PE20140390A1 - Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak - Google Patents
Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jakInfo
- Publication number
- PE20140390A1 PE20140390A1 PE2013000970A PE2013000970A PE20140390A1 PE 20140390 A1 PE20140390 A1 PE 20140390A1 PE 2013000970 A PE2013000970 A PE 2013000970A PE 2013000970 A PE2013000970 A PE 2013000970A PE 20140390 A1 PE20140390 A1 PE 20140390A1
- Authority
- PE
- Peru
- Prior art keywords
- imidazo
- alkyl
- pyridazine
- pyridine
- pyridazin
- Prior art date
Links
- 150000004942 imidazo[1,2-b]pyridazines Chemical class 0.000 title abstract 2
- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 title 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 abstract 2
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 abstract 1
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 abstract 1
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 abstract 1
- 208000014767 Myeloproliferative disease Diseases 0.000 abstract 1
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 abstract 1
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 abstract 1
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000030533 eye disease Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 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
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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
- A61K31/33—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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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
- A61K31/33—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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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
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
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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
- A61P1/04—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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
REFERIDA A UN DERIVADO DE IMIDAZO[1,2-b]PIRIDAZINA E IMIDAZO[4,5-B]PIRIDINA DE FORMULA (I), DONDE: m ES 0 O UN ENTERO DE 1 A 3; X E Y SON N O CR7; R7 ES H, HALOGENO, CIANO, ALQUILO C1-C6, ENTRE OTROS; G1 Y G2 SON N Y C; R1 Y R2 SON H, ALQUILO C1-C6, OH, ENTRE OTROS; R3 ES H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; R4 ES H, HALOALQUILO C1-C4, ALQUILO C1-C6, ENTRE OTROS; R5 Y R6 SON H, HALOALQUILO C1-C4, HIDROXIALQUILO C1-C4, ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3-OXO-3-((3R)-3-{[3-(2-OXO-1,2-DIHIDROPIRIDIN-3-IL)IMIDAZO[1,2-b]PIRIDAZIN-6-IL]AMINO}PIPERIDIN-1-IL)PROPANONITRILO, 3-(6-{[(1S)-1-FENILETIL AMINO}IMIDAZO[1,2-b]PIRIDAZIN-3-IL)PIRIDIN-2(1H)-ONA, 3-(6-{[(1S)-1-(5-FLUOROPIRIDIN-2-IL) ETIL]AMINO}IMIDAZO[1,2-b]PIRIDAZIN-3-IL)PIRIDIN-2(1H)-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS QUINASAS JAK1, JAK2 Y JAK3 Y SON UTILES EN EL TRATAMIENTO DE TRANSTORNOS MIELOPROLIFERATIVOS, ENFERMEDADES INFLAMATORIAS, ENFERMEDADES OCULARES, ENTRE OTRAS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20100382318 EP2463289A1 (en) | 2010-11-26 | 2010-11-26 | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| US201161436212P | 2011-01-26 | 2011-01-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20140390A1 true PE20140390A1 (es) | 2014-03-29 |
Family
ID=43585650
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013000970A PE20140390A1 (es) | 2010-11-26 | 2011-11-24 | Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9133200B2 (es) |
| EP (2) | EP2463289A1 (es) |
| JP (1) | JP5809704B2 (es) |
| KR (1) | KR20140004637A (es) |
| CN (1) | CN103228654A (es) |
| AR (1) | AR087328A1 (es) |
| AU (1) | AU2011334146A1 (es) |
| BR (1) | BR112013012965A2 (es) |
| CA (1) | CA2815029A1 (es) |
| CL (1) | CL2013001464A1 (es) |
| CO (1) | CO6781467A2 (es) |
| CR (1) | CR20130210A (es) |
| EA (1) | EA201300620A1 (es) |
| GT (1) | GT201300137A (es) |
| IL (1) | IL225232A0 (es) |
| MX (1) | MX2013005257A (es) |
| NZ (1) | NZ608718A (es) |
| PE (1) | PE20140390A1 (es) |
| PH (1) | PH12013500742A1 (es) |
| SG (1) | SG190042A1 (es) |
| TW (1) | TW201236683A (es) |
| UY (1) | UY33752A (es) |
| WO (1) | WO2012069202A1 (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2377318T3 (es) | 2002-09-06 | 2012-03-26 | Cerulean Pharma Inc. | Polímeros a base de ciclodextrina para el suministro de los agentes terapéuticos enlazados covalentemente a ellos |
| JP2010516625A (ja) | 2007-01-24 | 2010-05-20 | インサート セラピューティクス, インコーポレイテッド | 制御された薬物送達のためのテザー基を有するポリマー−薬物コンジュゲート |
| UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| US20140094432A1 (en) | 2012-10-02 | 2014-04-03 | Cerulean Pharma Inc. | Methods and systems for polymer precipitation and generation of particles |
| HK1215210A1 (zh) * | 2012-11-07 | 2016-08-19 | Teva Pharmaceutical Industries Ltd. | 拉喹莫德胺盐 |
| CN103845726A (zh) * | 2012-12-07 | 2014-06-11 | 天津市汉康医药生物技术有限公司 | 克拉屈滨和乙酸格拉默的组合用于治疗多发性硬化的用途 |
| US9370515B2 (en) | 2013-03-07 | 2016-06-21 | Califia Bio, Inc. | Mixed lineage kinase inhibitors and method of treatments |
| NZ630427A (en) | 2013-03-14 | 2017-06-30 | Teva Pharma | Crystals of laquinimod sodium and improved process for the manufacture thereof |
| WO2014194195A2 (en) * | 2013-05-31 | 2014-12-04 | Cerulean Pharma Inc. | Cyclodextrin-based polymers for the therapeutic delivery |
| GB201321734D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
| WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
| WO2017096262A1 (en) | 2015-12-04 | 2017-06-08 | Jomoco, Corp. | Compositions and methods to mitigate or prevent an immune response to an immunogenic therapeutic molecule in non-human primates |
| US11629124B2 (en) * | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| JP2021008407A (ja) * | 2017-10-02 | 2021-01-28 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| MA54551A (fr) | 2018-12-20 | 2021-10-27 | Incyte Corp | Composés d'imidazopyridazine et d'imidazopyridine utilisés en tant qu'inhibiteurs de la kinase 2 de type récepteur de l'activine |
| WO2021062163A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| PL3886858T3 (pl) | 2019-12-19 | 2022-08-29 | Active Biotech Ab | Związki do leczenia chorób oka związanych z nadmiernym unaczynieniem |
| CA3177830A1 (en) | 2020-05-13 | 2021-11-18 | Maria BECONI | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| PE20230491A1 (es) | 2020-06-12 | 2023-03-23 | Incyte Corp | Compuestos de imidazopiridazina con actividad como inhibidores de alk2 |
| KR20230157431A (ko) * | 2021-03-15 | 2023-11-16 | 키에시 파르마슈티시 엣스. 피. 에이. | 야누스 키나아제 억제제로서 헤테로사이클릭 유도체 |
| JP2024510247A (ja) * | 2021-03-15 | 2024-03-06 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | ヤヌスキナーゼ阻害剤としてのヘテロ環誘導体 |
| CN117098765A (zh) * | 2021-03-15 | 2023-11-21 | 奇斯药制品公司 | 作为詹纳斯激酶抑制剂的杂环衍生物 |
| CN117157293A (zh) * | 2021-03-16 | 2023-12-01 | 怡诺安有限公司 | 作为蛋白激酶抑制剂的杂环化合物的新型盐及其用途 |
| CA3212253A1 (en) * | 2021-03-16 | 2022-09-22 | Young Ju Kim | Crystalline form of heterocyclic compound as protein kinase inhibitor |
| KR20220129494A (ko) * | 2021-03-16 | 2022-09-23 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물의 신규 염 및 이들의 용도 |
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-
2010
- 2010-11-26 EP EP20100382318 patent/EP2463289A1/en not_active Withdrawn
-
2011
- 2011-11-18 TW TW100142217A patent/TW201236683A/zh unknown
- 2011-11-24 SG SG2013032453A patent/SG190042A1/en unknown
- 2011-11-24 CA CA2815029A patent/CA2815029A1/en active Pending
- 2011-11-24 AR ARP110104376 patent/AR087328A1/es unknown
- 2011-11-24 NZ NZ60871811A patent/NZ608718A/en not_active IP Right Cessation
- 2011-11-24 US US13/988,798 patent/US9133200B2/en not_active Expired - Fee Related
- 2011-11-24 AU AU2011334146A patent/AU2011334146A1/en not_active Abandoned
- 2011-11-24 WO PCT/EP2011/005929 patent/WO2012069202A1/en not_active Ceased
- 2011-11-24 MX MX2013005257A patent/MX2013005257A/es not_active Application Discontinuation
- 2011-11-24 KR KR1020137010392A patent/KR20140004637A/ko not_active Withdrawn
- 2011-11-24 EA EA201300620A patent/EA201300620A1/ru unknown
- 2011-11-24 PE PE2013000970A patent/PE20140390A1/es not_active Application Discontinuation
- 2011-11-24 PH PH1/2013/500742A patent/PH12013500742A1/en unknown
- 2011-11-24 BR BR112013012965A patent/BR112013012965A2/pt not_active IP Right Cessation
- 2011-11-24 JP JP2013540267A patent/JP5809704B2/ja not_active Expired - Fee Related
- 2011-11-24 CN CN2011800569943A patent/CN103228654A/zh active Pending
- 2011-11-24 EP EP11788775.2A patent/EP2643321A1/en not_active Withdrawn
- 2011-11-24 UY UY33752A patent/UY33752A/es unknown
-
2013
- 2013-03-14 IL IL225232A patent/IL225232A0/en unknown
- 2013-05-10 CO CO13117486A patent/CO6781467A2/es active IP Right Grant
- 2013-05-10 CR CR20130210A patent/CR20130210A/es unknown
- 2013-05-23 GT GT201300137A patent/GT201300137A/es unknown
- 2013-05-23 CL CL2013001464A patent/CL2013001464A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2014501724A (ja) | 2014-01-23 |
| WO2012069202A1 (en) | 2012-05-31 |
| EP2643321A1 (en) | 2013-10-02 |
| CN103228654A (zh) | 2013-07-31 |
| SG190042A1 (en) | 2013-06-28 |
| CR20130210A (es) | 2013-08-09 |
| CO6781467A2 (es) | 2013-10-31 |
| US20130309200A1 (en) | 2013-11-21 |
| CL2013001464A1 (es) | 2013-09-06 |
| KR20140004637A (ko) | 2014-01-13 |
| EP2463289A1 (en) | 2012-06-13 |
| CA2815029A1 (en) | 2012-05-31 |
| TW201236683A (en) | 2012-09-16 |
| AR087328A1 (es) | 2014-03-19 |
| PH12013500742A1 (en) | 2015-10-23 |
| EA201300620A1 (ru) | 2013-12-30 |
| JP5809704B2 (ja) | 2015-11-11 |
| MX2013005257A (es) | 2014-02-06 |
| IL225232A0 (en) | 2013-06-27 |
| AU2011334146A1 (en) | 2013-04-04 |
| NZ608718A (en) | 2015-04-24 |
| BR112013012965A2 (pt) | 2016-08-23 |
| GT201300137A (es) | 2014-04-03 |
| US9133200B2 (en) | 2015-09-15 |
| UY33752A (es) | 2012-05-31 |
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