ES2335438T3 - Derivados del benzimidazol y su uso para modular el complejor receptor gabaa. - Google Patents
Derivados del benzimidazol y su uso para modular el complejor receptor gabaa. Download PDFInfo
- Publication number
- ES2335438T3 ES2335438T3 ES06830303T ES06830303T ES2335438T3 ES 2335438 T3 ES2335438 T3 ES 2335438T3 ES 06830303 T ES06830303 T ES 06830303T ES 06830303 T ES06830303 T ES 06830303T ES 2335438 T3 ES2335438 T3 ES 2335438T3
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- Spain
- Prior art keywords
- biphenyl
- benzoimidazol
- ethylamine
- ethyl
- methoxide
- 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.)
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- 108091008681 GABAA receptors Proteins 0.000 title abstract 2
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- 229910052700 potassium Inorganic materials 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- ALDITMKAAPLVJK-UHFFFAOYSA-N prop-1-ene;hydrate Chemical group O.CC=C ALDITMKAAPLVJK-UHFFFAOYSA-N 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- USPWKWBDZOARPV-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1 USPWKWBDZOARPV-UHFFFAOYSA-N 0.000 description 1
- DNXIASIHZYFFRO-UHFFFAOYSA-N pyrazoline Chemical compound C1CN=NC1 DNXIASIHZYFFRO-UHFFFAOYSA-N 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 239000002510 pyrogen Substances 0.000 description 1
- ZVJHJDDKYZXRJI-UHFFFAOYSA-N pyrroline Natural products C1CC=NC1 ZVJHJDDKYZXRJI-UHFFFAOYSA-N 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 229940075554 sorbate Drugs 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 229940114926 stearate Drugs 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 229940086735 succinate Drugs 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 150000004685 tetrahydrates Chemical class 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 231100001274 therapeutic index Toxicity 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 239000011345 viscous material Substances 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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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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- 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
- 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
- A61P25/06—Antimigraine agents
-
- 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
- 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
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
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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
- A61P25/28—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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- 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
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- 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
- A61P25/32—Alcohol-abuse
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Diabetes (AREA)
- Otolaryngology (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK200501719 | 2005-12-05 | ||
| DKPA200501719 | 2005-12-05 | ||
| US74253505P | 2005-12-06 | 2005-12-06 | |
| US742535P | 2005-12-06 | ||
| DKPA200601326 | 2006-10-12 | ||
| DK200601326 | 2006-10-12 | ||
| US85129106P | 2006-10-13 | 2006-10-13 | |
| US851291P | 2006-10-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2335438T3 true ES2335438T3 (es) | 2010-03-26 |
Family
ID=37873123
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES06830303T Active ES2335438T3 (es) | 2005-12-05 | 2006-12-04 | Derivados del benzimidazol y su uso para modular el complejor receptor gabaa. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7923464B2 (enExample) |
| EP (1) | EP1996556B1 (enExample) |
| JP (1) | JP2009518292A (enExample) |
| KR (1) | KR20080077620A (enExample) |
| AT (1) | ATE449077T1 (enExample) |
| AU (1) | AU2006324046A1 (enExample) |
| CA (1) | CA2632395A1 (enExample) |
| DE (1) | DE602006010602D1 (enExample) |
| DK (1) | DK1996556T3 (enExample) |
| ES (1) | ES2335438T3 (enExample) |
| IL (1) | IL189974A0 (enExample) |
| NO (1) | NO20083045L (enExample) |
| PL (1) | PL1996556T3 (enExample) |
| WO (1) | WO2007065864A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI391381B (zh) | 2006-03-24 | 2013-04-01 | Neurosearch As | 新穎的苯并咪唑衍生物、含有其之醫藥組成物、及其於製造藥物之用途 |
| AU2008345696A1 (en) * | 2007-12-21 | 2009-07-09 | Wyeth Llc | Benzimidazole compounds |
| CN102036952A (zh) * | 2008-04-16 | 2011-04-27 | 比奥里波克斯公司 | 用作药物的双芳基化合物 |
| US20110301192A1 (en) * | 2008-10-01 | 2011-12-08 | The Regents Of The University Of California | Inhibitors of Cyclin Kinase Inhibitor p21 |
| WO2010055125A1 (en) * | 2008-11-14 | 2010-05-20 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the gabaa receptor complex |
| WO2010055127A1 (en) * | 2008-11-14 | 2010-05-20 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the gabaa receptor complex |
| RS62761B1 (sr) * | 2012-08-21 | 2022-01-31 | Sage Therapeutics Inc | Alopregnanolon za lečenje refraktornog epileptičkog statusa |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
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| DK40192D0 (da) * | 1992-03-26 | 1992-03-26 | Neurosearch As | Imidazolforbindelser, deres fremstilling og anvendelse |
| CA2218493C (en) | 1995-04-21 | 2005-02-22 | Neurosearch A/S | Benzimidazole compounds and their use as modulators of the gabaa receptor complex |
| AU726447B2 (en) * | 1996-10-21 | 2000-11-09 | Neurosearch A/S | 1-phenyl-benzimidazole compounds and their use as BAGA-A receptor modulators |
| CN1275127A (zh) | 1997-10-10 | 2000-11-29 | 神经研究公司 | 苯并咪唑化合物、含该化合物的药物组合物及其应用 |
| BR0011823A (pt) * | 1999-06-22 | 2002-03-19 | Neurosearch As | Derivado de benzimidazol, composto, composição farmacêutica, uso de um derivado de benzimidazol, e, método para tratamento, prevenção ou alìvio de uma doença ou de um distúrbio ou de uma condição de um corpo animal vivo |
| AU2002221566A1 (en) | 2000-12-20 | 2002-07-01 | Neurosearch A/S | Novel benzimidazole derivatives for the treatment of gaba-alpha mediated disorders |
| MXPA05010449A (es) | 2003-04-03 | 2006-05-31 | Neurosearch As | Derivados del bencimidazol y su uso para modular el complejo del receptor de gabaa. |
| US7335777B2 (en) * | 2003-04-03 | 2008-02-26 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the GABAA receptor complex |
| BRPI0413746A (pt) * | 2003-08-21 | 2006-10-24 | Osi Pharm Inc | composto ou um seu n-óxido ou seu sal farmaceuticamente aceitável, composição, e, método de tratamento de distúrbio hiperproliferativo |
| EP1678144A1 (en) | 2003-10-23 | 2006-07-12 | Akzo Nobel N.V. | 1,5,7-TRISUBSTITUTED BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABA-a RECEPTOR COMPLEX |
| CA2589770A1 (en) * | 2004-12-01 | 2006-06-08 | Osi Pharmaceuticals, Inc. | N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library |
| CA2604516A1 (en) * | 2005-04-13 | 2006-10-19 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the gabaa receptor complex |
| EP1874758A1 (en) * | 2005-04-19 | 2008-01-09 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the gabaa receptor complex |
| TWI391381B (zh) | 2006-03-24 | 2013-04-01 | Neurosearch As | 新穎的苯并咪唑衍生物、含有其之醫藥組成物、及其於製造藥物之用途 |
-
2006
- 2006-12-04 US US12/085,769 patent/US7923464B2/en not_active Expired - Fee Related
- 2006-12-04 DE DE602006010602T patent/DE602006010602D1/de active Active
- 2006-12-04 EP EP06830303A patent/EP1996556B1/en not_active Not-in-force
- 2006-12-04 KR KR1020087013766A patent/KR20080077620A/ko not_active Withdrawn
- 2006-12-04 AT AT06830303T patent/ATE449077T1/de active
- 2006-12-04 CA CA002632395A patent/CA2632395A1/en not_active Abandoned
- 2006-12-04 ES ES06830303T patent/ES2335438T3/es active Active
- 2006-12-04 WO PCT/EP2006/069237 patent/WO2007065864A1/en not_active Ceased
- 2006-12-04 JP JP2008542778A patent/JP2009518292A/ja not_active Abandoned
- 2006-12-04 DK DK06830303.1T patent/DK1996556T3/da active
- 2006-12-04 AU AU2006324046A patent/AU2006324046A1/en not_active Abandoned
- 2006-12-04 PL PL06830303T patent/PL1996556T3/pl unknown
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2008
- 2008-03-06 IL IL189974A patent/IL189974A0/en unknown
- 2008-07-04 NO NO20083045A patent/NO20083045L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20090048321A1 (en) | 2009-02-19 |
| KR20080077620A (ko) | 2008-08-25 |
| DE602006010602D1 (de) | 2009-12-31 |
| DK1996556T3 (da) | 2010-04-06 |
| JP2009518292A (ja) | 2009-05-07 |
| EP1996556A1 (en) | 2008-12-03 |
| ATE449077T1 (de) | 2009-12-15 |
| WO2007065864A1 (en) | 2007-06-14 |
| CA2632395A1 (en) | 2007-06-14 |
| US7923464B2 (en) | 2011-04-12 |
| NO20083045L (no) | 2008-09-04 |
| PL1996556T3 (pl) | 2010-05-31 |
| IL189974A0 (en) | 2008-08-07 |
| AU2006324046A1 (en) | 2007-06-14 |
| EP1996556B1 (en) | 2009-11-18 |
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