CN106795179B - 一类激酶抑制剂 - Google Patents
一类激酶抑制剂 Download PDFInfo
- Publication number
- CN106795179B CN106795179B CN201580027559.6A CN201580027559A CN106795179B CN 106795179 B CN106795179 B CN 106795179B CN 201580027559 A CN201580027559 A CN 201580027559A CN 106795179 B CN106795179 B CN 106795179B
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- China
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- base
- amino
- pyrimidine
- pyridine
- cyclopenta
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910743940.2A CN110372720B (zh) | 2014-05-28 | 2015-05-27 | 一类激酶抑制剂 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462003626P | 2014-05-28 | 2014-05-28 | |
| US62/003626 | 2014-05-28 | ||
| PCT/CN2015/079910 WO2015180642A1 (en) | 2014-05-28 | 2015-05-27 | Certain protein kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910743940.2A Division CN110372720B (zh) | 2014-05-28 | 2015-05-27 | 一类激酶抑制剂 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106795179A CN106795179A (zh) | 2017-05-31 |
| CN106795179B true CN106795179B (zh) | 2019-09-17 |
Family
ID=54698110
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580027559.6A Active CN106795179B (zh) | 2014-05-28 | 2015-05-27 | 一类激酶抑制剂 |
| CN201910743940.2A Active CN110372720B (zh) | 2014-05-28 | 2015-05-27 | 一类激酶抑制剂 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910743940.2A Active CN110372720B (zh) | 2014-05-28 | 2015-05-27 | 一类激酶抑制剂 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10087195B2 (enExample) |
| EP (1) | EP3149008B8 (enExample) |
| JP (1) | JP2017516855A (enExample) |
| KR (1) | KR101864589B1 (enExample) |
| CN (2) | CN106795179B (enExample) |
| AU (1) | AU2015266492B2 (enExample) |
| BR (1) | BR112016027679B1 (enExample) |
| CA (1) | CA2950330C (enExample) |
| DK (1) | DK3149008T3 (enExample) |
| ES (1) | ES2715462T3 (enExample) |
| MX (1) | MX381487B (enExample) |
| RU (1) | RU2671494C2 (enExample) |
| WO (1) | WO2015180642A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106188060A (zh) * | 2015-04-29 | 2016-12-07 | 厦门大学 | 嘧啶并吡咯类化合物、其制备方法、药用组合物及其应用 |
| CN105130992B (zh) * | 2015-07-16 | 2018-02-09 | 苏州大学 | 具有激酶抑制活性的含氮杂环化合物、制备方法和用途 |
| CN113549069A (zh) * | 2015-12-27 | 2021-10-26 | 重庆复创医药研究有限公司 | 一类激酶抑制剂 |
| WO2017161253A1 (en) | 2016-03-18 | 2017-09-21 | Tufts Medical Center | Compositions and methods for treating and preventing metabolic disorders |
| CN109153686B (zh) * | 2016-05-07 | 2021-04-30 | 上海复尚慧创医药研究有限公司 | 一类蛋白激酶抑制剂 |
| WO2018005860A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| JP6905069B2 (ja) * | 2016-11-11 | 2021-07-21 | 上海海雁醫藥科技有限公司 | ピリジルアミノ置換へテロ三環式化合物並びにその製造方法及び医薬用途 |
| CN107312006B (zh) * | 2017-06-28 | 2019-11-15 | 郑州大学第一附属医院 | 吡咯并嘧啶类衍生物及其应用 |
| JP7569688B2 (ja) | 2017-12-22 | 2024-10-18 | ハイバーセル,インコーポレイテッド | ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体 |
| US11174252B2 (en) | 2018-02-15 | 2021-11-16 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| WO2019168874A1 (en) | 2018-02-27 | 2019-09-06 | The Research Foundation For The State University Of New York | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
| EP3786161A4 (en) | 2018-04-24 | 2021-05-05 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd | CDK4 / 6 INHIBITOR, PHARMACEUTICALLY ACCEPTABLE SALT, POLYMORPHIC OF THEM AND ASSOCIATED USE |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| CN112094272A (zh) * | 2019-06-18 | 2020-12-18 | 北京睿熙生物科技有限公司 | Cdk激酶抑制剂 |
| EP4652997A2 (en) | 2020-05-19 | 2025-11-26 | Pharmacosmos Holding A/s | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| AR124154A1 (es) | 2020-11-27 | 2023-02-22 | Rhizen Pharmaceuticals Ag | Inhibidores de cdk |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| CA3249870A1 (en) * | 2022-01-25 | 2023-08-03 | Kinnate Biopharma Inc. | CDK4/6 KINASE INHIBITORS |
| CN116836177A (zh) * | 2022-09-28 | 2023-10-03 | 锦州奥鸿药业有限责任公司 | 一种蛋白激酶抑制剂的枸橼酸盐、其晶型、制备方法和用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1694886A (zh) * | 2002-09-23 | 2005-11-09 | 先灵公司 | 作为周期素依赖性激酶抑制剂的咪唑并吡嗪 |
| WO2005121107A1 (en) * | 2004-06-09 | 2005-12-22 | F. Hoffmann-La Roche Ag | Pyrazolo pyrimidines |
| WO2009062258A1 (en) * | 2007-11-15 | 2009-05-22 | Cytopia Research Pty Ltd | N-containing heterocyclic compounds |
| WO2011101409A1 (en) * | 2010-02-19 | 2011-08-25 | Novartis Ag | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
| WO2013150036A1 (en) * | 2012-04-03 | 2013-10-10 | Sanofi | Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3235B1 (ar) * | 2006-05-26 | 2018-03-08 | Astex Therapeutics Ltd | مركبات بيررولوبيريميدين و استعمالاتها |
| US8685980B2 (en) * | 2008-08-22 | 2014-04-01 | Novartis Ag | Pyrrolopyrimidine compounds and their uses |
| KR101147550B1 (ko) * | 2009-10-22 | 2012-05-17 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-d]피리미딘 화합물 |
| US20120115878A1 (en) * | 2010-11-10 | 2012-05-10 | John Vincent Calienni | Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof |
-
2015
- 2015-05-27 DK DK15800531.4T patent/DK3149008T3/en active
- 2015-05-27 ES ES15800531T patent/ES2715462T3/es active Active
- 2015-05-27 RU RU2016151315A patent/RU2671494C2/ru active
- 2015-05-27 JP JP2017514769A patent/JP2017516855A/ja active Pending
- 2015-05-27 KR KR1020167036619A patent/KR101864589B1/ko active Active
- 2015-05-27 CN CN201580027559.6A patent/CN106795179B/zh active Active
- 2015-05-27 BR BR112016027679-5A patent/BR112016027679B1/pt active IP Right Grant
- 2015-05-27 AU AU2015266492A patent/AU2015266492B2/en active Active
- 2015-05-27 MX MX2016015565A patent/MX381487B/es unknown
- 2015-05-27 CN CN201910743940.2A patent/CN110372720B/zh active Active
- 2015-05-27 CA CA2950330A patent/CA2950330C/en active Active
- 2015-05-27 US US15/314,006 patent/US10087195B2/en active Active
- 2015-05-27 WO PCT/CN2015/079910 patent/WO2015180642A1/en not_active Ceased
- 2015-05-27 EP EP15800531.4A patent/EP3149008B8/en active Active
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1694886A (zh) * | 2002-09-23 | 2005-11-09 | 先灵公司 | 作为周期素依赖性激酶抑制剂的咪唑并吡嗪 |
| WO2005121107A1 (en) * | 2004-06-09 | 2005-12-22 | F. Hoffmann-La Roche Ag | Pyrazolo pyrimidines |
| WO2009062258A1 (en) * | 2007-11-15 | 2009-05-22 | Cytopia Research Pty Ltd | N-containing heterocyclic compounds |
| WO2011101409A1 (en) * | 2010-02-19 | 2011-08-25 | Novartis Ag | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
| WO2013150036A1 (en) * | 2012-04-03 | 2013-10-10 | Sanofi | Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof |
| CN104540834A (zh) * | 2012-04-03 | 2015-04-22 | 赛诺菲 | 新噻吩并嘧啶衍生物、其制备方法及其治疗用途 |
Non-Patent Citations (2)
| Title |
|---|
| 4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6;Young Shin Cho et al.;《J. Med. Chem.》;20101101;第53卷(第22期);第7938-7957页 * |
| Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors;Yike Ni et al.;《Bioorganic & Medicinal Chemistry Letters》;20110726;第21卷;第5952-5956页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2015180642A1 (en) | 2015-12-03 |
| CA2950330A1 (en) | 2015-12-03 |
| KR101864589B1 (ko) | 2018-07-04 |
| CN106795179A (zh) | 2017-05-31 |
| BR112016027679B1 (pt) | 2022-10-25 |
| BR112016027679A2 (enExample) | 2017-08-15 |
| RU2016151315A (ru) | 2018-07-02 |
| US20170267696A1 (en) | 2017-09-21 |
| CN110372720A (zh) | 2019-10-25 |
| US10087195B2 (en) | 2018-10-02 |
| JP2017516855A (ja) | 2017-06-22 |
| EP3149008A4 (en) | 2018-01-17 |
| DK3149008T3 (en) | 2019-04-01 |
| MX2016015565A (es) | 2017-07-04 |
| MX381487B (es) | 2025-03-12 |
| AU2015266492B2 (en) | 2017-11-02 |
| RU2671494C2 (ru) | 2018-11-01 |
| CA2950330C (en) | 2019-04-30 |
| EP3149008B8 (en) | 2019-03-06 |
| RU2016151315A3 (enExample) | 2018-07-02 |
| EP3149008B1 (en) | 2018-12-12 |
| KR20170023872A (ko) | 2017-03-06 |
| CN110372720B (zh) | 2021-03-05 |
| EP3149008A1 (en) | 2017-04-05 |
| ES2715462T3 (es) | 2019-06-04 |
| AU2015266492A1 (en) | 2017-01-19 |
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