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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- UXQCFLDGVOIWFT-UHFFFAOYSA-N C=CC(Nc1cc(-c(nc(Nc(cc2F)cc(OCOP(O)(O)=O)c2N2CCOCC2)nc2)c2Cl)ccc1)=O Chemical compound C=CC(Nc1cc(-c(nc(Nc(cc2F)cc(OCOP(O)(O)=O)c2N2CCOCC2)nc2)c2Cl)ccc1)=O UXQCFLDGVOIWFT-UHFFFAOYSA-N 0.000 description 1
- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- 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
- C07F9/02—Phosphorus compounds
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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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- A61K31/66—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)
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- Life Sciences & Earth Sciences (AREA)
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- Biochemistry (AREA)
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- Pharmacology & Pharmacy (AREA)
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- 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 (enExample) |
| EP (1) | EP2903971B1 (enExample) |
| JP (1) | JP6313772B2 (enExample) |
| KR (1) | KR20150067298A (enExample) |
| CN (1) | CN104822663B (enExample) |
| CA (1) | CA2887465A1 (enExample) |
| WO (1) | WO2014055934A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012135801A1 (en) | 2011-04-01 | 2012-10-04 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| CN104822663B (zh) | 2012-10-04 | 2017-03-08 | 犹他大学研究基金会 | 作为酪氨酸受体激酶btk抑制剂的取代的n‑(3‑(嘧啶‑4‑基)苯基)丙烯酰胺类似物 |
| JP6401169B2 (ja) | 2012-10-04 | 2018-10-03 | 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 |
| CN109153680B (zh) | 2016-07-07 | 2021-04-23 | 株式会社大熊制药 | 4-氨基吡唑并[3,4-d]嘧啶基氮杂双环衍生物及含其的药物组合物 |
| WO2019013562A1 (ko) | 2017-07-12 | 2019-01-17 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| KR102384924B1 (ko) | 2017-07-12 | 2022-04-08 | 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 |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| 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 |
| JOP20220199A1 (ar) | 2020-02-26 | 2023-01-30 | Daewoong Pharmaceutical Co Ltd | طريقة لتحضير مشتقات أمين حلقي غير متجانس |
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 |
| JP2007500179A (ja) * | 2003-07-30 | 2007-01-11 | サイクラセル・リミテッド | キナーゼ阻害剤としての2−アミノフェニル−4−フェニルピリミジン |
| US7655649B2 (en) | 2004-04-09 | 2010-02-02 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| NZ592990A (en) | 2005-11-01 | 2013-01-25 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| 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 |
| WO2009032861A1 (en) * | 2007-09-04 | 2009-03-12 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| 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 |
| SG2014005318A (en) | 2009-01-23 | 2014-03-28 | Rigel Pharmaceuticals Inc | Compositions and methods for inhibition of the jak pathway |
| SG172857A1 (en) | 2009-02-09 | 2011-08-29 | Supergen Inc | Pyrrolopyrimidinyl axl kinase inhibitors |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
| US7741330B1 (en) | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| WO2012135801A1 (en) | 2011-04-01 | 2012-10-04 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| PL2693881T3 (pl) | 2011-04-01 | 2020-03-31 | University Of Utah Research Foundation | Podstawione analogi N-fenylopirymidyno-2-aminy jako inhibitory kinazy AXL |
| SG10201604682VA (en) * | 2011-06-10 | 2016-07-28 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| JP5826931B2 (ja) * | 2011-07-19 | 2015-12-02 | メルク・シャープ・エンド・ドーム・ベー・フェー | Btk阻害剤としての4−イミダゾピリダジン−1−イル−ベンズアミドおよび4−イミダゾトリアジン−1−イル−ベンズアミド |
| WO2013010869A1 (en) * | 2011-07-19 | 2013-01-24 | Msd Oss B.V. | 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides btk-inhibitors |
| US8993756B2 (en) | 2011-12-06 | 2015-03-31 | Merck Sharp & Dohme Corp. | Pyrrolopyrimidines as janus kinase inhibitors |
| JP6401169B2 (ja) | 2012-10-04 | 2018-10-03 | 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 |
| CN104822663B (zh) | 2012-10-04 | 2017-03-08 | 犹他大学研究基金会 | 作为酪氨酸受体激酶btk抑制剂的取代的n‑(3‑(嘧啶‑4‑基)苯基)丙烯酰胺类似物 |
-
2013
- 2013-10-04 CN CN201380063031.5A patent/CN104822663B/zh not_active Expired - Fee Related
- 2013-10-04 US US14/433,580 patent/US9296703B2/en not_active Expired - Fee Related
- 2013-10-04 KR KR1020157011754A patent/KR20150067298A/ko not_active Withdrawn
- 2013-10-04 CA CA 2887465 patent/CA2887465A1/en not_active Abandoned
- 2013-10-04 WO PCT/US2013/063555 patent/WO2014055934A2/en not_active Ceased
- 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 |
|---|---|
| JP6313772B2 (ja) | 2018-04-18 |
| EP2903971B1 (en) | 2019-06-12 |
| WO2014055934A2 (en) | 2014-04-10 |
| WO2014055934A3 (en) | 2014-06-26 |
| CA2887465A1 (en) | 2014-04-10 |
| EP2903971A4 (en) | 2016-05-25 |
| CN104822663A (zh) | 2015-08-05 |
| US20150368208A1 (en) | 2015-12-24 |
| US9296703B2 (en) | 2016-03-29 |
| EP2903971A2 (en) | 2015-08-12 |
| HK1213244A1 (en) | 2016-06-30 |
| JP2015535851A (ja) | 2015-12-17 |
| CN104822663B (zh) | 2017-03-08 |
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Legal Events
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| PA0105 | International application |
Patent event date: 20150504 Patent event code: PA01051R01D Comment text: International Patent Application |
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| PG1501 | Laying open of application | ||
| PC1203 | Withdrawal of no request for examination | ||
| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |