JP2005535608A - エポシロンを含む組み合わせおよびその薬学的使用 - Google Patents
エポシロンを含む組み合わせおよびその薬学的使用 Download PDFInfo
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- JP2005535608A JP2005535608A JP2004510831A JP2004510831A JP2005535608A JP 2005535608 A JP2005535608 A JP 2005535608A JP 2004510831 A JP2004510831 A JP 2004510831A JP 2004510831 A JP2004510831 A JP 2004510831A JP 2005535608 A JP2005535608 A JP 2005535608A
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- inhibitor
- topoisomerase
- hydrogen
- lower alkyl
- pharmaceutically acceptable
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- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical class C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000011477 surgical intervention Methods 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229960003454 tamoxifen citrate Drugs 0.000 description 1
- FQZYTYWMLGAPFJ-OQKDUQJOSA-N tamoxifen citrate Chemical compound [H+].[H+].[H+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 FQZYTYWMLGAPFJ-OQKDUQJOSA-N 0.000 description 1
- 229940063683 taxotere Drugs 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 210000001550 testis Anatomy 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
- 229960003433 thalidomide Drugs 0.000 description 1
- 229940034915 thalomid Drugs 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 229940098465 tincture Drugs 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- RTKIYFITIVXBLE-QEQCGCAPSA-N trichostatin A Chemical compound ONC(=O)/C=C/C(/C)=C/[C@@H](C)C(=O)C1=CC=C(N(C)C)C=C1 RTKIYFITIVXBLE-QEQCGCAPSA-N 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
- JXLYSJRDGCGARV-CFWMRBGOSA-N vinblastine Chemical compound C([C@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-CFWMRBGOSA-N 0.000 description 1
- 229960004528 vincristine Drugs 0.000 description 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 229940033942 zoladex Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/30—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
- C07K16/3015—Breast
-
- 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- C07D417/02—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 two hetero rings
- C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Genetics & Genomics (AREA)
- Cell Biology (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38702502P | 2002-06-10 | 2002-06-10 | |
| US40623902P | 2002-08-27 | 2002-08-27 | |
| US40623802P | 2002-08-27 | 2002-08-27 | |
| US43867703P | 2003-01-08 | 2003-01-08 | |
| US43867603P | 2003-01-08 | 2003-01-08 | |
| PCT/EP2003/005988 WO2003103712A1 (en) | 2002-06-01 | 2003-06-06 | Combinations comprising epothilones and pharmaceutical uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005535608A true JP2005535608A (ja) | 2005-11-24 |
| JP2005535608A5 JP2005535608A5 (enExample) | 2006-07-20 |
Family
ID=29741146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004510831A Pending JP2005535608A (ja) | 2002-06-10 | 2003-06-06 | エポシロンを含む組み合わせおよびその薬学的使用 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20050271669A1 (enExample) |
| EP (2) | EP2179745A1 (enExample) |
| JP (1) | JP2005535608A (enExample) |
| CN (2) | CN1658904A (enExample) |
| AT (1) | ATE476995T1 (enExample) |
| AU (1) | AU2003242646A1 (enExample) |
| BR (1) | BR0311714A (enExample) |
| CA (1) | CA2487147A1 (enExample) |
| DE (1) | DE60333754D1 (enExample) |
| IL (1) | IL165180A0 (enExample) |
| MX (1) | MXPA04012444A (enExample) |
| NO (1) | NO20050096L (enExample) |
| PL (1) | PL372070A1 (enExample) |
| SG (1) | SG162616A1 (enExample) |
| WO (1) | WO2003103712A1 (enExample) |
| ZA (1) | ZA200409137B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019537583A (ja) * | 2016-10-28 | 2019-12-26 | アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | ヒストン脱アセチル化酵素阻害剤及びエポチロンを含む医薬品組み合わせならびにその使用方法 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7154002B1 (en) | 2002-10-08 | 2006-12-26 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| CA2518318A1 (en) | 2003-03-17 | 2004-09-30 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| JO2596B1 (en) * | 2004-11-30 | 2011-02-27 | نوفارتيس ايه جي | Compositions include epothelones and tyrosine protein kinase inhibitors and their pharmaceutical uses |
| EP1824831A2 (en) | 2004-12-16 | 2007-08-29 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| JP2008540574A (ja) | 2005-05-11 | 2008-11-20 | タケダ サン ディエゴ インコーポレイテッド | ヒストンデアセチラーゼ阻害剤 |
| CN101263121A (zh) | 2005-07-14 | 2008-09-10 | 塔克达圣地亚哥公司 | 组蛋白脱乙酰基酶抑制剂 |
| WO2008058287A1 (en) * | 2006-11-10 | 2008-05-15 | Syndax Pharmaceuticals, Inc. | COMBINATION OF ERα+ LIGANDS AND HISTONE DEACETYLASE INHIBITORS FOR THE TREATMENT OF CANCER |
| WO2009015237A1 (en) * | 2007-07-23 | 2009-01-29 | Syndax Pharmaceuticals, Inc. | Novel compounds and methods of using them |
| US20100298270A1 (en) * | 2007-07-23 | 2010-11-25 | Syndax Pharmaceuticals, Inc. | Novel Compounds and Methods of Using Them |
| WO2009058895A1 (en) * | 2007-10-30 | 2009-05-07 | Syndax Pharmaceuticals, Inc. | Administration of an inhibitor of hdac and an mtor inhibitor |
| US20090131367A1 (en) * | 2007-11-19 | 2009-05-21 | The Regents Of The University Of Colorado | Combinations of HDAC Inhibitors and Proteasome Inhibitors |
| US20110182888A1 (en) * | 2008-04-08 | 2011-07-28 | Peter Ordentlich | Administration of an Inhibitor of HDAC, an Inhibitor of HER-2, and a Selective Estrogen Receptor Modulator |
| WO2011146638A1 (en) | 2010-05-18 | 2011-11-24 | Cerulean Pharma Inc. | Compositions and methods for treatment of autoimmune and other diseases |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001507716A (ja) * | 1996-12-03 | 2001-06-12 | スローン−ケッタリング インスティトュート フォア キャンサー リサーチ | エポチロンの合成とその中間体及びその類似物並びにその使用 |
| WO2001064650A2 (en) * | 2000-03-01 | 2001-09-07 | Sloan-Kettering Institute For Cancer Research Center | Synthesis of epothilones, intermediates thereto and analogues thereof |
| WO2001072721A2 (en) * | 2000-03-27 | 2001-10-04 | Bristol-Myers Squibb Company | Synergistic methods and compositions for treating cancer |
| WO2001081341A2 (de) * | 2000-04-20 | 2001-11-01 | Schering Aktiengesellschaft | 9-oxa-epothilon-derivate, verfahren zu deren herstellung sowie ihre verwendung in pharmazeutischen präparaten |
| WO2001081342A2 (de) * | 2000-04-19 | 2001-11-01 | Schering Aktiengesellschaft | Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung |
| JP2002504540A (ja) * | 1998-02-25 | 2002-02-12 | スローン−ケッタリング インスティトゥート フォア キャンサー リサーチ | エポチロンの合成、その中間体およびそのアナログ |
| WO2002022577A2 (en) * | 2000-09-01 | 2002-03-21 | Novartis Ag | Hydroxamate derivatives useful as deacetylase inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3040121B2 (ja) * | 1988-01-12 | 2000-05-08 | ジェネンテク，インコーポレイテッド | 増殖因子レセプターの機能を阻害することにより腫瘍細胞を処置する方法 |
| US5516775A (en) * | 1992-08-31 | 1996-05-14 | Ciba-Geigy Corporation | Further use of pyrimidine derivatives |
| EP1052974B1 (en) * | 1998-02-05 | 2009-05-20 | Novartis AG | Pharmaceutical formulation containing epothilone |
| AU5036999A (en) * | 1998-06-30 | 2000-01-17 | Schering Aktiengesellschaft | Epothilon derivatives, their preparation process, intermediate products and their pharmaceutical use |
| WO2000047584A2 (de) * | 1999-02-11 | 2000-08-17 | Schering Aktiengesellschaft | Epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung |
| DE19908760A1 (de) * | 1999-02-18 | 2000-08-24 | Schering Ag | Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
| US20020058286A1 (en) * | 1999-02-24 | 2002-05-16 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto and analogues thereof |
| CA2440555A1 (en) * | 2001-03-14 | 2002-09-19 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
-
2003
- 2003-06-06 AU AU2003242646A patent/AU2003242646A1/en not_active Abandoned
- 2003-06-06 EP EP20090178302 patent/EP2179745A1/en not_active Withdrawn
- 2003-06-06 MX MXPA04012444A patent/MXPA04012444A/es active IP Right Grant
- 2003-06-06 DE DE60333754T patent/DE60333754D1/de not_active Expired - Lifetime
- 2003-06-06 BR BR0311714-6A patent/BR0311714A/pt not_active IP Right Cessation
- 2003-06-06 JP JP2004510831A patent/JP2005535608A/ja active Pending
- 2003-06-06 US US10/517,074 patent/US20050271669A1/en not_active Abandoned
- 2003-06-06 EP EP03757040A patent/EP1515750B1/en not_active Expired - Lifetime
- 2003-06-06 AT AT03757040T patent/ATE476995T1/de not_active IP Right Cessation
- 2003-06-06 CA CA002487147A patent/CA2487147A1/en not_active Abandoned
- 2003-06-06 WO PCT/EP2003/005988 patent/WO2003103712A1/en not_active Ceased
- 2003-06-06 CN CN038134489A patent/CN1658904A/zh active Pending
- 2003-06-06 SG SG200608597-1A patent/SG162616A1/en unknown
- 2003-06-06 PL PL03372070A patent/PL372070A1/xx not_active Application Discontinuation
- 2003-06-06 CN CN201010166742A patent/CN101816792A/zh active Pending
-
2004
- 2004-11-11 IL IL16518004A patent/IL165180A0/xx unknown
- 2004-11-11 ZA ZA2004/09137A patent/ZA200409137B/en unknown
-
2005
- 2005-01-07 NO NO20050096A patent/NO20050096L/no unknown
-
2010
- 2010-10-20 US US12/908,533 patent/US20110033458A1/en not_active Abandoned
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001507716A (ja) * | 1996-12-03 | 2001-06-12 | スローン−ケッタリング インスティトュート フォア キャンサー リサーチ | エポチロンの合成とその中間体及びその類似物並びにその使用 |
| JP2002504540A (ja) * | 1998-02-25 | 2002-02-12 | スローン−ケッタリング インスティトゥート フォア キャンサー リサーチ | エポチロンの合成、その中間体およびそのアナログ |
| WO2001064650A2 (en) * | 2000-03-01 | 2001-09-07 | Sloan-Kettering Institute For Cancer Research Center | Synthesis of epothilones, intermediates thereto and analogues thereof |
| WO2001072721A2 (en) * | 2000-03-27 | 2001-10-04 | Bristol-Myers Squibb Company | Synergistic methods and compositions for treating cancer |
| WO2001081342A2 (de) * | 2000-04-19 | 2001-11-01 | Schering Aktiengesellschaft | Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung |
| WO2001081341A2 (de) * | 2000-04-20 | 2001-11-01 | Schering Aktiengesellschaft | 9-oxa-epothilon-derivate, verfahren zu deren herstellung sowie ihre verwendung in pharmazeutischen präparaten |
| WO2002022577A2 (en) * | 2000-09-01 | 2002-03-21 | Novartis Ag | Hydroxamate derivatives useful as deacetylase inhibitors |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019537583A (ja) * | 2016-10-28 | 2019-12-26 | アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | ヒストン脱アセチル化酵素阻害剤及びエポチロンを含む医薬品組み合わせならびにその使用方法 |
| JP2022184965A (ja) * | 2016-10-28 | 2022-12-13 | アセチロン ファーマシューティカルズ インコーポレイテッド | ヒストン脱アセチル化酵素阻害剤及びエポチロンを含む医薬品組み合わせならびにその使用方法 |
| US11998546B2 (en) | 2016-10-28 | 2024-06-04 | Acetylon Pharmaceuticals, Inc. | Pharmaceutical combinations comprising a histone deacetylase inhibitor and epothilone and methods of use thereof |
| JP7542947B2 (ja) | 2016-10-28 | 2024-09-02 | アセチロン ファーマシューティカルズ インコーポレイテッド | ヒストン脱アセチル化酵素阻害剤及びエポチロンを含む医薬品組み合わせならびにその使用方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| PL372070A1 (en) | 2005-07-11 |
| CN101816792A (zh) | 2010-09-01 |
| ATE476995T1 (de) | 2010-08-15 |
| NO20050096L (no) | 2005-02-04 |
| EP1515750B1 (en) | 2010-08-11 |
| WO2003103712A1 (en) | 2003-12-18 |
| CN1658904A (zh) | 2005-08-24 |
| EP1515750A1 (en) | 2005-03-23 |
| AU2003242646A1 (en) | 2003-12-22 |
| US20050271669A1 (en) | 2005-12-08 |
| ZA200409137B (en) | 2005-08-31 |
| EP2179745A1 (en) | 2010-04-28 |
| SG162616A1 (en) | 2010-07-29 |
| US20110033458A1 (en) | 2011-02-10 |
| HK1075208A1 (en) | 2005-12-09 |
| DE60333754D1 (de) | 2010-09-23 |
| CA2487147A1 (en) | 2003-12-18 |
| MXPA04012444A (es) | 2005-04-19 |
| BR0311714A (pt) | 2005-03-01 |
| IL165180A0 (en) | 2005-12-18 |
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