ZA200107259B - Biphenyl derivatives as antagonists of the neurokinine-1 receptor. - Google Patents
Biphenyl derivatives as antagonists of the neurokinine-1 receptor. Download PDFInfo
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- ZA200107259B ZA200107259B ZA200107259A ZA200107259A ZA200107259B ZA 200107259 B ZA200107259 B ZA 200107259B ZA 200107259 A ZA200107259 A ZA 200107259A ZA 200107259 A ZA200107259 A ZA 200107259A ZA 200107259 B ZA200107259 B ZA 200107259B
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- South Africa
- Prior art keywords
- compound
- formula
- methyl
- trifluoromethyl
- biphenyl
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- 239000005557 antagonist Substances 0.000 title description 4
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical class C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 106
- 238000000034 method Methods 0.000 claims description 24
- 125000001424 substituent group Chemical group 0.000 claims description 20
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 13
- -1 -N(R®) Chemical group 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000004571 thiomorpholin-4-yl group Chemical group N1(CCSCC1)* 0.000 description 1
- 229940086542 triethylamine Drugs 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
- A61P25/06—Antimigraine agents
-
- 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
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- 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]
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/12—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
- C07C233/15—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/44—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/66—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Addiction (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Otolaryngology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99104626 | 1999-03-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200107259B true ZA200107259B (en) | 2002-12-02 |
Family
ID=8237723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200107259A ZA200107259B (en) | 1999-03-09 | 2001-08-31 | Biphenyl derivatives as antagonists of the neurokinine-1 receptor. |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US6291465B1 (ja) |
| EP (1) | EP1171419B1 (ja) |
| JP (1) | JP3839668B2 (ja) |
| KR (1) | KR100473247B1 (ja) |
| CN (1) | CN1152006C (ja) |
| AR (1) | AR043273A1 (ja) |
| AT (1) | ATE286018T1 (ja) |
| AU (1) | AU767449B2 (ja) |
| BR (1) | BR0008862A (ja) |
| CA (1) | CA2366205C (ja) |
| CO (1) | CO5160261A1 (ja) |
| CZ (1) | CZ20013190A3 (ja) |
| DE (1) | DE60017110T2 (ja) |
| ES (1) | ES2233338T3 (ja) |
| HK (1) | HK1045684B (ja) |
| HR (1) | HRP20010629A2 (ja) |
| HU (1) | HUP0201710A3 (ja) |
| IL (2) | IL145166A0 (ja) |
| JO (1) | JO2235B1 (ja) |
| MA (1) | MA26778A1 (ja) |
| MY (1) | MY121145A (ja) |
| NO (1) | NO20014356L (ja) |
| NZ (1) | NZ513824A (ja) |
| PE (1) | PE20001549A1 (ja) |
| PL (1) | PL201681B1 (ja) |
| PT (1) | PT1171419E (ja) |
| RU (1) | RU2238266C2 (ja) |
| SI (1) | SI1171419T1 (ja) |
| TR (1) | TR200102585T2 (ja) |
| UY (1) | UY26051A1 (ja) |
| WO (1) | WO2000053572A1 (ja) |
| YU (1) | YU64901A (ja) |
| ZA (1) | ZA200107259B (ja) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR200102490T2 (tr) | 1999-02-24 | 2001-12-21 | F.Hoffmann-La Roche Ag | Fenil ve piridinil türevleri |
| AUPQ514600A0 (en) | 2000-01-18 | 2000-02-10 | James Cook University | Brain injury treatment |
| TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| US6642226B2 (en) | 2001-02-06 | 2003-11-04 | Hoffman-La Roche Inc. | Substituted phenyl-piperidine methanone compounds |
| US6531597B2 (en) * | 2001-02-13 | 2003-03-11 | Hoffmann-La Roche Inc. | Process for preparation of 2-phenyl acetic acid derivatives |
| NZ535366A (en) | 2002-03-13 | 2007-07-27 | Univ Tennessee Res Foundation | Substituted tetrahydroisoquinoline compounds, methods of making, and their use |
| EP1888549A2 (en) * | 2005-05-19 | 2008-02-20 | Vertex Pharmaceuticals, Inc. | Biaryls useful as modulators of ion channels |
| JP5388574B2 (ja) | 2005-05-31 | 2014-01-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとして有用なヘテロ環式類 |
| ES2672099T3 (es) | 2011-07-04 | 2018-06-12 | Irbm - Science Park S.P.A. | Antagonistas del receptor NK-1 para el tratamiento de la neovascularización corneal |
| US10975049B2 (en) | 2016-05-23 | 2021-04-13 | Institute Of Materia Medica, Chinese Academy Of Medical Sciences | Nicotinyl alcohol ether derivative, preparation method therefor, and pharmaceutical composition and uses thereof |
| AU2019223237A1 (en) | 2018-02-26 | 2020-09-03 | Ospedale San Raffaele S.R.L. | NK-1 antagonists for use in the treatment of ocular pain |
| WO2021180885A1 (en) | 2020-03-11 | 2021-09-16 | Ospedale San Raffaele S.R.L. | Treatment of stem cell deficiency |
| CN115466195B (zh) * | 2022-09-15 | 2024-04-19 | 中国科学院成都生物研究所 | 一类联苯类酰胺化合物及其制备方法和应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06227913A (ja) * | 1993-02-03 | 1994-08-16 | Sumitomo Chem Co Ltd | 安息香酸誘導体を有効成分とする植物病害防除剤 |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| BR9408442A (pt) | 1993-12-29 | 1997-08-05 | Merck Sharp & Dohme | Composto composição farmacêutica processos para tratamento ou prevenção de distúrbios fisiológicos associados com um excesso de taquiquininas e para a preparação do composto e de uso do composto |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| JP3839518B2 (ja) * | 1996-03-27 | 2006-11-01 | ポーラ化成工業株式会社 | 抗真菌剤 |
| CN1252792A (zh) | 1997-04-18 | 2000-05-10 | 辉瑞大药厂 | 制备4'－三氟甲基－联苯基－2－羧酸(1,2,3,4－四氢－异喹啉－6－基)酰胺的方法和中间体 |
| US5972938A (en) | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
| ATE496032T1 (de) * | 1999-02-24 | 2011-02-15 | Hoffmann La Roche | 4-phenylpyridinderivate und deren verwendung als nk-1 rezeptorantagonisten |
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2000
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- 2000-02-28 JP JP2000604013A patent/JP3839668B2/ja not_active Expired - Fee Related
- 2000-02-28 PT PT00909264T patent/PT1171419E/pt unknown
- 2000-02-28 RU RU2001126547A patent/RU2238266C2/ru not_active IP Right Cessation
- 2000-02-28 AT AT00909264T patent/ATE286018T1/de not_active IP Right Cessation
- 2000-02-28 EP EP00909264A patent/EP1171419B1/en not_active Expired - Lifetime
- 2000-02-28 HU HU0201710A patent/HUP0201710A3/hu unknown
- 2000-02-28 BR BR0008862-5A patent/BR0008862A/pt not_active Application Discontinuation
- 2000-02-28 TR TR2001/02585T patent/TR200102585T2/xx unknown
- 2000-02-28 DE DE60017110T patent/DE60017110T2/de not_active Expired - Lifetime
- 2000-02-28 NZ NZ513824A patent/NZ513824A/xx unknown
- 2000-02-28 CZ CZ20013190A patent/CZ20013190A3/cs unknown
- 2000-02-28 SI SI200030598T patent/SI1171419T1/xx unknown
- 2000-02-28 AU AU31612/00A patent/AU767449B2/en not_active Ceased
- 2000-02-28 CA CA002366205A patent/CA2366205C/en not_active Expired - Fee Related
- 2000-02-28 ES ES00909264T patent/ES2233338T3/es not_active Expired - Lifetime
- 2000-02-28 CN CNB008047812A patent/CN1152006C/zh not_active Expired - Fee Related
- 2000-02-28 PL PL350536A patent/PL201681B1/pl not_active IP Right Cessation
- 2000-02-28 IL IL14516600A patent/IL145166A0/xx active IP Right Grant
- 2000-02-28 KR KR10-2001-7011407A patent/KR100473247B1/ko not_active IP Right Cessation
- 2000-03-02 JO JO200017A patent/JO2235B1/en active
- 2000-03-03 PE PE2000000177A patent/PE20001549A1/es not_active Application Discontinuation
- 2000-03-06 MY MYPI20000864A patent/MY121145A/en unknown
- 2000-03-06 CO CO00016011A patent/CO5160261A1/es unknown
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- 2000-03-08 UY UY26051A patent/UY26051A1/es unknown
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2001
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- 2001-08-28 HR HR20010629A patent/HRP20010629A2/hr not_active Application Discontinuation
- 2001-08-28 IL IL145166A patent/IL145166A/en not_active IP Right Cessation
- 2001-08-31 ZA ZA200107259A patent/ZA200107259B/en unknown
- 2001-09-07 MA MA26322A patent/MA26778A1/fr unknown
- 2001-09-07 NO NO20014356A patent/NO20014356L/no not_active Application Discontinuation
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2002
- 2002-09-26 HK HK02107102.8A patent/HK1045684B/zh not_active IP Right Cessation
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