TW201141846A - Dimeric IAP inhibitors - Google Patents
Dimeric IAP inhibitors Download PDFInfo
- Publication number
- TW201141846A TW201141846A TW100106289A TW100106289A TW201141846A TW 201141846 A TW201141846 A TW 201141846A TW 100106289 A TW100106289 A TW 100106289A TW 100106289 A TW100106289 A TW 100106289A TW 201141846 A TW201141846 A TW 201141846A
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- Taiwan
- Prior art keywords
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- alkyl
- phenyl
- fluoro
- independently selected
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- 239000004094 surface-active agent Substances 0.000 description 1
- 229940034785 sutent Drugs 0.000 description 1
- 229940120982 tarceva Drugs 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229940069905 tasigna Drugs 0.000 description 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
- 229940063683 taxotere Drugs 0.000 description 1
- XSOKHXFFCGXDJZ-UHFFFAOYSA-N telluride(2-) Chemical compound [Te-2] XSOKHXFFCGXDJZ-UHFFFAOYSA-N 0.000 description 1
- 229940061353 temodar Drugs 0.000 description 1
- 229960004964 temozolomide Drugs 0.000 description 1
- 229960001278 teniposide Drugs 0.000 description 1
- 125000005888 tetrahydroindolyl group Chemical group 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- XDLNRRRJZOJTRW-UHFFFAOYSA-N thiohypochlorous acid Chemical compound ClS XDLNRRRJZOJTRW-UHFFFAOYSA-N 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 229960001196 thiotepa Drugs 0.000 description 1
- RLUJQBLWUQZMDG-UHFFFAOYSA-N toluene;hydrochloride Chemical compound Cl.CC1=CC=CC=C1 RLUJQBLWUQZMDG-UHFFFAOYSA-N 0.000 description 1
- 229940035307 toposar Drugs 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 229940066958 treanda Drugs 0.000 description 1
- 229950007217 tremelimumab Drugs 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 150000003648 triterpenes Chemical class 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 229910052721 tungsten Inorganic materials 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
- 229950008737 vadimezan Drugs 0.000 description 1
- XGOYIMQSIKSOBS-UHFFFAOYSA-N vadimezan Chemical compound C1=CC=C2C(=O)C3=CC=C(C)C(C)=C3OC2=C1CC(O)=O XGOYIMQSIKSOBS-UHFFFAOYSA-N 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 229940099039 velcade Drugs 0.000 description 1
- KDQAABAKXDWYSZ-PNYVAJAMSA-N vinblastine sulfate Chemical compound OS(O)(=O)=O.C([C@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 KDQAABAKXDWYSZ-PNYVAJAMSA-N 0.000 description 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 1
- 229960002110 vincristine sulfate Drugs 0.000 description 1
- GBABOYUKABKIAF-IELIFDKJSA-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-IELIFDKJSA-N 0.000 description 1
- 229960002066 vinorelbine Drugs 0.000 description 1
- CILBMBUYJCWATM-PYGJLNRPSA-N vinorelbine ditartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.OC(=O)[C@H](O)[C@@H](O)C(O)=O.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 CILBMBUYJCWATM-PYGJLNRPSA-N 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
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- 229940069559 votrient Drugs 0.000 description 1
- 229950003511 votumumab Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229940053867 xeloda Drugs 0.000 description 1
- 229940053890 zanosar Drugs 0.000 description 1
- 229940061261 zolinza Drugs 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30811410P | 2010-02-25 | 2010-02-25 | |
| US33392710P | 2010-05-12 | 2010-05-12 | |
| US38841010P | 2010-09-30 | 2010-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201141846A true TW201141846A (en) | 2011-12-01 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW100106289A TW201141846A (en) | 2010-02-25 | 2011-02-24 | Dimeric IAP inhibitors |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8445440B2 (enExample) |
| EP (1) | EP2539333A1 (enExample) |
| JP (1) | JP2013520466A (enExample) |
| KR (1) | KR20130010894A (enExample) |
| CN (1) | CN102834389A (enExample) |
| AR (1) | AR080253A1 (enExample) |
| BR (1) | BR112012021291A2 (enExample) |
| CA (1) | CA2790302A1 (enExample) |
| EA (1) | EA201201177A1 (enExample) |
| MX (1) | MX2012009894A (enExample) |
| TW (1) | TW201141846A (enExample) |
| UY (1) | UY33236A (enExample) |
| WO (1) | WO2011104266A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100317593A1 (en) * | 2009-06-12 | 2010-12-16 | Astrazeneca Ab | 2,3-dihydro-1h-indene compounds |
| UY33794A (es) * | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| US20140243276A1 (en) | 2011-09-30 | 2014-08-28 | Tetralogic Pharmaceuticals Corporation | Smac mimetic (birinapant) for use in the treatment of proliferative diseases (cancer) |
| US9453048B2 (en) | 2012-08-09 | 2016-09-27 | Bristol-Myers Squibb Company | IAP antagonists |
| EP2917218B1 (en) * | 2012-11-09 | 2017-01-04 | Ensemble Therapeutics Corporation | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| ES2982449T3 (es) | 2013-06-25 | 2024-10-16 | Walter & Eliza Hall Inst Medical Res | Miméticos Smac para su uso en el tratamiento de una infección persistente por VIH |
| WO2016079527A1 (en) | 2014-11-19 | 2016-05-26 | Tetralogic Birinapant Uk Ltd | Combination therapy |
| WO2016097773A1 (en) | 2014-12-19 | 2016-06-23 | Children's Cancer Institute | Therapeutic iap antagonists for treating proliferative disorders |
| CN109705191B (zh) * | 2017-10-25 | 2022-04-29 | 广东东阳光药业有限公司 | Iap抑制剂及其在药物中的应用 |
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| JPS6041077B2 (ja) | 1976-09-06 | 1985-09-13 | 喜徳 喜谷 | 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体 |
| US5281620A (en) | 1986-12-23 | 1994-01-25 | Cancer Research Campaign Technology Limited | Compounds having antitumor and antibacterial properties |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| GB0018891D0 (en) | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
| JP2002037626A (ja) | 2000-07-27 | 2002-02-06 | Internatl Superconductivity Technology Center | ビスマス系高温超電導体の製造方法。 |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| DE60334247D1 (de) | 2002-11-27 | 2010-10-28 | Irm Llc | Verfahren und zusammensetzungen zur apoptoseinduktion in krebszellen |
| CA2514733A1 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| JP2007520522A (ja) | 2004-02-05 | 2007-07-26 | ノバルティス アクチエンゲゼルシャフト | (a)DNAトポイソメラーゼ阻害剤および(b)IAP阻害剤の組み合わせ剤 |
| AU2005218555B2 (en) * | 2004-03-01 | 2008-01-03 | Board Of Regents, The University Of Texas System | Dimeric small molecule potentiators of apoptosis |
| JP5230865B2 (ja) | 2004-07-15 | 2013-07-10 | テトラロジック ファーマシューティカルズ コーポレーション | Iap結合性化合物 |
| DK1851200T3 (da) | 2005-02-25 | 2014-04-14 | Tetralogic Pharm Corp | Dimere iap-inhibitorer |
| CA2607940C (en) | 2005-05-18 | 2009-12-15 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| AU2006279929A1 (en) | 2005-08-09 | 2007-02-22 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| WO2007048224A1 (en) * | 2005-10-25 | 2007-05-03 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| CN101340947B (zh) * | 2005-12-20 | 2012-09-05 | 诺瓦提斯公司 | Iap-抑制剂和紫杉烷7的组合 |
| TWI543988B (zh) | 2006-03-16 | 2016-08-01 | 科學製藥股份有限公司 | 結合於細胞凋亡抑制蛋白(iap)之桿狀病毒iap重複序列(bir)區域之化合物 |
| BRPI0708942A2 (pt) | 2006-03-21 | 2011-06-14 | Joyant Pharmaceuticals Inc | composto promotor de apoptose, uso e mÉtodo de produÇço do mesmo e composiÇço farmacÊutica |
| US8202902B2 (en) * | 2006-05-05 | 2012-06-19 | The Regents Of The University Of Michigan | Bivalent SMAC mimetics and the uses thereof |
| MY159563A (en) * | 2006-05-16 | 2017-01-13 | Pharmascience Inc | Iap bir domain binding compounds |
| WO2008014238A2 (en) | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| JP5452223B2 (ja) * | 2006-07-24 | 2014-03-26 | テトラロジック ファーマシューティカルズ コーポレーション | Iap阻害剤 |
| US20100113326A1 (en) | 2006-07-24 | 2010-05-06 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| US20100144650A1 (en) | 2006-07-24 | 2010-06-10 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
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| EP2049563B1 (en) | 2006-07-24 | 2014-03-12 | Tetralogic Pharmaceuticals Corporation | Dimeric iap antagonists |
| PE20110224A1 (es) * | 2006-08-02 | 2011-04-05 | Novartis Ag | PROCEDIMIENTO PARA LA SINTESIS DE UN PEPTIDOMIMETICO DE Smac INHIBIDOR DE IAP, Y COMPUESTOS INTERMEDIARIOS PARA LA SINTESIS DEL MISMO |
| KR20090082221A (ko) * | 2006-10-19 | 2009-07-29 | 노파르티스 아게 | 유기 화합물 |
| MX2009005551A (es) | 2006-11-28 | 2009-06-08 | Novartis Ag | Uso de inhibidores de iap para el tratamiento de leucemia mieloide aguda. |
| WO2008066854A2 (en) | 2006-11-28 | 2008-06-05 | Novartis Ag | Methods and compositions for inducing apoptosis in cancer cells |
| KR101149449B1 (ko) | 2007-03-20 | 2012-05-25 | 삼성전자주식회사 | 오디오 신호의 인코딩 방법 및 장치, 그리고 오디오 신호의디코딩 방법 및 장치 |
| EP2079309B1 (en) * | 2007-04-12 | 2015-11-11 | Joyant Pharmaceuticals Inc | SMAC MIMEE DIMERS AND TRIMERS USEFUL AS ANTICANCER AGENTS |
| AR066348A1 (es) | 2007-04-30 | 2009-08-12 | Genentech Inc | Inhibidores de las iap |
| JP2010528587A (ja) | 2007-05-07 | 2010-08-26 | テトラロジック ファーマシューティカルズ コーポレーション | アポトーシス阻害タンパク質のアンタゴニストに対する感受性のバイオマーカーとしてTNFα遺伝子の発現を用いる方法 |
| TWI471134B (zh) | 2007-09-12 | 2015-02-01 | Genentech Inc | 肌醇磷脂3-激酶抑制劑化合物及化療劑之組合及使用方法 |
| CA2701292C (en) | 2007-10-25 | 2015-03-24 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| EP2058312A1 (en) | 2007-11-09 | 2009-05-13 | Universita' degli Studi di Milano | SMAC mimetic compounds as apoptosis inducers |
| PL2240506T3 (pl) | 2008-01-11 | 2013-05-31 | Genentech Inc | Inhibitory IAP |
| BRPI0906785A2 (pt) | 2008-01-24 | 2015-07-14 | Tetralogic Pharm Corp | Composto, composição farmacêutica, e, métodos para induzir a apoptose em uma célula, para tratar câncer e uma doença autoimune |
| WO2009136290A1 (en) | 2008-05-05 | 2009-11-12 | Aegera Therapeutics, Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| EP2310402A1 (en) | 2008-06-27 | 2011-04-20 | Aegera Therapeutics Inc. | Bridged secondary amines and use thereof as iap bir domain binding compounds |
| NZ590550A (en) | 2008-08-02 | 2013-05-31 | Genentech Inc | Inhibitors of Apoptosis (IAP) for treating cancer |
| WO2010015090A1 (en) | 2008-08-07 | 2010-02-11 | Aegera Therapeutics Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
| AU2009293403A1 (en) | 2008-09-17 | 2010-03-25 | Tetralogic Pharmaceuticals Corp. | IAP inhibitors |
| JP2012502994A (ja) | 2008-09-22 | 2012-02-02 | アムジエン・インコーポレーテツド | 治療方法 |
| US8283372B2 (en) * | 2009-07-02 | 2012-10-09 | Tetralogic Pharmaceuticals Corp. | 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic |
-
2011
- 2011-02-21 UY UY0001033236A patent/UY33236A/es not_active Application Discontinuation
- 2011-02-23 CA CA2790302A patent/CA2790302A1/en not_active Abandoned
- 2011-02-23 US US13/033,463 patent/US8445440B2/en not_active Expired - Fee Related
- 2011-02-23 EP EP11705532A patent/EP2539333A1/en not_active Withdrawn
- 2011-02-23 BR BR112012021291A patent/BR112012021291A2/pt not_active IP Right Cessation
- 2011-02-23 CN CN2011800177078A patent/CN102834389A/zh active Pending
- 2011-02-23 KR KR1020127024875A patent/KR20130010894A/ko not_active Withdrawn
- 2011-02-23 EA EA201201177A patent/EA201201177A1/ru unknown
- 2011-02-23 MX MX2012009894A patent/MX2012009894A/es active IP Right Grant
- 2011-02-23 JP JP2012554332A patent/JP2013520466A/ja active Pending
- 2011-02-23 AR ARP110100547A patent/AR080253A1/es unknown
- 2011-02-23 WO PCT/EP2011/052662 patent/WO2011104266A1/en not_active Ceased
- 2011-02-24 TW TW100106289A patent/TW201141846A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UY33236A (es) | 2011-09-30 |
| KR20130010894A (ko) | 2013-01-29 |
| US20110206690A1 (en) | 2011-08-25 |
| BR112012021291A2 (pt) | 2016-10-25 |
| US8445440B2 (en) | 2013-05-21 |
| MX2012009894A (es) | 2012-09-12 |
| WO2011104266A1 (en) | 2011-09-01 |
| AR080253A1 (es) | 2012-03-21 |
| JP2013520466A (ja) | 2013-06-06 |
| AU2011219862A1 (en) | 2012-09-06 |
| CA2790302A1 (en) | 2011-09-01 |
| EA201201177A1 (ru) | 2013-04-30 |
| EP2539333A1 (en) | 2013-01-02 |
| CN102834389A (zh) | 2012-12-19 |
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