CN103492372B - 调节雄激素受体的甲酰胺类化合物 - Google Patents
调节雄激素受体的甲酰胺类化合物 Download PDFInfo
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- CN103492372B CN103492372B CN201280019463.1A CN201280019463A CN103492372B CN 103492372 B CN103492372 B CN 103492372B CN 201280019463 A CN201280019463 A CN 201280019463A CN 103492372 B CN103492372 B CN 103492372B
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- pyrazol
- chloro
- carboxamide
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- imidazole
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- 0 Cc1cc(*)n[n]1 Chemical compound Cc1cc(*)n[n]1 0.000 description 9
- LOGLLGYRXMGXFN-UHFFFAOYSA-N Cc([nH]1)c(C)nc1[RnH] Chemical compound Cc([nH]1)c(C)nc1[RnH] LOGLLGYRXMGXFN-UHFFFAOYSA-N 0.000 description 1
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
- C07D417/14—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 three or more hetero rings
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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
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN570KO2011 | 2011-04-21 | ||
| IN570/KOL/2011 | 2011-04-21 | ||
| PCT/FI2012/000022 WO2012143599A1 (en) | 2011-04-21 | 2012-04-20 | Androgen receptor modulating carboxamides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103492372A CN103492372A (zh) | 2014-01-01 |
| CN103492372B true CN103492372B (zh) | 2015-09-30 |
Family
ID=46125469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280019463.1A Active CN103492372B (zh) | 2011-04-21 | 2012-04-20 | 调节雄激素受体的甲酰胺类化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8921378B2 (https=) |
| EP (1) | EP2699561B1 (https=) |
| JP (1) | JP5964407B2 (https=) |
| KR (1) | KR101958177B1 (https=) |
| CN (1) | CN103492372B (https=) |
| AU (1) | AU2012245106B2 (https=) |
| BR (1) | BR112013026905B1 (https=) |
| CA (1) | CA2831338C (https=) |
| EA (1) | EA024245B1 (https=) |
| ES (1) | ES2541295T3 (https=) |
| IL (1) | IL228580A (https=) |
| MX (1) | MX360611B (https=) |
| WO (1) | WO2012143599A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107903213A (zh) * | 2017-09-28 | 2018-04-13 | 山东大学 | 5‑甲基‑1h‑吡唑衍生物及其制备方法和应用 |
| US11236073B2 (en) | 2017-08-09 | 2022-02-01 | Hangzhou Solipharma Co., Ltd. | ODM-201 crystalline form, preparation method therefor, and pharmaceutical composition thereof |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3456700A1 (en) | 2013-10-18 | 2019-03-20 | Deutsches Krebsforschungszentrum | Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer |
| US9682960B2 (en) | 2013-12-19 | 2017-06-20 | Endorecherche, Inc. | Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety |
| BR112016018691A2 (pt) * | 2014-02-14 | 2017-08-08 | Univ British Columbia | Compostos do domínio de ligação ao dna (dbd) de receptor de andrógeno humano como terapêuticos e métodos para seu uso |
| JP6817962B2 (ja) * | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3250554B1 (en) | 2015-01-30 | 2022-05-18 | Orion Corporation | A carboxamide derivative and its diastereomers in stable crystalline form |
| HUE049144T2 (hu) * | 2015-04-09 | 2020-08-28 | Orion Corp | Eljárás anrdogén receptorantagonisták és azok intermedierjeinek elõállítására |
| US10865184B2 (en) | 2015-04-21 | 2020-12-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10806720B2 (en) | 2015-04-21 | 2020-10-20 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10654809B2 (en) | 2016-06-10 | 2020-05-19 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10017471B2 (en) | 2015-04-21 | 2018-07-10 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10441570B2 (en) | 2015-04-21 | 2019-10-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) Ligands and methods of use thereof |
| US10093613B2 (en) | 2015-04-21 | 2018-10-09 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US9834507B2 (en) | 2015-04-21 | 2017-12-05 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| CN107709290B (zh) * | 2015-04-21 | 2023-02-28 | Gtx公司 | 选择性雄激素受体降解剂(sard)配体和其使用方法 |
| RU2724103C2 (ru) | 2015-04-21 | 2020-06-22 | Джи Ти Икс, ИНК. | Селективные лиганды-разрушители андрогенных рецептов (sard) и способы их применения |
| US10035763B2 (en) | 2015-04-21 | 2018-07-31 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| WO2017020944A1 (en) * | 2015-07-31 | 2017-02-09 | Universite De Nantes | Novel fused pyrimidinone and triazinone derivatives, their process of preparation and their therapeutic uses as antifungal and/or antiparasitic agents |
| WO2017093180A1 (de) | 2015-12-01 | 2017-06-08 | Bayer Cropscience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| TWI726969B (zh) | 2016-01-11 | 2021-05-11 | 比利時商健生藥品公司 | 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物 |
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| CN110506039A (zh) * | 2016-10-11 | 2019-11-26 | 阿尔维纳斯股份有限公司 | 用于雄激素受体靶向降解的化合物和方法 |
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| UY37556A (es) | 2017-01-10 | 2018-07-31 | Bayer Ag | Derivados heterocíclicos como pesticidas |
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| CN121226255A (zh) * | 2025-09-25 | 2025-12-30 | 安徽益普克医药科技发展有限公司 | 一种达罗他胺衍生物及其制备方法与用途 |
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| WO2007056155A1 (en) * | 2005-11-03 | 2007-05-18 | Chembridge Research Laboratories, Inc. | Heterocyclic compounds as tyrosine kinase modulators |
| WO2008062878A1 (fr) * | 2006-11-22 | 2008-05-29 | Nihon Nohyaku Co., Ltd. | Nouveau dérivé de pyrazole, agent de lutte contre des organismes nuisibles et utilisation de l'agent de lutte contre des organismes nuisibles |
| WO2008124000A2 (en) * | 2007-04-02 | 2008-10-16 | Ligand Pharmaceuticals Incorporated | Thiazole derivatives as androgen receptor modulator compounds |
| WO2011051540A1 (en) * | 2009-10-27 | 2011-05-05 | Orion Corporation | Androgen receptor modulating compounds |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| ATE28864T1 (de) | 1982-07-23 | 1987-08-15 | Ici Plc | Amide-derivate. |
| FR2741342B1 (fr) | 1995-11-22 | 1998-02-06 | Roussel Uclaf | Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques |
| CN1129581C (zh) | 1998-09-22 | 2003-12-03 | 山之内制药株式会社 | 氰基苯基衍生物 |
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- 2012-04-20 WO PCT/FI2012/000022 patent/WO2012143599A1/en not_active Ceased
- 2012-04-20 ES ES12722174.5T patent/ES2541295T3/es active Active
- 2012-04-20 JP JP2014505683A patent/JP5964407B2/ja active Active
- 2012-04-20 US US14/112,727 patent/US8921378B2/en active Active
- 2012-04-20 EP EP12722174.5A patent/EP2699561B1/en active Active
- 2012-04-20 CA CA2831338A patent/CA2831338C/en active Active
- 2012-04-20 KR KR1020137030986A patent/KR101958177B1/ko active Active
- 2012-04-20 BR BR112013026905-7A patent/BR112013026905B1/pt active IP Right Grant
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| WO2007056155A1 (en) * | 2005-11-03 | 2007-05-18 | Chembridge Research Laboratories, Inc. | Heterocyclic compounds as tyrosine kinase modulators |
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| WO2011051540A1 (en) * | 2009-10-27 | 2011-05-05 | Orion Corporation | Androgen receptor modulating compounds |
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| US11236073B2 (en) | 2017-08-09 | 2022-02-01 | Hangzhou Solipharma Co., Ltd. | ODM-201 crystalline form, preparation method therefor, and pharmaceutical composition thereof |
| CN107903213A (zh) * | 2017-09-28 | 2018-04-13 | 山东大学 | 5‑甲基‑1h‑吡唑衍生物及其制备方法和应用 |
Also Published As
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| US20140094474A1 (en) | 2014-04-03 |
| CN103492372A (zh) | 2014-01-01 |
| CA2831338C (en) | 2018-07-17 |
| EP2699561A1 (en) | 2014-02-26 |
| AU2012245106B2 (en) | 2016-09-08 |
| JP5964407B2 (ja) | 2016-08-03 |
| KR20140025486A (ko) | 2014-03-04 |
| NZ616395A (en) | 2015-07-31 |
| EA201391560A1 (ru) | 2014-02-28 |
| EA024245B1 (ru) | 2016-08-31 |
| ES2541295T3 (es) | 2015-07-17 |
| MX2013012265A (es) | 2013-11-22 |
| KR101958177B1 (ko) | 2019-03-15 |
| BR112013026905B1 (pt) | 2021-09-14 |
| WO2012143599A1 (en) | 2012-10-26 |
| MX360611B (es) | 2018-11-09 |
| IL228580A0 (en) | 2013-12-31 |
| JP2014511895A (ja) | 2014-05-19 |
| CA2831338A1 (en) | 2012-10-26 |
| AU2012245106A1 (en) | 2013-10-24 |
| US8921378B2 (en) | 2014-12-30 |
| HK1195305A1 (en) | 2014-11-07 |
| IL228580A (en) | 2015-06-30 |
| BR112013026905A2 (https=) | 2017-01-03 |
| EP2699561B1 (en) | 2015-06-03 |
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