JO3295B1 - بنزوثينيل- بيرولوترايازينات مستبدلة ثنائيا واستخداماتها - Google Patents
بنزوثينيل- بيرولوترايازينات مستبدلة ثنائيا واستخداماتهاInfo
- Publication number
- JO3295B1 JO3295B1 JOP/2012/0377A JOP20120377A JO3295B1 JO 3295 B1 JO3295 B1 JO 3295B1 JO P20120377 A JOP20120377 A JO P20120377A JO 3295 B1 JO3295 B1 JO 3295B1
- Authority
- JO
- Jordan
- Prior art keywords
- pyrrolotriazines
- compounds
- benzothienyl
- disubstituted
- prepa
- Prior art date
Links
- SSTMBTQFNVRJDU-UHFFFAOYSA-N C1=CC=C2SC(C=3N=NNC4=CC=NC4=3)=CC2=C1 Chemical class C1=CC=C2SC(C=3N=NNC4=CC=NC4=3)=CC2=C1 SSTMBTQFNVRJDU-UHFFFAOYSA-N 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- KVBXVOSVQPIXSL-UHFFFAOYSA-N 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical class C1=CC=C2SC(C=3C=CN4N=CN=C(C=34)N)=CC2=C1 KVBXVOSVQPIXSL-UHFFFAOYSA-N 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/5355—Non-condensed oxazines and 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
- A61K31/535—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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines 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
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Treatment Of Liquids With Adsorbents In General (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
يتعلق الاختراع الحالي بمشتقات 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]-triazin-4-amine مستبدلة جديدة لها نشاطات مثبطة لأجل protein tyrosine kinase، بعمليات لتحضير هذه المركبات، بتركيبات دوائية (pharmaceutical compositions) تحتوي على هذه المركبات، وباستخدام هذه المركبات أو التركيبات لمعالجة اضطرابات انقسامية، تحديدا السرطان وأمراض الورم.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193841 | 2011-12-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3295B1 true JO3295B1 (ar) | 2018-09-16 |
Family
ID=47326168
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2012/0377A JO3295B1 (ar) | 2011-12-15 | 2012-12-12 | بنزوثينيل- بيرولوترايازينات مستبدلة ثنائيا واستخداماتها |
Country Status (42)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10388493B2 (en) | 2011-09-16 | 2019-08-20 | Lam Research Corporation | Component of a substrate support assembly producing localized magnetic fields |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
| TW201536293A (zh) | 2013-07-18 | 2015-10-01 | Taiho Pharmaceutical Co Ltd | 對ｆｇｆｒ抑制劑具耐受性之癌的治療藥 |
| EP3023100B1 (en) | 2013-07-18 | 2019-03-13 | Taiho Pharmaceutical Co., Ltd. | Antitumor drug for intermittent administration of fgfr inhibitor |
| PT3060562T (pt) * | 2013-10-21 | 2021-09-02 | Genosco | Compostos de pirimidina substituídos e sua utilização como inibidores da syk |
| MX2017007656A (es) * | 2014-12-11 | 2017-10-11 | Bayer Pharma AG | Uso de los inhibidores de pan fgfr y metodo para identificacion de pacientes con cancer elegibles para el tratamiento con un inhibidor de pan fgfr. |
| EP3268490B1 (en) | 2015-03-09 | 2020-07-08 | Bayer Pharma Aktiengesellschaft | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations |
| US10221191B2 (en) | 2015-12-22 | 2019-03-05 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| KR102793563B1 (ko) | 2016-03-04 | 2025-04-11 | 다이호야쿠힌고교 가부시키가이샤 | 악성 종양 치료용 제제 및 조성물 |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| JP7034084B2 (ja) | 2016-03-28 | 2022-03-11 | インサイト・コーポレイション | Ｔａｍ阻害剤としてのピロロトリアジン化合物 |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| RU2753056C2 (ru) | 2016-12-16 | 2021-08-11 | Систик Файбросис Фаундейшн | Бициклические гетероарильные производные в качестве стимуляторов cftr |
| SG11201911929XA (en) | 2017-06-21 | 2020-01-30 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| WO2019034075A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr和egfr抑制剂 |
| KR102707041B1 (ko) * | 2017-08-15 | 2024-09-19 | 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 | Fgfr 억제제 및 그의 의학적 용도 |
| CA3077308A1 (en) | 2017-09-27 | 2019-04-04 | Incyte Corporation | Salts of pyrrolotriazine derivatives useful as tam inhibitors |
| AU2018354780A1 (en) * | 2017-10-25 | 2020-04-09 | Bayer Pharma Aktiengesellschaft | Process for preparing benzothiophen-2yl boronate |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| EP4353222A1 (en) | 2018-03-19 | 2024-04-17 | Taiho Pharmaceutical Co., Ltd. | Use of sodium alkyl sulfate |
| WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
| EA202190153A1 (ru) | 2018-06-29 | 2021-04-09 | Инсайт Корпорейшн | Составы ингибитора axl/mer |
| WO2020132071A1 (en) | 2018-12-19 | 2020-06-25 | Shy Therapeutics. Llc | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and f1brotic disease |
| MX2021009173A (es) * | 2019-01-31 | 2021-09-10 | Bayer Ag | El monohidrato de clorhidrato de rogaratinib y estados solidos del mismo. |
| CA3130247C (en) | 2019-02-15 | 2024-02-13 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd | Fgfr inhibitor compound in solid form and preparation method therefor |
| WO2020170355A1 (ja) * | 2019-02-20 | 2020-08-27 | 大鵬薬品工業株式会社 | Ｆｇｆｒ１変異腫瘍の治療方法 |
| CN109928976A (zh) * | 2019-02-26 | 2019-06-25 | 泰州亿腾景昂药业有限公司 | 一种工业化生产eoc317的方法 |
| ES2974985T3 (es) * | 2019-05-13 | 2024-07-02 | Relay Therapeutics Inc | Inhibidores de FGFR y métodos de uso de los mismos |
| CN114641293B (zh) * | 2019-11-08 | 2024-05-31 | 石药集团中奇制药技术（石家庄）有限公司 | 一种fgfr抑制剂的用途 |
| CN111004234A (zh) * | 2019-11-28 | 2020-04-14 | 湖南农业大学 | 一种2-苯基咪唑并[1,2-α]吡啶类化合物的C3位卤化方法 |
| AU2021230385A1 (en) | 2020-03-06 | 2022-09-22 | Incyte Corporation | Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors |
| CN117402161A (zh) * | 2022-07-06 | 2024-01-16 | 上海科恩泰生物医药科技有限公司 | 一种具有fgfr抑制作用的亚砜亚胺类化合物、包含其的药物组合物及其用途 |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ516292A (en) * | 1999-05-21 | 2004-01-30 | Bristol Myers Squibb Co | Pyrrolotriazine inhibitors of kinases |
| NZ517759A (en) | 1999-09-17 | 2004-04-30 | Abbott Gmbh & Co | Kinase inhibitors as therapeutic agents |
| WO2004096806A1 (ja) * | 2003-04-30 | 2004-11-11 | Sumitomo Pharmaceuticals Co. Ltd. | 縮合イミダゾール誘導体 |
| DE10327439A1 (de) * | 2003-06-18 | 2005-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Imidazopyridazinon- und Imidazopyridonderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| EP2168968B1 (en) | 2004-04-02 | 2017-08-23 | OSI Pharmaceuticals, LLC | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
| UY28931A1 (es) | 2004-06-03 | 2005-12-30 | Bayer Pharmaceuticals Corp | Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis |
| TW200635927A (en) * | 2004-12-22 | 2006-10-16 | Bristol Myers Squibb Co | Synthetic process |
| WO2007056170A2 (en) | 2005-11-02 | 2007-05-18 | Bayer Healthcare Ag | Pyrrolo[2,1-f] [1,2,4] triazin-4-ylamines igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases |
| AU2006316605B2 (en) * | 2005-11-17 | 2012-04-26 | Osi Pharmaceuticals, Inc. | Fused bicyclic mTOR inhibitors |
| US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| CN101448506A (zh) | 2005-12-02 | 2009-06-03 | 拜尔健康护理有限责任公司 | 通过抑制有丝分裂酶激酶治疗癌症的吡咯并三嗪衍生物 |
| KR20130141706A (ko) | 2005-12-02 | 2013-12-26 | 바이엘 헬스케어 엘엘씨 | 과다-증식성 장애 및 맥관형성과 관련된 질환의 치료에 유용한 치환된 4-아미노-피롤로트리아진 유도체 |
| PE20070855A1 (es) * | 2005-12-02 | 2007-10-14 | Bayer Pharmaceuticals Corp | Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas |
| TW201307354A (zh) * | 2005-12-29 | 2013-02-16 | Abbott Lab | 蛋白質激酶抑制劑 |
| US8124759B2 (en) | 2007-05-09 | 2012-02-28 | Abbott Laboratories | Inhibitors of protein kinases |
| US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
| US8765754B2 (en) | 2009-04-29 | 2014-07-01 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
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2012
- 2012-12-03 UY UY0001034484A patent/UY34484A/es unknown
- 2012-12-10 MX MX2014006905A patent/MX367158B/es active IP Right Grant
- 2012-12-10 SI SI201230702A patent/SI2791140T1/sl unknown
- 2012-12-10 DK DK12798738.6T patent/DK2791140T3/en active
- 2012-12-10 BR BR112014014531-8A patent/BR112014014531B1/pt not_active IP Right Cessation
- 2012-12-10 UA UAA201407930A patent/UA116768C2/uk unknown
- 2012-12-10 LT LTEP12798738.6T patent/LT2791140T/lt unknown
- 2012-12-10 CN CN201280069882.6A patent/CN104245700B/zh not_active Expired - Fee Related
- 2012-12-10 US US14/365,424 patent/US20140336173A1/en not_active Abandoned
- 2012-12-10 IN IN4310CHN2014 patent/IN2014CN04310A/en unknown
- 2012-12-10 RS RS20160733A patent/RS55144B1/sr unknown
- 2012-12-10 EP EP12798738.6A patent/EP2791140B1/en active Active
- 2012-12-10 PL PL12798738T patent/PL2791140T3/pl unknown
- 2012-12-10 AU AU2012350750A patent/AU2012350750B2/en not_active Ceased
- 2012-12-10 MY MYPI2014701550A patent/MY178660A/en unknown
- 2012-12-10 SG SG11201402325QA patent/SG11201402325QA/en unknown
- 2012-12-10 EA EA201400707A patent/EA029556B1/ru not_active IP Right Cessation
- 2012-12-10 JP JP2014546445A patent/JP6050829B2/ja not_active Expired - Fee Related
- 2012-12-10 ES ES12798738.6T patent/ES2591203T3/es active Active
- 2012-12-10 KR KR1020147019406A patent/KR102057444B1/ko not_active Expired - Fee Related
- 2012-12-10 PT PT127987386T patent/PT2791140T/pt unknown
- 2012-12-10 HU HUE12798738A patent/HUE029582T2/en unknown
- 2012-12-10 PE PE2014000926A patent/PE20141855A1/es active IP Right Grant
- 2012-12-10 WO PCT/EP2012/074977 patent/WO2013087578A1/en not_active Ceased
- 2012-12-10 CU CU2016000039A patent/CU24426B1/es unknown
- 2012-12-10 ME MEP-2016-181A patent/ME02517B/me unknown
- 2012-12-10 CA CA2859133A patent/CA2859133C/en active Active
- 2012-12-10 HR HRP20161130TT patent/HRP20161130T1/hr unknown
- 2012-12-12 JO JOP/2012/0377A patent/JO3295B1/ar active
- 2012-12-12 AR ARP120104679A patent/AR089207A1/es unknown
- 2012-12-14 TW TW101147336A patent/TWI567076B/zh not_active IP Right Cessation
- 2012-12-14 US US13/715,553 patent/US9206184B2/en active Active
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2014
- 2014-05-14 IL IL232611A patent/IL232611A/en active IP Right Grant
- 2014-06-09 CO CO14123802A patent/CO7030961A2/es unknown
- 2014-06-09 CU CUP2014000065A patent/CU20140065A7/es unknown
- 2014-06-10 DO DO2014000127A patent/DOP2014000127A/es unknown
- 2014-06-11 TN TNP2014000255A patent/TN2014000255A1/en unknown
- 2014-06-12 CL CL2014001547A patent/CL2014001547A1/es unknown
- 2014-06-12 EC ECIEPI20144722A patent/ECSP14004722A/es unknown
- 2014-06-13 GT GT201400113A patent/GT201400113A/es unknown
- 2014-06-13 PH PH12014501355A patent/PH12014501355B1/en unknown
- 2014-06-17 CR CR20140288A patent/CR20140288A/es unknown
- 2014-07-14 ZA ZA2014/05140A patent/ZA201405140B/en unknown
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2016
- 2016-08-31 CY CY20161100853T patent/CY1118112T1/el unknown
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2017
- 2017-07-17 AU AU2017206140A patent/AU2017206140A1/en not_active Abandoned
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2018
- 2018-02-20 US US15/900,725 patent/US20190016724A1/en not_active Abandoned
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2019
- 2019-06-18 AU AU2019204255A patent/AU2019204255A1/en not_active Abandoned
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2021
- 2021-11-01 US US17/516,542 patent/US20220153745A1/en not_active Abandoned
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