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AR104512A1 - Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap) - Google Patents

Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap)

Info

Publication number
AR104512A1
AR104512A1 ARP160101257A ARP160101257A AR104512A1 AR 104512 A1 AR104512 A1 AR 104512A1 AR P160101257 A ARP160101257 A AR P160101257A AR P160101257 A ARP160101257 A AR P160101257A AR 104512 A1 AR104512 A1 AR 104512A1
Authority
AR
Argentina
Prior art keywords
ring
independently
halo
alkyl
heterocyclyl
Prior art date
Application number
ARP160101257A
Other languages
English (en)
Inventor
Thomas Plowright Alleyn
Johan Andreas Ulander Lars
Tor Pettersen Daniel
Anita Lemurell Malin
Lars Granberg Kenneth
Fredrik Emtens Hans
Olof Broddefalk Johan
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR104512A1 publication Critical patent/AR104512A1/es

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    • 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/44Oxygen and nitrogen or sulfur and nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/44Oxygen and nitrogen or sulfur and nitrogen atoms
    • C07D231/46Oxygen atom in position 3 or 5 and nitrogen atom in position 4
    • C07D231/50Acylated on said nitrogen atom
    • 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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 two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

A su uso en el tratamiento y/o prevención de afecciones clínicas que incluyen enfermedades cardiovasculares (CVD), a métodos para su uso terapéutico, a composiciones farmacéuticas que los contienen y a procesos para preparar dichos compuestos. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), o una sal farmacéuticamente aceptable de este, donde: R¹ es H, alquilo C₁₋₃, halo, alcoxi C₁₋₃, haloalquilo C₁₋₃ o haloalcoxi C₁₋₃; cada uno de R² y R³ es independientemente H, alquilo C₁₋₃, alcoxi C₁₋₃, -CN o halo; R⁴ es H, -CH₃, -CH₂F, -CHF₂, -CF₃, o halo; Anillo A contiene 2 enlaces dobles; cada X¹, X², X³ y X⁴ del Anillo A es independientemente CR⁵, CH, O, S, NR⁶ o N; donde al menos uno de X¹, X², X³ y X⁴ en el Anillo A es NR⁶; cada R⁵ es opcional e independientemente alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₃, haloalcoxi C₁₋₃, -S(O)ₚR⁷, -CN, -CONRR, o cicloalquilo C₃₋₆; cada p es independientemente 0, 1 ó 2; R⁶ es H, -CH₃ o -CH₂CH₃; o donde cuando X⁴ es CR⁵ y X³ es NR⁶, entonces R⁵ y R⁶ pueden tomarse juntos para formar un anillo heterociclilo de 5 a 6 miembros fusionado al Anillo A, cuyo heterociclilo puede contener opcionalmente un heteroátomo adicional que se selecciona de N, O y S; tal heterociclilo fusionado puede contener adicionalmente un carbonilo o S(O)₂ directamente adyacente a un heteroátomo en este; y puede además sustituirse con uno o dos sustituyentes que se seleccionan del grupo que consiste en CH₃ y halo; R⁷ es -CH₃ o -NRR; y cada R y R es independientemente -H o -CH₃; siempre que la cantidad total de sustituyentes en el Anillo A sea 0, 1 ó 2; y además siempre que cuando R⁵ y R⁶ no estén combinados para formar un anillo heterociclilo fusionado al Anillo A, que la cantidad total de sustituyentes de R⁵ y R⁶ que es alquilo y/o haloalquilo sea 0 ó 1.
ARP160101257A 2015-05-04 2016-05-03 Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap) AR104512A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562156424P 2015-05-04 2015-05-04

Publications (1)

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AR104512A1 true AR104512A1 (es) 2017-07-26

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ARP160101257A AR104512A1 (es) 2015-05-04 2016-05-03 Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap)

Country Status (38)

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US (6) US10183947B2 (es)
EP (2) EP3292105B1 (es)
JP (1) JP6564062B2 (es)
KR (1) KR102623474B1 (es)
CN (1) CN107646036B (es)
AR (1) AR104512A1 (es)
AU (1) AU2016258874B2 (es)
BR (1) BR112017022757B1 (es)
CA (1) CA2983668C (es)
CL (1) CL2017002660A1 (es)
CO (1) CO2017011506A2 (es)
CR (1) CR20170513A (es)
CY (2) CY1122689T1 (es)
DK (2) DK3292105T3 (es)
DO (1) DOP2017000244A (es)
EA (1) EA032221B1 (es)
ES (2) ES2902139T3 (es)
GT (1) GT201700220A (es)
HK (1) HK1245255A1 (es)
HR (2) HRP20211993T1 (es)
HU (2) HUE056875T2 (es)
IL (1) IL255069B (es)
LT (1) LT3670499T (es)
ME (1) ME03663B (es)
MX (1) MX2017013571A (es)
MY (1) MY186647A (es)
PE (1) PE20180247A1 (es)
PH (1) PH12017502112B1 (es)
PL (2) PL3292105T3 (es)
PT (2) PT3292105T (es)
RS (2) RS59671B1 (es)
SG (1) SG11201708558RA (es)
SI (2) SI3670499T1 (es)
SV (1) SV2017005549A (es)
TN (1) TN2017000458A1 (es)
TW (1) TWI718146B (es)
WO (1) WO2016177703A1 (es)
ZA (1) ZA201708189B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2017013571A (es) 2015-05-04 2018-02-26 Astrazeneca Ab Derivados de pirazol utiles como inhibidores de proteina activadora de 5-lipoxigenasa (flap).
MX2019004574A (es) * 2016-10-28 2019-08-21 Astrazeneca Ab Forma cristalina de (1r,2r)-2-[4-(3-metil-1h-pirazol-5-il)benzoil- n-(4-oxo-4,5,6,7-tetrahidropirazolo[1,5-a]pirazin-3-il)ciclohexan ocarboxamida.
CN110169969B (zh) * 2019-06-28 2022-05-27 南京医科大学 Mk571在制备预防和治疗心脏病药物中应用
CN111084775A (zh) * 2020-02-17 2020-05-01 牡丹江医学院 一种用于治疗癫痫的药物组合物
CN111419800B (zh) * 2020-04-23 2021-03-19 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 用于治疗红斑狼疮的药物制剂及其制备方法
CN111643498B (zh) * 2020-07-20 2021-05-07 黑龙江中医药大学 一种治疗肾结石的药物组合物及其用途
CN111714499B (zh) * 2020-07-27 2021-05-11 黑龙江中医药大学 一种用于治疗多囊卵巢综合征的药物组合物

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EP2114876A4 (en) * 2007-02-05 2010-12-22 Amira Pharmaceuticals Inc INVERSE INDOLES AS INHIBITORS OF THE 5-LIPOXYGENASE ACTIVATION PROTEIN (FLAP)
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WO2009045700A2 (en) * 2007-10-05 2009-04-09 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
MX2017013571A (es) * 2015-05-04 2018-02-26 Astrazeneca Ab Derivados de pirazol utiles como inhibidores de proteina activadora de 5-lipoxigenasa (flap).

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US12024523B2 (en) 2024-07-02
PE20180247A1 (es) 2018-02-02
IL255069B (en) 2019-12-31
ME03663B (me) 2020-07-20
MX2017013571A (es) 2018-02-26
ES2902139T3 (es) 2022-03-25
CL2017002660A1 (es) 2018-04-13
CA2983668A1 (en) 2016-11-10
BR112017022757A2 (pt) 2018-07-17
NZ737672A (en) 2020-11-27
IL255069A0 (en) 2017-12-31
JP6564062B2 (ja) 2019-08-21
DK3292105T3 (da) 2019-12-09
SV2017005549A (es) 2018-03-12
ZA201708189B (en) 2018-11-28
HK1245255A1 (zh) 2018-08-24
MY186647A (en) 2021-08-03
PH12017502112A1 (en) 2018-05-07
US20240317767A1 (en) 2024-09-26
EA201792341A1 (ru) 2018-05-31
US20200157113A1 (en) 2020-05-21
US10183947B2 (en) 2019-01-22
EP3292105A1 (en) 2018-03-14
EP3670499A1 (en) 2020-06-24
CY1122689T1 (el) 2021-03-12
HRP20192172T1 (hr) 2020-02-21
EP3292105B1 (en) 2019-10-02
PH12017502112B1 (en) 2018-05-07
SI3292105T1 (sl) 2020-01-31
US20180237439A1 (en) 2018-08-23
DOP2017000244A (es) 2017-11-15
CO2017011506A2 (es) 2018-01-31
SG11201708558RA (en) 2017-11-29
CR20170513A (es) 2018-02-13
EA032221B1 (ru) 2019-04-30
ES2760466T3 (es) 2020-05-14
KR102623474B1 (ko) 2024-01-09
HUE056875T2 (hu) 2022-03-28
WO2016177703A1 (en) 2016-11-10
HUE047445T2 (hu) 2020-04-28
US20190084991A1 (en) 2019-03-21
EP3670499B1 (en) 2021-09-29
PT3292105T (pt) 2019-12-13
PT3670499T (pt) 2021-12-24
KR20180002784A (ko) 2018-01-08
LT3670499T (lt) 2021-12-27
CN107646036A (zh) 2018-01-30
AU2016258874A1 (en) 2017-12-14
JP2018514535A (ja) 2018-06-07
AU2016258874B2 (en) 2020-04-30
TWI718146B (zh) 2021-02-11
TW201713625A (zh) 2017-04-16
US20210355127A1 (en) 2021-11-18
DK3670499T3 (da) 2022-01-03
BR112017022757B1 (pt) 2023-02-23
PL3670499T3 (pl) 2022-02-14
RS62729B1 (sr) 2022-01-31
SI3670499T1 (sl) 2022-02-28
US11691978B2 (en) 2023-07-04
RS59671B1 (sr) 2020-01-31
CN107646036B (zh) 2020-05-19
US11001589B2 (en) 2021-05-11
US20230219967A1 (en) 2023-07-13
GT201700220A (es) 2018-12-19
TN2017000458A1 (en) 2019-04-12
CY1125179T1 (el) 2023-03-24
PL3292105T3 (pl) 2020-04-30
US10508119B2 (en) 2019-12-17
CA2983668C (en) 2023-06-27
HRP20211993T1 (hr) 2022-04-01

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