EA022815B1 - Антагонист рецептора cgrp - Google Patents
Антагонист рецептора cgrp Download PDFInfo
- Publication number
- EA022815B1 EA022815B1 EA201270751A EA201270751A EA022815B1 EA 022815 B1 EA022815 B1 EA 022815B1 EA 201270751 A EA201270751 A EA 201270751A EA 201270751 A EA201270751 A EA 201270751A EA 022815 B1 EA022815 B1 EA 022815B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compound
- pharmaceutically acceptable
- oxopropan
- dihydroquinolin
- indazol
- Prior art date
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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
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
- A61K31/495—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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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
-
- 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
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
Изобретение, в целом, относится к соединению формулы I, (R)-N-(3-(7-метил-1Н-индазол-5-ил)-1-(4-(1-метилпиперидин-4-ил)пиперазин-1-ил)-1-оксопропан-2-ил)-4-(2-оксо-1,2-дигидрохинолин-3-ил)пиперидин-1-карбоксамиду, включающему в себя фармацевтически приемлемые соли, которое представляет собой антагонист CGRP-рецептора. Изобретение также относится к фармацевтическим композициям и способам для применения соединения в лечении расстройств, связанных с CGRP, включающих в себя мигренозные головные боли, нейрогенную вазодилатацию, нейрогенное воспаление, термическое повреждение, циркуляторный шок, гиперемию, связанную с менопаузой, воспалительные заболевания дыхательных путей, такие как астма, хроническое обструктивное заболевание легких (ХОЗЛ), и раковая опухоль.
Description
(57) Изобретение, в целом, относится к соединению формулы I, (К.)-И-(3-(7-метил-1Н-индазол-5-ил)-1(4-( 1 -метилпиперидин-4-ил)пиперазин-1 -ил)- 1-оксопропан-2-ил)-4-(2-оксо-1,2дигидрохинолин-3-ил)пиперидин-1-карбоксамиду, включающему в себя фармацевтически приемлемые соли, которое представляет собой антагонист ССКР-рецептора. Изобретение также относится к фармацевтическим композициям и способам для применения соединения в лечении расстройств, связанных с ССКР, включающих в себя мигренозные головные боли, нейрогенную вазодилатацию, нейрогенное воспаление, термическое повреждение, циркуляторный шок, гиперемию, связанную с менопаузой, воспалительные заболевания дыхательных путей, такие как астма, хроническое обструктивное заболевание легких (ХОЗЛ), и раковая опухоль.
Claims (7)
1. Соединение (К)-И-(3-(7-метил-1Н-индазол-5-ил)-1-(4-(1-метилпиперидин-4-ил)пиперазин-1-ил)1-оксопропан-2-ил)-4-(2-оксо-1,2-дигидрохинолин-3-ил)пиперидин-1-карбоксамид или его фармацевтически приемлемая соль
2. Фармацевтическая композиция для лечения состояния, связанного с аберрантными уровнями ССКР или сигнального ССКР рецептора, содержащая фармацевтически эффективное количество (К)-И(3 -(7 -метил-1Н-индазол-5-ил)-1 -(4-( 1 -метилпиперидин-4-ил)пиперазин-1 -ил)-1-оксопропан-2-ил)-4-(2-оксо-1,2-дигидрохинолин-3-ил)пиперидин-1-карбоксамида в сочетании с фармацевтически приемлемым адъювантом, носителем или растворителем.
3. Способ лечения состояния, связанного с аберрантными уровнями ССКР или сигнального ССКР рецептора, включающий введение терапевтически эффективного количества соединения по п. 1 или его фармацевтически приемлемой соли пациенту.
4. Способ по п.3, отличающийся тем, что состояние представляет собой мигрень.
- 19 022815
5. Способ по п.3, отличающийся тем, что состояние представляет собой нейропатическую боль.
6. Способ лечения пролиферативного заболевания, включающий в себя введение терапевтически эффективного количества соединения по п.1 или его фармацевтически приемлемой соли пациенту.
7. Способ по п.6, отличающийся тем, что пролиферативное заболевание представляет собой рак молочной железы или глиому.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31901510P | 2010-03-30 | 2010-03-30 | |
| PCT/US2011/028168 WO2011123232A1 (en) | 2010-03-30 | 2011-03-11 | Cgrp receptor antagonist |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201270751A1 EA201270751A1 (ru) | 2013-02-28 |
| EA022815B1 true EA022815B1 (ru) | 2016-03-31 |
Family
ID=43896902
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201270751A EA022815B1 (ru) | 2010-03-30 | 2011-03-11 | Антагонист рецептора cgrp |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US8481546B2 (ru) |
| EP (1) | EP2552906B1 (ru) |
| JP (1) | JP5908455B2 (ru) |
| KR (3) | KR20180049168A (ru) |
| CN (1) | CN102834388B (ru) |
| AR (1) | AR080746A1 (ru) |
| AU (1) | AU2011233627B2 (ru) |
| BR (1) | BR112012024785B1 (ru) |
| CA (1) | CA2794950C (ru) |
| CL (1) | CL2012002739A1 (ru) |
| CY (1) | CY1117593T1 (ru) |
| DK (1) | DK2552906T3 (ru) |
| EA (1) | EA022815B1 (ru) |
| ES (1) | ES2562610T3 (ru) |
| HR (1) | HRP20160287T1 (ru) |
| HU (1) | HUE028735T2 (ru) |
| IL (1) | IL221665A (ru) |
| MX (1) | MX2012010725A (ru) |
| NZ (1) | NZ603231A (ru) |
| PE (1) | PE20130340A1 (ru) |
| PL (1) | PL2552906T3 (ru) |
| PT (1) | PT2552906E (ru) |
| RS (1) | RS54608B1 (ru) |
| SG (1) | SG183918A1 (ru) |
| SI (1) | SI2552906T1 (ru) |
| SM (1) | SMT201600078B (ru) |
| TW (1) | TWI483937B (ru) |
| WO (1) | WO2011123232A1 (ru) |
| ZA (1) | ZA201207292B (ru) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201519194D0 (en) * | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP receptor antagonists |
| GB201519195D0 (en) | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201519196D0 (en) | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201707938D0 (en) | 2017-05-17 | 2017-06-28 | Univ Sheffield | Compounds |
| MX2021003689A (es) * | 2018-10-13 | 2021-06-04 | Biohaven Pharm Holding Co Ltd | Farmacos precursores de antagonistas del peptido relacionado con el gen para calcitonina (gcrp). |
| JP2022517433A (ja) * | 2019-01-20 | 2022-03-08 | バイオヘイブン・ファーマシューティカル・ホールディング・カンパニー・リミテッド | 突出性の片頭痛を処置するためのｃｇｒｐアンタゴニスト |
| EA202192793A1 (ru) | 2019-04-11 | 2022-01-12 | Ар.Пи. ШЕРЕР ТЕКНОЛОДЖИЗ, ЭлЭлСи | Композиция для пероральной доставки белков, пептидов и малых молекул со слабой проницаемостью |
| EP4076395A4 (en) * | 2019-12-17 | 2024-02-07 | Pfizer Ireland Pharmaceuticals | INTRANASAL PHARMACEUTICAL COMPOSITIONS OF CGRP INHIBITORS |
| CN116456981A (zh) * | 2020-11-19 | 2023-07-18 | 辉瑞爱尔兰制药公司 | 用于改善的grp抑制剂递送的组合物 |
| KR20230088442A (ko) * | 2020-11-19 | 2023-06-19 | 화이자 아일랜드 파마슈티컬즈 | Cgrp 억제제의 개선된 전달을 위한 조성물 |
| EP4301362A1 (en) | 2021-03-02 | 2024-01-10 | CGRP Diagnostics GmbH | Treatment and/or reduction of occurrence of migraine |
| WO2022217008A1 (en) | 2021-04-09 | 2022-10-13 | Teva Czech Industries S.R.O | Solid state forms of zavegepant and process for preparation thereof |
| US20250109188A1 (en) | 2021-08-24 | 2025-04-03 | Cgrp Diagnostics Gmbh | Preventative treatment of migraine |
| WO2024046223A1 (zh) * | 2022-08-30 | 2024-03-07 | 熙源安健医药（上海）有限公司 | 吲唑甲酰胺类衍生物及其制备方法和用途 |
| JP2025536064A (ja) | 2022-11-09 | 2025-10-30 | テバ チェク インダストリーズ スポレチノスト ス ルチェニーム オメゼニーム | ザベゲパント塩酸塩の固体形態及びその調製方法 |
| CN116003387B (zh) * | 2022-11-20 | 2024-03-26 | 药康众拓(北京)医药科技有限公司 | 一种氘代吲唑丙酰胺类化合物、药物组合物和用途 |
| WO2025003905A1 (en) | 2023-06-29 | 2025-01-02 | Pfizer Inc. | Solid forms of (r)-n-(3-(7-methyl-1h-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide |
| CN119462607B (zh) * | 2023-08-10 | 2025-11-28 | 南京宁丹新药技术股份有限公司 | 一类喹啉酮衍生物及其用途 |
| CN117551081A (zh) * | 2023-11-13 | 2024-02-13 | 北京康立生医药技术开发有限公司 | 一种偏头痛治疗药物新的制备方法 |
| ES3027457A1 (es) * | 2023-12-13 | 2025-06-13 | Moehs Iberica Sl | Metodo de preparacion de zavegepant, intermedios de sintesis de zavegepant y metodos de preparacion de los mismos |
| WO2025238595A1 (en) | 2024-05-16 | 2025-11-20 | Olon S.P.A. | Process for preparing (r)-2-amino-3-(7-methyl-1h-indazol-5-yl) methyl propanoate, and use thereof as intermediate for the synthesis of zavegepant |
| CN119306698B (zh) * | 2024-10-09 | 2025-10-21 | 浙江工业大学 | 一种制备扎维吉泮中间体的新方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7220862B2 (en) | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| ES2616539T3 (es) | 2002-06-05 | 2017-06-13 | Bristol-Myers Squibb Company | Antagonistas de receptores de péptidos relacionados con el gen de calcitonina |
| EP1722792A1 (de) | 2004-03-03 | 2006-11-22 | Boehringer Ingelheim International GmbH | Ausgewählte cgrp-antagonisten, verfahren zu deren herstellung sowie deren verwendung als arzneimittel |
| US7834007B2 (en) | 2005-08-25 | 2010-11-16 | Bristol-Myers Squibb Company | CGRP antagonists |
| CN101495480B (zh) * | 2006-05-03 | 2013-07-10 | 百时美施贵宝公司 | 作为降钙素基因相关肽受体拮抗剂的受限化合物 |
| WO2010006168A2 (en) | 2008-07-09 | 2010-01-14 | University Of Rochester | Methods of treating cancer using and agent that modulates activity of the calcitonin-gene related peptide ("cgrp") receptor |
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2011
- 2011-03-02 US US13/038,550 patent/US8481546B2/en active Active
- 2011-03-11 CA CA2794950A patent/CA2794950C/en active Active
- 2011-03-11 PT PT117100875T patent/PT2552906E/pt unknown
- 2011-03-11 PE PE2012001746A patent/PE20130340A1/es active IP Right Grant
- 2011-03-11 CN CN201180016888.2A patent/CN102834388B/zh active Active
- 2011-03-11 HU HUE11710087A patent/HUE028735T2/en unknown
- 2011-03-11 RS RS20160164A patent/RS54608B1/sr unknown
- 2011-03-11 EP EP11710087.5A patent/EP2552906B1/en active Active
- 2011-03-11 KR KR1020187011875A patent/KR20180049168A/ko not_active Ceased
- 2011-03-11 ES ES11710087.5T patent/ES2562610T3/es active Active
- 2011-03-11 BR BR112012024785-9A patent/BR112012024785B1/pt active IP Right Grant
- 2011-03-11 AU AU2011233627A patent/AU2011233627B2/en active Active
- 2011-03-11 HR HRP20160287TT patent/HRP20160287T1/hr unknown
- 2011-03-11 PL PL11710087T patent/PL2552906T3/pl unknown
- 2011-03-11 DK DK11710087.5T patent/DK2552906T3/en active
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- 2011-03-11 MX MX2012010725A patent/MX2012010725A/es active IP Right Grant
- 2011-03-11 SI SI201130765A patent/SI2552906T1/sl unknown
- 2011-03-11 KR KR1020127028213A patent/KR101747477B1/ko active Active
- 2011-03-11 WO PCT/US2011/028168 patent/WO2011123232A1/en not_active Ceased
- 2011-03-11 SG SG2012065744A patent/SG183918A1/en unknown
- 2011-03-11 JP JP2013502610A patent/JP5908455B2/ja active Active
- 2011-03-11 KR KR1020177015456A patent/KR101854249B1/ko active Active
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2012
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2016
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