| IL (1) | IL135714A0 (tr) |
| IS (1) | IS5452A (tr) |
| MA (1) | MA26562A1 (tr) |
| NO (1) | NO20002127L (tr) |
| NZ (1) | NZ503995A (tr) |
| OA (1) | OA11353A (tr) |
| PA (1) | PA8462601A1 (tr) |
| PE (1) | PE131099A1 (tr) |
| PL (1) | PL340799A1 (tr) |
| SK (1) | SK6262000A3 (tr) |
| TN (1) | TNSN98199A1 (tr) |
| TR (1) | TR200001256T2 (tr) |
| UY (1) | UY25232A1 (tr) |
| WO (1) | WO1999023076A1 (tr) |
| YU (1) | YU25400A (tr) |
| ZA (1) | ZA9810042B (tr) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL126745A (en) * | 1997-11-04 | 2003-09-17 | Pfizer Prod Inc | Methods of preparing 4-cyano-4- (substituted indazole) cyclohexanecarboxylic acids useful as pde4 inhibitors |
| UA71971C2 (en) | 1999-06-04 | 2005-01-17 | Agoron Pharmaceuticals Inc | Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases |
| PE20010306A1 (es) * | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| US7141581B2 (en) | 1999-07-02 | 2006-11-28 | Agouron Pharmaceuticals, Inc. | Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| WO2001079198A1 (en) | 2000-04-18 | 2001-10-25 | Agouron Pharmaceuticals, Inc. | Pyrazoles for inhibiting protein kinase |
| US7211594B2 (en) * | 2000-07-31 | 2007-05-01 | Signal Pharmaceuticals, Llc | Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith |
| US6897231B2 (en) * | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| JP4510383B2 (ja) * | 2001-05-23 | 2010-07-21 | 田辺三菱製薬株式会社 | 軟骨疾患修復治療用組成物 |
| EP1567136A1 (en) * | 2002-11-27 | 2005-08-31 | ALTANA Pharma AG | Pde4 and pde3/4 inhibitors for use in the treatment of cachexia |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| JP2005089457A (ja) | 2003-09-03 | 2005-04-07 | Yung Shin Pharmaceutical Industry Co Ltd | 骨成長を促進するまたは骨吸収を阻害するための薬剤組成物 |
| US6984652B2 (en) | 2003-09-05 | 2006-01-10 | Warner-Lambert Company Llc | Gyrase inhibitors |
| AU2005219576B2 (en) * | 2004-03-03 | 2011-06-30 | Takeda Gmbh | Novel hydroxy-6-heteroarylphenanthridines and their use as PDE4 inhibitors |
| EP1799673A1 (en) * | 2004-10-15 | 2007-06-27 | Memory Pharmaceuticals Corporation | Pyrazole derivatives as phosphodiesterase 4 inhibitors |
| US7601847B2 (en) | 2004-10-26 | 2009-10-13 | Wyeth | Preparation and purification of 4-(indazol-3-yl)phenols |
| US20070004777A1 (en) * | 2005-03-23 | 2007-01-04 | Bhagwat Shripad S | Methods for treating or preventing acute myelogenous leukemia |
| US7781460B2 (en) | 2005-09-05 | 2010-08-24 | Ranbaxy Laboratories Limited | Substituted indazoles as inhibitors of phosphodiesterase type-IV |
| EP1934219A1 (en) | 2005-09-16 | 2008-06-25 | Ranbaxy Laboratories Limited | Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors |
| CN101370775A (zh) | 2006-01-13 | 2009-02-18 | 惠氏公司 | 作为5-羟基色胺受体配体的经磺酰基取代1h-吲哚 |
| UA94733C2 (ru) | 2006-01-31 | 2011-06-10 | Эррей Биофарма Инк. | Ингибиторы киназы и способы их использования |
| NZ579645A (en) | 2007-03-14 | 2012-01-12 | Ranbaxy Lab Ltd | Pyrazolo (3, 4-b) pyridine derivatives as phosphodiesterase inhibitors |
| WO2009067597A1 (en) * | 2007-11-21 | 2009-05-28 | Decode Genetics Ehf | 4- (or 5-) substituted catechol derivatives |
| JP5216912B2 (ja) | 2008-04-29 | 2013-06-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｃｒ１受容体拮抗薬としてのインダゾール化合物 |
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| CN102596908A (zh) * | 2009-12-08 | 2012-07-18 | 贝林格尔.英格海姆国际有限公司 | 用于制备取代的吲唑和氮杂吲唑化合物的中间体的合成方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| DE2064304A1 (de) * | 1970-12-29 | 1972-07-20 | Agfa-Gevaert Ag, 5090 Leverkusen | Lichtempfindliches farbfotografisches Material |
| US5494911A (en) * | 1990-05-18 | 1996-02-27 | Hoechst Aktiengesellschaft | Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their use |
| US5440038A (en) * | 1993-12-07 | 1995-08-08 | Miles Inc. | Process for the purification of substituted 4-amino-1,2,4-triazine-5-ones |
| AP1147A (en) * | 1996-05-03 | 2003-02-25 | Pfizer | Substituted indazole derivatives and related compounds. |
| US6005118A (en) * | 1996-05-03 | 1999-12-21 | Caron; Stephane | Methods of preparing 4-cyano-4 (substituted indazole) cyclohexane-carboxylic acids useful as PDE4 inhibitors |
| AU716376B2 (en) * | 1996-06-25 | 2000-02-24 | Pfizer Inc. | Substituted indazole derivatives and their use as phosphodiesterase (PDE) type IV and tumor necrosis factor (TNF) inhibitors |
| DE69709493T2 (de) * | 1996-06-27 | 2002-10-31 | Pfizer | Substituierte Indazolderivate |
| CA2264798A1 (en) * | 1996-09-04 | 1998-03-12 | Pfizer Inc. | Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf) |
| JP3399546B2 (ja) * | 1997-05-08 | 2003-04-21 | ファイザー・プロダクツ・インク | 置換されたインダゾール誘導体製造のための方法及び中間体 |
| EP1028946A1 (en) * | 1997-11-04 | 2000-08-23 | Pfizer Products Inc. | Indazole bioisostere replacement of catechol in therapeutically active compounds |
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1998
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- 1998-10-09 YU YU25400A patent/YU25400A/sh unknown
- 1998-10-09 CZ CZ20001623A patent/CZ20001623A3/cs unknown
- 1998-10-09 IL IL13571498A patent/IL135714A0/xx unknown
- 1998-10-09 PL PL98340799A patent/PL340799A1/xx not_active Application Discontinuation
- 1998-10-09 CN CN98811981A patent/CN1281441A/zh active Pending
- 1998-10-09 ID IDW20000820A patent/ID24942A/id unknown
- 1998-10-09 HU HU0100330A patent/HUP0100330A3/hu unknown
- 1998-10-09 KR KR1020007004849A patent/KR20010031783A/ko active IP Right Grant
- 1998-10-09 US US09/381,446 patent/US6716978B2/en not_active Expired - Fee Related
- 1998-10-09 AU AU92777/98A patent/AU754184B2/en not_active Ceased
- 1998-10-09 JP JP2000518951A patent/JP2001521925A/ja not_active Ceased
- 1998-10-09 EA EA200000385A patent/EA200000385A1/ru unknown
- 1998-10-09 BR BR9813938-0A patent/BR9813938A/pt not_active Application Discontinuation
- 1998-10-09 WO PCT/IB1998/001579 patent/WO1999023076A1/en not_active Application Discontinuation
- 1998-10-09 NZ NZ503995A patent/NZ503995A/xx unknown
- 1998-10-09 TR TR2000/01256T patent/TR200001256T2/tr unknown
- 1998-10-09 EP EP98945473A patent/EP1040100A1/en not_active Withdrawn
- 1998-10-09 CA CA002309175A patent/CA2309175A1/en not_active Abandoned
- 1998-10-30 PA PA19988462601A patent/PA8462601A1/es unknown
- 1998-11-02 AP APAP/P/1998/001376A patent/AP1122A/en active
- 1998-11-03 MA MA25331A patent/MA26562A1/fr unknown
- 1998-11-03 TN TNTNSN98199A patent/TNSN98199A1/fr unknown
- 1998-11-03 DZ DZ980249A patent/DZ2639A1/xx active
- 1998-11-03 ZA ZA9810042A patent/ZA9810042B/xx unknown
- 1998-11-03 AR ARP980105533A patent/AR016413A1/es not_active Application Discontinuation
- 1998-11-03 PE PE1998001040A patent/PE131099A1/es not_active Application Discontinuation
- 1998-11-04 UY UY25232A patent/UY25232A1/es not_active Application Discontinuation
- 1998-11-04 HN HN1998000172A patent/HN1998000172A/es unknown
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2000
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- 2000-04-26 NO NO20002127A patent/NO20002127L/no unknown
- 2000-04-28 BG BG104391A patent/BG104391A/xx unknown
- 2000-04-28 OA OA1200000126A patent/OA11353A/en unknown
- 2000-05-04 HR HR20000262A patent/HRP20000262A2/xx not_active Application Discontinuation
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2002
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