RU2013154355A - Способ лечения мезотелиомы ингибитором рi3к - Google Patents
Способ лечения мезотелиомы ингибитором рi3к Download PDFInfo
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- RU2013154355A RU2013154355A RU2013154355/15A RU2013154355A RU2013154355A RU 2013154355 A RU2013154355 A RU 2013154355A RU 2013154355/15 A RU2013154355/15 A RU 2013154355/15A RU 2013154355 A RU2013154355 A RU 2013154355A RU 2013154355 A RU2013154355 A RU 2013154355A
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- gdc
- patient
- mesothelioma
- effective amount
- therapeutically effective
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- 238000000034 method Methods 0.000 title claims abstract 24
- 206010027406 Mesothelioma Diseases 0.000 title claims abstract 11
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 title 1
- 108091007960 PI3Ks Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- YOVVNQKCSKSHKT-HNNXBMFYSA-N (2s)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one Chemical compound C1CN(C(=O)[C@@H](O)C)CCN1CC1=C(C)C2=NC(C=3C=NC(N)=NC=3)=NC(N3CCOCC3)=C2S1 YOVVNQKCSKSHKT-HNNXBMFYSA-N 0.000 claims abstract 20
- -1 bevacizumab Chemical compound 0.000 claims abstract 5
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims abstract 4
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims abstract 4
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims abstract 4
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims abstract 4
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims abstract 4
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims abstract 4
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims abstract 4
- 239000002246 antineoplastic agent Substances 0.000 claims abstract 4
- 229960000397 bevacizumab Drugs 0.000 claims abstract 4
- 230000037396 body weight Effects 0.000 claims abstract 4
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims abstract 4
- 229960004316 cisplatin Drugs 0.000 claims abstract 4
- 229940127089 cytotoxic agent Drugs 0.000 claims abstract 4
- 229960002448 dasatinib Drugs 0.000 claims abstract 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims abstract 4
- 229960001433 erlotinib Drugs 0.000 claims abstract 4
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims abstract 4
- 229960005277 gemcitabine Drugs 0.000 claims abstract 4
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims abstract 4
- 229960002411 imatinib Drugs 0.000 claims abstract 4
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 claims abstract 4
- 229960005079 pemetrexed Drugs 0.000 claims abstract 4
- 229960003787 sorafenib Drugs 0.000 claims abstract 4
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims abstract 4
- 229960001796 sunitinib Drugs 0.000 claims abstract 4
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims abstract 4
- 229960002066 vinorelbine Drugs 0.000 claims abstract 3
- 238000002512 chemotherapy Methods 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims abstract 2
- 239000004615 ingredient Substances 0.000 claims abstract 2
- 208000006178 malignant mesothelioma Diseases 0.000 claims abstract 2
- 201000005282 malignant pleural mesothelioma Diseases 0.000 claims abstract 2
- 238000001959 radiotherapy Methods 0.000 claims abstract 2
- 238000002271 resection Methods 0.000 claims abstract 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229910000503 Na-aluminosilicate Inorganic materials 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- 239000000378 calcium silicate Substances 0.000 claims 1
- 229910052918 calcium silicate Inorganic materials 0.000 claims 1
- 235000012241 calcium silicate Nutrition 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical class [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920001531 copovidone Polymers 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 229960001021 lactose monohydrate Drugs 0.000 claims 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims 1
- 239000001095 magnesium carbonate Substances 0.000 claims 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims 1
- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims 1
- 239000000395 magnesium oxide Substances 0.000 claims 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims 1
- 229910052751 metal Inorganic materials 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 229920003124 powdered cellulose Polymers 0.000 claims 1
- 235000019814 powdered cellulose Nutrition 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 239000000429 sodium aluminium silicate Substances 0.000 claims 1
- 235000012217 sodium aluminium silicate Nutrition 0.000 claims 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 claims 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims 1
- 239000004299 sodium benzoate Substances 0.000 claims 1
- 235000010234 sodium benzoate Nutrition 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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- A61K31/7068—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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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Abstract
1. GDC-0980, имеющий структуру:для применения для лечения мезотелиомы.2. Применение GDC-0980, имеющего структуру:для получения лекарственного средства для лечения мезотелиомы.3. Применение GDC-0980, имеющего структуру:для лечения мезотелиомы.4. Способ лечения мезотелиомы, включающий введение пациенту с мезотелиомой терапевтически эффективного количества GDC-0980, имеющего структуру:5. Способ по п. 4, когда пациент имеет злокачественную плевральную мезотелиому.6. Способ по п. 4, когда пациента ранее лечили химиотерапией, лучевой терапией и/или хирургической резекцией.7. Способ по п. 6, когда пациента ранее лечили одним или более чем одним химиотерапевтическим агентом, выбранным из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба и сорафениба.8. Способ по п. 4, в котором GDC-0980 вводится пациенту ежесуточно с интервалами три недели или четыре недели.9. Способ по п. 8, в котором после трехнедельного интервала следует однонедельный перерыв, когда пациенту не вводится GDC-0980.10. Способ по п. 4, в котором GDC-0980 вводится перорально.11. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 1 мг до 100 мг в сутки на массу тела пациента.12. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 10 мг до 50 мг в сутки в зависимости от массы тела пациента.13. Способ по п. 4, кроме того, включающий введение химиотерапевтического агента, выбранного из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба или сорафениба.14. Способ по п. 4, в котором GDC-0980 приготовлен в виде композиции с ингредиентом,
Claims (15)
5. Способ по п. 4, когда пациент имеет злокачественную плевральную мезотелиому.
6. Способ по п. 4, когда пациента ранее лечили химиотерапией, лучевой терапией и/или хирургической резекцией.
7. Способ по п. 6, когда пациента ранее лечили одним или более чем одним химиотерапевтическим агентом, выбранным из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба и сорафениба.
8. Способ по п. 4, в котором GDC-0980 вводится пациенту ежесуточно с интервалами три недели или четыре недели.
9. Способ по п. 8, в котором после трехнедельного интервала следует однонедельный перерыв, когда пациенту не вводится GDC-0980.
10. Способ по п. 4, в котором GDC-0980 вводится перорально.
11. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 1 мг до 100 мг в сутки на массу тела пациента.
12. Способ по п. 4, в котором терапевтически эффективное количество GDC-0980 составляет от 10 мг до 50 мг в сутки в зависимости от массы тела пациента.
13. Способ по п. 4, кроме того, включающий введение химиотерапевтического агента, выбранного из пеметрекседа, бевацизумаба, цисплатина, гемцитабина, винорелбина, иматиниба, дазатиниба, эрлотиниба, сунитиниба или сорафениба.
14. Способ по п. 4, в котором GDC-0980 приготовлен в виде композиции с ингредиентом, выбранным из микрокристаллической целлюлозы, моногидрата лактозы, кроскармеллозы натрия, коповидона и стеарата магния.
15. Способ по п. 4, в котором GDC-0980 приготовлен в виде композиции с фармацевтически приемлемым скользящим веществом, выбранным из диоксида кремния, порошковой целлюлозы, микрокристаллической целлюлозы, стеаратов металлов, алюмосиликата натрия, бензоата натрия, карбоната кальция, силиката кальция, кукурузного крахмала, карбоната магния, талька, не содержащего асбест, стеаровета С, крахмала, крахмала 1500, лаурилсульфата магния, оксида магния и их комбинаций.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161492966P | 2011-06-03 | 2011-06-03 | |
| US61/492,966 | 2011-06-03 | ||
| PCT/EP2012/060341 WO2012164060A1 (en) | 2011-06-03 | 2012-06-01 | Methods of treating mesothelioma with a pi3k inhibitor compound |
Publications (1)
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| RU2013154355A true RU2013154355A (ru) | 2015-07-20 |
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| RU2013154355/15A RU2013154355A (ru) | 2011-06-03 | 2012-06-01 | Способ лечения мезотелиомы ингибитором рi3к |
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| US (1) | US20120308562A1 (ru) |
| EP (1) | EP2714046A1 (ru) |
| JP (1) | JP2014515390A (ru) |
| KR (1) | KR20140040728A (ru) |
| CN (1) | CN103582479A (ru) |
| AR (1) | AR086647A1 (ru) |
| BR (1) | BR112013030991A2 (ru) |
| CA (1) | CA2835760A1 (ru) |
| MX (1) | MX2013014151A (ru) |
| RU (1) | RU2013154355A (ru) |
| WO (1) | WO2012164060A1 (ru) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MX2013006858A (es) | 2010-12-16 | 2013-07-29 | Hoffmann La Roche | Compuesto triciclicos inhibidores de la pi3k y metodos de uso. |
| CA2883513A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | Process for making thienopyrimidine compounds |
| CN105307669A (zh) * | 2013-05-23 | 2016-02-03 | 戊瑞治疗有限公司 | 治疗癌症的方法 |
| HK1223286A1 (zh) | 2013-05-29 | 2017-07-28 | 西格诺药品有限公司 | 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法 |
| SG10201802815UA (en) * | 2013-12-12 | 2018-05-30 | Almirall Sa | Pharmaceutical compositions comprising dimethyl fumarate |
| JP6592097B2 (ja) * | 2014-10-30 | 2019-10-16 | ビッグ ディーエヌエイ リミテッドBig Dna Ltd | 併用療法 |
| SI3316867T1 (sl) * | 2015-06-30 | 2021-08-31 | Genentech, Inc. | Tablete s takojšnjim sproščanjem, ki vsebujejo zdravilo in postopek za pripravo tablet |
| WO2018234584A1 (en) | 2017-06-23 | 2018-12-27 | Almirall, S.A. | Pharmaceutical compositions comprising dimethyl fumarate |
| US11103594B2 (en) | 2018-02-01 | 2021-08-31 | Imam Abdulrahman Bin Faisal University | Hierarchical siliceous mesosilicalite nanocarrier loaded with platinum(II) complex |
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| US6274327B1 (en) | 1992-04-13 | 2001-08-14 | Ludwig Institute For Cancer Research | Polypeptides having kinase activity, their preparation and use |
| US5846824A (en) | 1994-02-07 | 1998-12-08 | Ludwig Institute For Cancer Research | Polypeptides having kinase activity, their preparation and use |
| GB9208135D0 (en) | 1992-04-13 | 1992-05-27 | Ludwig Inst Cancer Res | Polypeptides having kinase activity,their preparation and use |
| SI1934174T1 (sl) | 2005-10-07 | 2011-08-31 | Exelixis Inc | Inhibitorji MEK in postopki za njihovo uporabo |
| KR101101443B1 (ko) * | 2006-08-14 | 2012-01-03 | 시코르, 인크. | 페메트렉세드의 중간체의 제조 방법 |
| TWI499420B (zh) | 2006-12-07 | 2015-09-11 | Hoffmann La Roche | 肌醇磷脂3-激酶抑制劑化合物及使用方法 |
| CA2699202C (en) * | 2007-09-12 | 2016-09-27 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| US8354528B2 (en) | 2007-10-25 | 2013-01-15 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| US9042479B2 (en) | 2008-10-16 | 2015-05-26 | Qualcomm Incorporated | Method and apparatus for avoiding interference between coexisting wireless systems |
| AU2010224125B2 (en) | 2009-03-12 | 2015-05-14 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents for the treatment of hematopoietic malignancies |
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2012
- 2012-06-01 CA CA2835760A patent/CA2835760A1/en not_active Abandoned
- 2012-06-01 CN CN201280027267.9A patent/CN103582479A/zh active Pending
- 2012-06-01 JP JP2014513200A patent/JP2014515390A/ja active Pending
- 2012-06-01 BR BR112013030991A patent/BR112013030991A2/pt not_active IP Right Cessation
- 2012-06-01 US US13/486,141 patent/US20120308562A1/en not_active Abandoned
- 2012-06-01 KR KR1020137031910A patent/KR20140040728A/ko not_active Withdrawn
- 2012-06-01 MX MX2013014151A patent/MX2013014151A/es unknown
- 2012-06-01 EP EP12726085.9A patent/EP2714046A1/en not_active Withdrawn
- 2012-06-01 RU RU2013154355/15A patent/RU2013154355A/ru not_active Application Discontinuation
- 2012-06-01 AR ARP120101945A patent/AR086647A1/es unknown
- 2012-06-01 WO PCT/EP2012/060341 patent/WO2012164060A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JP2014515390A (ja) | 2014-06-30 |
| EP2714046A1 (en) | 2014-04-09 |
| MX2013014151A (es) | 2014-01-23 |
| CN103582479A (zh) | 2014-02-12 |
| US20120308562A1 (en) | 2012-12-06 |
| AR086647A1 (es) | 2014-01-15 |
| BR112013030991A2 (pt) | 2016-11-29 |
| WO2012164060A1 (en) | 2012-12-06 |
| KR20140040728A (ko) | 2014-04-03 |
| CA2835760A1 (en) | 2012-12-06 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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