CN107428765B - 用作irak抑制剂的哒嗪酮类大环化合物及其用途 - Google Patents
用作irak抑制剂的哒嗪酮类大环化合物及其用途 Download PDFInfo
- Publication number
- CN107428765B CN107428765B CN201680018681.1A CN201680018681A CN107428765B CN 107428765 B CN107428765 B CN 107428765B CN 201680018681 A CN201680018681 A CN 201680018681A CN 107428765 B CN107428765 B CN 107428765B
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- Prior art keywords
- compound
- disease
- compounds
- cancer
- irak
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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
- C07D487/12—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
- C07D487/18—Bridged 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D471/18—Bridged systems
-
- 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
- C07D471/22—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 systems contains four 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
- C07D487/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Nutrition Science (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562112793P | 2015-02-06 | 2015-02-06 | |
| US62/112,793 | 2015-02-06 | ||
| PCT/US2016/016708 WO2016127024A1 (en) | 2015-02-06 | 2016-02-05 | Pyridazinone macrocycles as irak inhibitors and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107428765A CN107428765A (zh) | 2017-12-01 |
| CN107428765B true CN107428765B (zh) | 2020-12-29 |
Family
ID=55436166
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680018681.1A Expired - Fee Related CN107428765B (zh) | 2015-02-06 | 2016-02-05 | 用作irak抑制剂的哒嗪酮类大环化合物及其用途 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9624246B2 (enExample) |
| EP (1) | EP3253763B1 (enExample) |
| JP (1) | JP6920202B2 (enExample) |
| KR (1) | KR102551597B1 (enExample) |
| CN (1) | CN107428765B (enExample) |
| AU (1) | AU2016215184B2 (enExample) |
| BR (1) | BR112017014970B1 (enExample) |
| CA (1) | CA2970550C (enExample) |
| ES (1) | ES2841452T3 (enExample) |
| IL (1) | IL253519B (enExample) |
| MX (1) | MX380929B (enExample) |
| RU (1) | RU2708066C2 (enExample) |
| SG (1) | SG11201704651UA (enExample) |
| WO (1) | WO2016127024A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2708066C2 (ru) * | 2015-02-06 | 2019-12-04 | Мерк Патент Гмбх | Макроциклы пиридазинона в качестве ингибиторов irak-киназы и их применения |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| WO2019111218A1 (en) | 2017-12-08 | 2019-06-13 | Cadila Healthcare Limited | Novel heterocyclic compounds as irak4 inhibitors |
| CN109956957B (zh) * | 2017-12-22 | 2021-11-09 | 广州白云山医药集团股份有限公司白云山制药总厂 | 一种咪唑并[1,2-b]哒嗪大环类激酶抑制剂 |
| IL277408B2 (en) * | 2018-04-05 | 2024-08-01 | Merck Patent Gmbh | Heteroaryl compounds as type ii irak inhibitors and uses thereof |
| TWI842978B (zh) | 2018-07-13 | 2024-05-21 | 美商基利科學股份有限公司 | 衍生物 |
| TWI727392B (zh) | 2018-08-13 | 2021-05-11 | 美商基利科學股份有限公司 | 噻二唑irak4抑制劑 |
| JP7169429B2 (ja) | 2018-08-13 | 2022-11-10 | ギリアード サイエンシーズ， インコーポレイテッド | ＩＲＡＫ４阻害剤としてのピロロ［１，２－ｂ］ピリダジン誘導体 |
| WO2020036830A1 (en) | 2018-08-13 | 2020-02-20 | Gilead Sciences, Inc. | Pyrrolo[1,2-b]pyridazine derivatives as irak4 inhibitors |
| US11998534B2 (en) * | 2020-02-12 | 2024-06-04 | Eubulus Biotherapeutics Inc. | GPX4 inhibitor in combination with anticancer agent for treating proliferative disease |
| CN111603471B (zh) * | 2020-06-24 | 2021-07-09 | 山东省科学院生物研究所 | 一种邻二氮杂环化合物在制备抑制tlr4受体的药物中的用途 |
| KR102871840B1 (ko) * | 2020-09-30 | 2025-10-15 | 아사히 가세이 파마 가부시키가이샤 | 거대고리 화합물 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014058691A1 (en) * | 2012-10-08 | 2014-04-17 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| WO2014121942A1 (en) * | 2013-02-07 | 2014-08-14 | Merck Patent Gmbh | Macrocyclic pyridazinone derivatives |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000247959A (ja) * | 1999-02-26 | 2000-09-12 | Kowa Co | ピリダジン−３−オン誘導体及びこれを含有する医薬 |
| JP2010138073A (ja) * | 2007-03-30 | 2010-06-24 | Taisho Pharmaceutical Co Ltd | ピコリン酸アミド化合物 |
| US8703768B2 (en) * | 2010-06-09 | 2014-04-22 | Hoffmann-La Roche Inc. | Nitrogen containing heteroaryl compounds |
| US9567320B2 (en) * | 2013-02-07 | 2017-02-14 | Merck Patent Gmbh | Pyridazinone-amides derivatives |
| RU2708066C2 (ru) * | 2015-02-06 | 2019-12-04 | Мерк Патент Гмбх | Макроциклы пиридазинона в качестве ингибиторов irak-киназы и их применения |
-
2016
- 2016-02-05 RU RU2017130761A patent/RU2708066C2/ru active
- 2016-02-05 AU AU2016215184A patent/AU2016215184B2/en not_active Ceased
- 2016-02-05 ES ES16706471T patent/ES2841452T3/es active Active
- 2016-02-05 EP EP16706471.6A patent/EP3253763B1/en active Active
- 2016-02-05 BR BR112017014970-2A patent/BR112017014970B1/pt not_active IP Right Cessation
- 2016-02-05 MX MX2017009624A patent/MX380929B/es unknown
- 2016-02-05 KR KR1020177020262A patent/KR102551597B1/ko active Active
- 2016-02-05 SG SG11201704651UA patent/SG11201704651UA/en unknown
- 2016-02-05 CA CA2970550A patent/CA2970550C/en active Active
- 2016-02-05 WO PCT/US2016/016708 patent/WO2016127024A1/en not_active Ceased
- 2016-02-05 US US15/016,584 patent/US9624246B2/en not_active Expired - Fee Related
- 2016-02-05 JP JP2017539435A patent/JP6920202B2/ja not_active Expired - Fee Related
- 2016-02-05 CN CN201680018681.1A patent/CN107428765B/zh not_active Expired - Fee Related
-
2017
- 2017-03-06 US US15/450,463 patent/US10517872B2/en active Active
- 2017-07-17 IL IL253519A patent/IL253519B/en active IP Right Grant
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014058691A1 (en) * | 2012-10-08 | 2014-04-17 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| WO2014121942A1 (en) * | 2013-02-07 | 2014-08-14 | Merck Patent Gmbh | Macrocyclic pyridazinone derivatives |
Also Published As
| Publication number | Publication date |
|---|---|
| JP6920202B2 (ja) | 2021-08-18 |
| SG11201704651UA (en) | 2017-07-28 |
| US10517872B2 (en) | 2019-12-31 |
| ES2841452T3 (es) | 2021-07-08 |
| IL253519A0 (en) | 2017-09-28 |
| US20160229871A1 (en) | 2016-08-11 |
| EP3253763B1 (en) | 2020-09-30 |
| WO2016127024A1 (en) | 2016-08-11 |
| IL253519B (en) | 2021-01-31 |
| CA2970550A1 (en) | 2016-08-11 |
| EP3253763A1 (en) | 2017-12-13 |
| AU2016215184A1 (en) | 2017-06-29 |
| US20170173019A1 (en) | 2017-06-22 |
| KR102551597B1 (ko) | 2023-07-05 |
| RU2708066C2 (ru) | 2019-12-04 |
| BR112017014970B1 (pt) | 2022-11-16 |
| CN107428765A (zh) | 2017-12-01 |
| KR20170113551A (ko) | 2017-10-12 |
| RU2017130761A (ru) | 2019-03-06 |
| CA2970550C (en) | 2023-09-19 |
| AU2016215184B2 (en) | 2020-11-12 |
| JP2018505166A (ja) | 2018-02-22 |
| HK1246287A1 (zh) | 2018-09-07 |
| MX380929B (es) | 2025-03-12 |
| RU2017130761A3 (enExample) | 2019-07-17 |
| MX2017009624A (es) | 2017-11-20 |
| US9624246B2 (en) | 2017-04-18 |
| NZ732527A (en) | 2022-03-25 |
| BR112017014970A2 (pt) | 2018-03-27 |
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