AU2005285035B2 - Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS) - Google Patents
Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS) Download PDFInfo
- Publication number
- AU2005285035B2 AU2005285035B2 AU2005285035A AU2005285035A AU2005285035B2 AU 2005285035 B2 AU2005285035 B2 AU 2005285035B2 AU 2005285035 A AU2005285035 A AU 2005285035A AU 2005285035 A AU2005285035 A AU 2005285035A AU 2005285035 B2 AU2005285035 B2 AU 2005285035B2
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- Australia
- Prior art keywords
- lower alkyl
- phenyl
- compound
- methyl
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
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- YAMHXTCMCPHKLN-UHFFFAOYSA-N imidazolidin-2-one Chemical class O=C1NCCN1 YAMHXTCMCPHKLN-UHFFFAOYSA-N 0.000 title abstract description 4
- 239000000849 selective androgen receptor modulator Substances 0.000 title description 5
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- 108010080146 androgen receptors Proteins 0.000 claims abstract description 29
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- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
- 150000001875 compounds Chemical class 0.000 claims description 115
- 125000000217 alkyl group Chemical group 0.000 claims description 67
- -1 hydroxy, carboxy Chemical group 0.000 claims description 38
- 229910052736 halogen Chemical group 0.000 claims description 36
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- 238000000034 method Methods 0.000 claims description 26
- 125000003545 alkoxy group Chemical group 0.000 claims description 23
- 125000003118 aryl group Chemical group 0.000 claims description 22
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- 125000001424 substituent group Chemical group 0.000 claims description 16
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- 150000003839 salts Chemical class 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 125000003282 alkyl amino group Chemical group 0.000 claims description 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 9
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- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- 229960004418 trolamine Drugs 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 229960002703 undecylenic acid Drugs 0.000 description 1
- 229940070710 valerate Drugs 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
- UGZADUVQMDAIAO-UHFFFAOYSA-L zinc hydroxide Chemical compound [OH-].[OH-].[Zn+2] UGZADUVQMDAIAO-UHFFFAOYSA-L 0.000 description 1
- 229940007718 zinc hydroxide Drugs 0.000 description 1
- 229910021511 zinc hydroxide Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/30—Oxygen or sulfur atoms
- C07D233/32—One oxygen atom
- C07D233/34—Ethylene-urea
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Urology & Nephrology (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60915704P | 2004-09-10 | 2004-09-10 | |
| US60/609,157 | 2004-09-10 | ||
| PCT/US2005/032381 WO2006031715A2 (en) | 2004-09-10 | 2005-09-09 | Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (sarms) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2005285035A1 AU2005285035A1 (en) | 2006-03-23 |
| AU2005285035B2 true AU2005285035B2 (en) | 2012-03-22 |
Family
ID=36060597
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2005285035A Ceased AU2005285035B2 (en) | 2004-09-10 | 2005-09-09 | Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS) |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7531565B2 (https=) |
| EP (1) | EP1791821B1 (https=) |
| JP (1) | JP5031568B2 (https=) |
| CN (1) | CN101056862B (https=) |
| AU (1) | AU2005285035B2 (https=) |
| CA (1) | CA2579514A1 (https=) |
| ES (1) | ES2422204T3 (https=) |
| WO (1) | WO2006031715A2 (https=) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104803916B (zh) | 2004-11-16 | 2017-08-11 | 詹森药业有限公司 | 用作选择性雄激素受体调节剂(sarms)的杂环衍生物 |
| US7709516B2 (en) * | 2005-06-17 | 2010-05-04 | Endorecherche, Inc. | Helix 12 directed non-steroidal antiandrogens |
| CA2678577A1 (en) * | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| EP2183228B1 (en) * | 2007-07-26 | 2014-08-20 | Vitae Pharmaceuticals, Inc. | CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1 |
| AR069207A1 (es) * | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CA2708303A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW200934490A (en) * | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| WO2009094169A1 (en) * | 2008-01-24 | 2009-07-30 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5734666B2 (ja) * | 2008-02-11 | 2015-06-17 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
| US8598160B2 (en) * | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| JP5538356B2 (ja) * | 2008-03-18 | 2014-07-02 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤 |
| AR071236A1 (es) | 2008-05-01 | 2010-06-02 | Vitae Pharmaceuticals Inc | Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 |
| WO2009134387A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2723032A1 (en) * | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CL2009001059A1 (es) * | 2008-05-01 | 2010-11-12 | Boehringer Ingelheim Int | Compuestos derivados de 1,3-oxazin-2-ona-3,6 sustituidos, inhibidores de la actividad de la 11-beta-hidroxiesteroide deshidrogenasa i; composicion farmaceutica que los comprende; utiles en el tratamiento de enfermedades tales como diabetes mellitus, entre otras. |
| WO2010011314A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1 |
| US8846668B2 (en) | 2008-07-25 | 2014-09-30 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CN102105454A (zh) | 2008-07-25 | 2011-06-22 | 贝林格尔.英格海姆国际有限公司 | 合成1型11β-羟基类固醇脱氢酶的抑制剂 |
| GB2463514C (en) * | 2008-09-11 | 2018-09-26 | Galapagos Nv | Imidazolidine compounds and uses therefor |
| CA2744946A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW201039034A (en) * | 2009-04-27 | 2010-11-01 | Chunghwa Picture Tubes Ltd | Pixel structure and the method of forming the same |
| UA109255C2 (ru) | 2009-04-30 | 2015-08-10 | Берінгер Інгельхайм Інтернешнл Гмбх | Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1 |
| KR20120061771A (ko) * | 2009-04-30 | 2012-06-13 | 비타이 파마슈티컬즈, 인코포레이티드 | 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제 |
| EP2440537A1 (en) | 2009-06-11 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| WO2011002910A1 (en) | 2009-07-01 | 2011-01-06 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| TW201124138A (en) * | 2009-09-02 | 2011-07-16 | Valletta Health B V | Imidazole-4-carboxylic acid for use in treating a disease related to extracellular reactive oxygen species |
| JP5750449B2 (ja) | 2009-11-05 | 2015-07-22 | 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 | 新規キラルリンリガンド |
| MX338831B (es) | 2010-02-04 | 2016-05-03 | Radius Health Inc | Moduladores selectivos de receptores de androgenos. |
| EP2568806B1 (en) | 2010-05-12 | 2016-05-11 | Radius Health, Inc. | Therapeutic regimens |
| US8648192B2 (en) | 2010-05-26 | 2014-02-11 | Boehringer Ingelheim International Gmbh | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| US8933072B2 (en) | 2010-06-16 | 2015-01-13 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| JP5813106B2 (ja) | 2010-06-25 | 2015-11-17 | 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 | 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン |
| RU2434851C1 (ru) * | 2010-07-22 | 2011-11-27 | Александр Васильевич Иващенко | Циклические n, n'-диарилтиомочевины или n, n'-диарилмочевины - антагонисты андрогенных рецепторов, противораковое средство, способ получения и применения |
| US9133182B2 (en) | 2010-09-28 | 2015-09-15 | Radius Health, Inc. | Selective androgen receptor modulators |
| PH12013500808A1 (en) | 2010-11-02 | 2015-10-07 | Boehringer Ingelheim Int | Pharmaceutical combinations for the treatment of metabolic disorders |
| WO2013084138A1 (en) * | 2011-12-05 | 2013-06-13 | Novartis Ag | Cyclic urea derivatives as androgen receptor antagonists |
| LT3474841T (lt) | 2016-06-22 | 2022-06-10 | Ellipses Pharma Ltd | Ar+ krūties vėžio gydymo būdai |
| WO2019222272A1 (en) | 2018-05-14 | 2019-11-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| CN113811333B (zh) | 2019-05-14 | 2024-03-12 | 诺维逊生物股份有限公司 | 靶向抗癌核激素受体的化合物 |
| WO2021097046A1 (en) | 2019-11-13 | 2021-05-20 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| KR20230160299A (ko) | 2021-03-23 | 2023-11-23 | 누베이션 바이오 인크. | 항암 핵 호르몬 수용체 표적화 화합물 |
| US12006314B2 (en) | 2021-05-03 | 2024-06-11 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005217074A1 (en) * | 2004-02-28 | 2005-09-09 | Boehringer Ingelheim International Gmbh | Novel carboxamides for use as Xa inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2329276A1 (fr) * | 1975-10-29 | 1977-05-27 | Roussel Uclaf | Nouvelles imidazolidines substituees, procede de preparation, application comme medicament et compositions les renfermant |
| TW521073B (en) * | 1994-01-05 | 2003-02-21 | Hoechst Marion Roussel Inc | New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them |
| FR2724169B1 (fr) * | 1994-09-06 | 1997-01-03 | Roussel Uclaf | Nouvelles phenylimidazolidines eventuellement substituees, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant |
| FR2715402B1 (fr) | 1994-01-05 | 1996-10-04 | Roussel Uclaf | Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant. |
| DE102004009835A1 (de) * | 2004-02-28 | 2005-09-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel |
-
2005
- 2005-09-09 EP EP05800947.3A patent/EP1791821B1/en not_active Expired - Lifetime
- 2005-09-09 AU AU2005285035A patent/AU2005285035B2/en not_active Ceased
- 2005-09-09 WO PCT/US2005/032381 patent/WO2006031715A2/en not_active Ceased
- 2005-09-09 ES ES05800947T patent/ES2422204T3/es not_active Expired - Lifetime
- 2005-09-09 CA CA002579514A patent/CA2579514A1/en not_active Abandoned
- 2005-09-09 CN CN2005800381110A patent/CN101056862B/zh not_active Expired - Fee Related
- 2005-09-09 US US11/223,187 patent/US7531565B2/en active Active
- 2005-09-09 JP JP2007531421A patent/JP5031568B2/ja not_active Expired - Fee Related
-
2009
- 2009-03-30 US US12/413,873 patent/US7968580B2/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005217074A1 (en) * | 2004-02-28 | 2005-09-09 | Boehringer Ingelheim International Gmbh | Novel carboxamides for use as Xa inhibitors |
Non-Patent Citations (4)
| Title |
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| FERM R. J. et al, J. Organic Chem., 1952, 17(2), 181-184 * |
| GOUBET F. et al, Tetrahedron Letters, 1996, 37(43), 7727-7730 * |
| KIM T. H. et al, J. Organic Chem., 1999, 64(8), 2941-2943 * |
| SCHOLLKOPF U. et al, Liebigs Ann. Chem., 1980, 4, 600-610 * |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2422204T3 (es) | 2013-09-09 |
| WO2006031715A2 (en) | 2006-03-23 |
| AU2005285035A1 (en) | 2006-03-23 |
| JP2008512492A (ja) | 2008-04-24 |
| EP1791821A2 (en) | 2007-06-06 |
| US7531565B2 (en) | 2009-05-12 |
| CN101056862A (zh) | 2007-10-17 |
| EP1791821B1 (en) | 2013-06-05 |
| JP5031568B2 (ja) | 2012-09-19 |
| CA2579514A1 (en) | 2006-03-23 |
| US20060063819A1 (en) | 2006-03-23 |
| US7968580B2 (en) | 2011-06-28 |
| US20090215848A1 (en) | 2009-08-27 |
| CN101056862B (zh) | 2013-03-13 |
| WO2006031715A3 (en) | 2006-07-20 |
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