ATE520692T1 - Thiazolyl-mglur5-antagonisten und verfahren zu ihrer verwendung - Google Patents
Thiazolyl-mglur5-antagonisten und verfahren zu ihrer verwendungInfo
- Publication number
- ATE520692T1 ATE520692T1 AT05858618T AT05858618T ATE520692T1 AT E520692 T1 ATE520692 T1 AT E520692T1 AT 05858618 T AT05858618 T AT 05858618T AT 05858618 T AT05858618 T AT 05858618T AT E520692 T1 ATE520692 T1 AT E520692T1
- Authority
- AT
- Austria
- Prior art keywords
- properties
- ring
- terms
- drug
- thiazolyl
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title 1
- -1 1,3-thiazol-2-yl ring Chemical group 0.000 abstract 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical class C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 abstract 1
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical class OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 abstract 1
- 150000003841 chloride salts Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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
-
- 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
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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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
- A61P25/06—Antimigraine agents
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Addiction (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Anesthesiology (AREA)
- Transplantation (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61680504P | 2004-10-07 | 2004-10-07 | |
| PCT/US2005/035921 WO2007050050A2 (en) | 2004-10-07 | 2005-10-06 | Thiazolyl mglur5 antagonists and methods for their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE520692T1 true ATE520692T1 (de) | 2011-09-15 |
Family
ID=37968242
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT05858618T ATE520692T1 (de) | 2004-10-07 | 2005-10-06 | Thiazolyl-mglur5-antagonisten und verfahren zu ihrer verwendung |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US7879882B2 (OSRAM) |
| EP (2) | EP1893608B1 (OSRAM) |
| JP (2) | JP5635727B2 (OSRAM) |
| CN (1) | CN101223166B (OSRAM) |
| AT (1) | ATE520692T1 (OSRAM) |
| AU (1) | AU2005336513B2 (OSRAM) |
| CA (1) | CA2583572C (OSRAM) |
| ES (1) | ES2369783T3 (OSRAM) |
| WO (1) | WO2007050050A2 (OSRAM) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5635727B2 (ja) * | 2004-10-07 | 2014-12-03 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | チアゾリルmglur5アンタゴニスト及びそれらの使用のための方法 |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| TW201124391A (en) * | 2009-10-20 | 2011-07-16 | Lundbeck & Co As H | 2-substituted-ethynylthiazole derivatives and uses of same |
| CN102762572A (zh) | 2010-02-01 | 2012-10-31 | 诺瓦提斯公司 | 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物 |
| WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
| US8835444B2 (en) | 2010-02-02 | 2014-09-16 | Novartis Ag | Cyclohexyl amide derivatives as CRF receptor antagonists |
| US8420661B2 (en) | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| US8772300B2 (en) * | 2011-04-19 | 2014-07-08 | Hoffmann-La Roche Inc. | Phenyl or pyridinyl-ethynyl derivatives |
| CN103492374B (zh) * | 2011-04-26 | 2016-06-01 | 霍夫曼-拉罗奇有限公司 | 吡唑烷-3-酮衍生物 |
| SG194120A1 (en) * | 2011-04-26 | 2013-11-29 | Hoffmann La Roche | Ethynyl derivatives as positive allosteric modulators of the mglur5 |
| JP2016507537A (ja) | 2013-02-07 | 2016-03-10 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 置換アセチレン誘導体およびmGluR4の正のアロステリックモジュレーターとしてのそれらの使用 |
| UA116023C2 (uk) * | 2013-07-08 | 2018-01-25 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як антагоністи метаботропного глутаматного рецептора |
| WO2015188368A1 (en) * | 2014-06-13 | 2015-12-17 | Merck Sharp & Dohme Corp. | Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles |
| JP6603334B2 (ja) | 2015-06-03 | 2019-11-06 | エフ.ホフマン−ラ ロシュ アーゲー | エチニル誘導体 |
| MX2020001425A (es) | 2017-08-04 | 2020-08-06 | Skyhawk Therapeutics Inc | Metodos y composiciones para modular el empalme. |
| CN114007613A (zh) | 2019-02-05 | 2022-02-01 | 斯基霍克疗法公司 | 用于调节剪接的方法和组合物 |
| JP7603595B2 (ja) | 2019-02-06 | 2024-12-20 | スカイホーク・セラピューティクス・インコーポレーテッド | スプライシングを調節するための方法および組成物 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU780009B2 (en) * | 1999-08-31 | 2005-02-24 | Merck Sharp & Dohme Corp. | Heterocyclic compounds and methods of use thereof |
| US7462619B2 (en) * | 1999-08-31 | 2008-12-09 | Merck & Co., Inc. | Pyridazine, pyrimidine and pyrazine ethyne compounds |
| US7365074B2 (en) * | 1999-08-31 | 2008-04-29 | Merck & Co., Inc. | Pyridazine, pyrimidine and pyrazine ethyne compounds |
| US6956049B1 (en) * | 1999-08-31 | 2005-10-18 | Merck & Co., Inc. | Methods of modulating processes mediated by excitatory amino acid receptors |
| US6774138B2 (en) | 1999-08-31 | 2004-08-10 | Merck & Co., Inc. | Thiazolyl(pyridyl)ethyne compounds |
| US6551270B1 (en) | 2000-08-30 | 2003-04-22 | Snowden Pencer, Inc. | Dual lumen access port |
| US6903005B1 (en) * | 2000-08-30 | 2005-06-07 | Micron Technology, Inc. | Method for the formation of RuSixOy-containing barrier layers for high-k dielectrics |
| WO2004038374A2 (en) * | 2002-10-24 | 2004-05-06 | Merck & Co., Inc. | Alkyne derivatives as tracers for metabotropic glutamate receptor binding |
| JP5635727B2 (ja) | 2004-10-07 | 2014-12-03 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | チアゾリルmglur5アンタゴニスト及びそれらの使用のための方法 |
-
2005
- 2005-10-06 JP JP2007543041A patent/JP5635727B2/ja not_active Expired - Fee Related
- 2005-10-06 CN CN2005800415189A patent/CN101223166B/zh not_active Expired - Fee Related
- 2005-10-06 EP EP05858618A patent/EP1893608B1/en not_active Expired - Lifetime
- 2005-10-06 US US11/664,902 patent/US7879882B2/en active Active
- 2005-10-06 EP EP11167527.8A patent/EP2380889B1/en not_active Expired - Lifetime
- 2005-10-06 WO PCT/US2005/035921 patent/WO2007050050A2/en not_active Ceased
- 2005-10-06 CA CA2583572A patent/CA2583572C/en not_active Expired - Lifetime
- 2005-10-06 AU AU2005336513A patent/AU2005336513B2/en not_active Ceased
- 2005-10-06 AT AT05858618T patent/ATE520692T1/de not_active IP Right Cessation
- 2005-10-06 ES ES05858618T patent/ES2369783T3/es not_active Expired - Lifetime
-
2011
- 2011-01-28 US US13/016,304 patent/US8242143B2/en not_active Expired - Lifetime
-
2012
- 2012-07-26 US US13/558,537 patent/US8609852B2/en not_active Expired - Lifetime
-
2014
- 2014-09-10 JP JP2014184615A patent/JP2015013885A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP2380889A2 (en) | 2011-10-26 |
| JP2008516004A (ja) | 2008-05-15 |
| EP2380889A3 (en) | 2012-01-18 |
| US7879882B2 (en) | 2011-02-01 |
| US8609852B2 (en) | 2013-12-17 |
| WO2007050050A3 (en) | 2008-02-07 |
| JP5635727B2 (ja) | 2014-12-03 |
| AU2005336513A1 (en) | 2007-05-17 |
| US8242143B2 (en) | 2012-08-14 |
| ES2369783T3 (es) | 2011-12-05 |
| US20110230526A1 (en) | 2011-09-22 |
| CA2583572A1 (en) | 2006-04-07 |
| EP1893608A2 (en) | 2008-03-05 |
| US20090203903A1 (en) | 2009-08-13 |
| CA2583572C (en) | 2016-07-12 |
| JP2015013885A (ja) | 2015-01-22 |
| CN101223166B (zh) | 2011-10-19 |
| EP1893608A4 (en) | 2009-04-22 |
| AU2005336513B2 (en) | 2012-08-09 |
| CN101223166A (zh) | 2008-07-16 |
| WO2007050050A2 (en) | 2007-05-03 |
| AU2005336513A8 (en) | 2009-01-08 |
| EP2380889B1 (en) | 2013-06-26 |
| US20120289696A1 (en) | 2012-11-15 |
| EP1893608B1 (en) | 2011-08-17 |
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