EA023824B1 - ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) - Google Patents
ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) Download PDFInfo
- Publication number
- EA023824B1 EA023824B1 EA201391296A EA201391296A EA023824B1 EA 023824 B1 EA023824 B1 EA 023824B1 EA 201391296 A EA201391296 A EA 201391296A EA 201391296 A EA201391296 A EA 201391296A EA 023824 B1 EA023824 B1 EA 023824B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- group
- dementia
- alkyl
- compound according
- heteroaryl
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract description 5
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract description 5
- 239000003112 inhibitor Substances 0.000 title abstract 2
- MBVCQKKUMUXAMH-UHFFFAOYSA-N 3,4-dihydropyrrolo[1,2-a]pyrazin-1-amine Chemical class NC1=NCCN2C=CC=C12 MBVCQKKUMUXAMH-UHFFFAOYSA-N 0.000 title description 2
- 206010012289 Dementia Diseases 0.000 claims abstract description 19
- 150000001875 compounds Chemical class 0.000 claims abstract description 14
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 5
- 201000010374 Down Syndrome Diseases 0.000 claims abstract description 4
- 208000018737 Parkinson disease Diseases 0.000 claims abstract description 4
- 208000010877 cognitive disease Diseases 0.000 claims abstract description 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims abstract description 4
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims abstract description 3
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims abstract description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 3
- 208000035475 disorder Diseases 0.000 claims abstract description 3
- 230000002265 prevention Effects 0.000 claims abstract description 3
- 230000008033 biological extinction Effects 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 6
- -1 chloro, fluoro, cyano, methyl Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000013256 coordination polymer Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract description 6
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract description 4
- 239000000203 mixture Substances 0.000 abstract description 4
- 108090000790 Enzymes Proteins 0.000 abstract description 2
- 102000004190 Enzymes Human genes 0.000 abstract description 2
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 abstract description 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 206010067889 Dementia with Lewy bodies Diseases 0.000 abstract 1
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 239000002439 beta secretase inhibitor Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11157418 | 2011-03-09 | ||
| PCT/EP2012/053863 WO2012120023A1 (en) | 2011-03-09 | 2012-03-07 | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201391296A1 EA201391296A1 (ru) | 2014-01-30 |
| EA023824B1 true EA023824B1 (ru) | 2016-07-29 |
Family
ID=43833325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391296A EA023824B1 (ru) | 2011-03-09 | 2012-03-07 | ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9845326B2 (enExample) |
| EP (1) | EP2683721B1 (enExample) |
| JP (1) | JP5853035B2 (enExample) |
| KR (1) | KR102012675B1 (enExample) |
| CN (1) | CN103415521B (enExample) |
| AU (1) | AU2012224632B2 (enExample) |
| BR (1) | BR112013022917A2 (enExample) |
| CA (1) | CA2825620C (enExample) |
| CL (1) | CL2013002511A1 (enExample) |
| CO (1) | CO6751283A2 (enExample) |
| EA (1) | EA023824B1 (enExample) |
| ES (1) | ES2534973T3 (enExample) |
| IL (1) | IL228239A (enExample) |
| MX (1) | MX340031B (enExample) |
| MY (1) | MY163346A (enExample) |
| PH (1) | PH12013501805A1 (enExample) |
| SG (1) | SG193342A1 (enExample) |
| UA (1) | UA109687C2 (enExample) |
| WO (1) | WO2012120023A1 (enExample) |
| ZA (1) | ZA201306719B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害活性を有する２－アミノピリミジン－４－オンおよび２－アミノピリジン誘導体 |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| AR081587A1 (es) | 2010-06-09 | 2012-10-03 | Janssen Pharmaceutica Nv | DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE) |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| ES2648143T3 (es) | 2010-12-22 | 2017-12-28 | Janssen Pharmaceutica Nv | Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE) |
| US9346811B2 (en) | 2011-03-01 | 2016-05-24 | Janssen Pharmaceutica Nv | 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
| JP5853035B2 (ja) * | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体 |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| EP3008067B1 (en) | 2013-06-12 | 2017-03-29 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| KR102243134B1 (ko) * | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체 |
| BR112015030597A2 (pt) * | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace) |
| RU2572076C2 (ru) * | 2014-03-26 | 2015-12-27 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | 1-арилпирроло[1,2-a]пиразин-3-карбоксамиды с нейропсихотропной активностью |
| JP2017538753A (ja) | 2014-12-18 | 2017-12-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ２，３，４，５−テトラヒドロピリジン−６−アミンおよび３，４−ジヒドロ−２Ｈ−ピロール−５−アミンの化合物のβセクレターゼ阻害剤 |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
| WO2022169985A1 (en) | 2021-02-03 | 2022-08-11 | Eikonizo Therapeutics, Inc. | Hdac6 inhibitors and uses thereof |
| AU2023250964A1 (en) | 2022-04-08 | 2024-11-07 | Eikonizo Therapeutics, Inc. | Oxadiazole hdac6 inhibitors and uses thereof |
| CN117471007B (zh) * | 2023-10-31 | 2024-08-09 | 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） | 一种血浆β-淀粉样蛋白检测方法 |
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| WO2009022961A1 (en) * | 2007-05-15 | 2009-02-19 | Astrazeneca Ab | Pyrrolopyridine derivatives and their use as bace inhibitors |
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| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
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| JP2012147763A (ja) | 2011-01-17 | 2012-08-09 | Toshitaka Kobayashi | 乾物穿孔具 |
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| JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体 |
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| CN104870000A (zh) | 2012-12-20 | 2015-08-26 | 默沙东公司 | 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途 |
| EP3008067B1 (en) | 2013-06-12 | 2017-03-29 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| KR102243134B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체 |
| BR112015030597A2 (pt) | 2013-06-12 | 2017-07-25 | Janssen Pharmaceutica Nv | derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (bace) |
| JP2017538753A (ja) | 2014-12-18 | 2017-12-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ２，３，４，５−テトラヒドロピリジン−６−アミンおよび３，４−ジヒドロ−２Ｈ−ピロール−５−アミンの化合物のβセクレターゼ阻害剤 |
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2012
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- 2012-03-07 KR KR1020137022396A patent/KR102012675B1/ko not_active Expired - Fee Related
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- 2012-03-07 EA EA201391296A patent/EA023824B1/ru not_active IP Right Cessation
- 2012-03-07 AU AU2012224632A patent/AU2012224632B2/en not_active Ceased
- 2012-03-07 CN CN201280012485.5A patent/CN103415521B/zh not_active Expired - Fee Related
- 2012-03-07 ES ES12707319.5T patent/ES2534973T3/es active Active
- 2012-03-07 PH PH1/2013/501805A patent/PH12013501805A1/en unknown
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- 2012-03-07 BR BR112013022917A patent/BR112013022917A2/pt not_active Application Discontinuation
- 2012-03-07 WO PCT/EP2012/053863 patent/WO2012120023A1/en not_active Ceased
- 2012-03-07 EP EP12707319.5A patent/EP2683721B1/en not_active Not-in-force
- 2012-03-07 SG SG2013067210A patent/SG193342A1/en unknown
- 2012-07-03 UA UAA201308782A patent/UA109687C2/ru unknown
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| WO2006076284A2 (en) * | 2005-01-14 | 2006-07-20 | Wyeth | AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE |
| WO2009022961A1 (en) * | 2007-05-15 | 2009-02-19 | Astrazeneca Ab | Pyrrolopyridine derivatives and their use as bace inhibitors |
Also Published As
| Publication number | Publication date |
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| AU2012224632B2 (en) | 2016-06-16 |
| WO2012120023A1 (en) | 2012-09-13 |
| IL228239A0 (en) | 2013-11-25 |
| HK1189223A1 (zh) | 2014-05-30 |
| CL2013002511A1 (es) | 2014-01-24 |
| EP2683721B1 (en) | 2015-01-28 |
| MY163346A (en) | 2017-09-15 |
| CN103415521B (zh) | 2016-01-06 |
| PH12013501805A1 (en) | 2013-11-18 |
| CN103415521A (zh) | 2013-11-27 |
| UA109687C2 (xx) | 2015-09-25 |
| CO6751283A2 (es) | 2013-09-16 |
| MX2013010280A (es) | 2013-10-01 |
| US20130345228A1 (en) | 2013-12-26 |
| IL228239A (en) | 2016-06-30 |
| SG193342A1 (en) | 2013-10-30 |
| KR102012675B1 (ko) | 2019-08-21 |
| AU2012224632A1 (en) | 2013-08-01 |
| CA2825620C (en) | 2019-04-23 |
| JP5853035B2 (ja) | 2016-02-09 |
| ES2534973T3 (es) | 2015-04-30 |
| EA201391296A1 (ru) | 2014-01-30 |
| EP2683721A1 (en) | 2014-01-15 |
| NZ615720A (en) | 2014-08-29 |
| ZA201306719B (en) | 2015-04-29 |
| BR112013022917A2 (pt) | 2016-12-06 |
| JP2014507455A (ja) | 2014-03-27 |
| CA2825620A1 (en) | 2012-09-13 |
| US9845326B2 (en) | 2017-12-19 |
| KR20140019332A (ko) | 2014-02-14 |
| MX340031B (es) | 2016-06-21 |
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