AR082960A1 - Uso de analogos de carba-nucleosidos-2-fluor sustituidos para preparar medicamentos para el tratamiento de infecciones por virus de la influenza, y compuestos relacionados - Google Patents
Uso de analogos de carba-nucleosidos-2-fluor sustituidos para preparar medicamentos para el tratamiento de infecciones por virus de la influenza, y compuestos relacionadosInfo
- Publication number
- AR082960A1 AR082960A1 ARP110103311A ARP110103311A AR082960A1 AR 082960 A1 AR082960 A1 AR 082960A1 AR P110103311 A ARP110103311 A AR P110103311A AR P110103311 A ARP110103311 A AR P110103311A AR 082960 A1 AR082960 A1 AR 082960A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- substituted
- alkynyl
- alkenyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 2
- 229940079593 drug Drugs 0.000 title 1
- 208000015181 infectious disease Diseases 0.000 title 1
- 241000712461 unidentified influenza virus Species 0.000 title 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 14
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 10
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 9
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 125000005884 carbocyclylalkyl group Chemical group 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000009620 Orthomyxoviridae Infections Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
Classifications
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- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- 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
- A61K31/4965—Non-condensed pyrazines
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
- C07H7/06—Heterocyclic radicals
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Virology (AREA)
- Emergency Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicación 1: Uso de un compuesto de fórmula (1) o una de sus sales o ésteres farmacéuticamente aceptables; donde cada R1 es H o halógeno; cada R2 es halógeno; cada R3 o R5 es de manera independiente, H, ORa, N(Ra)2, N3, CN, NO2, S(O)nRa, halógeno, alquilo C1-8, carbociclilalquilo C4-8, alquilo C1-8 sustituido, alquenilo C2-8, alquenilo C2-8 sustituido, alquinilo C2-8 o alquinilo C2-8 sustituido; R6 es H, ORa, N(Ra)2, N3, CN, NO2, S(O)nRa, -C(=O)R11, -C(=O)OR11, -C(=O)NR11R12, -C(=O)SR11, -S(O)R11, -S(O)2R11, -S(O)(OR11), -S(O)2(OR11), -SO2NR11R12, halógeno, alquilo C1-8, carbociclilalquilo C4-8, alquilo C1-8 sustituido, alquenilo C2-8, alquenilo C2-8 sustituido, alquinilo C2-8, alquinilo C2-8 sustituido o arilalquilo C1-8; cada n es, de manera independiente, 0, 1 ó 2; cada Ra es, de manera independiente, H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, arilalquilo C1-8, carbociclilalquilo C4-8, -C(=O)R11, -C(=O)OR11, -C(=O)NR11R12, -C(=O)SR11, -S(O)R11, -S(O)2R11, -S(O)(OR11), -S(O)2(OR11), o -SO2NR11R12; R7 es H, -C(=O)R11, -C(=O)OR11, -C(=O)NR11R12, -C(=O)SR11, -S(O)R11, -S(O)2R11, -S(O)(OR11), -S(O)2(OR11), -SO2NR11R12, o bien un resto de fórmula (2); cada Y o Y1 es, de manera independiente, O, S, NR, +N(O)(R), N(OR), +N(O)(OR), o N-NR2; W1 y W2, cuando se los toma en conjunto, son -Y3(C(Ry)2)3Y3-; o uno de W1 o W2 en conjunto con R3 es -Y3- y el otro de W1 o W2 tiene la fórmula (3); cada uno de W1 y W2 es, de manera independiente, un grupo de la fórmula (3), donde cada Y2 es, de manera independiente, una unión, O, CR2, NR, +N(O)(R), N(OR), +N(O)(OR), N-NR2, S, S-S, S(O), o S(O)2; cada Y3 es, de manera independiente, O, S, o NR; M2 es 0, 1 ó 2; cada Rx es, de manera independiente, Ry o la fórmula (4) donde cada M1a, M1c, y M1d es, de manera independiente, 0 ó 1; M12c es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ó 12; cada Ry es, de manera independiente, H, F, Cl, Br, I, OH, R, -C(=Y1)R, -C(=Y1)OR, -C(=Y1)N(R)2, -N(R)2, -+N(R)3, -SR, -S(O)R, -S(O)2R, -S(O)(OR), -S(O)2(OR), -OC(=Y1)R, -OC(=Y1)OR, -OC(=Y1)(N(R)2), -SC(=Y1)R, -SC(=Y1)OR, -SC(=Y1)(N(R)2), -N(R)C(=Y1)R, -N(R)C(=Y1)OR, -N(R)C(=Y1)N(R)2, -SO2NR2, -CN, -N3, -NO2, -OR, o W3; o cuando se los toma en conjunto, dos Ry en el mismo átomo de carbono forman un anillo carbocíclico de entre 3 y 7 átomos de carbono; cada R es, de manera independiente, H, alquilo C1-8, alquilo C1-8 sustituido, alquenilo C2-8, alquenilo C2-8 sustituido, alquinilo C2-8, alquinilo C2-8 sustituido, arilo C6-20, arilo C6-20 sustituido, heterociclilo C2-20, heterociclilo C2-20 sustituido, arilalquilo o arilalquilo sustituido; W3 es W4 o W5; W4 es R, -C(Y1)Ry, -C(Y1)W5, -SO2Ry, o -SO2W5; y W5 es un carbociclo o un heterociclo donde W5 está, de manera independiente, sustituido con 0 a 3 grupos Ry; cada R8 es halógeno, NR11R12, N(R11)OR11, NR11NR11R12, N3, NO, NO2, CHO, CN, -CH(=NR11), -CH=NNHR11, -CH=N(OR11), -CH(OR11)2, -C(=O)NR11R12, -C(=S)NR11R12, -C(=O)OR11, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilalquilo C4-8, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(=O)alquilo C1-8, -S(O)n-alquilo C1-8, arilalquilo C1-8, OR11 o SR11; cada R9 o R10 es, de manera independiente, H, halógeno, NR11R12, N(R11)OR11, NR11NR11R12, N3, NO, NO2, CHO, CN, -CH(=NR11), -CH=NHNR11, -CH=N(OR11), -CH(OR11)2, -C(=O)NR11R12, -C(=S)NR11R12, -C(=O)OR11, R11, OR11 o SR11; cada R11 o R12 es, de manera independiente, H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilalquilo C4-8, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(=O)alquilo C1-8, -S(O)alquilo C1-8 o arilalquilo C1-8; o R11 y R12 tomados en conjunto con un nitrógeno al cual ambos están unidos forman un anillo heterocíclico de 3 a 7 miembros donde cualquiera de los átomos de carbono de dicho anillo heterocíclico puede ser opcionalmente reemplazados con -O-, -S- o -NRa-; y donde cada alquilo C1-8, alquenilo C2-8, alquinilo C2-8 o arilalquilo C1-8 de cada R3, R5, R6, R11 o R12 está, de manera independiente, opcionalmente sustituido con uno o más halo, hidroxi, CN, N3, N(Ra)2 o ORa; y donde uno o más de los átomos de carbono no terminales de cada uno de dicho alquilo C1-8 pueden ser opcionalmente reemplazados con -O-, -S- o -NRa-; para la preparación de un medicamento para el tratamiento de una infección por Orthomyxoviridae.Reivindicación 30: Un compuesto que tiene una estructura de fórmula (5) ó (6); o una de sus sales o ésteres farmacéuticamente aceptables.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38214510P | 2010-09-13 | 2010-09-13 |
Publications (1)
Publication Number | Publication Date |
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AR082960A1 true AR082960A1 (es) | 2013-01-23 |
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ID=44678052
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP110103311A AR082960A1 (es) | 2010-09-13 | 2011-09-12 | Uso de analogos de carba-nucleosidos-2-fluor sustituidos para preparar medicamentos para el tratamiento de infecciones por virus de la influenza, y compuestos relacionados |
Country Status (14)
Country | Link |
---|---|
US (3) | US20120107274A1 (es) |
EP (1) | EP2616080A1 (es) |
JP (1) | JP2013541519A (es) |
KR (1) | KR20140091459A (es) |
CN (1) | CN103153314A (es) |
AR (1) | AR082960A1 (es) |
AU (1) | AU2011302310A1 (es) |
BR (1) | BR112013005888A2 (es) |
CA (1) | CA2807584C (es) |
EA (1) | EA201390142A1 (es) |
MX (1) | MX2013002871A (es) |
TW (1) | TW201305185A (es) |
UY (1) | UY33600A (es) |
WO (1) | WO2012037038A1 (es) |
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BR112013001267A2 (pt) | 2010-07-19 | 2016-05-17 | Gilead Sciences Inc | métodos para a preparação de pró-fármacos de fosforamidato diasteromericamente puro |
US20120027752A1 (en) | 2010-07-22 | 2012-02-02 | Gilead Sciences, Inc. | Methods and compounds for treating paramyxoviridae virus infections |
EP2691409B1 (en) | 2011-03-31 | 2018-02-21 | Idenix Pharmaceuticals LLC. | Compounds and pharmaceutical compositions for the treatment of viral infections |
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WO2014197578A1 (en) | 2013-06-05 | 2014-12-11 | Idenix Pharmaceuticals, Inc. | 1',4'-thio nucleosides for the treatment of hcv |
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- 2011-09-12 MX MX2013002871A patent/MX2013002871A/es unknown
- 2011-09-12 EA EA201390142A patent/EA201390142A1/ru unknown
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- 2011-09-12 KR KR1020137009336A patent/KR20140091459A/ko not_active Application Discontinuation
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- 2011-09-12 CN CN201180048992XA patent/CN103153314A/zh active Pending
- 2011-09-12 AU AU2011302310A patent/AU2011302310A1/en not_active Abandoned
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- 2011-09-12 US US13/230,634 patent/US20120107274A1/en not_active Abandoned
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CN103153314A (zh) | 2013-06-12 |
CA2807584A1 (en) | 2012-03-22 |
US20140200188A1 (en) | 2014-07-17 |
US20120107274A1 (en) | 2012-05-03 |
TW201305185A (zh) | 2013-02-01 |
AU2011302310A1 (en) | 2013-02-28 |
EP2616080A1 (en) | 2013-07-24 |
CA2807584C (en) | 2018-10-23 |
MX2013002871A (es) | 2013-06-28 |
KR20140091459A (ko) | 2014-07-21 |
EA201390142A1 (ru) | 2013-09-30 |
BR112013005888A2 (pt) | 2016-05-10 |
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