JP6991585B2 - メニン阻害剤としてのピペリジン - Google Patents
メニン阻害剤としてのピペリジン Download PDFInfo
- Publication number
- JP6991585B2 JP6991585B2 JP2018557418A JP2018557418A JP6991585B2 JP 6991585 B2 JP6991585 B2 JP 6991585B2 JP 2018557418 A JP2018557418 A JP 2018557418A JP 2018557418 A JP2018557418 A JP 2018557418A JP 6991585 B2 JP6991585 B2 JP 6991585B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- optionally substituted
- pharmaceutically acceptable
- cancer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 0 CC(C)C(C)NC(C)* Chemical compound CC(C)C(C)NC(C)* 0.000 description 22
- XILPCSMEKCBYFO-UHFFFAOYSA-N C[n]1cnnc1 Chemical compound C[n]1cnnc1 XILPCSMEKCBYFO-UHFFFAOYSA-N 0.000 description 2
- MHFBISFDLRWTLQ-UHFFFAOYSA-N N#CC(C1CCN(Cc2ccccc2)CC1)c1ccccc1 Chemical compound N#CC(C1CCN(Cc2ccccc2)CC1)c1ccccc1 MHFBISFDLRWTLQ-UHFFFAOYSA-N 0.000 description 2
- RTKAORMIRLPJCV-UBFHEZILSA-N N#CC([C@@H](CCC1)[C@H]1O)(C1CCNCC1)c1ccccc1 Chemical compound N#CC([C@@H](CCC1)[C@H]1O)(C1CCNCC1)c1ccccc1 RTKAORMIRLPJCV-UBFHEZILSA-N 0.000 description 2
- BHHGXPLMPWCGHP-UHFFFAOYSA-N NCCc1ccccc1 Chemical compound NCCc1ccccc1 BHHGXPLMPWCGHP-UHFFFAOYSA-N 0.000 description 2
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- HFAJKGQCFGQDTQ-UHFFFAOYSA-N CCc1ncc[n]1C(C)C Chemical compound CCc1ncc[n]1C(C)C HFAJKGQCFGQDTQ-UHFFFAOYSA-N 0.000 description 1
- GZXCSMZEPVRSLL-KKUQBAQOSA-N CN[C@](CCC1)([C@H]1N)[C@](C1CCN(Cc2ccccc2)CC1)(c1ccccc1)C#N Chemical compound CN[C@](CCC1)([C@H]1N)[C@](C1CCN(Cc2ccccc2)CC1)(c1ccccc1)C#N GZXCSMZEPVRSLL-KKUQBAQOSA-N 0.000 description 1
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- DSZYFHYERQIEAF-UHFFFAOYSA-N C[n]1c(CC(F)(F)F)nnc1 Chemical compound C[n]1c(CC(F)(F)F)nnc1 DSZYFHYERQIEAF-UHFFFAOYSA-N 0.000 description 1
- MCTWTZJPVLRJOU-UHFFFAOYSA-N C[n]1cncc1 Chemical compound C[n]1cncc1 MCTWTZJPVLRJOU-UHFFFAOYSA-N 0.000 description 1
- GIWQSPITLQVMSG-UHFFFAOYSA-N Cc1ncc[n]1C Chemical compound Cc1ncc[n]1C GIWQSPITLQVMSG-UHFFFAOYSA-N 0.000 description 1
- XKIHZSIFRKRCKY-SKCDSABHSA-N N#CC(C1CCN(Cc2ccccc2)CC1)(C1=CCC[C@@H]1O)c1ccccc1 Chemical compound N#CC(C1CCN(Cc2ccccc2)CC1)(C1=CCC[C@@H]1O)c1ccccc1 XKIHZSIFRKRCKY-SKCDSABHSA-N 0.000 description 1
- NECGMGJIOIEQNL-KOPQTXDBSA-N N#CC([C@@H](CCC1)[C@H]1O)(C1CCN(CC(C2)CN2c(cc2)ccc2S(c2ccncc2)(=O)=O)CC1)c1ccccc1 Chemical compound N#CC([C@@H](CCC1)[C@H]1O)(C1CCN(CC(C2)CN2c(cc2)ccc2S(c2ccncc2)(=O)=O)CC1)c1ccccc1 NECGMGJIOIEQNL-KOPQTXDBSA-N 0.000 description 1
- WUAHWFBUFSMXMG-LGTSYYJHSA-N N#CC([C@@H](CCC1)[C@H]1O)(C1CCN(CC2CNC2)CC1)c1ccccc1 Chemical compound N#CC([C@@H](CCC1)[C@H]1O)(C1CCN(CC2CNC2)CC1)c1ccccc1 WUAHWFBUFSMXMG-LGTSYYJHSA-N 0.000 description 1
- JWTYDFNVTXWZAZ-AEAWWFNXSA-N N#CC([C@H](CCC1)[C@@H]1O)(C1CCN(Cc2ccccc2)CC1)c1ccccc1 Chemical compound N#CC([C@H](CCC1)[C@@H]1O)(C1CCN(Cc2ccccc2)CC1)c1ccccc1 JWTYDFNVTXWZAZ-AEAWWFNXSA-N 0.000 description 1
- GYGWKIHINPEOAM-UHFFFAOYSA-N O=S(C(F)(F)F)(c(cc1)ccc1F)=O Chemical compound O=S(C(F)(F)F)(c(cc1)ccc1F)=O GYGWKIHINPEOAM-UHFFFAOYSA-N 0.000 description 1
- GVMCBTFAQSEFQY-UHFFFAOYSA-N O=S(c(cc1)ccc1F)(c1ccncc1)=O Chemical compound O=S(c(cc1)ccc1F)(c1ccncc1)=O GVMCBTFAQSEFQY-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
- 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
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662330350P | 2016-05-02 | 2016-05-02 | |
| US62/330,350 | 2016-05-02 | ||
| PCT/US2017/030577 WO2017192543A1 (en) | 2016-05-02 | 2017-05-02 | Piperidines as menin inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019514950A JP2019514950A (ja) | 2019-06-06 |
| JP2019514950A5 JP2019514950A5 (cg-RX-API-DMAC7.html) | 2020-06-18 |
| JP6991585B2 true JP6991585B2 (ja) | 2022-01-12 |
Family
ID=58699299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018557418A Expired - Fee Related JP6991585B2 (ja) | 2016-05-02 | 2017-05-02 | メニン阻害剤としてのピペリジン |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10899738B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3452461B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6991585B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR20190015275A (cg-RX-API-DMAC7.html) |
| CN (1) | CN109415337B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2017259436B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BR112018072570A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA3022868A1 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2899936T3 (cg-RX-API-DMAC7.html) |
| IL (2) | IL262697B (cg-RX-API-DMAC7.html) |
| MX (1) | MX384087B (cg-RX-API-DMAC7.html) |
| SG (1) | SG11201809714TA (cg-RX-API-DMAC7.html) |
| WO (1) | WO2017192543A1 (cg-RX-API-DMAC7.html) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020515571A (ja) * | 2017-03-31 | 2020-05-28 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | 共有結合性メニン阻害剤としてのピペリジン |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016040330A1 (en) | 2014-09-09 | 2016-03-17 | The Regents Of The University Of Michigan | Thienopyrimidine and thienopyridine compounds and methods of use thereof |
| TWI703150B (zh) | 2015-06-04 | 2020-09-01 | 美商庫拉腫瘤技術股份有限公司 | 用於抑制menin及mll蛋白之交互作用的方法及組合物 |
| US10588907B2 (en) | 2015-06-04 | 2020-03-17 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| SI3429591T1 (sl) | 2016-03-16 | 2023-07-31 | Kura Oncology, Inc. | Substituirani tieno(2,3-d)pirimidinski derivati kot inhibitorji menin-MLL in postopki uporabe |
| PH12018501955B1 (en) | 2016-03-16 | 2024-01-24 | Kura Oncology Inc | Bridged bicyclic inhibitors of menin-mll and methods of use |
| WO2017192543A1 (en) | 2016-05-02 | 2017-11-09 | Regents Of The University Of Michigan | Piperidines as menin inhibitors |
| JP7007302B2 (ja) | 2016-06-10 | 2022-01-24 | ヴァイティー ファーマシューティカルズ,エルエルシー | メニン-mll相互作用の阻害剤 |
| MX392051B (es) | 2016-09-14 | 2025-03-21 | Janssen Pharmaceutica Nv | Inhibidores espirobiciclicos de la interaccion de menina-mll |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| CA3033020A1 (en) | 2016-09-14 | 2018-03-22 | Janssen Pharmaceutica Nv | Fused bicyclic inhibitors of menin-mll interaction |
| JP7142010B2 (ja) | 2016-12-15 | 2022-09-26 | ヤンセン ファーマシューティカ エヌ.ベー. | メニン-mll相互作用のアゼパン阻害剤 |
| CN110691779B (zh) | 2017-03-24 | 2023-10-10 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
| US11542248B2 (en) | 2017-06-08 | 2023-01-03 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| WO2019060365A1 (en) | 2017-09-20 | 2019-03-28 | Kura Oncology, Inc. | SUBSTITUTED MÉNINE-MLL INHIBITORS AND METHODS OF USE |
| US11396517B1 (en) | 2017-12-20 | 2022-07-26 | Janssen Pharmaceutica Nv | Exo-aza spiro inhibitors of menin-MLL interaction |
| CN112105621B (zh) | 2018-03-30 | 2024-02-20 | 住友制药株式会社 | 光学活性桥型环状仲胺衍生物 |
| CN111936465A (zh) * | 2018-03-30 | 2020-11-13 | 密歇根大学董事会 | 作为共价menin抑制剂的哌啶化合物 |
| EP3856173A4 (en) * | 2018-09-26 | 2022-07-06 | Kura Oncology, Inc. | TREATMENT OF HEMOPATHY MALIGNANCE WITH MENIN INHIBITORS |
| SG11202101733TA (en) | 2018-10-03 | 2021-03-30 | Univ Michigan Regents | Small molecule menin inhibitors |
| US11174263B2 (en) | 2018-12-31 | 2021-11-16 | Biomea Fusion, Inc. | Inhibitors of menin-MLL interaction |
| JP7536767B2 (ja) | 2018-12-31 | 2024-08-20 | バイオメア フュージョン,インコーポレイテッド | メニン-mll相互作用の不可逆的阻害剤 |
| WO2021067215A1 (en) | 2019-09-30 | 2021-04-08 | Agios Pharmaceuticals, Inc. | Piperidine compounds as menin inhibitors |
| UA129208C2 (uk) | 2019-12-19 | 2025-02-05 | Янссен Фармацевтика Нв | Заміщені спіропохідні з прямим ланцюгом |
| TW202204334A (zh) | 2020-04-08 | 2022-02-01 | 美商阿吉歐斯製藥公司 | Menin抑制劑及治療癌症之使用方法 |
| TW202204333A (zh) | 2020-04-08 | 2022-02-01 | 美商阿吉歐斯製藥公司 | Menin抑制劑及治療癌症之使用方法 |
| EP4334320A1 (en) | 2021-05-08 | 2024-03-13 | JANSSEN Pharmaceutica NV | Substituted spiro derivatives |
| KR20240006542A (ko) | 2021-05-08 | 2024-01-15 | 얀센 파마슈티카 엔브이 | 치환된 스피로 유도체 |
| EP4337329A4 (en) * | 2021-05-12 | 2025-01-01 | Syndax Pharmaceuticals, Inc. | COMBINATIONS FOR CANCER TREATMENT |
| CR20230605A (es) | 2021-06-01 | 2024-05-24 | Janssen Pharmaceutica Nv | Derivados de fenil-1h-pirrolo[2,3-c]piridina sustituidos |
| US20250333421A1 (en) | 2021-06-03 | 2025-10-30 | Janssen Pharmaceutica Nv | Pyridazines or 1,2,4-triazines substituted by spirocyclic amines |
| IL309359A (en) | 2021-06-17 | 2024-02-01 | Janssen Pharmaceutica Nv | (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cancer |
| TW202320796A (zh) | 2021-08-11 | 2023-06-01 | 美商拜歐米富士恩股份有限公司 | 用於糖尿病的menin-mll相互作用之共價抑制劑 |
| TW202313004A (zh) | 2021-08-20 | 2023-04-01 | 美商拜歐米富士恩股份有限公司 | Menin-mll相互作用之不可逆抑制劑的結晶形式 |
| WO2023056589A1 (en) | 2021-10-08 | 2023-04-13 | Servier Pharmaceuticals Llc | Menin inhibitors and methods of use for treating cancer |
| EP4525873A1 (en) * | 2022-05-17 | 2025-03-26 | Biomea Fusion, Inc. | Flt3 combination therapy for cancer and compositions therefor |
| KR20250109775A (ko) | 2022-11-24 | 2025-07-17 | 오리존 지노믹스 에스.에이. | 암 치료를 위한 lsd1 억제제 및 메닌 억제제의 조합 |
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| JP2020515571A (ja) * | 2017-03-31 | 2020-05-28 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | 共有結合性メニン阻害剤としてのピペリジン |
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| CN109415337B (zh) | 2022-01-18 |
| WO2017192543A1 (en) | 2017-11-09 |
| BR112018072570A2 (pt) | 2019-02-19 |
| CA3022868A1 (en) | 2017-11-09 |
| KR20190015275A (ko) | 2019-02-13 |
| US20210198237A1 (en) | 2021-07-01 |
| IL262697A (en) | 2018-12-31 |
| JP2019514950A (ja) | 2019-06-06 |
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| US10899738B2 (en) | 2021-01-26 |
| SG11201809714TA (en) | 2018-11-29 |
| ES2899936T3 (es) | 2022-03-15 |
| IL262697B (en) | 2021-04-29 |
| IL281182A (en) | 2021-04-29 |
| MX2018013433A (es) | 2019-07-18 |
| AU2017259436B2 (en) | 2021-08-26 |
| AU2017259436A1 (en) | 2018-12-20 |
| CN109415337A (zh) | 2019-03-01 |
| EP3452461B1 (en) | 2021-09-08 |
| EP3452461A1 (en) | 2019-03-13 |
| US20190152947A1 (en) | 2019-05-23 |
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