BRPI0607385A2 - piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3 - Google Patents
piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3Info
- Publication number
- BRPI0607385A2 BRPI0607385A2 BRPI0607385-9A BRPI0607385A BRPI0607385A2 BR PI0607385 A2 BRPI0607385 A2 BR PI0607385A2 BR PI0607385 A BRPI0607385 A BR PI0607385A BR PI0607385 A2 BRPI0607385 A2 BR PI0607385A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- diseases
- limiting example
- therapy
- antagonist activity
- Prior art date
Links
- 229940126692 CXCR3 antagonist Drugs 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title abstract 2
- 150000004885 piperazines Chemical class 0.000 title abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 150000002148 esters Chemical class 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 102000019034 Chemokines Human genes 0.000 abstract 1
- 108010012236 Chemokines Proteins 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 206010016741 Fixed eruption Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010027260 Meningitis viral Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010052779 Transplant rejections Diseases 0.000 abstract 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 238000009109 curative therapy Methods 0.000 abstract 1
- 230000003111 delayed effect Effects 0.000 abstract 1
- 230000009610 hypersensitivity Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 238000009116 palliative therapy Methods 0.000 abstract 1
- 238000009117 preventive therapy Methods 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 230000036555 skin type Effects 0.000 abstract 1
- 201000006382 tuberculoid leprosy Diseases 0.000 abstract 1
- 201000010044 viral meningitis Diseases 0.000 abstract 1
Classifications
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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P17/06—Antipsoriatics
-
- 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
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/08—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
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
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- 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
- A61P31/04—Antibacterial agents
- A61P31/08—Antibacterial agents for leprosy
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- 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
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- 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
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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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
- A61P37/08—Antiallergic 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
PIPERAZINAS SUBSTITUìDAS HETEROCìCLICAS COM ATIVIDADE DE ANTAGONISTA DE CXCR3. A presente invenção refere-se a um composto, ou enantiómeros, estereoisómeros, rotâmeros, tautómeros, racematos ou pró-fármacos do dito composto, ou sais, solvatos ou ésteres do dito composto farmaceuticamente aceitáveis, ou do dito pró-fármaco, o dito composto tendo uma estrutura geral apresentada na Fórmula 1: ou um sal, solvato ou éster do mesmo farmaceuticamente aceitável, em que as diversas porções estão definidas aqui. Está também descrito um método de tratar doenças mediadas por quimiocina, tais como, terapia paliativa, terapia curativa, terapia profilática de certas doenças e condições tais como doenças inflamatórias (exemplo(s) não limitante(s) inclui(incluem) psoríase), doenças auto-imunes (exemplo(s) não limitante(s) inclui(incluem) artrite reumatóide, esclerose múltipla), rejeição de enxerto (exemplo(s) não limitante(s) inclui(incluem) rejeição de aloenxerto, rejeição de xenoenxerto), doenças infecciosas (por exemplo, lepra tuberculóide), erupções fixas por fármaco, respostas de hipersensibilidade do tipo demorado cutâneo, inflamação oftálmica, diabetes tipo 1, meningite viral e tumores usando um composto da Fórmula 1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65330905P | 2005-02-16 | 2005-02-16 | |
| PCT/US2006/005123 WO2006088837A2 (en) | 2005-02-16 | 2006-02-14 | Heterocyclic substituted piperazines with cxcr3 antagonist activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0607385A2 true BRPI0607385A2 (pt) | 2009-09-01 |
Family
ID=36637011
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0607385-9A BRPI0607385A2 (pt) | 2005-02-16 | 2006-02-14 | piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US7868006B2 (pt) |
| EP (1) | EP1848710B1 (pt) |
| JP (2) | JP4873352B2 (pt) |
| KR (1) | KR20070107046A (pt) |
| CN (1) | CN101163692B (pt) |
| AR (1) | AR052911A1 (pt) |
| AU (1) | AU2006214477A1 (pt) |
| BR (1) | BRPI0607385A2 (pt) |
| CA (1) | CA2598456A1 (pt) |
| IL (1) | IL185072A0 (pt) |
| MX (1) | MX2007009945A (pt) |
| NO (1) | NO20074690L (pt) |
| PE (1) | PE20061093A1 (pt) |
| RU (1) | RU2007134259A (pt) |
| TW (1) | TW200640907A (pt) |
| WO (1) | WO2006088837A2 (pt) |
| ZA (1) | ZA200706790B (pt) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2526586C (en) | 2003-09-09 | 2010-03-16 | Biogen International Gmbh | The use of fumaric acid derivatives for treating cardiac insufficiency, and asthma |
| EA015517B1 (ru) | 2004-04-13 | 2011-08-30 | Инсайт Корпорейшн | Производные пиперазинилпиперидина в качестве антагонистов хемокинового рецептора |
| JP4873352B2 (ja) * | 2005-02-16 | 2012-02-08 | シェーリング コーポレイション | Cxcr3アンタゴニスト活性を有する、複素環で置換されたピペラジン |
| MX2007009949A (es) * | 2005-02-16 | 2007-09-26 | Schering Corp | Pirazinil-piperazin-piperidinas sustituidas con heteroarilo con actividad antagonista de cxcr3. |
| EP1853583B1 (en) * | 2005-02-16 | 2011-09-07 | Schering Corporation | Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity |
| MX2007010067A (es) * | 2005-02-16 | 2007-12-07 | Schering Corp | Compuestos heterociclicos novedosos sustituidos con piridina o fenilo con actividad antagonista de cxcr3. |
| PE20061164A1 (es) * | 2005-02-16 | 2006-10-27 | Schering Corp | Piperazin-piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3 |
| TW200714610A (en) | 2005-02-16 | 2007-04-16 | Univ Maryland | CXCR3 is a gliadin receptor |
| JP2008530218A (ja) * | 2005-02-16 | 2008-08-07 | シェーリング コーポレイション | Cxcr3アンタゴニスト活性を有する、ピリジルおよびフェニルで置換されたピペラジン−ピペリジン |
| CA2625762A1 (en) * | 2005-10-11 | 2007-04-26 | Schering Corporation | Substituted heterocyclic compounds with cxcr3 antagonist activity |
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| MX2009000577A (es) * | 2006-07-14 | 2009-03-09 | Schering Corp | Compuestos de piperazina sustituida heterociclica con actividad antagonista de cxcr3. |
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| EP2680010A1 (en) | 2007-02-08 | 2014-01-01 | Biogen Idec MA Inc. | Nrf2 screening assays and related methods and compositions |
| WO2008103378A2 (en) | 2007-02-20 | 2008-08-28 | Merrimack Pharmaceuticals, Inc. | Methods of treating multiple sclerosis by administration of alpha-fetoprotein in combination with an integrin antagonist |
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| CN101678082B (zh) | 2007-03-26 | 2013-06-19 | 再生医药有限公司 | 使用cxcl9和抗cxcl9抗体促进骨髓保护和再生的方法 |
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2006
- 2006-02-14 JP JP2007556236A patent/JP4873352B2/ja not_active Expired - Fee Related
- 2006-02-14 BR BRPI0607385-9A patent/BRPI0607385A2/pt not_active IP Right Cessation
- 2006-02-14 WO PCT/US2006/005123 patent/WO2006088837A2/en not_active Ceased
- 2006-02-14 PE PE2006000177A patent/PE20061093A1/es not_active Application Discontinuation
- 2006-02-14 US US11/353,641 patent/US7868006B2/en active Active
- 2006-02-14 KR KR1020077018805A patent/KR20070107046A/ko not_active Withdrawn
- 2006-02-14 MX MX2007009945A patent/MX2007009945A/es active IP Right Grant
- 2006-02-14 CA CA002598456A patent/CA2598456A1/en not_active Abandoned
- 2006-02-14 RU RU2007134259/04A patent/RU2007134259A/ru not_active Application Discontinuation
- 2006-02-14 CN CN2006800124385A patent/CN101163692B/zh not_active Expired - Fee Related
- 2006-02-14 AU AU2006214477A patent/AU2006214477A1/en not_active Abandoned
- 2006-02-14 EP EP06735000.9A patent/EP1848710B1/en not_active Expired - Lifetime
- 2006-02-15 AR ARP060100546A patent/AR052911A1/es not_active Application Discontinuation
- 2006-02-15 TW TW095105138A patent/TW200640907A/zh unknown
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2007
- 2007-08-06 IL IL185072A patent/IL185072A0/en unknown
- 2007-08-15 ZA ZA200706790A patent/ZA200706790B/xx unknown
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2010
- 2010-11-23 US US12/952,994 patent/US8207170B2/en not_active Expired - Lifetime
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- 2011-02-18 JP JP2011033992A patent/JP2011126901A/ja not_active Withdrawn
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| NO20074690L (no) | 2007-11-16 |
| WO2006088837A2 (en) | 2006-08-24 |
| RU2007134259A (ru) | 2009-03-27 |
| MX2007009945A (es) | 2007-09-26 |
| EP1848710B1 (en) | 2013-10-16 |
| CN101163692B (zh) | 2012-01-18 |
| KR20070107046A (ko) | 2007-11-06 |
| IL185072A0 (en) | 2007-12-03 |
| US20110065651A1 (en) | 2011-03-17 |
| PE20061093A1 (es) | 2006-11-10 |
| ZA200706790B (en) | 2008-11-26 |
| AU2006214477A1 (en) | 2006-08-24 |
| US20060276479A1 (en) | 2006-12-07 |
| WO2006088837A3 (en) | 2006-11-02 |
| JP2008530214A (ja) | 2008-08-07 |
| CN101163692A (zh) | 2008-04-16 |
| US7868006B2 (en) | 2011-01-11 |
| JP4873352B2 (ja) | 2012-02-08 |
| TW200640907A (en) | 2006-12-01 |
| EP1848710A2 (en) | 2007-10-31 |
| CA2598456A1 (en) | 2006-08-24 |
| US8207170B2 (en) | 2012-06-26 |
| JP2011126901A (ja) | 2011-06-30 |
| AR052911A1 (es) | 2007-04-11 |
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