BR112018072246A2 - síntese de indazóis - Google Patents
síntese de indazóisInfo
- Publication number
- BR112018072246A2 BR112018072246A2 BR112018072246-4A BR112018072246A BR112018072246A2 BR 112018072246 A2 BR112018072246 A2 BR 112018072246A2 BR 112018072246 A BR112018072246 A BR 112018072246A BR 112018072246 A2 BR112018072246 A2 BR 112018072246A2
- Authority
- BR
- Brazil
- Prior art keywords
- indazole
- indazole synthesis
- synthesis
- substituted
- intermediate compounds
- Prior art date
Links
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/86—Hydrazides; Thio or imino analogues thereof
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- 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
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- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
síntese de indazóis. a presente invenção refere-se a um novo método de preparação de um 2-indazol substituído da estrutura: , a compostos intermediários e ao uso de compostos intermediários para a preparação do dito 2-indazol substituído.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16167652.3 | 2016-04-29 | ||
| EP16167652 | 2016-04-29 | ||
| PCT/EP2017/059744 WO2017186689A1 (en) | 2016-04-29 | 2017-04-25 | Synthesis of indazoles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112018072246A2 true BR112018072246A2 (pt) | 2019-02-12 |
Family
ID=55860769
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112018072242-1A BR112018072242A2 (pt) | 2016-04-29 | 2017-04-25 | forma polimórfica de n-{6-(2-hidróxipropan-2-il)-2-[2-(metilsulfonil)etil]-2h-indazol-5-il}-6-(trifluorometil)piridina-2-carboxamida |
| BR112018072246-4A BR112018072246A2 (pt) | 2016-04-29 | 2017-04-25 | síntese de indazóis |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112018072242-1A BR112018072242A2 (pt) | 2016-04-29 | 2017-04-25 | forma polimórfica de n-{6-(2-hidróxipropan-2-il)-2-[2-(metilsulfonil)etil]-2h-indazol-5-il}-6-(trifluorometil)piridina-2-carboxamida |
Country Status (43)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3705B1 (ar) | 2014-11-26 | 2021-01-31 | Bayer Pharma AG | إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية |
| US10435396B2 (en) | 2016-03-03 | 2019-10-08 | Bayer Pharma Aktiegesellschaft | 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs |
| RS64928B1 (sr) * | 2016-04-29 | 2023-12-29 | Bayer Pharma AG | Polimorfni oblik n-{6-(2-hidroksipropan-2-il)-2-[2-(metilsulfonil)etil]-2h-indazol-5-il}-6-(trifluorometil)piridin-2-karboksamida |
| TN2018000359A1 (en) | 2016-04-29 | 2020-06-15 | Bayer Pharma AG | Crystalline forms of n-[2-(3-hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2h-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide. |
| CA3025847A1 (en) * | 2016-06-01 | 2017-12-07 | Bayer Animal Health Gmbh | Substituted indazoles ueful in the treatment of allergic dermatitis in animals |
| SG10202011653WA (en) | 2016-06-01 | 2020-12-30 | Bayer Pharma AG | Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| BR112020026507A8 (pt) | 2018-06-25 | 2023-01-31 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Composto de isotiazolo[5,4-d]pirimidinas como inibidor de irak4 |
| TWI721483B (zh) | 2018-07-13 | 2021-03-11 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| CN110981903A (zh) * | 2019-11-28 | 2020-04-10 | 南京正济医药研究有限公司 | 一种艾日布林中间体化合物提高光学纯度的精制方法 |
| US10947552B1 (en) | 2020-09-30 | 2021-03-16 | Alpine Roads, Inc. | Recombinant fusion proteins for producing milk proteins in plants |
| US10894812B1 (en) | 2020-09-30 | 2021-01-19 | Alpine Roads, Inc. | Recombinant milk proteins |
| CA3191387A1 (en) | 2020-09-30 | 2022-04-07 | Nobell Foods, Inc. | Recombinant milk proteins and food compositions comprising the same |
| CN114469979B (zh) * | 2021-12-15 | 2024-04-09 | 安徽贝克生物制药有限公司 | 一种核糖核苷类似物的药物组合物、吸入剂及其应用 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7163937B2 (en) | 2003-08-21 | 2007-01-16 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
| WO2007091107A1 (en) | 2006-02-10 | 2007-08-16 | Summit Corporation Plc | Treatment of duchenne muscular dystrophy |
| WO2008001883A1 (fr) | 2006-06-29 | 2008-01-03 | Nissan Chemical Industries, Ltd. | DÉRIVÉ D'ACIDE α-AMINÉ ET PRODUIT PHARMACEUTIQUE QUI LE COMPREND EN TANT QUE MATIÈRE ACTIVE |
| RU2459821C2 (ru) | 2006-09-07 | 2012-08-27 | Байоджен Айдек Ма Инк. | Модуляторы киназы, ассоциированной с рецептором интерлейкина-1 |
| JP5620393B2 (ja) | 2009-10-09 | 2014-11-05 | 田辺三菱製薬株式会社 | 脳梗塞治療薬 |
| WO2011153588A1 (en) | 2010-06-10 | 2011-12-15 | Biota Scientific Management Pty Ltd | Viral polymerase inhibitors |
| CA2822166C (en) | 2010-12-20 | 2019-10-29 | Merck Serono S.A. | Indazolyl triazole derivatives as irak inhibitors |
| WO2013106254A1 (en) | 2012-01-11 | 2013-07-18 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
| CA2929650C (en) | 2013-11-08 | 2017-08-22 | Iteos Therapeutics | 4-(indol-3-yl)-pyrazole derivatives, pharmaceutical compositions and methods for use |
| US9126984B2 (en) * | 2013-11-08 | 2015-09-08 | Iteos Therapeutics | 4-(indol-3-yl)-pyrazole derivatives, pharmaceutical compositions and methods for use |
| TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
| EA201691401A1 (ru) * | 2014-01-10 | 2016-11-30 | Ориджин Дискавери Текнолоджиз Лимитед | Индазольные соединения в качестве ингибиторов irak4 |
| JO3705B1 (ar) * | 2014-11-26 | 2021-01-31 | Bayer Pharma AG | إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية |
| CA2984259C (en) | 2015-04-30 | 2024-02-13 | Bayer Pharma Aktiengesellschaft | Combinations of inhibitors of irak4 with inhibitors of btk |
| BR112018000624A2 (pt) | 2015-07-15 | 2018-09-18 | Aurigene Discovery Technologies Limited | compostos de indazol e azaindazol como inibidores de irak-4 |
| US10435396B2 (en) | 2016-03-03 | 2019-10-08 | Bayer Pharma Aktiegesellschaft | 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs |
| EP3219329A1 (en) | 2016-03-17 | 2017-09-20 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib |
| TN2018000359A1 (en) | 2016-04-29 | 2020-06-15 | Bayer Pharma AG | Crystalline forms of n-[2-(3-hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2h-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide. |
| RS64928B1 (sr) | 2016-04-29 | 2023-12-29 | Bayer Pharma AG | Polimorfni oblik n-{6-(2-hidroksipropan-2-il)-2-[2-(metilsulfonil)etil]-2h-indazol-5-il}-6-(trifluorometil)piridin-2-karboksamida |
| CA3025847A1 (en) | 2016-06-01 | 2017-12-07 | Bayer Animal Health Gmbh | Substituted indazoles ueful in the treatment of allergic dermatitis in animals |
| SG10202011653WA (en) | 2016-06-01 | 2020-12-30 | Bayer Pharma AG | Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases |
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2017
- 2017-04-25 RS RS20231171A patent/RS64928B1/sr unknown
- 2017-04-25 LT LTEP17718558.4T patent/LT3448846T/lt unknown
- 2017-04-25 EP EP17718558.4A patent/EP3448846B1/en active Active
- 2017-04-25 KR KR1020187030699A patent/KR102373017B1/ko active IP Right Grant
- 2017-04-25 JP JP2018556408A patent/JP6954924B2/ja active Active
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