CL2014001664A1 - Compuestos derivados de 2-([1,4]dioxan-2-ilmetoxi)-6,7-dihidropirimido[6,1-a]isoquinolin-4-ona, antagonistas del receptor gpr84; composicion farmaceutica; metodo de tratamiento o profilaxis; y uso en el tratamiento o profilaxis de afecciones inflamatorias tales como artritis reumatoide, vasculitis, asma y psoriasis, entre otras. - Google Patents

Compuestos derivados de 2-([1,4]dioxan-2-ilmetoxi)-6,7-dihidropirimido[6,1-a]isoquinolin-4-ona, antagonistas del receptor gpr84; composicion farmaceutica; metodo de tratamiento o profilaxis; y uso en el tratamiento o profilaxis de afecciones inflamatorias tales como artritis reumatoide, vasculitis, asma y psoriasis, entre otras.

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Publication number
CL2014001664A1
CL2014001664A1 CL2014001664A CL2014001664A CL2014001664A1 CL 2014001664 A1 CL2014001664 A1 CL 2014001664A1 CL 2014001664 A CL2014001664 A CL 2014001664A CL 2014001664 A CL2014001664 A CL 2014001664A CL 2014001664 A1 CL2014001664 A1 CL 2014001664A1
Authority
CL
Chile
Prior art keywords
prophylaxis
treatment
dihydropyrimido
ylmethoxy
isoquinolin
Prior art date
Application number
CL2014001664A
Other languages
English (en)
Spanish (es)
Inventor
Fréderic Gilbert Labéguére
Gregory John Robert Newsome
Luke Jonathan Alvey
Laurent Raymond Maurice Saniére
Stephen Robert Fletcher
Original Assignee
Galapagos Nv
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 Galapagos Nv filed Critical Galapagos Nv
Publication of CL2014001664A1 publication Critical patent/CL2014001664A1/es

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    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CL2014001664A 2011-12-22 2014-06-20 Compuestos derivados de 2-([1,4]dioxan-2-ilmetoxi)-6,7-dihidropirimido[6,1-a]isoquinolin-4-ona, antagonistas del receptor gpr84; composicion farmaceutica; metodo de tratamiento o profilaxis; y uso en el tratamiento o profilaxis de afecciones inflamatorias tales como artritis reumatoide, vasculitis, asma y psoriasis, entre otras. CL2014001664A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161578979P 2011-12-22 2011-12-22

Publications (1)

Publication Number Publication Date
CL2014001664A1 true CL2014001664A1 (es) 2014-10-03

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Family Applications (1)

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CL2014001664A CL2014001664A1 (es) 2011-12-22 2014-06-20 Compuestos derivados de 2-([1,4]dioxan-2-ilmetoxi)-6,7-dihidropirimido[6,1-a]isoquinolin-4-ona, antagonistas del receptor gpr84; composicion farmaceutica; metodo de tratamiento o profilaxis; y uso en el tratamiento o profilaxis de afecciones inflamatorias tales como artritis reumatoide, vasculitis, asma y psoriasis, entre otras.

Country Status (34)

Country Link
US (5) US8927543B2 (https=)
EP (3) EP2794604B1 (https=)
JP (1) JP6062453B2 (https=)
KR (1) KR102012268B1 (https=)
CN (1) CN103998448B (https=)
AR (1) AR089284A1 (https=)
AU (1) AU2012357067B2 (https=)
BR (1) BR112014015142B1 (https=)
CA (1) CA2859578C (https=)
CL (1) CL2014001664A1 (https=)
CO (1) CO7010835A2 (https=)
CR (1) CR20140305A (https=)
CY (2) CY1119434T1 (https=)
DK (2) DK2794604T3 (https=)
EA (1) EA023826B1 (https=)
ES (2) ES2643379T3 (https=)
HR (2) HRP20171404T1 (https=)
HU (1) HUE12812237T4 (https=)
IL (2) IL233212B (https=)
IN (1) IN2014MN01033A (https=)
LT (2) LT2794604T (https=)
MX (1) MX351681B (https=)
NI (1) NI201400060A (https=)
PE (1) PE20141685A1 (https=)
PH (1) PH12014501178B1 (https=)
PL (2) PL2794604T3 (https=)
PT (2) PT3378862T (https=)
SG (1) SG11201403169PA (https=)
SI (2) SI3378862T1 (https=)
TW (1) TWI567073B (https=)
UA (1) UA111767C2 (https=)
UY (1) UY34545A (https=)
WO (1) WO2013092791A1 (https=)
ZA (1) ZA201404607B (https=)

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USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
US11021509B2 (en) 2011-12-22 2021-06-01 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof

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AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
WO2014095798A1 (en) * 2012-12-20 2014-06-26 Galapagos Nv Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)
GB201319677D0 (en) * 2013-11-07 2013-12-25 Eth Z Rich Cyclopropanation
GB201411241D0 (en) * 2014-06-25 2014-08-06 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
GB201506894D0 (en) * 2015-04-23 2015-06-10 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
KR102305710B1 (ko) * 2017-03-06 2021-09-30 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 Gpr84 수용체 길항제 및 이의 용도
EP3403649A1 (en) * 2017-05-16 2018-11-21 Bayer Pharma Aktiengesellschaft Inhibitors and antagonists of gpr84 for the treatment of endometriosis
RU2020119415A (ru) * 2017-11-15 2021-12-16 Галапагос Нв Соединения и их фармацевтические композиции для применения при лечении фиброзных заболеваний
BR112022011237A2 (pt) 2019-12-19 2022-08-30 Bayer Ag Derivados de furoindazol
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
WO2022112186A1 (en) 2020-11-24 2022-06-02 Galapagos Nv Compound for use in and methods of treatment of fibrotic diseases
US12378229B2 (en) 2021-02-02 2025-08-05 Liminal Biosciences Limited GPR84 antagonists and uses thereof
WO2022179940A1 (en) 2021-02-23 2022-09-01 Bayer Aktiengesellschaft Furoindazole derivatives as gpr84 antagonists
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WO2022218372A1 (zh) * 2021-04-14 2022-10-20 武汉人福创新药物研发中心有限公司 一种二氢嘧啶并异喹啉酮类衍生物及用途
EP4330260A1 (en) 2021-04-29 2024-03-06 Bayer Aktiengesellschaft Furoindazole derivatives as antagonists or inhibitors of gpr84
EP4355743A1 (en) 2021-06-18 2024-04-24 University of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
WO2022268088A1 (zh) * 2021-06-21 2022-12-29 武汉人福创新药物研发中心有限公司 用于gpr84拮抗剂的三环化合物
CN115611944A (zh) 2021-07-15 2023-01-17 中国科学院上海药物研究所 不对称gpr84拮抗剂及其用途
WO2023076668A1 (en) * 2021-10-29 2023-05-04 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Compositions and methods for treatment of cancer
GB202202297D0 (en) 2022-02-21 2022-04-06 Verona Pharma Plc Formulation production process
WO2024083705A1 (en) 2022-10-18 2024-04-25 Bayer Aktiengesellschaft Furoindazole derivatives for the treatment of pain
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EP4698177A2 (en) * 2023-04-17 2026-02-25 The Board of Trustees of the Leland Stanford Junior University Method for detecting innate immune action in vivo using gpr84-pet
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AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11021509B2 (en) 2011-12-22 2021-06-01 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof

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CA2859578A1 (en) 2013-06-27
BR112014015142B1 (pt) 2022-03-29
PH12014501178A1 (en) 2014-10-20
PE20141685A1 (es) 2014-11-25
EA201491245A1 (ru) 2014-10-30
IL233212A0 (en) 2014-08-31
US9255095B2 (en) 2016-02-09
TWI567073B (zh) 2017-01-21
PL3378862T3 (pl) 2022-05-16
US8927543B2 (en) 2015-01-06
SI3378862T1 (sl) 2022-05-31
MX351681B (es) 2017-10-25
KR20140117427A (ko) 2014-10-07
CA2859578C (en) 2020-03-10
ZA201404607B (en) 2020-02-26
AU2012357067A1 (en) 2014-07-10
CN103998448B (zh) 2016-04-20
US20160244442A1 (en) 2016-08-25
US20190002458A1 (en) 2019-01-03
JP2015500861A (ja) 2015-01-08
SI2794604T1 (sl) 2017-12-29
NZ626473A (en) 2016-03-31
PH12014501178B1 (en) 2014-10-20
PT3378862T (pt) 2022-04-11
EP3378862B1 (en) 2022-03-16
CO7010835A2 (es) 2014-07-31
EA023826B1 (ru) 2016-07-29
HRP20171404T1 (hr) 2017-11-17
DK2794604T3 (da) 2017-11-06
CY1119434T1 (el) 2018-03-07
AR089284A1 (es) 2014-08-13
LT3378862T (lt) 2022-04-25
EP2794604A1 (en) 2014-10-29
TW201331201A (zh) 2013-08-01
EP4019519A1 (en) 2022-06-29
EP2794604B1 (en) 2017-09-13
AU2012357067B2 (en) 2017-01-05
CR20140305A (es) 2014-07-23
MX2014007363A (es) 2014-08-01
DK3378862T3 (da) 2022-04-11
KR102012268B1 (ko) 2019-08-21
JP6062453B2 (ja) 2017-01-18
HK1201528A1 (en) 2015-09-04
HRP20220456T1 (hr) 2022-05-27
US20220227751A1 (en) 2022-07-21
SG11201403169PA (en) 2014-07-30
IL257581A (en) 2018-04-30
ES2643379T3 (es) 2017-11-22
CN103998448A (zh) 2014-08-20
IL233212B (en) 2018-03-29
IN2014MN01033A (https=) 2015-05-01
ES2911449T3 (es) 2022-05-19
UA111767C2 (uk) 2016-06-10
NI201400060A (es) 2015-04-27
US10047083B2 (en) 2018-08-14
PT2794604T (pt) 2017-10-23
EP3378862A1 (en) 2018-09-26
US11220499B2 (en) 2022-01-11
PL2794604T3 (pl) 2017-12-29
LT2794604T (lt) 2017-10-25
US20140121204A1 (en) 2014-05-01
HUE12812237T4 (hu) 2017-12-28
US20130165437A1 (en) 2013-06-27
BR112014015142A2 (pt) 2017-06-13
WO2013092791A1 (en) 2013-06-27
ES2643379T9 (es) 2018-01-05
UY34545A (es) 2013-07-31
CY1125167T1 (el) 2024-09-20

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