SG11201700579XA - Cyclohexyl-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (ido) antagonists for the treatment of cancer - Google Patents
Cyclohexyl-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (ido) antagonists for the treatment of cancerInfo
- Publication number
- SG11201700579XA SG11201700579XA SG11201700579XA SG11201700579XA SG11201700579XA SG 11201700579X A SG11201700579X A SG 11201700579XA SG 11201700579X A SG11201700579X A SG 11201700579XA SG 11201700579X A SG11201700579X A SG 11201700579XA SG 11201700579X A SG11201700579X A SG 11201700579XA
- Authority
- SG
- Singapore
- Prior art keywords
- triaza
- ido
- dioxygenase
- indole
- antagonists
- Prior art date
Links
Classifications
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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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/44—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
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
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- 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
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462046242P | 2014-09-05 | 2014-09-05 | |
| US201562151011P | 2015-04-22 | 2015-04-22 | |
| PCT/US2015/048474 WO2016037026A1 (en) | 2014-09-05 | 2015-09-04 | Cyclohexyl-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (ido) antagonists for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201700579XA true SG11201700579XA (en) | 2017-02-27 |
Family
ID=54147306
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG10201804868PA SG10201804868PA (en) | 2014-09-05 | 2015-09-04 | Compounds for the inhibition of indoleamine-2,3-dioxygenase |
| SG11201700579XA SG11201700579XA (en) | 2014-09-05 | 2015-09-04 | Cyclohexyl-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (ido) antagonists for the treatment of cancer |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG10201804868PA SG10201804868PA (en) | 2014-09-05 | 2015-09-04 | Compounds for the inhibition of indoleamine-2,3-dioxygenase |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US9771370B2 (en) |
| EP (1) | EP3189054B1 (en) |
| JP (1) | JP6680766B2 (en) |
| KR (1) | KR20170044144A (en) |
| CN (1) | CN107074859B (en) |
| AU (1) | AU2015311826B2 (en) |
| BR (1) | BR112017003764A2 (en) |
| CA (1) | CA2956465A1 (en) |
| CL (1) | CL2017000420A1 (en) |
| ES (1) | ES2751602T3 (en) |
| IL (1) | IL250890B (en) |
| MX (1) | MX2017002365A (en) |
| PH (1) | PH12017500196A1 (en) |
| RU (1) | RU2017111200A (en) |
| SG (2) | SG10201804868PA (en) |
| WO (1) | WO2016037026A1 (en) |
| ZA (1) | ZA201700737B (en) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| EP3189054B1 (en) * | 2014-09-05 | 2019-07-24 | Merck Patent GmbH | (1-fluoro-cyclohex-1-yl)-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (ido) antagonists for the treatment of cancer |
| CN105884828A (en) * | 2015-02-16 | 2016-08-24 | 上海迪诺医药科技有限公司 | Polycyclic compound, pharmaceutical composition and application thereof |
| US10358451B2 (en) | 2015-04-12 | 2019-07-23 | Hangzhou Innogate Pharma Co., Ltd. | Heterocycles useful as IDO and TDO inhibitors |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| WO2017075341A1 (en) * | 2015-10-29 | 2017-05-04 | Scifluor Life Sciences, Inc. | Fused imidazole derivatives as ido/tdo inhibitors |
| WO2017134555A1 (en) | 2016-02-02 | 2017-08-10 | Emcure Pharmaceuticals Limited | Derivatives of pyrroloimidazole or analogues thereof which are useful for the treatment of inter alia cancer |
| WO2017149469A1 (en) | 2016-03-03 | 2017-09-08 | Emcure Pharmaceuticals Limited | Heterocyclic compounds useful as ido and/or tdo modulators |
| CN105732643A (en) * | 2016-04-18 | 2016-07-06 | 苏州大学 | Conjugate and preparation method thereof and application to preparation of IDO enzyme inhibitor and non-steroidal anti-inflammatory drugs |
| CN107312005B (en) * | 2016-04-27 | 2021-12-17 | 上海翰森生物医药科技有限公司 | Fused imidazole derivative with IDO/TDO inhibitory activity and preparation method and application thereof |
| CN107383012B (en) * | 2016-05-16 | 2021-09-28 | 鲁南制药集团股份有限公司 | Bicyclic imidazole alcohol derivatives |
| WO2017198159A1 (en) * | 2016-05-16 | 2017-11-23 | 鲁南制药集团股份有限公司 | Imidazole derivative containing bridge ring |
| CN105902542A (en) * | 2016-05-16 | 2016-08-31 | 张阳 | Application of conjugate in preparation of medicine for treating cardiovascular diseases |
| CN107556316B (en) * | 2016-06-30 | 2021-11-12 | 鲁南制药集团股份有限公司 | Bridged ring-containing imidazole derivatives |
| WO2018028491A1 (en) * | 2016-08-09 | 2018-02-15 | 苏州国匡医药科技有限公司 | Indoleamine2,3-dioxygenase inhibitors and uses thereof in pharmacy |
| US11046682B2 (en) | 2016-08-23 | 2021-06-29 | Beijing Innocare Pharma Tech Co., Ltd. | Fused heterocyclic derivatives, their preparation methods thereof and medical uses thereof |
| CN107383024B (en) * | 2016-09-12 | 2018-06-08 | 广州必贝特医药技术有限公司 | The class compound of fused tricyclic containing imidazoles and its application |
| EP3515914A4 (en) | 2016-09-24 | 2020-04-15 | BeiGene, Ltd. | NOVEL 5 or 8-SUBSTITUTED IMIDAZO [1, 5-a]PYRIDINES AS SELECTIVE INHIBITORS OF INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES |
| CN108203438B (en) | 2016-12-20 | 2021-09-28 | 深圳微芯生物科技股份有限公司 | Fused imidazole compounds having indoleamine 2,3-dioxygenase inhibitory activity |
| KR102579849B1 (en) | 2016-12-22 | 2023-09-18 | 칼리테라 바이오사이언시즈, 인코포레이티드 | Compositions and methods for inhibiting arginase activity |
| JP2020506895A (en) | 2017-01-17 | 2020-03-05 | ボード オブ レジェンツ, ザ ユニバーシティ オブ テキサス システムBoard Of Regents, The University Of Texas System | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and / or tryptophan dioxygenase |
| WO2018175954A1 (en) * | 2017-03-23 | 2018-09-27 | F. Hoffmann-La Roche Ag | Synthesis of imidazo[5,1-a]isoindole derivative useful as ido inhibitors |
| SG11201909115WA (en) | 2017-04-05 | 2019-10-30 | Broad Inst Inc | Tricyclic compounds as glycogen synthase kinase 3 (gsk3) inhibitors and uses thereof |
| WO2019005559A1 (en) * | 2017-06-28 | 2019-01-03 | Genentech, Inc. | Tdo2 and ido1 inhibitors |
| CN109384791B (en) * | 2017-08-09 | 2020-09-11 | 江苏恒瑞医药股份有限公司 | Crystal form of imidazo isoindole derivative free alkali and preparation method thereof |
| CN107501272B (en) * | 2017-09-05 | 2020-03-31 | 中国药科大学 | Imidazoisoindole IDO1 inhibitor, and preparation method and application thereof |
| CN108424414A (en) * | 2017-12-08 | 2018-08-21 | 苏州国匡医药科技有限公司 | Indoleamine 2,3-dioxygenase modulating compound of the one kind containing heterocycle and its purposes in pharmacy |
| US20210002371A1 (en) * | 2017-12-21 | 2021-01-07 | Brian A. Sherer | Combination of an anti-pd-l1 antibody and ido1 inhibitor for the treatment of cancer |
| KR20200106513A (en) | 2018-01-05 | 2020-09-14 | 다이서나 파마수이티컬, 인크. | Reduction of beta-catenin and IDO expression to enhance immunotherapy |
| US11046649B2 (en) | 2018-07-17 | 2021-06-29 | Board Of Regents, The University Of Texas System | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
| EP4052705A1 (en) | 2021-03-05 | 2022-09-07 | Universität Basel Vizerektorat Forschung | Compositions for the treatment of ebv associated diseases or conditions |
| WO2022184930A2 (en) | 2021-03-05 | 2022-09-09 | Universität Basel | Compositions for the treatment of ebv associated diseases or conditions |
| CN113816965B (en) * | 2021-11-23 | 2022-03-08 | 北京鑫开元医药科技有限公司 | Compound with IDO (indomethacin diphosphate) inhibitory activity and preparation method thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002009706A1 (en) | 2000-07-27 | 2002-02-07 | Smithkline Beecham Corporation | Agonists of follicle stimulating hormone activity |
| US8541595B2 (en) * | 2008-11-13 | 2013-09-24 | Merch Sharp & Dohme Corp. | Imidazoisoindole neuropeptide S receptor antagonists |
| NO2694640T3 (en) * | 2011-04-15 | 2018-03-17 | ||
| RU2667509C2 (en) * | 2013-03-14 | 2018-09-21 | Ньюлинк Джинетикс Корпорейшин | Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization |
| EP3189054B1 (en) * | 2014-09-05 | 2019-07-24 | Merck Patent GmbH | (1-fluoro-cyclohex-1-yl)-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (ido) antagonists for the treatment of cancer |
| GB201418300D0 (en) * | 2014-10-15 | 2014-11-26 | Redx Pharma Ltd | Compounds |
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2015
- 2015-09-04 EP EP15766320.4A patent/EP3189054B1/en active Active
- 2015-09-04 ES ES15766320T patent/ES2751602T3/en active Active
- 2015-09-04 RU RU2017111200A patent/RU2017111200A/en not_active Application Discontinuation
- 2015-09-04 CA CA2956465A patent/CA2956465A1/en active Pending
- 2015-09-04 US US14/845,428 patent/US9771370B2/en active Active
- 2015-09-04 AU AU2015311826A patent/AU2015311826B2/en not_active Ceased
- 2015-09-04 SG SG10201804868PA patent/SG10201804868PA/en unknown
- 2015-09-04 BR BR112017003764A patent/BR112017003764A2/en not_active IP Right Cessation
- 2015-09-04 CN CN201580059548.6A patent/CN107074859B/en active Active
- 2015-09-04 MX MX2017002365A patent/MX2017002365A/en unknown
- 2015-09-04 KR KR1020177007060A patent/KR20170044144A/en unknown
- 2015-09-04 SG SG11201700579XA patent/SG11201700579XA/en unknown
- 2015-09-04 JP JP2017512706A patent/JP6680766B2/en active Active
- 2015-09-04 WO PCT/US2015/048474 patent/WO2016037026A1/en active Application Filing
-
2017
- 2017-01-30 ZA ZA2017/00737A patent/ZA201700737B/en unknown
- 2017-02-01 PH PH12017500196A patent/PH12017500196A1/en unknown
- 2017-02-21 CL CL2017000420A patent/CL2017000420A1/en unknown
- 2017-03-02 IL IL250890A patent/IL250890B/en active IP Right Grant
- 2017-08-18 US US15/680,683 patent/US10329297B2/en active Active
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| IL250890A0 (en) | 2017-04-30 |
| PH12017500196A1 (en) | 2017-07-10 |
| JP2017525742A (en) | 2017-09-07 |
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| US20160075711A1 (en) | 2016-03-17 |
| EP3189054B1 (en) | 2019-07-24 |
| MX2017002365A (en) | 2017-05-17 |
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| CN107074859B (en) | 2021-08-06 |
| US20170355703A1 (en) | 2017-12-14 |
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| US9771370B2 (en) | 2017-09-26 |
| US10329297B2 (en) | 2019-06-25 |
| EP3189054A1 (en) | 2017-07-12 |
| IL250890B (en) | 2019-12-31 |
| BR112017003764A2 (en) | 2017-12-05 |
| ZA201700737B (en) | 2019-04-24 |
| CN107074859A (en) | 2017-08-18 |
| SG10201804868PA (en) | 2018-07-30 |
| JP6680766B2 (en) | 2020-04-15 |
| AU2015311826B2 (en) | 2019-05-23 |
| CA2956465A1 (en) | 2016-03-10 |
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