PH12018500736A1 - Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity - Google Patents

Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity

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Publication number
PH12018500736A1
PH12018500736A1 PH12018500736A PH12018500736A PH12018500736A1 PH 12018500736 A1 PH12018500736 A1 PH 12018500736A1 PH 12018500736 A PH12018500736 A PH 12018500736A PH 12018500736 A PH12018500736 A PH 12018500736A PH 12018500736 A1 PH12018500736 A1 PH 12018500736A1
Authority
PH
Philippines
Prior art keywords
pyrimidine
methods
multiple sclerosis
pyridine compounds
inhibitory activity
Prior art date
Application number
PH12018500736A
Other languages
English (en)
Inventor
Tammy Dellovade
Original Assignee
Merck Patent Gmbh
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 Patent Gmbh filed Critical Merck Patent Gmbh
Publication of PH12018500736A1 publication Critical patent/PH12018500736A1/en

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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
    • A61K31/495—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
    • A61K31/435—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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/69—Boron compounds
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • 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
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
PH12018500736A 2015-11-17 2018-04-03 Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity PH12018500736A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562256199P 2015-11-17 2015-11-17
PCT/US2016/062154 WO2017087445A1 (en) 2015-11-17 2016-11-16 Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity

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Publication Number Publication Date
PH12018500736A1 true PH12018500736A1 (en) 2018-10-01

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PH12018500736A PH12018500736A1 (en) 2015-11-17 2018-04-03 Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity

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EP (2) EP3377484B1 (enExample)
JP (1) JP6891173B2 (enExample)
KR (1) KR102780243B1 (enExample)
CN (1) CN108884076B (enExample)
AU (1) AU2016357735B2 (enExample)
BR (1) BR112018007517B1 (enExample)
CL (1) CL2018001252A1 (enExample)
DK (1) DK3377484T3 (enExample)
ES (1) ES2964946T3 (enExample)
FI (1) FI3377484T3 (enExample)
HR (1) HRP20231547T1 (enExample)
HU (1) HUE064244T2 (enExample)
IL (1) IL258978B (enExample)
LT (1) LT3377484T (enExample)
MX (1) MX386146B (enExample)
MY (1) MY199473A (enExample)
NZ (1) NZ741294A (enExample)
PH (1) PH12018500736A1 (enExample)
PL (1) PL3377484T3 (enExample)
PT (1) PT3377484T (enExample)
RS (1) RS64908B1 (enExample)
SI (1) SI3377484T1 (enExample)
UA (1) UA123159C2 (enExample)
WO (1) WO2017087445A1 (enExample)
ZA (1) ZA201802348B (enExample)

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CA3001735A1 (en) * 2015-11-04 2017-05-11 Merck Patent Gmbh Methods for treating cancer using pyrimidine and pyridine compounds with btk inhibitory activity
CN108884076B (zh) * 2015-11-17 2021-07-30 默克专利有限公司 使用具有btk抑制活性的嘧啶和吡啶化合物治疗多发性硬化症的方法
KR20210022674A (ko) * 2018-06-19 2021-03-03 메르크 파텐트 게엠베하 1-(4-｛[6-아미노-5-(4-페녹시-페닐)-피리미딘-4-일아미노]-메틸｝-4-플루오로-피페리딘-1-일)-프로펜온의 신규한 결정 형태, 이의 염 형태, 및 이를 수득하는 방법
HRP20241737T1 (hr) * 2018-07-20 2025-02-28 Merck Patent Gmbh Supstituirani amino-pirimidinski spoj za upotrebu u postupku za liječenje i prevenciju multiple skleroze
IL294560A (en) 2020-01-20 2022-09-01 Genzyme Corp Medicinal tyrosine kinase inhibitors for relapsing multiple sclerosis
CN112250666B (zh) * 2020-10-09 2022-01-14 广东东阳光药业有限公司 取代的嘧啶类化合物及其用途
CA3200332A1 (en) * 2020-12-02 2022-06-09 Telios Pharma, Inc. Methods and compositions for treating an ophthalmic condition
WO2022121670A1 (zh) 2020-12-10 2022-06-16 苏州科睿思制药有限公司 Tolebrutinib的晶型及其制备方法和用途
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
CN119744171A (zh) 2022-06-24 2025-04-01 默克专利股份公司 自身免疫病和炎性疾病的治疗方案
WO2024099241A1 (zh) * 2022-11-07 2024-05-16 天津征程医药科技有限公司 氘代的嘧啶衍生物以及包含该化合物的药物组合物
WO2025096900A1 (en) * 2023-11-03 2025-05-08 Board Of Regents, The University Of Texas System Synthetic network materials and methods of making and use thereof

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GB0512844D0 (en) * 2005-06-23 2005-08-03 Novartis Ag Organic compounds
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PT2718270T (pt) 2011-06-10 2022-07-29 Merck Patent Gmbh Composições e métodos para a produção de compostos de pirimidina e piridina com atividade inibidora de btk
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CA3001735A1 (en) * 2015-11-04 2017-05-11 Merck Patent Gmbh Methods for treating cancer using pyrimidine and pyridine compounds with btk inhibitory activity
CN108884076B (zh) * 2015-11-17 2021-07-30 默克专利有限公司 使用具有btk抑制活性的嘧啶和吡啶化合物治疗多发性硬化症的方法

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LT3377484T (lt) 2023-12-27
PT3377484T (pt) 2023-12-14
IL258978B (en) 2021-04-29
US10716788B2 (en) 2020-07-21
BR112018007517A2 (pt) 2018-10-23
CA3002224A1 (en) 2017-05-26
CN108884076A (zh) 2018-11-23
FI3377484T3 (fi) 2023-11-30
EP4295910A2 (en) 2023-12-27
EP4295910A3 (en) 2024-03-20
BR112018007517B1 (pt) 2023-09-26
KR20180080243A (ko) 2018-07-11
JP2018538264A (ja) 2018-12-27
PL3377484T3 (pl) 2024-04-08
US20170136018A1 (en) 2017-05-18
DK3377484T3 (da) 2023-11-27
JP6891173B2 (ja) 2021-06-18
MX386146B (es) 2025-03-18
ES2964946T3 (es) 2024-04-10
MY199473A (en) 2023-10-31
EP3377484B1 (en) 2023-09-06
UA123159C2 (uk) 2021-02-24
HRP20231547T1 (hr) 2024-03-15
AU2016357735A1 (en) 2018-04-26
RS64908B1 (sr) 2023-12-29
WO2017087445A1 (en) 2017-05-26
MX2018005463A (es) 2018-08-01
AU2016357735B2 (en) 2021-01-14
KR102780243B1 (ko) 2025-03-14
EP3377484A1 (en) 2018-09-26
ZA201802348B (en) 2020-08-26
US20200316068A1 (en) 2020-10-08
CL2018001252A1 (es) 2018-08-17
SI3377484T1 (sl) 2024-02-29
NZ741294A (en) 2023-07-28
IL258978A (en) 2018-07-31
CN108884076B (zh) 2021-07-30
RU2018120151A3 (enExample) 2020-03-24
RU2018120151A (ru) 2019-12-18
HUE064244T2 (hu) 2024-02-28

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