MD3468957T2 - Formă cristalină a (R)-4-(5-(ciclopropiletinil)izoxazol-3-il)-N-hidroxi-2-metil-2-(metilsulfonil)butanamidei în calitate de agent antibacterian - Google Patents
Formă cristalină a (R)-4-(5-(ciclopropiletinil)izoxazol-3-il)-N-hidroxi-2-metil-2-(metilsulfonil)butanamidei în calitate de agent antibacterianInfo
- Publication number
- MD3468957T2 MD3468957T2 MDE20190477T MDE20190477T MD3468957T2 MD 3468957 T2 MD3468957 T2 MD 3468957T2 MD E20190477 T MDE20190477 T MD E20190477T MD E20190477 T MDE20190477 T MD E20190477T MD 3468957 T2 MD3468957 T2 MD 3468957T2
- Authority
- MD
- Moldova
- Prior art keywords
- cyclopropylethynyl
- butanamide
- isoxazol
- methylsulfonyl
- hydroxy
- Prior art date
Links
- YSKCELXYZFBKNU-CQSZACIVSA-N (2R)-4-[5-(2-cyclopropylethynyl)-1,2-oxazol-3-yl]-N-hydroxy-2-methyl-2-methylsulfonylbutanamide Chemical compound C1(CC1)C#CC1=CC(=NO1)CC[C@](C(=O)NO)(S(=O)(=O)C)C YSKCELXYZFBKNU-CQSZACIVSA-N 0.000 title 1
- 239000003242 anti bacterial agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000000203 mixture Substances 0.000 abstract 2
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 208000027096 gram-negative bacterial infections Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- 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
- A61K31/42—Oxazoles
-
- 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
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
-
- 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
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
- A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/5383—1,4-Oxazines, e.g. morpholine 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
- A61K31/54—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
- A61K31/542—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
- A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
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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
- A61K31/65—Tetracyclines
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/14—Peptides containing saccharide radicals; Derivatives thereof, e.g. bleomycin, phleomycin, muramylpeptides or vancomycin
-
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- 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
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Această invenţie se referă la un compus cristalin cu Formula (A) aşa cum este descris în aceasta şi la compoziţii conţinând acest compus cristalin, precum şi la metode de utilizare a compusului sau compoziţiilor farmaceutice care îl cuprind pentru a trata infecţii bacteriene. Compusul şi compoziţiile sunt în mod special folositori pentru a trata infecţii bacteriene Gram-negative, inclusiv tulpini rezistente la multiple medicamente.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2016085694 | 2016-06-14 | ||
PCT/IB2017/053468 WO2017216705A1 (en) | 2016-06-14 | 2017-06-12 | Crystalline form of (r)-4-(5-(cyclopropylethynyl)isoxazol-3-yl)-n-hydroxy-2-methyl-2-(methylsulfonyl)butanamide as an antibacterial agent |
Publications (1)
Publication Number | Publication Date |
---|---|
MD3468957T2 true MD3468957T2 (ro) | 2020-11-30 |
Family
ID=59337734
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MDE20190477T MD3468957T2 (ro) | 2016-06-14 | 2017-06-12 | Formă cristalină a (R)-4-(5-(ciclopropiletinil)izoxazol-3-il)-N-hidroxi-2-metil-2-(metilsulfonil)butanamidei în calitate de agent antibacterian |
Country Status (28)
Country | Link |
---|---|
US (1) | US10071973B2 (ro) |
EP (1) | EP3468957B1 (ro) |
JP (1) | JP6941630B2 (ro) |
KR (1) | KR20190018637A (ro) |
CN (1) | CN109311828A (ro) |
AU (1) | AU2017283768B2 (ro) |
BR (1) | BR112018074983A2 (ro) |
CA (1) | CA3026356A1 (ro) |
CL (1) | CL2018003559A1 (ro) |
CY (1) | CY1123368T1 (ro) |
DK (1) | DK3468957T3 (ro) |
EA (1) | EA036243B1 (ro) |
ES (1) | ES2820502T3 (ro) |
HR (1) | HRP20201524T1 (ro) |
HU (1) | HUE050796T2 (ro) |
IL (1) | IL263299A (ro) |
MA (1) | MA45250B1 (ro) |
MD (1) | MD3468957T2 (ro) |
MX (1) | MX2018015634A (ro) |
PH (1) | PH12018502523A1 (ro) |
PL (1) | PL3468957T3 (ro) |
PT (1) | PT3468957T (ro) |
SG (1) | SG11201810656WA (ro) |
SI (1) | SI3468957T1 (ro) |
TW (1) | TWI746572B (ro) |
UA (1) | UA123790C2 (ro) |
WO (1) | WO2017216705A1 (ro) |
ZA (1) | ZA201807680B (ro) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107375211B (zh) * | 2017-08-24 | 2021-02-26 | 正大制药(青岛)有限公司 | 一种甲苯磺酸妥舒沙星小儿用舌下喷雾剂及其制备方法 |
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WO2014160649A1 (en) | 2013-03-29 | 2014-10-02 | Novartis Ag | Hydroxamic acid derivatives as lpxc inhibitors for the treatment of bacterial infections |
JPWO2015056799A1 (ja) * | 2013-10-18 | 2017-03-09 | 大正製薬株式会社 | ヒドロキサム酸誘導体 |
JP6514716B2 (ja) | 2014-04-22 | 2019-05-15 | ノバルティス アーゲー | LpxC阻害剤としてのイソオキサゾリンヒドロキサム酸誘導体 |
US9549916B2 (en) | 2014-12-16 | 2017-01-24 | Novartis Ag | Isoxazole hydroxamic acid compounds as LpxC inhibitors |
-
2017
- 2017-06-12 SI SI201730409T patent/SI3468957T1/sl unknown
- 2017-06-12 HU HUE17739696A patent/HUE050796T2/hu unknown
- 2017-06-12 EA EA201990012A patent/EA036243B1/ru not_active IP Right Cessation
- 2017-06-12 KR KR1020187035895A patent/KR20190018637A/ko active IP Right Grant
- 2017-06-12 UA UAA201811400A patent/UA123790C2/uk unknown
- 2017-06-12 MD MDE20190477T patent/MD3468957T2/ro not_active IP Right Cessation
- 2017-06-12 BR BR112018074983-4A patent/BR112018074983A2/pt not_active IP Right Cessation
- 2017-06-12 ES ES17739696T patent/ES2820502T3/es active Active
- 2017-06-12 CN CN201780036712.0A patent/CN109311828A/zh active Pending
- 2017-06-12 PL PL17739696T patent/PL3468957T3/pl unknown
- 2017-06-12 SG SG11201810656WA patent/SG11201810656WA/en unknown
- 2017-06-12 US US15/620,373 patent/US10071973B2/en not_active Expired - Fee Related
- 2017-06-12 MX MX2018015634A patent/MX2018015634A/es unknown
- 2017-06-12 EP EP17739696.7A patent/EP3468957B1/en active Active
- 2017-06-12 CA CA3026356A patent/CA3026356A1/en not_active Abandoned
- 2017-06-12 DK DK17739696.7T patent/DK3468957T3/da active
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- 2017-06-12 AU AU2017283768A patent/AU2017283768B2/en not_active Ceased
- 2017-06-12 PT PT177396967T patent/PT3468957T/pt unknown
- 2017-06-12 MA MA45250A patent/MA45250B1/fr unknown
- 2017-06-12 JP JP2018565302A patent/JP6941630B2/ja active Active
- 2017-06-13 TW TW106119562A patent/TWI746572B/zh not_active IP Right Cessation
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2018
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- 2018-11-29 PH PH12018502523A patent/PH12018502523A1/en unknown
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2020
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Also Published As
Publication number | Publication date |
---|---|
MX2018015634A (es) | 2019-03-06 |
EP3468957A1 (en) | 2019-04-17 |
AU2017283768A1 (en) | 2018-12-06 |
US10071973B2 (en) | 2018-09-11 |
IL263299A (en) | 2018-12-31 |
AU2017283768B2 (en) | 2019-05-23 |
CY1123368T1 (el) | 2021-12-31 |
US20170355684A1 (en) | 2017-12-14 |
TW201803858A (zh) | 2018-02-01 |
WO2017216705A1 (en) | 2017-12-21 |
KR20190018637A (ko) | 2019-02-25 |
CA3026356A1 (en) | 2017-12-21 |
MA45250B1 (fr) | 2020-09-30 |
EA201990012A1 (ru) | 2019-05-31 |
EA036243B1 (ru) | 2020-10-16 |
PH12018502523A1 (en) | 2019-10-14 |
JP2019522645A (ja) | 2019-08-15 |
CL2018003559A1 (es) | 2019-01-18 |
PT3468957T (pt) | 2020-09-24 |
UA123790C2 (uk) | 2021-06-02 |
SI3468957T1 (sl) | 2020-11-30 |
ES2820502T3 (es) | 2021-04-21 |
PL3468957T3 (pl) | 2021-01-25 |
JP6941630B2 (ja) | 2021-09-29 |
EP3468957B1 (en) | 2020-08-26 |
ZA201807680B (en) | 2019-08-28 |
TWI746572B (zh) | 2021-11-21 |
HRP20201524T1 (hr) | 2021-03-05 |
SG11201810656WA (en) | 2018-12-28 |
BR112018074983A2 (pt) | 2019-03-12 |
DK3468957T3 (da) | 2020-09-14 |
HUE050796T2 (hu) | 2021-01-28 |
CN109311828A (zh) | 2019-02-05 |
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