EA200970455A1 - ЗАМЕЩЕННЫЙ 8-ПИПЕРИДИНИЛ-2-ПИРИДИНИЛПИРИМИДО[1,2-a]ПИРИМИДИН-6-ОН И ПРОИЗВОДНЫЕ 8-ПИПЕРИДИНИЛ-2-ПИРИМИДИНИЛПИРИМИДО[1,2-a]ПИРИМИДИН-6-ОНА - Google Patents
ЗАМЕЩЕННЫЙ 8-ПИПЕРИДИНИЛ-2-ПИРИДИНИЛПИРИМИДО[1,2-a]ПИРИМИДИН-6-ОН И ПРОИЗВОДНЫЕ 8-ПИПЕРИДИНИЛ-2-ПИРИМИДИНИЛПИРИМИДО[1,2-a]ПИРИМИДИН-6-ОНАInfo
- Publication number
- EA200970455A1 EA200970455A1 EA200970455A EA200970455A EA200970455A1 EA 200970455 A1 EA200970455 A1 EA 200970455A1 EA 200970455 A EA200970455 A EA 200970455A EA 200970455 A EA200970455 A EA 200970455A EA 200970455 A1 EA200970455 A1 EA 200970455A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- optionally substituted
- pyrimidine
- piperidinyl
- ring
- takes
- Prior art date
Links
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 102000019058 Glycogen Synthase Kinase 3 beta Human genes 0.000 abstract 1
- 108010051975 Glycogen Synthase Kinase 3 beta Proteins 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 229940126601 medicinal product Drugs 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 150000008318 pyrimidones Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
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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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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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
- A61P25/14—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
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- 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
- A61P25/24—Antidepressants
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P27/00—Drugs for disorders of the senses
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A61P27/06—Antiglaucoma agents or miotics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- 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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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Dermatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
Abstract
Изобретение относится к производному пиримидона, представленному формулой I или его солигде Х представляет собой два атома водорода, атом серы, атом кислорода или Cалкильную группу и атом водорода; Y представляет собой связь, карбонильную группу или необязательно замещенную метиленовую группу; R1 представляет собой 2, 3 или 4-пиридиновое кольцо или 2, 4 или 5-пиримидиновое кольцо, где кольцо необязательно является замещенным; R2 представляет собой бензольное кольцо или нафталиновую систему колец, где кольца необязательно являются замещенными; R3 представляет собой атом водорода, Cалкильную группу или атом галогена; R4 представляет собой атом водорода, Cалкоксикарбонильную группу или необязательно замещенную Cалкильную группу; n принимает значения от 0 до 3, р обозначает 2; q является 0; о принимает значения 0, 1 или 2; m, соответственно, принимает значения 4, 3 или 2, при том что о+m равно 4. Изобретение относится также к лекарственному средству, содержащему указанное производное или его соль в качестве активного ингредиента, которое используют для профилактического и/или терапевтического лечения такого нейродегенеративного заболевания, как болезнь Альцгеймера, вызываемого аномальной активностью GSK3β.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06291725A EP1921080B1 (en) | 2006-11-07 | 2006-11-07 | Subsitituted 8-piperidinyl-2-pyridinyl-pyrimido(1,2-a)pyrimidin-6-one and 8-piperidinyl-2-pyrimidinyl-pyrimido(1,2-a)pyrimidin-6-one derivatives |
| PCT/IB2007/004272 WO2008056266A2 (en) | 2006-11-07 | 2007-11-06 | Substituted 8-piperidinyl-2-pyridinyl-pyrimido [1,2-a]pyrimidin-6-one and 8-piperidinyl-2-pyrimidinyl-pyrimido[1,2-a]pyrimidin-6-one derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200970455A1 true EA200970455A1 (ru) | 2009-12-30 |
| EA016251B1 EA016251B1 (ru) | 2012-03-30 |
Family
ID=38331403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200970455A EA016251B1 (ru) | 2006-11-07 | 2007-11-06 | ПРОИЗВОДНЫЕ 8-ПИПЕРИДИНИЛ-2-ПИРИДИНИЛПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20090281121A1 (ru) |
| EP (2) | EP1921080B1 (ru) |
| JP (1) | JP2010509203A (ru) |
| KR (1) | KR20090091123A (ru) |
| CN (1) | CN101535314A (ru) |
| AR (1) | AR063577A1 (ru) |
| AU (1) | AU2007318927A1 (ru) |
| BR (1) | BRPI0718519A2 (ru) |
| CA (1) | CA2668682A1 (ru) |
| EA (1) | EA016251B1 (ru) |
| IL (1) | IL198239A0 (ru) |
| MX (1) | MX2009004884A (ru) |
| NZ (1) | NZ576773A (ru) |
| TW (1) | TW200835495A (ru) |
| WO (1) | WO2008056266A2 (ru) |
| ZA (1) | ZA200902630B (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| FR2992316A1 (fr) * | 2012-06-22 | 2013-12-27 | Sanofi Sa | Derives de pyrimidinones, leur preparation et leur application en therapeutique |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005000800A1 (en) * | 2003-06-30 | 2005-01-06 | Merck Frosst Canada Ltd. | Cathepsin cysteine protease inhibitors |
| EP1557417B1 (en) * | 2003-12-19 | 2007-03-07 | Sanofi-Aventis | Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives |
-
2006
- 2006-11-07 EP EP06291725A patent/EP1921080B1/en not_active Expired - Fee Related
-
2007
- 2007-11-06 AU AU2007318927A patent/AU2007318927A1/en not_active Abandoned
- 2007-11-06 EP EP07859310A patent/EP2081938A2/en not_active Withdrawn
- 2007-11-06 CA CA002668682A patent/CA2668682A1/en not_active Abandoned
- 2007-11-06 NZ NZ576773A patent/NZ576773A/en not_active IP Right Cessation
- 2007-11-06 ZA ZA200902630A patent/ZA200902630B/xx unknown
- 2007-11-06 AR ARP070104932A patent/AR063577A1/es unknown
- 2007-11-06 EA EA200970455A patent/EA016251B1/ru not_active IP Right Cessation
- 2007-11-06 WO PCT/IB2007/004272 patent/WO2008056266A2/en active Application Filing
- 2007-11-06 JP JP2009535149A patent/JP2010509203A/ja not_active Withdrawn
- 2007-11-06 MX MX2009004884A patent/MX2009004884A/es active IP Right Grant
- 2007-11-06 CN CNA200780041338XA patent/CN101535314A/zh active Pending
- 2007-11-06 TW TW096141872A patent/TW200835495A/zh unknown
- 2007-11-06 BR BRPI0718519-7A patent/BRPI0718519A2/pt not_active IP Right Cessation
- 2007-11-06 KR KR1020097009377A patent/KR20090091123A/ko not_active Withdrawn
-
2009
- 2009-04-20 IL IL198239A patent/IL198239A0/en unknown
- 2009-05-01 US US12/434,053 patent/US20090281121A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN101535314A (zh) | 2009-09-16 |
| WO2008056266A3 (en) | 2008-07-10 |
| WO2008056266A2 (en) | 2008-05-15 |
| NZ576773A (en) | 2011-09-30 |
| IL198239A0 (en) | 2009-12-24 |
| EP1921080B1 (en) | 2009-08-05 |
| WO2008056266A8 (en) | 2009-06-18 |
| BRPI0718519A2 (pt) | 2014-04-15 |
| EP2081938A2 (en) | 2009-07-29 |
| US20090281121A1 (en) | 2009-11-12 |
| AR063577A1 (es) | 2009-02-04 |
| KR20090091123A (ko) | 2009-08-26 |
| MX2009004884A (es) | 2009-05-21 |
| ZA200902630B (en) | 2010-06-30 |
| AU2007318927A1 (en) | 2008-05-15 |
| CA2668682A1 (en) | 2008-05-15 |
| EP1921080A1 (en) | 2008-05-14 |
| TW200835495A (en) | 2008-09-01 |
| JP2010509203A (ja) | 2010-03-25 |
| EA016251B1 (ru) | 2012-03-30 |
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