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DK3218358T3 - Ifluorometyl-aminopyridiner og difluorometyl-aminopyrimidiner - Google Patents

Ifluorometyl-aminopyridiner og difluorometyl-aminopyrimidiner Download PDF

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Publication number
DK3218358T3
DK3218358T3 DK15791315.3T DK15791315T DK3218358T3 DK 3218358 T3 DK3218358 T3 DK 3218358T3 DK 15791315 T DK15791315 T DK 15791315T DK 3218358 T3 DK3218358 T3 DK 3218358T3
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DK
Denmark
Prior art keywords
ifluoromethyl
aminopyrimidines
aminopyridines
difluoromethyl
Prior art date
Application number
DK15791315.3T
Other languages
English (en)
Inventor
Vladimir Cmiljanovic
Paul Hebeisen
Florent Beaufils
Thomas Bohnacker
Denise Rageot
Alexander Sele
Matthias Wymann
Jean-Baptiste Langlois
Original Assignee
Univ Basel
Torqur Ag
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 Univ Basel, Torqur Ag filed Critical Univ Basel
Application granted granted Critical
Publication of DK3218358T3 publication Critical patent/DK3218358T3/da

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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-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
    • C07D498/02—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 two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Pyridine Compounds (AREA)
DK15791315.3T 2014-11-11 2015-11-10 Ifluorometyl-aminopyridiner og difluorometyl-aminopyrimidiner DK3218358T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14192617 2014-11-11
PCT/EP2015/076192 WO2016075130A1 (en) 2014-11-11 2015-11-10 Difluoromethyl-aminopyridines and difluoromethyl-aminopyrimidines

Publications (1)

Publication Number Publication Date
DK3218358T3 true DK3218358T3 (da) 2021-08-30

Family

ID=51868133

Family Applications (1)

Application Number Title Priority Date Filing Date
DK15791315.3T DK3218358T3 (da) 2014-11-11 2015-11-10 Ifluorometyl-aminopyridiner og difluorometyl-aminopyrimidiner

Country Status (23)

Country Link
US (3) US10640516B2 (da)
EP (1) EP3218358B1 (da)
JP (1) JP6689843B2 (da)
KR (1) KR20170101899A (da)
CN (1) CN107108644B (da)
AU (1) AU2015345233B2 (da)
CA (1) CA2965565C (da)
CY (1) CY1124444T1 (da)
DK (1) DK3218358T3 (da)
ES (1) ES2886008T3 (da)
HR (1) HRP20211336T1 (da)
HU (1) HUE055473T2 (da)
IL (1) IL252216B (da)
MA (1) MA40933A (da)
MX (1) MX2017006152A (da)
PH (1) PH12017500854B1 (da)
PL (1) PL3218358T3 (da)
PT (1) PT3218358T (da)
RS (1) RS62289B1 (da)
RU (1) RU2712091C2 (da)
SG (1) SG11201703579UA (da)
SI (1) SI3218358T1 (da)
WO (1) WO2016075130A1 (da)

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GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
JP6871919B2 (ja) 2015-06-16 2021-05-19 ナノファギックス エルエルシー 薬物送達及びイメージング化学コンジュゲート、製剤及びその使用方法
GB201514760D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds and method of use
GB201514758D0 (en) * 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
LT3371190T (lt) 2015-11-06 2022-08-10 Incyte Corporation Heterocikliniai junginiai, kaip pi3k-gama inhibitoriai
AR107293A1 (es) 2016-01-05 2018-04-18 Incyte Corp COMPUESTOS DE PIRIDINA Y PIRIDIMINA COMO INHIBIDORES DE PI3K-g
RU2018140001A (ru) 2016-05-18 2020-06-18 Пикур Терапьютикс Аг Лечение повреждений кожи
HRP20210477T1 (hr) * 2016-05-18 2021-05-14 Torqur Ag Liječenje neuroloških poremećaja
WO2017198347A1 (en) * 2016-05-18 2017-11-23 Piqur Therapeutics Ag Treatment of skin lesions
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
CN107266422A (zh) * 2017-06-12 2017-10-20 西安交通大学 2‑（5‑嘧啶基）‑4‑吗啉基‑6‑取代均三嗪类化合物及其盐、制备方法和应用
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
CN109810100B (zh) * 2017-11-21 2022-03-11 中国药科大学 含有苯并呋喃的parp-1和pi3k双靶点抑制剂
AU2018371168C1 (en) * 2017-11-23 2024-12-05 Torqur Ag Treatment of skin disorders
US20210299133A1 (en) 2018-08-07 2021-09-30 Piqur Therapeutics Ag Treatment of squamous cell carcinoma
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
EP3967694A4 (en) * 2019-06-06 2022-12-07 Beijing Tide Pharmaceutical Co., Ltd. 2, 4, 6-TRI-SUBSTITUTED PYRIMIDINE COMPOUND AS ATR-KINASE INHIBITOR
CN111039874B (zh) * 2019-12-13 2022-11-04 南开大学 一种2-胺基-4-甲基嘧啶化合物的零废水制备方法
KR20210158019A (ko) 2020-06-23 2021-12-30 주식회사 온코빅스 포스파티딜이노시톨 3-키나제(pi3k) 억제제로써 pten 과오종 증후군에 의한 종양 세포의 성장 또는 증식을 억제하는데 유용한 신규한 피리미딘 유도체 및 이의 약제학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 약제학적 조성물
US20240217960A1 (en) * 2021-04-09 2024-07-04 Universität Basel Triazine derivative as covalent inhibitors of pi3k
CN116239580B (zh) * 2023-03-06 2025-05-23 中国药科大学 三嗪类化合物及其制备方法、药物组合物和应用
WO2025125469A1 (en) 2023-12-13 2025-06-19 Swiss Rockets Ag Combination therapy using psma-targeted radiopharmaceuticals and an inhibitor of pi3k, akt, and/or mtor
CN119019440A (zh) * 2024-10-24 2024-11-26 浙江雅辰药物科技股份有限公司 一种6-环丙基吡啶-3-硼酸频那醇酯的制备方法

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DK1389617T3 (da) * 2001-04-27 2007-05-07 Zenyaku Kogyo Kk Heterocyclisk forbindelse og antitumormiddel indeholdende denne som den aktive bestanddel
PL1864665T3 (pl) * 2005-03-11 2012-10-31 Zenyaku Kogyo Kk Środek immunosupresyjny obejmujący związek heterocykliczny jako składnik aktywny
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
CA2675558A1 (en) * 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
GB2465405A (en) * 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
WO2014090147A1 (zh) * 2012-12-14 2014-06-19 上海恒瑞医药有限公司 嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用

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Publication number Publication date
IL252216A0 (en) 2017-07-31
PL3218358T3 (pl) 2022-03-14
RU2017111265A (ru) 2018-12-14
BR112017009457A2 (pt) 2017-12-19
PH12017500854A1 (en) 2017-11-06
US10640516B2 (en) 2020-05-05
IL252216B (en) 2021-12-01
US20190031682A1 (en) 2019-01-31
CA2965565A1 (en) 2016-05-19
BR112017009457A8 (pt) 2023-01-10
MX2017006152A (es) 2017-07-19
JP6689843B2 (ja) 2020-04-28
AU2015345233A1 (en) 2017-05-25
US11186591B2 (en) 2021-11-30
AU2015345233B2 (en) 2020-01-02
PH12017500854B1 (en) 2022-09-02
EP3218358B1 (en) 2021-06-16
RU2017111265A3 (da) 2019-02-19
KR20170101899A (ko) 2017-09-06
CN107108644A (zh) 2017-08-29
MA40933A (fr) 2017-09-19
NZ731504A (en) 2021-04-30
EP3218358A1 (en) 2017-09-20
PT3218358T (pt) 2021-09-10
SG11201703579UA (en) 2017-05-30
JP2017533246A (ja) 2017-11-09
CY1124444T1 (el) 2022-07-22
WO2016075130A1 (en) 2016-05-19
RS62289B1 (sr) 2021-09-30
CN107108644B (zh) 2021-01-05
HUE055473T2 (hu) 2021-11-29
HRP20211336T1 (hr) 2021-11-26
CA2965565C (en) 2023-09-19
ES2886008T3 (es) 2021-12-16
RU2712091C2 (ru) 2020-01-24
US20200277304A1 (en) 2020-09-03
US20220153752A1 (en) 2022-05-19
SI3218358T1 (sl) 2021-10-29

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