CN102725291B - 作为沉默调节蛋白调节剂的双环吡啶和相关的类似物 - Google Patents
作为沉默调节蛋白调节剂的双环吡啶和相关的类似物 Download PDFInfo
- Publication number
- CN102725291B CN102725291B CN201080060180.2A CN201080060180A CN102725291B CN 102725291 B CN102725291 B CN 102725291B CN 201080060180 A CN201080060180 A CN 201080060180A CN 102725291 B CN102725291 B CN 102725291B
- Authority
- CN
- China
- Prior art keywords
- alkyl
- fluorine
- compound
- substituted
- sirtuin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 C*(C)c1ccccn1 Chemical compound C*(C)c1ccccn1 0.000 description 31
- ZICRALLMHKILDG-UHFFFAOYSA-N CC(C)c1ccn[nH]1 Chemical compound CC(C)c1ccn[nH]1 ZICRALLMHKILDG-UHFFFAOYSA-N 0.000 description 2
- OTGDCHNSXQUISE-UHFFFAOYSA-N Brc1ccc2OCCNc2n1 Chemical compound Brc1ccc2OCCNc2n1 OTGDCHNSXQUISE-UHFFFAOYSA-N 0.000 description 1
- OAXRKEIAAXLLLO-MFGFFKQHSA-N C=C(c1cc([IH+])ccc1)/N=C(\C(OC1)=C(N)N[C@H]1O)/[ClH+] Chemical compound C=C(c1cc([IH+])ccc1)/N=C(\C(OC1)=C(N)N[C@H]1O)/[ClH+] OAXRKEIAAXLLLO-MFGFFKQHSA-N 0.000 description 1
- NGCGYTPSRNKABQ-QYEKGNEQSA-N CC(C)/C(/C)=C/C=N\NC Chemical compound CC(C)/C(/C)=C/C=N\NC NGCGYTPSRNKABQ-QYEKGNEQSA-N 0.000 description 1
- WVMBISZHWMJNNM-UHFFFAOYSA-N CC(C)c1c[nH]nc1 Chemical compound CC(C)c1c[nH]nc1 WVMBISZHWMJNNM-UHFFFAOYSA-N 0.000 description 1
- GABKDWUBEVLXEW-UHFFFAOYSA-N CC1(CN(C)C2=CC=CNN2)COC1 Chemical compound CC1(CN(C)C2=CC=CNN2)COC1 GABKDWUBEVLXEW-UHFFFAOYSA-N 0.000 description 1
- PXRDDNBENPRBAG-UHFFFAOYSA-N CC1=[I]C=NC(N2CC[U+]CC2)=C1 Chemical compound CC1=[I]C=NC(N2CC[U+]CC2)=C1 PXRDDNBENPRBAG-UHFFFAOYSA-N 0.000 description 1
- FNUWEHVZWXPRIV-UHFFFAOYSA-N CC1NNC11COC1 Chemical compound CC1NNC11COC1 FNUWEHVZWXPRIV-UHFFFAOYSA-N 0.000 description 1
- OLKDHWGNKXDYOQ-UHFFFAOYSA-N CCOC/[U]=C/CNC1=NC(C2=CCCC(C(F)(F)F)=C2)=CCC1[N+]([O-])=O Chemical compound CCOC/[U]=C/CNC1=NC(C2=CCCC(C(F)(F)F)=C2)=CCC1[N+]([O-])=O OLKDHWGNKXDYOQ-UHFFFAOYSA-N 0.000 description 1
- HLBPEOXJBLQZRH-VOMCLLRMSA-N CC[IH]1(CC(C)[C@H](C)C1)C1=CC=CC2C(Br)=C12 Chemical compound CC[IH]1(CC(C)[C@H](C)C1)C1=CC=CC2C(Br)=C12 HLBPEOXJBLQZRH-VOMCLLRMSA-N 0.000 description 1
- HHFJHCXBGHXHLU-UHFFFAOYSA-N Cc(cc1)cc2c1NCCO2 Chemical compound Cc(cc1)cc2c1NCCO2 HHFJHCXBGHXHLU-UHFFFAOYSA-N 0.000 description 1
- GHPODDMCSOYWNE-UHFFFAOYSA-N Cc(cc1)cc2c1OCO2 Chemical compound Cc(cc1)cc2c1OCO2 GHPODDMCSOYWNE-UHFFFAOYSA-N 0.000 description 1
- LRSFUCPDCKILCL-UHFFFAOYSA-N Cc1cccc(N(CC2)CC2F)c1 Chemical compound Cc1cccc(N(CC2)CC2F)c1 LRSFUCPDCKILCL-UHFFFAOYSA-N 0.000 description 1
- XPNMCOGUXSYLBP-UHFFFAOYSA-N Fc1cccc(C([Ar]=C2Cl)=CC[IH]C3=C2OCCN3)c1 Chemical compound Fc1cccc(C([Ar]=C2Cl)=CC[IH]C3=C2OCCN3)c1 XPNMCOGUXSYLBP-UHFFFAOYSA-N 0.000 description 1
- CJTDPUUGKHXTHT-UHFFFAOYSA-N O=C(Nc1ccncc1)N1c(nc(cc2)Br)c2OCC1 Chemical compound O=C(Nc1ccncc1)N1c(nc(cc2)Br)c2OCC1 CJTDPUUGKHXTHT-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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- A—HUMAN NECESSITIES
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25626909P | 2009-10-29 | 2009-10-29 | |
| US61/256,269 | 2009-10-29 | ||
| PCT/US2010/054880 WO2011059839A1 (en) | 2009-10-29 | 2010-10-29 | Bicyclic pyridines and analogs as sirtuin modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102725291A CN102725291A (zh) | 2012-10-10 |
| CN102725291B true CN102725291B (zh) | 2016-12-21 |
Family
ID=43991957
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080060180.2A Expired - Fee Related CN102725291B (zh) | 2009-10-29 | 2010-10-29 | 作为沉默调节蛋白调节剂的双环吡啶和相关的类似物 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9556201B2 (enExample) |
| EP (1) | EP2493888B1 (enExample) |
| JP (1) | JP2013509442A (enExample) |
| KR (1) | KR20120092141A (enExample) |
| CN (1) | CN102725291B (enExample) |
| AU (1) | AU2010319842A1 (enExample) |
| BR (1) | BR112012010010A2 (enExample) |
| CA (1) | CA2779303A1 (enExample) |
| ES (1) | ES2574927T3 (enExample) |
| IL (1) | IL219372A0 (enExample) |
| IN (1) | IN2012DN03799A (enExample) |
| MX (1) | MX2012004995A (enExample) |
| RU (1) | RU2550821C2 (enExample) |
| WO (1) | WO2011059839A1 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0820669A2 (pt) | 2007-12-10 | 2020-08-04 | Novartis Ag | compostos orgânicos |
| CA2738794C (en) | 2008-09-29 | 2016-01-05 | Sirtris Pharmaceuticals, Inc. | Chromenone analogs as sirtuin modulators |
| EA029892B1 (ru) | 2012-04-25 | 2018-05-31 | Такеда Фармасьютикал Компани Лимитед | Азотсодержащее гетероциклическое соединение |
| EP2847198B1 (en) | 2012-05-08 | 2016-12-14 | Lycera Corporation | Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of ror-gamma and the treatment of disease |
| RU2014149136A (ru) | 2012-05-08 | 2016-07-10 | Мерк Шарп И Доум Корп. | ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ |
| JP6205356B2 (ja) | 2012-07-13 | 2017-09-27 | 武田薬品工業株式会社 | 複素環化合物 |
| EP2890698B1 (en) * | 2012-08-30 | 2017-03-01 | F. Hoffmann-La Roche AG | Dioxino- and oxazin-[2,3-d]pyrimidine pi3k inhibitor compounds and methods of use |
| CN102977117A (zh) * | 2012-11-26 | 2013-03-20 | 盛世泰科生物医药技术(苏州)有限公司 | 一种6-溴-2,2-二甲基-2h-吡啶并[3,2-b][1,4]恶嗪-3(4h)-酮的合成方法 |
| GEP201606554B (en) * | 2012-12-26 | 2016-10-10 | Takeda Pharmaceuticals Co | Nitrogenated heterocyclic compound |
| EP2975031A4 (en) | 2013-03-14 | 2017-04-19 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| JP6376707B2 (ja) | 2013-05-13 | 2018-08-22 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | サーチュイン調節剤としての置換架橋尿素類似体 |
| WO2016081692A2 (en) * | 2014-11-19 | 2016-05-26 | Glaxosmithkline Llc | Substituted bridged urea analogs as sirtuin modulators |
| JP6411342B2 (ja) | 2013-07-03 | 2018-10-24 | 武田薬品工業株式会社 | アミド化合物 |
| EP3018126A4 (en) | 2013-07-03 | 2016-12-07 | Takeda Pharmaceuticals Co | HETEROCYCLIC CONNECTION |
| DK3929196T3 (da) | 2013-09-24 | 2023-09-25 | Fujifilm Corp | Farmaceutisk sammensætning af en nitrogenholdig forbindelse eller salt deraf, eller metalkompleks deraf |
| US10172915B2 (en) | 2013-10-20 | 2019-01-08 | Duke University | Methods and compositions for activation of sirtuins with Annexin A1 peptides |
| CN105683188B (zh) | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| WO2015095788A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| WO2015095792A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease |
| JP6510539B2 (ja) | 2014-01-09 | 2019-05-08 | ザ ジェイ． デヴィッド グラッドストーン インスティテューツ， ア テスタメンタリー トラスト エスタブリッシュド アンダー ザ ウィル オブ ジェイ． デヴィッド グラッドストーン | 置換ベンゾオキサジン及び関連化合物 |
| AU2015222917A1 (en) | 2014-02-27 | 2016-09-15 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods |
| JP2017114764A (ja) * | 2014-04-25 | 2017-06-29 | 武田薬品工業株式会社 | 片頭痛治療剤 |
| EP3140291A4 (en) | 2014-05-05 | 2018-01-10 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease |
| WO2015171558A2 (en) | 2014-05-05 | 2015-11-12 | Lycera Corporation | BENZENESULFONAMIDO AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORγ AND THE TREATEMENT OF DISEASE |
| US10316054B2 (en) | 2014-06-02 | 2019-06-11 | Glaxosmithkline Intellectual Property (No. 2) Limited | Preparation and use of crystalline beta-D-nicotinamide riboside |
| RU2016149767A (ru) | 2014-06-06 | 2018-07-16 | Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед | Аналоги никотинамидрибозида и фармацевтические композиции и их применение |
| ES2756748T3 (es) | 2014-10-03 | 2020-04-27 | Novartis Ag | Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 |
| CN107207520A (zh) * | 2014-11-19 | 2017-09-26 | 葛兰素史密斯克莱知识产权（第2 号）有限公司 | 作为沉默调节蛋白调节剂的取代的桥环脲类似物 |
| CA2975997A1 (en) | 2015-02-11 | 2016-08-18 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as rorgammat inhibitors and uses thereof |
| US9802917B2 (en) | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
| WO2016179343A1 (en) | 2015-05-05 | 2016-11-10 | Lycera Corporation | DIHYDRO-2H-BENZO[b][1,4]OXAZINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORy AND THE TREATMENT OF DISEASE |
| CN107980042B (zh) | 2015-06-11 | 2021-10-08 | 莱斯拉公司 | 用作RORγ激动剂和用于治疗疾病的芳基二氢-2H-苯并[b][1,4]噁嗪磺酰胺和相关化合物 |
| JP2018531958A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ＲＯＲγＴ阻害薬としてのヘテロアリール置換安息香酸及びその使用 |
| EP3368516B1 (en) | 2015-10-27 | 2020-07-15 | Merck Sharp & Dohme Corp. | SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| US10287272B2 (en) | 2015-10-27 | 2019-05-14 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as RORgammaT inhibitors and uses thereof |
| US9815850B2 (en) | 2016-02-05 | 2017-11-14 | Denali Therapeutics Inc. | Compounds, compositions and methods |
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| US9556201B2 (en) | 2017-01-31 |
| RU2012122065A (ru) | 2013-12-10 |
| US20120252780A1 (en) | 2012-10-04 |
| EP2493888A1 (en) | 2012-09-05 |
| EP2493888A4 (en) | 2013-05-01 |
| EP2493888B1 (en) | 2016-04-06 |
| WO2011059839A1 (en) | 2011-05-19 |
| BR112012010010A2 (pt) | 2018-03-20 |
| CN102725291A (zh) | 2012-10-10 |
| KR20120092141A (ko) | 2012-08-20 |
| ES2574927T3 (es) | 2016-06-23 |
| IL219372A0 (en) | 2012-06-28 |
| CA2779303A1 (en) | 2011-05-19 |
| RU2550821C2 (ru) | 2015-05-20 |
| MX2012004995A (es) | 2012-10-03 |
| AU2010319842A1 (en) | 2012-05-17 |
| JP2013509442A (ja) | 2013-03-14 |
| IN2012DN03799A (enExample) | 2015-08-28 |
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