LT3788043T - Nikotino acetilcholino receptorių alosteriniai spiropiperidino moduliatoriai - Google Patents

Nikotino acetilcholino receptorių alosteriniai spiropiperidino moduliatoriai

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Publication number
LT3788043T
LT3788043T LTEPPCT/US2019/029561T LTUS2019029561T LT3788043T LT 3788043 T LT3788043 T LT 3788043T LT US2019029561 T LTUS2019029561 T LT US2019029561T LT 3788043 T LT3788043 T LT 3788043T
Authority
LT
Lithuania
Prior art keywords
spiropiperidine
allosteric
modulators
acetylcholine receptors
nicotine acetylcholine
Prior art date
Application number
LTEPPCT/US2019/029561T
Other languages
English (en)
Inventor
Brendan CROWLEY
Brian Campbell
Harry Chobanian
James Fells
Deodial Guiadeen
Thomas Greshock
Kenneth LEAVITT
Vanessa RADA
Ian Bell
Original Assignee
Merck Sharp & Dohme Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme Llc filed Critical Merck Sharp & Dohme Llc
Publication of LT3788043T publication Critical patent/LT3788043T/lt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/542Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/08Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/08Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
LTEPPCT/US2019/029561T 2018-05-01 2019-04-29 Nikotino acetilcholino receptorių alosteriniai spiropiperidino moduliatoriai LT3788043T (lt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862665091P 2018-05-01 2018-05-01
PCT/US2019/029561 WO2019212927A1 (en) 2018-05-01 2019-04-29 Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors

Publications (1)

Publication Number Publication Date
LT3788043T true LT3788043T (lt) 2024-12-27

Family

ID=66429709

Family Applications (1)

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LTEPPCT/US2019/029561T LT3788043T (lt) 2018-05-01 2019-04-29 Nikotino acetilcholino receptorių alosteriniai spiropiperidino moduliatoriai

Country Status (39)

Country Link
US (1) US11332463B2 (lt)
EP (1) EP3788043B1 (lt)
JP (1) JP7073533B2 (lt)
KR (1) KR102587811B1 (lt)
CN (1) CN112119076B (lt)
AR (1) AR115065A1 (lt)
AU (1) AU2019262917B2 (lt)
BR (1) BR112020022088A8 (lt)
CA (1) CA3098583C (lt)
CL (2) CL2020002820A1 (lt)
CO (1) CO2020013462A2 (lt)
CR (1) CR20200509A (lt)
DK (1) DK3788043T3 (lt)
EA (1) EA202092608A1 (lt)
EC (1) ECSP20067907A (lt)
ES (1) ES2995040T3 (lt)
FI (1) FI3788043T3 (lt)
GE (2) GEP20227409B (lt)
HR (1) HRP20241704T1 (lt)
HU (1) HUE070339T2 (lt)
IL (1) IL278154B2 (lt)
JO (1) JOP20200272A1 (lt)
LT (1) LT3788043T (lt)
MA (1) MA52482B1 (lt)
MD (1) MD3788043T2 (lt)
MX (1) MX2020011489A (lt)
MY (1) MY205690A (lt)
NI (1) NI202000074A (lt)
PE (1) PE20210052A1 (lt)
PH (1) PH12020551779A1 (lt)
PL (1) PL3788043T3 (lt)
PT (1) PT3788043T (lt)
RS (1) RS66290B1 (lt)
SG (1) SG11202010459XA (lt)
SI (1) SI3788043T1 (lt)
TW (1) TWI839355B (lt)
UA (1) UA126834C2 (lt)
WO (1) WO2019212927A1 (lt)
ZA (1) ZA202006507B (lt)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
EP3962483A4 (en) * 2019-05-02 2023-01-25 Merck Sharp & Dohme LLC ALLOSTERIC SPIROPIPERIDINE MODULATORS OF NICOTINE ACETYLCHOLINE RECEPTORS
CN114727974A (zh) 2019-07-30 2022-07-08 艾科尼佐治疗股份有限公司 Hdac6抑制剂及其用途
WO2021091751A1 (en) * 2019-11-05 2021-05-14 Merck Sharp & Dohme Corp. Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors
JP7648027B2 (ja) * 2019-12-19 2025-03-18 クリア、スペイン、エセ、ア、ウ ウパダシチニブの調製のための方法及び中間体

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR044010A1 (es) 2003-04-11 2005-08-24 Janssen Pharmaceutica Nv Uso de derivados de 4-fenil-4- [1h-imidazol-2-il]- piperidina sustituidos como agonistas delta opioideos no peptidos selectivos, con actividad antidepresiva y ansiolitica
CN101815512B (zh) 2007-10-04 2013-04-24 弗·哈夫曼-拉罗切有限公司 环丙基芳基酰胺衍生物和其用途
KR101925971B1 (ko) 2011-01-28 2018-12-06 에스케이바이오팜 주식회사 피리돈 유도체 및 이를 포함하는 약학적 조성물
WO2012103583A1 (en) 2011-02-02 2012-08-09 Bionomics Limited Positive allosteric modulators of the alpha 7 nicotinic acetylcholine receptor and uses thereof.
UA111746C2 (uk) 2011-07-08 2016-06-10 Х. Луннбек А/С Позитивні алостеричні модулятори нікотинового рецептора ацетилхоліну
HRP20180913T1 (hr) 2011-07-08 2018-07-27 H. Lundbeck A/S Pozitivni alosterni modulatori receptora nikotinskog acetilkolina
WO2014006117A1 (en) 2012-07-06 2014-01-09 H. Lundbeck A/S New positive allosteric modulators of nicotinic acetylcholine receptor
US20150175534A1 (en) 2012-08-01 2015-06-25 Merck Sharp & Dohme Corp. Alpha-7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEROF-I
CN104837820A (zh) 2012-10-02 2015-08-12 大日本住友制药株式会社 咪唑衍生物
CN104837811A (zh) 2012-12-10 2015-08-12 H.隆德贝克有限公司 烟碱乙酰胆碱受体的新的正向別构调节剂
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
US10800780B2 (en) 2015-12-24 2020-10-13 Genentech, Inc. TDO2 Inhibitors
CR20180452A (es) * 2016-03-22 2019-02-06 Merck Sharp & Dohme Moduladores alostéricos de receptores de acetilcolina nicotícos

Also Published As

Publication number Publication date
PH12020551779A1 (en) 2021-06-07
GEP20227409B (en) 2022-09-12
JP7073533B2 (ja) 2022-05-23
US11332463B2 (en) 2022-05-17
UA126834C2 (uk) 2023-02-08
CR20200509A (es) 2020-12-23
MY205690A (en) 2024-11-06
ZA202006507B (en) 2025-06-25
SI3788043T1 (sl) 2025-01-31
DK3788043T3 (da) 2024-12-16
TWI839355B (zh) 2024-04-21
CN112119076A (zh) 2020-12-22
KR102587811B1 (ko) 2023-10-11
PE20210052A1 (es) 2021-01-08
PL3788043T3 (pl) 2025-03-10
CL2020002820A1 (es) 2021-02-19
IL278154B2 (en) 2025-06-01
CA3098583C (en) 2023-05-16
CN112119076B (zh) 2025-01-10
BR112020022088A8 (pt) 2023-02-07
CA3098583A1 (en) 2019-11-07
FI3788043T3 (fi) 2025-01-15
CL2021001795A1 (es) 2021-12-24
IL278154A (en) 2020-11-30
AU2019262917B2 (en) 2021-12-23
GEAP202215499A (en) 2022-05-10
ECSP20067907A (es) 2021-02-26
HRP20241704T1 (hr) 2025-02-14
ES2995040T3 (en) 2025-02-05
IL278154B1 (en) 2025-02-01
PT3788043T (pt) 2024-12-03
RS66290B1 (sr) 2025-01-31
AR115065A1 (es) 2020-11-25
MA52482A (fr) 2021-03-10
TW202014419A (zh) 2020-04-16
SG11202010459XA (en) 2020-11-27
BR112020022088A2 (pt) 2021-02-02
MA52482B1 (fr) 2024-12-31
KR20210005697A (ko) 2021-01-14
US20210070745A1 (en) 2021-03-11
EA202092608A1 (ru) 2021-03-02
EP3788043A1 (en) 2021-03-10
MD3788043T2 (ro) 2025-03-31
MX2020011489A (es) 2020-12-07
JOP20200272A1 (ar) 2020-11-01
WO2019212927A1 (en) 2019-11-07
NZ768954A (en) 2025-06-27
JP2021523102A (ja) 2021-09-02
EP3788043B1 (en) 2024-11-06
NI202000074A (es) 2021-03-05
HUE070339T2 (hu) 2025-05-28
CO2020013462A2 (es) 2020-11-10
AU2019262917A1 (en) 2020-11-05

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