ZA200105280B - Nonsteroidal antiinflammatories. - Google Patents
Nonsteroidal antiinflammatories. Download PDFInfo
- Publication number
- ZA200105280B ZA200105280B ZA200105280A ZA200105280A ZA200105280B ZA 200105280 B ZA200105280 B ZA 200105280B ZA 200105280 A ZA200105280 A ZA 200105280A ZA 200105280 A ZA200105280 A ZA 200105280A ZA 200105280 B ZA200105280 B ZA 200105280B
- Authority
- ZA
- South Africa
- Prior art keywords
- group
- methyl
- trifluoromethyl
- hydroxy
- stands
- Prior art date
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- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 title description 2
- -1 5,5,5,4,4-pentafluoropentyl group Chemical group 0.000 claims description 63
- 150000001875 compounds Chemical class 0.000 claims description 63
- 229910052799 carbon Inorganic materials 0.000 claims description 32
- 239000000203 mixture Substances 0.000 claims description 31
- 238000000034 method Methods 0.000 claims description 30
- 239000000126 substance Substances 0.000 claims description 30
- 125000000217 alkyl group Chemical group 0.000 claims description 26
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 22
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 17
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 13
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 12
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 11
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 claims description 11
- 229910052731 fluorine Inorganic materials 0.000 claims description 10
- 125000002252 acyl group Chemical group 0.000 claims description 9
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 9
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 229910052801 chlorine Inorganic materials 0.000 claims description 8
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 125000001153 fluoro group Chemical group F* 0.000 claims description 7
- 125000005843 halogen group Chemical group 0.000 claims description 7
- KLZXOGNPHLCBRX-UHFFFAOYSA-N 3,3,3-trifluoro-2-[[1-(5-fluoro-2-hydroxyphenyl)cyclopropyl]methyl]-2-hydroxy-n-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)propanamide Chemical compound C1=C2C(C)=NOC(=O)C2=CC=C1NC(=O)C(O)(C(F)(F)F)CC1(C=2C(=CC=C(F)C=2)O)CC1 KLZXOGNPHLCBRX-UHFFFAOYSA-N 0.000 claims description 6
- PTRUFSHZSSJJNB-UHFFFAOYSA-N 4-bromo-5-[[4-(5-fluoro-2-hydroxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentyl]amino]-3h-2-benzofuran-1-one Chemical compound C=1C=C2C(=O)OCC2=C(Br)C=1NCC(O)(C(F)(F)F)CC(C)(C)C1=CC(F)=CC=C1O PTRUFSHZSSJJNB-UHFFFAOYSA-N 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims description 6
- 239000011737 fluorine Substances 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 230000002757 inflammatory effect Effects 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
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- 125000004122 cyclic group Chemical group 0.000 claims description 5
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 5
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- JFRDFBMXCNARFQ-UHFFFAOYSA-N 3,3,3-trifluoro-2-[[1-(5-fluoro-2-hydroxyphenyl)cyclopropyl]methyl]-2-hydroxy-n-(1-oxo-3h-2-benzofuran-5-yl)propanamide Chemical compound OC1=CC=C(F)C=C1C1(CC(O)(C(=O)NC=2C=C3COC(=O)C3=CC=2)C(F)(F)F)CC1 JFRDFBMXCNARFQ-UHFFFAOYSA-N 0.000 claims description 4
- HRDWGLORAAHIRG-UHFFFAOYSA-N 3,3,3-trifluoro-2-[[1-(5-fluoro-2-methoxyphenyl)cyclopropyl]methyl]-2-hydroxy-n-(1-oxo-3h-2-benzofuran-5-yl)propanamide Chemical compound COC1=CC=C(F)C=C1C1(CC(O)(C(=O)NC=2C=C3COC(=O)C3=CC=2)C(F)(F)F)CC1 HRDWGLORAAHIRG-UHFFFAOYSA-N 0.000 claims description 4
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- DUSKZEWQNAKIFC-UHFFFAOYSA-N 6-[[4-(4-bromo-2-methoxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentyl]amino]-4-methyl-2,3-benzoxazin-1-one Chemical compound COC1=CC(Br)=CC=C1C(C)(C)CC(O)(C(F)(F)F)CNC1=CC=C2C(=O)ON=C(C)C2=C1 DUSKZEWQNAKIFC-UHFFFAOYSA-N 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
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- 229910052794 bromium Inorganic materials 0.000 claims description 4
- 239000000460 chlorine Substances 0.000 claims description 4
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 4
- 238000002560 therapeutic procedure Methods 0.000 claims description 4
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- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 3
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- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- 229910002651 NO3 Inorganic materials 0.000 claims description 3
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
- 125000003647 acryloyl group Chemical group O=C([*])C([H])=C([H])[H] 0.000 claims description 3
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 3
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 3
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
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- C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
- C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
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- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19856475A DE19856475A1 (de) | 1998-11-27 | 1998-11-27 | Nichtsteroidale Entzündungshemmer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200105280B true ZA200105280B (en) | 2002-06-26 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200105280A ZA200105280B (en) | 1998-11-27 | 2001-06-26 | Nonsteroidal antiinflammatories. |
Country Status (31)
| Country | Link |
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| US (1) | US6323199B1 (no) |
| EP (1) | EP1133486B1 (no) |
| JP (1) | JP2002531446A (no) |
| KR (1) | KR100762058B1 (no) |
| CN (1) | CN1171883C (no) |
| AR (1) | AR021419A1 (no) |
| AT (1) | ATE285405T1 (no) |
| AU (1) | AU762735B2 (no) |
| BG (1) | BG65030B1 (no) |
| BR (1) | BR9915755A (no) |
| CA (1) | CA2352367A1 (no) |
| CO (1) | CO5140109A1 (no) |
| CZ (1) | CZ20011866A3 (no) |
| DE (2) | DE19856475A1 (no) |
| EA (1) | EA003299B1 (no) |
| EE (1) | EE200100283A (no) |
| ES (1) | ES2235543T3 (no) |
| HK (1) | HK1043592B (no) |
| HR (1) | HRP20010483B1 (no) |
| HU (1) | HUP0104578A3 (no) |
| IL (2) | IL143393A0 (no) |
| MY (1) | MY136016A (no) |
| NO (1) | NO20012562L (no) |
| NZ (1) | NZ511950A (no) |
| PE (1) | PE20001245A1 (no) |
| PL (1) | PL348329A1 (no) |
| PT (1) | PT1133486E (no) |
| SK (1) | SK7212001A3 (no) |
| UA (1) | UA73102C2 (no) |
| WO (1) | WO2000032584A2 (no) |
| ZA (1) | ZA200105280B (no) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US7238707B2 (en) * | 2000-07-28 | 2007-07-03 | Schering Ag | Substituted pentanols, a process for their production and their use as anti-inflammatory agents |
| DE10346940B3 (de) * | 2003-10-06 | 2005-06-16 | Schering Ag | Substituierte Pentanole, ihre Verwendung zur Herstellung von Arzneimitteln speziell Entzündungshemmer sowie diese enthaltende pharmazeutische Präparate |
| DE10038639A1 (de) * | 2000-07-28 | 2002-02-21 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| CA2446136C (en) * | 2001-05-03 | 2011-07-05 | Galileo Pharmaceuticals, Inc. | Pyruvate derivatives |
| CA2472746A1 (en) * | 2002-01-14 | 2003-07-24 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof |
| JP2005521717A (ja) * | 2002-03-26 | 2005-07-21 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用 |
| CN1633296A (zh) * | 2002-03-26 | 2005-06-29 | 贝林格尔·英格海姆药物公司 | 糖皮质素模拟物、其制备方法、药物组合物及其用途 |
| US6897224B2 (en) * | 2002-04-02 | 2005-05-24 | Schering Ag | Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors |
| DE10215316C1 (de) * | 2002-04-02 | 2003-12-18 | Schering Ag | Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer |
| US7186864B2 (en) | 2002-05-29 | 2007-03-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| US7074806B2 (en) * | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| JP2006504678A (ja) * | 2002-08-21 | 2006-02-09 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用 |
| EP1539141B1 (en) * | 2002-08-29 | 2010-07-14 | Boehringer Ingelheim Pharmaceuticals Inc. | 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases |
| US7112584B2 (en) * | 2002-12-20 | 2006-09-26 | Schering Ag | Nonsteroidal antiinflammatory agents |
| DE10261874A1 (de) * | 2002-12-20 | 2004-07-08 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| MXPA05006872A (es) * | 2003-01-03 | 2005-08-16 | Boehringer Ingelheim Pharma | Derivados de 1-propanol y 1-propilamina y su uso como ligandos glucocorticoides. |
| WO2004071389A2 (en) * | 2003-02-15 | 2004-08-26 | Glaxo Group Limited | Non-steroidal infalmmation inhibitors |
| US20040224992A1 (en) * | 2003-02-27 | 2004-11-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| US20050090559A1 (en) * | 2003-07-01 | 2005-04-28 | Markus Berger | Heterocyclically-substituted pentanol derivatives, process for their production and their use as anti-inflammatory agents |
| JP2008529963A (ja) * | 2003-07-01 | 2008-08-07 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | 複素環式−置換されたペンタノール誘導体類、それらの生成方法及び抗炎症剤としてのそれらの使用 |
| UY28526A1 (es) | 2003-09-24 | 2005-04-29 | Boehringer Ingelheim Pharma | Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos |
| DE10347385A1 (de) * | 2003-10-08 | 2005-05-12 | Schering Ag | Umgelagerte Pentanole, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| JP4468369B2 (ja) * | 2003-10-16 | 2010-05-26 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | ある種のトリフルオロメチル置換アルコールの立体選択的合成 |
| US7795272B2 (en) * | 2004-03-13 | 2010-09-14 | Boehringer Ingelheim Pharmaceutical, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof |
| GB0418045D0 (en) | 2004-08-12 | 2004-09-15 | Glaxo Group Ltd | Compounds |
| ES2326907T3 (es) * | 2004-12-27 | 2009-10-21 | Boehringer Ingelheim Pharmaceuticals Inc. | Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y su uso. |
| RU2007148225A (ru) | 2005-06-10 | 2009-07-20 | БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) | Глюкокортикоидные миметики, способы их получения, фармацевтические композиции и их применение |
| DE102005030292A1 (de) * | 2005-06-24 | 2007-01-11 | Schering Ag | Nichtsteroidale Progesteronrezeptor-Modulatoren |
| GB0513297D0 (en) * | 2005-06-29 | 2005-08-03 | Glaxo Group Ltd | Novel compounds |
| CA2519010A1 (en) | 2005-09-13 | 2007-03-13 | Cognos Incorporated | Query framework system and method |
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| CN101326169B (zh) * | 2005-12-09 | 2011-11-16 | 霍夫曼-拉罗奇有限公司 | 作为抗炎剂的糖皮质激素受体调节剂 |
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| WO2007120083A1 (en) * | 2006-04-13 | 2007-10-25 | Astrazeneca Ab | The use of carboxamide derivatives in the manufacture of a medicament for the treatment of inflammatory, allergic and dermatological conditions |
| CA2649509A1 (en) * | 2006-04-20 | 2007-11-01 | Glaxo Group Limited | Novel compounds |
| GB0611587D0 (en) * | 2006-06-12 | 2006-07-19 | Glaxo Group Ltd | Novel compounds |
| WO2008000777A2 (en) * | 2006-06-29 | 2008-01-03 | Glaxo Group Limited | Phenyl- pyrazole derivatives, process for their preparation and their pharmaceutical use |
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| WO2008074814A1 (en) * | 2006-12-20 | 2008-06-26 | Glaxo Group Limited | Pyrazole derivatives as non-steroidal glucocorticoid receptor ligands |
| JO2754B1 (en) * | 2006-12-21 | 2014-03-15 | استرازينكا ايه بي | Amylendazoleil derivatives for the treatment of glucocorticoid-mediated disorders |
| UY30805A1 (es) * | 2006-12-21 | 2008-07-31 | Bayer Schering Pharma Ag | Moduladores no esteroides de receptores de progesterona |
| CL2008000474A1 (es) * | 2007-02-15 | 2008-08-22 | Argenta Discovery Ltd | Compuestos derivados de azonia-biciclo-[2.2.2]octano, moduladores del receptor m3; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como epoc, asma, sindrome del intestino irritable, entre otras. |
| SA109300309B1 (ar) | 2008-05-20 | 2013-01-22 | باير شيرنج فارما ايه جي | مشتقات فينيل وبنزو داي أوكسينيل إندازول بها استبدال |
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| GB0814729D0 (en) * | 2008-08-12 | 2008-09-17 | Argenta Discovery Ltd | New combination |
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| WO2011061527A1 (en) | 2009-11-17 | 2011-05-26 | Astrazeneca Ab | Combinations comprising a glucocorticoid receptor modulator for the treatment of respiratory diseases |
| EP3569228A1 (en) * | 2018-05-17 | 2019-11-20 | Association pour la recherche à l'IGBMC (ARI) | Non-steroidal selective glucocorticoid receptor agonistic modulators (segrams) and uses thereof |
| US20190151283A1 (en) | 2017-10-27 | 2019-05-23 | Association Pour La Recherche À L'igbmc (Ari) | NON-STEROIDAL SELECTIVE GLUCOCORTICOID RECEPTOR AGONISTIC MODULATORS (SEGRAMs) AND USES THEREOF |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1261835A (en) | 1984-08-20 | 1989-09-26 | Masaaki Toda | (fused) benz(thio)amides |
| GB8617652D0 (en) * | 1986-07-18 | 1986-08-28 | Ici Plc | Acylanilide derivatives |
| GB8617653D0 (en) | 1986-07-18 | 1986-08-28 | Ici Plc | Amide derivatives |
| DE19723722A1 (de) * | 1997-05-30 | 1998-12-10 | Schering Ag | Nichtsteroidale Gestagene |
-
1998
- 1998-11-27 DE DE19856475A patent/DE19856475A1/de not_active Withdrawn
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1999
- 1999-11-24 US US09/448,278 patent/US6323199B1/en not_active Expired - Fee Related
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- 1999-11-26 PE PE1999001188A patent/PE20001245A1/es not_active Application Discontinuation
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- 1999-11-29 BR BR9915755-1A patent/BR9915755A/pt not_active Application Discontinuation
- 1999-11-29 EE EEP200100283A patent/EE200100283A/xx unknown
- 1999-11-29 AU AU19760/00A patent/AU762735B2/en not_active Ceased
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- 1999-11-29 EP EP99963476A patent/EP1133486B1/de not_active Expired - Lifetime
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- 1999-11-29 WO PCT/EP1999/009754 patent/WO2000032584A2/de not_active Application Discontinuation
- 1999-11-29 KR KR1020017006613A patent/KR100762058B1/ko not_active IP Right Cessation
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- 1999-11-29 CA CA002352367A patent/CA2352367A1/en not_active Abandoned
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