AR045378A1 - Analogos de quinazolina como inhibidores del receptor de tirosin quinasas - Google Patents
Analogos de quinazolina como inhibidores del receptor de tirosin quinasasInfo
- Publication number
- AR045378A1 AR045378A1 ARP040102929A ARP040102929A AR045378A1 AR 045378 A1 AR045378 A1 AR 045378A1 AR P040102929 A ARP040102929 A AR P040102929A AR P040102929 A ARP040102929 A AR P040102929A AR 045378 A1 AR045378 A1 AR 045378A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocyclyl
- cycloalkyl
- alkyl
- nr4r6
- nr4c
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 35
- 125000001072 heteroaryl group Chemical group 0.000 abstract 21
- 125000003118 aryl group Chemical group 0.000 abstract 20
- 125000004429 atom Chemical group 0.000 abstract 18
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 17
- 125000000304 alkynyl group Chemical group 0.000 abstract 16
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 16
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 15
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 15
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 15
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 14
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 13
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 13
- 229910052736 halogen Inorganic materials 0.000 abstract 13
- 150000002367 halogens Chemical class 0.000 abstract 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 12
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 11
- BPXYEYJNCXITEY-UHFFFAOYSA-N diazonio(trifluoromethoxy)azanide Chemical compound FC(F)(F)ON=[N+]=[N-] BPXYEYJNCXITEY-UHFFFAOYSA-N 0.000 abstract 10
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 10
- OFDNQWIFNXBECV-VFSYNPLYSA-N dolastatin 10 Chemical compound CC(C)[C@H](N(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C=1SC=CN=1)CC1=CC=CC=C1 OFDNQWIFNXBECV-VFSYNPLYSA-N 0.000 abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- 125000004043 oxo group Chemical group O=* 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- -1 heteroaryloalkyl lo Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
-
- 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
- A61P35/00—Antineoplastic 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
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Health & Medical Sciences (AREA)
- Manufacturing & Machinery (AREA)
- Ceramic Engineering (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Materials Engineering (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Structural Engineering (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/642,440 US7501427B2 (en) | 2003-08-14 | 2003-08-14 | Quinazoline analogs as receptor tyrosine kinase inhibitors |
| US55171804P | 2004-03-10 | 2004-03-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045378A1 true AR045378A1 (es) | 2005-10-26 |
Family
ID=34198338
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102929A AR045378A1 (es) | 2003-08-14 | 2004-08-13 | Analogos de quinazolina como inhibidores del receptor de tirosin quinasas |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US7452895B2 (enExample) |
| EP (1) | EP1660090B1 (enExample) |
| JP (1) | JP4828421B2 (enExample) |
| KR (2) | KR101028952B1 (enExample) |
| CN (3) | CN102432552B (enExample) |
| AR (1) | AR045378A1 (enExample) |
| AU (1) | AU2004264937B2 (enExample) |
| BR (1) | BRPI0413565B8 (enExample) |
| CA (1) | CA2535614C (enExample) |
| CL (1) | CL2004002066A1 (enExample) |
| CY (1) | CY1113992T1 (enExample) |
| DK (1) | DK1660090T3 (enExample) |
| ES (1) | ES2399427T3 (enExample) |
| IL (1) | IL173593A (enExample) |
| IS (1) | IS8288A (enExample) |
| MX (1) | MXPA06001767A (enExample) |
| NO (1) | NO336275B1 (enExample) |
| NZ (1) | NZ545459A (enExample) |
| PL (1) | PL1660090T3 (enExample) |
| PT (1) | PT1660090E (enExample) |
| RU (1) | RU2350605C2 (enExample) |
| TW (1) | TWI353982B (enExample) |
| WO (1) | WO2005016346A1 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7488823B2 (en) * | 2003-11-10 | 2009-02-10 | Array Biopharma, Inc. | Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors |
| JP4828421B2 (ja) * | 2003-08-14 | 2011-11-30 | アレイ バイオファーマ、インコーポレイテッド | 受容体チロシンキナーゼ阻害剤としてのキナゾリン誘導体 |
| US7501427B2 (en) | 2003-08-14 | 2009-03-10 | Array Biopharma, Inc. | Quinazoline analogs as receptor tyrosine kinase inhibitors |
| CA2755268C (en) | 2005-11-15 | 2013-12-31 | Array Biopharma, Inc. | Erbb inhibitors |
| DK2765990T3 (da) | 2011-10-14 | 2017-11-13 | Array Biopharma Inc | Faststofdispersion |
| RU2629116C2 (ru) | 2011-10-14 | 2017-08-24 | Эррэй Биофарма Инк. | Полиморфы arry-380, селективного ингибитора erbb2, и фармацевтические составы, содержащие их |
| KR102317166B1 (ko) | 2012-03-23 | 2021-10-26 | 어레이 바이오파마 인크. | 뇌암의 치료 |
| JP2018526382A (ja) * | 2015-09-04 | 2018-09-13 | アスラン ファーマシューティカルズ ピーティーイー リミテッド | 耐性癌または難治性癌の治療用バルリチニブ |
| JP2019514864A (ja) * | 2016-04-21 | 2019-06-06 | アスラン ファーマシューティカルズ ピーティーイー リミテッド | 肝癌の治療方法 |
| GB201611580D0 (en) * | 2016-07-01 | 2016-08-17 | Aslan Pharmaceuticals Pte Ltd | Method |
| CN106317040A (zh) * | 2016-08-09 | 2017-01-11 | 浙江医药高等专科学校 | 含噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及用途 |
| CN106317039A (zh) * | 2016-08-09 | 2017-01-11 | 浙江医药高等专科学校 | 一种含噻吩磺酰胺结构的乙氧苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及用途 |
| CN106349230A (zh) * | 2016-08-09 | 2017-01-25 | 浙江医药高等专科学校 | 一种含硝基噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂及用途 |
| CN106349231A (zh) * | 2016-08-09 | 2017-01-25 | 浙江医药高等专科学校 | 一类含卤代噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂 |
| CN106279135A (zh) * | 2016-08-09 | 2017-01-04 | 浙江医药高等专科学校 | 一种噻吩磺酰胺结构的苯并喹唑啉类酪氨酸激酶抑制剂 |
| SG10201913858WA (en) | 2016-08-26 | 2020-03-30 | Agency Science Tech & Res | Macrophage stimulating protein receptor (or ron - recepteur d' origine nantais) antibodies and uses thereof |
| TW201834649A (zh) | 2017-03-02 | 2018-10-01 | 新加坡商亞獅康私人有限公司 | 癌症療法 |
| WO2018201016A1 (en) | 2017-04-28 | 2018-11-01 | Cascadian Therapeutics, Inc. | Treatment of her2 positive cancers |
| WO2018222134A1 (en) | 2017-06-02 | 2018-12-06 | Aslan Pharmaceuticals Pte Ltd | Cancer therapy |
| WO2018222135A1 (en) | 2017-06-02 | 2018-12-06 | Aslan Pharmaceuticals Pte Ltd | Cancer therapy |
| HUE065578T2 (hu) | 2018-09-18 | 2024-06-28 | Hoffmann La Roche | Kinazolin-származékok, mint daganatellenes szerek |
| KR20210090625A (ko) | 2018-10-09 | 2021-07-20 | 아슬란 파마슈티컬스 피티이 엘티디 | 바를리티닙의 말론산 염 |
| ES2989387T3 (es) | 2019-05-31 | 2024-11-26 | Janssen Pharmaceutica Nv | Pequeñas moléculas inhibidoras de la quinasa inductora de nf-kb |
| CN111499622B (zh) * | 2019-07-08 | 2023-06-06 | 山东省科学院菏泽分院 | 一种治疗胆管癌的药物的制备方法 |
| TW202214641A (zh) | 2020-06-30 | 2022-04-16 | 美商艾瑞生藥股份有限公司 | Ｈｅｒ２突變抑制劑 |
| JP7511097B1 (ja) | 2021-06-26 | 2024-07-04 | アレイ バイオファーマ インコーポレイテッド | Ｈｅｒ２変異阻害薬 |
| WO2023081637A1 (en) * | 2021-11-02 | 2023-05-11 | Enliven Therapeutics, Inc. | Fused tetracyclic quinazoline derivatives as inhibitors of erbb2 |
| JP2025509995A (ja) * | 2022-03-28 | 2025-04-11 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 含窒素複素環系化合物、その調製方法及びその医薬的使用 |
| AU2024353411A1 (en) * | 2023-09-27 | 2026-05-07 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Pharmaceutically acceptable salt and crystalline form of quinazoline derivative, and use thereof |
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| US2583774A (en) * | 1948-04-30 | 1952-01-29 | Merck & Co Inc | Vitamin b6 derivatives |
| BE795970A (fr) * | 1972-02-29 | 1973-08-27 | Pfizer | Nouveaux derives de quinoleine, quinoxaline et quinazoline er composition pharmaceutiques les contenant |
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| CA1340821C (en) | 1988-10-06 | 1999-11-16 | Nobuyuki Fukazawa | Heterocyclic compounds and anticancer-drug reinforcing agents containing them as effective components |
| US5502187A (en) * | 1992-04-03 | 1996-03-26 | The Upjohn Company | Pharmaceutically active bicyclic-heterocyclic amines |
| GB9510757D0 (en) | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
| TW321649B (enExample) * | 1994-11-12 | 1997-12-01 | Zeneca Ltd | |
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| DE69536015D1 (de) * | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Chinazolinone Derivate |
| GB9508538D0 (en) * | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| AR004010A1 (es) * | 1995-10-11 | 1998-09-30 | Glaxo Group Ltd | Compuestos heterociclicos |
| WO1997030035A1 (en) | 1996-02-13 | 1997-08-21 | Zeneca Limited | Quinazoline derivatives as vegf inhibitors |
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| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
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| US7169788B2 (en) | 2001-10-30 | 2007-01-30 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| JP2005515176A (ja) | 2001-11-03 | 2005-05-26 | アストラゼネカ アクチボラグ | 抗腫瘍剤としてのキナゾリン誘導体 |
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| US7488823B2 (en) | 2003-11-10 | 2009-02-10 | Array Biopharma, Inc. | Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors |
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2004
- 2004-08-10 JP JP2006523384A patent/JP4828421B2/ja not_active Expired - Lifetime
- 2004-08-10 KR KR1020107000942A patent/KR101028952B1/ko not_active Expired - Lifetime
- 2004-08-10 NZ NZ545459A patent/NZ545459A/en not_active IP Right Cessation
- 2004-08-10 PL PL04780990T patent/PL1660090T3/pl unknown
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- 2004-08-10 CA CA002535614A patent/CA2535614C/en not_active Expired - Lifetime
- 2004-08-10 RU RU2006103493/04A patent/RU2350605C2/ru active
- 2004-08-10 AU AU2004264937A patent/AU2004264937B2/en active Active
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- 2004-08-10 CN CN201110283526.1A patent/CN102432552B/zh not_active Expired - Lifetime
- 2004-08-10 KR KR1020067003060A patent/KR100953246B1/ko not_active Expired - Lifetime
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