KR20150067298A - 티로신 수용체 키나아제 btk 억제제로서의 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 - Google Patents
티로신 수용체 키나아제 btk 억제제로서의 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 Download PDFInfo
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- KR20150067298A KR20150067298A KR1020157011754A KR20157011754A KR20150067298A KR 20150067298 A KR20150067298 A KR 20150067298A KR 1020157011754 A KR1020157011754 A KR 1020157011754A KR 20157011754 A KR20157011754 A KR 20157011754A KR 20150067298 A KR20150067298 A KR 20150067298A
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- 0 *c1cc(Nc2nc([n](*)nc3)c3c(-c3cccc(NC(C=C)=O)c3)n2)cc(*)c1* Chemical compound *c1cc(Nc2nc([n](*)nc3)c3c(-c3cccc(NC(C=C)=O)c3)n2)cc(*)c1* 0.000 description 32
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- HKSLLYYKHMKANB-UHFFFAOYSA-N C=CC(Nc1cc(-c(nc(Nc(cc2F)cc(OP(O)(O)=O)c2N2CCOCC2)nc2)c2Cl)ccc1)=O Chemical compound C=CC(Nc1cc(-c(nc(Nc(cc2F)cc(OP(O)(O)=O)c2N2CCOCC2)nc2)c2Cl)ccc1)=O HKSLLYYKHMKANB-UHFFFAOYSA-N 0.000 description 1
- GZUWQJVRBIQEHT-UHFFFAOYSA-N C=CC(Nc1cc(-c(nc(Nc(cc2O)cc(F)c2N2CCOCC2)nc2)c2Cl)ccc1)=O Chemical compound C=CC(Nc1cc(-c(nc(Nc(cc2O)cc(F)c2N2CCOCC2)nc2)c2Cl)ccc1)=O GZUWQJVRBIQEHT-UHFFFAOYSA-N 0.000 description 1
- WJMZZLWZRIOXSQ-UHFFFAOYSA-N C=CC(Nc1cc(-c2c(cn[nH]3)c3nc(Nc(cc3)cc(OCOP(O)(O)=O)c3N3CCOCC3)n2)ccc1)=O Chemical compound C=CC(Nc1cc(-c2c(cn[nH]3)c3nc(Nc(cc3)cc(OCOP(O)(O)=O)c3N3CCOCC3)n2)ccc1)=O WJMZZLWZRIOXSQ-UHFFFAOYSA-N 0.000 description 1
- VTNXRMZWXKHPAT-UHFFFAOYSA-N C=CC(Nc1cc(-c2c(cn[n]3C4OCCCC4)c3nc(Cl)n2)ccc1)=O Chemical compound C=CC(Nc1cc(-c2c(cn[n]3C4OCCCC4)c3nc(Cl)n2)ccc1)=O VTNXRMZWXKHPAT-UHFFFAOYSA-N 0.000 description 1
- OBUHXVMMGDSSLU-UHFFFAOYSA-N CC(C)OCOC(OCc1ccccc1)=C=O Chemical compound CC(C)OCOC(OCc1ccccc1)=C=O OBUHXVMMGDSSLU-UHFFFAOYSA-N 0.000 description 1
- GQKZBCPTCWJTAS-UHFFFAOYSA-N COCc1ccccc1 Chemical compound COCc1ccccc1 GQKZBCPTCWJTAS-UHFFFAOYSA-N 0.000 description 1
- CTYPROOLWJDUTA-UHFFFAOYSA-N Clc1c(cn[nH]2)c2nc(Cl)n1 Chemical compound Clc1c(cn[nH]2)c2nc(Cl)n1 CTYPROOLWJDUTA-UHFFFAOYSA-N 0.000 description 1
- VMIPTJUFAWNUEU-UHFFFAOYSA-N Clc1c(cn[n]2C3OCCCC3)c2nc(Cl)n1 Chemical compound Clc1c(cn[n]2C3OCCCC3)c2nc(Cl)n1 VMIPTJUFAWNUEU-UHFFFAOYSA-N 0.000 description 1
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- C07—ORGANIC CHEMISTRY
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
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- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
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- C07F9/06—Phosphorus compounds without P—C bonds
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- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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- C07F9/6509—Six-membered rings
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A—HUMAN NECESSITIES
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
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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
- A61K31/66—Phosphorus compounds
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
- A61K31/6615—Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Biochemistry (AREA)
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- Animal Behavior & Ethology (AREA)
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- Pain & Pain Management (AREA)
- Oncology (AREA)
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- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261709534P | 2012-10-04 | 2012-10-04 | |
| US61/709,534 | 2012-10-04 | ||
| PCT/US2013/063555 WO2014055934A2 (en) | 2012-10-04 | 2013-10-04 | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20150067298A true KR20150067298A (ko) | 2015-06-17 |
Family
ID=50435583
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157011754A Withdrawn KR20150067298A (ko) | 2012-10-04 | 2013-10-04 | 티로신 수용체 키나아제 btk 억제제로서의 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9296703B2 (https=) |
| EP (1) | EP2903971B1 (https=) |
| JP (1) | JP6313772B2 (https=) |
| KR (1) | KR20150067298A (https=) |
| CN (1) | CN104822663B (https=) |
| CA (1) | CA2887465A1 (https=) |
| WO (1) | WO2014055934A2 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6147727B2 (ja) | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼbtk阻害剤としての置換n−(3−(ピリミジン−4−イル)フェニル)アクリルアミド類似体 |
| WO2014055928A2 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| CA2887465A1 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| ES2965081T3 (es) | 2016-07-07 | 2024-04-11 | Daewoong Pharmaceutical Co Ltd | Derivados 4-aminopirazolo[3,4-d]pirimidinil-azabiciclo y composición farmacéutica que comprende dichos derivados |
| KR102384924B1 (ko) | 2017-07-12 | 2022-04-08 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| WO2019013562A1 (ko) | 2017-07-12 | 2019-01-17 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| KR102613433B1 (ko) | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
| WO2020045941A1 (ko) | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| BR112022016729A2 (pt) | 2020-02-26 | 2022-10-11 | Daewoong Pharmaceutical Co Ltd | Método para preparação de derivados de heterociclicamina |
| CN121002017A (zh) | 2023-05-04 | 2025-11-21 | 株式会社大熊制药 | 新颖的杂环胺衍生物以及包含其的药物组合物 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9924862D0 (en) | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| EP1648875A1 (en) * | 2003-07-30 | 2006-04-26 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| CA2561311A1 (en) | 2004-04-09 | 2005-10-27 | Merck & Co., Inc. | Inhibitors of akt activity |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| JP5191391B2 (ja) | 2005-11-01 | 2013-05-08 | ターゲジェン インコーポレーティッド | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
| KR20080110998A (ko) * | 2006-01-30 | 2008-12-22 | 엑셀리시스, 인코포레이티드 | Jak2 조절자로서 4아릴2아미노피리미딘 또는 4아릴2아미노알킬피리미딘 및 이들을 포함하는 약제학적 조성물 |
| KR101122481B1 (ko) | 2007-05-04 | 2012-02-29 | 아이알엠 엘엘씨 | C-kit 및 pdgfr 키나제 억제제로서의 피리미딘 유도체 및 조성물 |
| JP5611826B2 (ja) * | 2007-09-04 | 2014-10-22 | ザ スクリプス リサーチ インスティテュート | タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| BRPI1006942A2 (pt) | 2009-01-23 | 2016-04-12 | Rigel Pharmaceuticals Inc | composto, composição farmacêutica, kit, métodos para inibir uma atividade de uma jak quinase, para tratar uma doença, para tratar a rejeição de transplante de aloenxerto em um receptor de transplante, para tratar uma reação de hipersensibilidade, e para inibir uma cascata de transdução de sinal, e, uso do composto |
| TW201041892A (en) | 2009-02-09 | 2010-12-01 | Supergen Inc | Pyrrolopyrimidinyl Axl kinase inhibitors |
| US9908884B2 (en) | 2009-05-05 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | EGFR inhibitors and methods of treating disorders |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| JP6147727B2 (ja) * | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼbtk阻害剤としての置換n−(3−(ピリミジン−4−イル)フェニル)アクリルアミド類似体 |
| ES2759615T3 (es) | 2011-04-01 | 2020-05-11 | Univ Utah Res Found | Análogos de N-fenilpirimidina-2-amina sustituidos como inhibidores de la quinasa AXL |
| MX354412B (es) * | 2011-06-10 | 2018-03-05 | Merck Patent Gmbh | Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton. |
| CA2841887A1 (en) * | 2011-07-19 | 2013-01-24 | Merck Sharp & Dohme B.V. | 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk - inhibitors |
| EP3689878B1 (en) * | 2011-07-19 | 2021-10-06 | Merck Sharp & Dohme B.V. | 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk-inhibitors |
| EP2788000B1 (en) | 2011-12-06 | 2018-05-30 | Merck Sharp & Dohme Corp. | Pyrrolopyrimidines as janus kinase inhibitors |
| CA2887465A1 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| WO2014055928A2 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
-
2013
- 2013-10-04 CA CA 2887465 patent/CA2887465A1/en not_active Abandoned
- 2013-10-04 US US14/433,580 patent/US9296703B2/en not_active Expired - Fee Related
- 2013-10-04 WO PCT/US2013/063555 patent/WO2014055934A2/en not_active Ceased
- 2013-10-04 CN CN201380063031.5A patent/CN104822663B/zh not_active Expired - Fee Related
- 2013-10-04 KR KR1020157011754A patent/KR20150067298A/ko not_active Withdrawn
- 2013-10-04 EP EP13844062.3A patent/EP2903971B1/en not_active Not-in-force
- 2013-10-04 JP JP2015535840A patent/JP6313772B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| HK1213244A1 (en) | 2016-06-30 |
| CN104822663B (zh) | 2017-03-08 |
| EP2903971A2 (en) | 2015-08-12 |
| EP2903971A4 (en) | 2016-05-25 |
| US20150368208A1 (en) | 2015-12-24 |
| WO2014055934A2 (en) | 2014-04-10 |
| US9296703B2 (en) | 2016-03-29 |
| WO2014055934A3 (en) | 2014-06-26 |
| EP2903971B1 (en) | 2019-06-12 |
| CN104822663A (zh) | 2015-08-05 |
| JP2015535851A (ja) | 2015-12-17 |
| CA2887465A1 (en) | 2014-04-10 |
| JP6313772B2 (ja) | 2018-04-18 |
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