JP5209479B2 - Ｍ１受容体にて活性を有するベンゾイミダゾロン類 - Google Patents
Ｍ１受容体にて活性を有するベンゾイミダゾロン類 Download PDFInfo
- Publication number
- JP5209479B2 JP5209479B2 JP2008532862A JP2008532862A JP5209479B2 JP 5209479 B2 JP5209479 B2 JP 5209479B2 JP 2008532862 A JP2008532862 A JP 2008532862A JP 2008532862 A JP2008532862 A JP 2008532862A JP 5209479 B2 JP5209479 B2 JP 5209479B2
- Authority
- JP
- Japan
- Prior art keywords
- pyran
- dihydro
- piperidinyl
- formula
- benzimidazol
- 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.)
- Expired - Fee Related
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- 239000003755 preservative agent Substances 0.000 description 1
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- 150000003141 primary amines Chemical class 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- DSKIOWHQLUWFLG-SPIKMXEPSA-N prochlorperazine maleate Chemical compound [H+].[H+].[H+].[H+].[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O.C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 DSKIOWHQLUWFLG-SPIKMXEPSA-N 0.000 description 1
- 229960005253 procyclidine Drugs 0.000 description 1
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- 238000009256 replacement therapy Methods 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
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- 208000015891 sexual disease Diseases 0.000 description 1
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- 238000009097 single-agent therapy Methods 0.000 description 1
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- 235000017281 sodium acetate Nutrition 0.000 description 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 description 1
- 239000012279 sodium borohydride Substances 0.000 description 1
- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- 239000003195 sodium channel blocking agent Substances 0.000 description 1
- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
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- 229910000080 stannane Inorganic materials 0.000 description 1
- 235000011150 stannous chloride Nutrition 0.000 description 1
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- 235000019698 starch Nutrition 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000006190 sub-lingual tablet Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 231100000736 substance abuse Toxicity 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
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- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
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- 238000002636 symptomatic treatment Methods 0.000 description 1
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- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 229960001685 tacrine Drugs 0.000 description 1
- YLJREFDVOIBQDA-UHFFFAOYSA-N tacrine Chemical compound C1=CC=C2C(N)=C(CCCC3)C3=NC2=C1 YLJREFDVOIBQDA-UHFFFAOYSA-N 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- MCEVVYDLRADCDT-UHFFFAOYSA-N tert-butyl 4-(2-amino-5-chloroanilino)piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1NC1=CC(Cl)=CC=C1N MCEVVYDLRADCDT-UHFFFAOYSA-N 0.000 description 1
- FRPUIHSPFWDJTE-UHFFFAOYSA-N tert-butyl 4-(3-cyclopropyl-4-nitroanilino)piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1NC1=CC=C([N+]([O-])=O)C(C2CC2)=C1 FRPUIHSPFWDJTE-UHFFFAOYSA-N 0.000 description 1
- CBJZORRKQUKBTA-UHFFFAOYSA-N tert-butyl 4-(6-cyclopropyl-2-oxo-3h-benzimidazol-1-yl)piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1N1C(=O)NC2=CC=C(C3CC3)C=C21 CBJZORRKQUKBTA-UHFFFAOYSA-N 0.000 description 1
- CKXZPVPIDOJLLM-UHFFFAOYSA-N tert-butyl n-piperidin-4-ylcarbamate Chemical compound CC(C)(C)OC(=O)NC1CCNCC1 CKXZPVPIDOJLLM-UHFFFAOYSA-N 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 125000005207 tetraalkylammonium group Chemical group 0.000 description 1
- 229960000882 thiothixene hydrochloride Drugs 0.000 description 1
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- 208000016686 tic disease Diseases 0.000 description 1
- AXZWODMDQAVCJE-UHFFFAOYSA-L tin(II) chloride (anhydrous) Chemical compound [Cl-].[Cl-].[Sn+2] AXZWODMDQAVCJE-UHFFFAOYSA-L 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
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- QIWRFOJWQSSRJZ-UHFFFAOYSA-N tributyl(ethenyl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C=C QIWRFOJWQSSRJZ-UHFFFAOYSA-N 0.000 description 1
- 229960001032 trihexyphenidyl Drugs 0.000 description 1
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Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/28—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
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0519966.6 | 2005-09-30 | ||
| GBGB0519966.6A GB0519966D0 (en) | 2005-09-30 | 2005-09-30 | Compounds |
| GB0602853.4 | 2006-02-13 | ||
| GB0602853A GB0602853D0 (en) | 2006-02-13 | 2006-02-13 | Compounds |
| PCT/GB2006/003585 WO2007036711A1 (en) | 2005-09-30 | 2006-09-27 | BENZIMIDAZOLONES WHICH HAVE ACTIVITY AT Ml RECEPTOR |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009510037A JP2009510037A (ja) | 2009-03-12 |
| JP2009510037A5 JP2009510037A5 (https=) | 2009-11-12 |
| JP5209479B2 true JP5209479B2 (ja) | 2013-06-12 |
Family
ID=37398768
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008532862A Expired - Fee Related JP5209479B2 (ja) | 2005-09-30 | 2006-09-27 | Ｍ１受容体にて活性を有するベンゾイミダゾロン類 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US8288413B2 (https=) |
| EP (1) | EP1937670A1 (https=) |
| JP (1) | JP5209479B2 (https=) |
| WO (1) | WO2007036711A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0616609A2 (pt) | 2005-09-30 | 2011-06-28 | Glaxo Group Ltd | compostos que têm atividade no receptor m1, composição farmacêutica contendo tais compostos, processo para preparação dos mesmos, bem como seus usos em medicina |
| WO2007036711A1 (en) | 2005-09-30 | 2007-04-05 | Glaxo Group Limited | BENZIMIDAZOLONES WHICH HAVE ACTIVITY AT Ml RECEPTOR |
| EP1960389B1 (en) | 2005-09-30 | 2012-08-15 | Glaxo Group Limited | Compounds which have activity at m1 receptor and their uses in medicine |
| GB0605785D0 (en) * | 2006-03-22 | 2006-05-03 | Glaxo Group Ltd | Compounds |
| GB0605784D0 (en) * | 2006-03-22 | 2006-05-03 | Glaxo Group Ltd | Compounds |
| GB0605786D0 (en) * | 2006-03-22 | 2006-05-03 | Glaxo Group Ltd | Compounds |
| GB0706165D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706170D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706164D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706174D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| US8119661B2 (en) | 2007-09-11 | 2012-02-21 | Astrazeneca Ab | Piperidine derivatives and their use as muscarinic receptor modulators |
| PE20091194A1 (es) * | 2007-09-20 | 2009-09-05 | Glaxo Group Ltd | Derivados de heterociclicos como moduladores del receptor m1 |
| WO2009037294A1 (en) * | 2007-09-20 | 2009-03-26 | Glaxo Group Limited | Compounds which have activity at m1 receptor and their uses in medicine |
| GB0718415D0 (en) * | 2007-09-20 | 2007-10-31 | Glaxo Group Ltd | Compounds |
| CN103497146B (zh) * | 2013-09-27 | 2016-04-13 | 山东大学 | 2-(n-芳甲基哌啶-4-氨基)-4-(取代苯酚)苯环衍生物及其制备方法与应用 |
| CN106045916B (zh) * | 2016-05-31 | 2018-08-31 | 江苏之江化工有限公司 | 一种咪唑酮类化合物的合成方法 |
| CN109206323A (zh) * | 2017-07-07 | 2019-01-15 | 上海现代制药股份有限公司 | 一种萘胺药物中间体的制备方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3161645A (en) | 1962-12-18 | 1964-12-15 | Res Lab Dr C Janssen N V | 1-(1-aroylpropyl-4-piperidyl)-2-benzimidazolinones and related compounds |
| US3989707A (en) * | 1974-06-21 | 1976-11-02 | Janssen Pharmaceutica N.V. | Benzimidazolinone derivatives |
| US4292321A (en) | 1979-05-24 | 1981-09-29 | Warner-Lambert Company | 1,3,8-Triazaspirodecane-4-ones, pharmaceutical compositions thereof and method of use thereof |
| DE3124366A1 (de) | 1981-06-20 | 1982-12-30 | Hoechst Ag, 6000 Frankfurt | N-oxacyclyl-alkylpiperidin-derivate, verfahren zu ihrer herstellung, sie enthaltende pharmazeutische praeparate und deren verwendung |
| DE4040300A1 (de) | 1990-12-17 | 1992-07-02 | Leifeld Gmbh & Co | Drueckmaschine mit wenigstens einem rollenhalter |
| JP3916093B2 (ja) * | 1993-09-17 | 2007-05-16 | 杏林製薬株式会社 | 光学活性イミダゾリジノン誘導体とその製造方法 |
| US5574044A (en) | 1994-10-27 | 1996-11-12 | Merck & Co., Inc. | Muscarine antagonists |
| JP2002515008A (ja) * | 1994-10-27 | 2002-05-21 | メルク エンド カンパニー インコーポレーテッド | ムスカリン・アンタゴニスト |
| US5691323A (en) * | 1995-05-12 | 1997-11-25 | Merck & Co., Inc. | Muscarine antagonists |
| WO1997016186A1 (en) | 1995-10-31 | 1997-05-09 | Merck & Co., Inc. | Muscarine agonists |
| US5718912A (en) | 1996-10-28 | 1998-02-17 | Merck & Co., Inc. | Muscarine agonists |
| US5977134A (en) | 1996-12-05 | 1999-11-02 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US6465484B1 (en) | 1997-09-26 | 2002-10-15 | Merck & Co., Inc. | Angiogenesis inhibitors |
| US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| AU2307999A (en) * | 1997-12-23 | 1999-07-12 | Alcon Laboratories, Inc. | Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions |
| ATE275141T1 (de) | 1999-10-13 | 2004-09-15 | Banyu Pharma Co Ltd | Substituierte imidazolin-derivate |
| SE9904652D0 (sv) | 1999-12-17 | 1999-12-17 | Astra Pharma Prod | Novel Compounds |
| US20020019395A1 (en) | 2000-02-01 | 2002-02-14 | Bing-Yan Zhu | Indalone and benzimidazolone inhibitors of factor Xa |
| US6872733B2 (en) | 2001-04-18 | 2005-03-29 | Euro-Celtique S.A. | Benzimidazolone compounds |
| JPWO2002085890A1 (ja) | 2001-04-20 | 2004-08-12 | 萬有製薬株式会社 | ベンズイミダゾロン誘導体 |
| ATE516030T1 (de) | 2001-10-02 | 2011-07-15 | Acadia Pharm Inc | Benzimidazolidinon-derivate als muscarinische mittel |
| US6951849B2 (en) | 2001-10-02 | 2005-10-04 | Acadia Pharmaceuticals Inc. | Benzimidazolidinone derivatives as muscarinic agents |
| WO2004089942A2 (en) | 2001-10-02 | 2004-10-21 | Acadia Pharmaceuticals Inc. | Benzimidazolidinone derivatives as muscarinic agents |
| WO2003037890A2 (en) * | 2001-11-01 | 2003-05-08 | Icagen, Inc. | Piperidines |
| JP4056977B2 (ja) | 2002-03-29 | 2008-03-05 | 田辺三菱製薬株式会社 | 睡眠障害治療薬 |
| JP2005532361A (ja) | 2002-06-17 | 2005-10-27 | メルク エンド カムパニー インコーポレーテッド | 高眼圧症の治療用の眼科用組成物 |
| BR0317230A (pt) | 2002-12-13 | 2005-10-25 | Smithkline Beecham Corp | Composto, composição, métodos de antagonizar uma atividade do receptor de quimiocina ccr-5, e de tratar uma infecção viral em um paciente, e, uso de um composto |
| WO2005009996A1 (en) | 2003-07-23 | 2005-02-03 | Wyeth | Sulfonyldihydro- benzimidazolone compounds as 5-hydroxytryptamine-6 ligands |
| KR100738784B1 (ko) | 2003-09-03 | 2007-07-12 | 화이자 인코포레이티드 | 5-ｈｔ4 수용체 효능 활성을 갖는 벤즈이미다졸론 |
| MX2007005290A (es) | 2004-11-02 | 2007-07-09 | Pfizer | Derivados de sulfonilbencimidazol. |
| US7300947B2 (en) | 2005-07-13 | 2007-11-27 | Banyu Pharmaceutical Co., Ltd. | N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives |
| WO2007036711A1 (en) | 2005-09-30 | 2007-04-05 | Glaxo Group Limited | BENZIMIDAZOLONES WHICH HAVE ACTIVITY AT Ml RECEPTOR |
| EP1960389B1 (en) | 2005-09-30 | 2012-08-15 | Glaxo Group Limited | Compounds which have activity at m1 receptor and their uses in medicine |
| BRPI0616609A2 (pt) | 2005-09-30 | 2011-06-28 | Glaxo Group Ltd | compostos que têm atividade no receptor m1, composição farmacêutica contendo tais compostos, processo para preparação dos mesmos, bem como seus usos em medicina |
| WO2008029377A2 (en) | 2006-09-08 | 2008-03-13 | The Gillette Company | Toothbrush with multiple bristle states |
| GB0706190D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706170D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706188D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706187D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706168D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706189D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706173D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706164D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706165D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706174D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| GB0706167D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
-
2006
- 2006-09-27 WO PCT/GB2006/003585 patent/WO2007036711A1/en not_active Ceased
- 2006-09-27 US US12/088,489 patent/US8288413B2/en not_active Expired - Fee Related
- 2006-09-27 EP EP06794581A patent/EP1937670A1/en not_active Withdrawn
- 2006-09-27 JP JP2008532862A patent/JP5209479B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1937670A1 (en) | 2008-07-02 |
| US20080306112A1 (en) | 2008-12-11 |
| US8288413B2 (en) | 2012-10-16 |
| JP2009510037A (ja) | 2009-03-12 |
| WO2007036711A1 (en) | 2007-04-05 |
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