DK3590517T3 - Heteroaryl-ketonkondenserede azadecalin som modulatorer af glucocorticoidreceptorer - Google Patents

Heteroaryl-ketonkondenserede azadecalin som modulatorer af glucocorticoidreceptorer Download PDF

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Publication number
DK3590517T3
DK3590517T3 DK19188885.8T DK19188885T DK3590517T3 DK 3590517 T3 DK3590517 T3 DK 3590517T3 DK 19188885 T DK19188885 T DK 19188885T DK 3590517 T3 DK3590517 T3 DK 3590517T3
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Prior art keywords
modulators
heteroaryl
glucocorticoid receptors
condensed azadecalin
ketone condensed
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DK19188885.8T
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Danish (da)
English (en)
Inventor
Hazel Hunt
Tony Johnson
Nicholas Ray
Iain Walters
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Corcept Therapeutics Inc
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Publication of DK3590517T3 publication Critical patent/DK3590517T3/da

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    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
    • A61K31/535Heterocyclic 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
    • 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
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P3/04Anorexiants; Antiobesity 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Electroluminescent Light Sources (AREA)
DK19188885.8T 2012-05-25 2013-05-24 Heteroaryl-ketonkondenserede azadecalin som modulatorer af glucocorticoidreceptorer DK3590517T3 (da)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201261651669P 2012-05-25 2012-05-25
US201261691083P 2012-08-20 2012-08-20
US201261715907P 2012-10-19 2012-10-19
US201361759520P 2013-02-01 2013-02-01
US201361781629P 2013-03-14 2013-03-14
EP18154256.4A EP3338781B1 (en) 2012-05-25 2013-05-24 Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

Publications (1)

Publication Number Publication Date
DK3590517T3 true DK3590517T3 (da) 2021-05-03

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Application Number Title Priority Date Filing Date
DK19188885.8T DK3590517T3 (da) 2012-05-25 2013-05-24 Heteroaryl-ketonkondenserede azadecalin som modulatorer af glucocorticoidreceptorer
DK13793417.0T DK2854814T3 (en) 2012-05-25 2013-05-24 Heteroberl ketone condensed azadecaline as modulators of glucocorticoid receptors
DK22193438.3T DK4119561T3 (da) 2012-05-25 2013-05-24 Heteroaryl-ketonkondenserede azadecalin-glucocorticoidreceptormodulatorer
DK21154665.0T DK3851107T3 (da) 2012-05-25 2013-05-24 Heteroaryl-ketonkondenseret azadecalin som glucocorticoidreceptormodulatorer
DK18154256T DK3338781T3 (da) 2012-05-25 2013-05-24 Heteroaryl-keton-kondenseret azadecalin som modulatorer af glucocorticoidreceptorer

Family Applications After (4)

Application Number Title Priority Date Filing Date
DK13793417.0T DK2854814T3 (en) 2012-05-25 2013-05-24 Heteroberl ketone condensed azadecaline as modulators of glucocorticoid receptors
DK22193438.3T DK4119561T3 (da) 2012-05-25 2013-05-24 Heteroaryl-ketonkondenserede azadecalin-glucocorticoidreceptormodulatorer
DK21154665.0T DK3851107T3 (da) 2012-05-25 2013-05-24 Heteroaryl-ketonkondenseret azadecalin som glucocorticoidreceptormodulatorer
DK18154256T DK3338781T3 (da) 2012-05-25 2013-05-24 Heteroaryl-keton-kondenseret azadecalin som modulatorer af glucocorticoidreceptorer

Country Status (24)

Country Link
EP (6) EP2854814B1 (enExample)
JP (1) JP6172871B2 (enExample)
KR (1) KR102062640B1 (enExample)
CN (1) CN104619328B (enExample)
AU (1) AU2013266110C1 (enExample)
BR (1) BR112014028857B1 (enExample)
CA (1) CA2872260C (enExample)
CL (1) CL2014003173A1 (enExample)
DK (5) DK3590517T3 (enExample)
ES (5) ES2995026T3 (enExample)
FI (1) FI4119561T3 (enExample)
HK (1) HK1250014B (enExample)
IL (1) IL235868A (enExample)
MX (1) MX365423B (enExample)
MY (1) MY172739A (enExample)
NZ (1) NZ701469A (enExample)
PE (1) PE20150352A1 (enExample)
PH (1) PH12014502584A1 (enExample)
PL (5) PL3338781T3 (enExample)
PT (5) PT3338781T (enExample)
RU (1) RU2639867C2 (enExample)
SG (1) SG11201407682TA (enExample)
WO (1) WO2013177559A2 (enExample)
ZA (1) ZA201408182B (enExample)

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US8859774B2 (en) 2012-05-25 2014-10-14 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US12226412B2 (en) 2012-05-25 2025-02-18 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
EP4219494B1 (en) 2013-11-25 2026-03-25 Corcept Therapeutics Incorporated Octahydro fused azadecalin glucocorticoid receptor modulators
WO2016140867A1 (en) * 2015-03-02 2016-09-09 Corcept Therapeutics, Inc. Use of glucocorticoid receptor antagonist and somatostatin analogues to treat acth-secreting tumors
US10610534B2 (en) * 2015-03-30 2020-04-07 Corcept Therapeutics, Inc. Use of glucocorticoid receptor antagonists in combination with glucocorticoids to treat adrenal insufficiency
CA2984623C (en) 2015-05-18 2023-05-02 Corcept Therapeutics, Inc. Methods for diagnosing and assessing treatment for cushing's syndrome
KR20180052120A (ko) 2015-08-13 2018-05-17 코어셉트 쎄라퓨틱스, 잉크. Acth-의존성 쿠싱 증후군을 감별 진단하는 방법
MX390517B (es) * 2016-03-01 2025-03-20 Corcept Therapeutics Inc Uso de moduladores del receptor de glucocorticoides para potenciar inhibidores de puntos de regulacion.
US9943505B2 (en) 2016-09-09 2018-04-17 Corcept Therapeutics, Inc. Glucocorticoid receptor modulators to treat pancreatic cancer
SG11201908790PA (en) 2017-03-31 2019-10-30 Corcept Therapeutics Inc Glucocorticoid receptor modulators to treat cervical cancer
MX393313B (es) 2017-06-20 2025-03-24 Corcept Therapeutics Inc Metodos de tratamiento de tumores neuroepiteliales usando moduladores selectivos del receptor de glucocorticoide.
CN112004803B (zh) * 2018-04-23 2023-11-03 科赛普特治疗公司 区域选择的n-烷基三唑的制备方法
BR112021008719A2 (pt) * 2018-11-09 2021-08-03 Corcept Therapeutics, Inc. método para reduzir o tamanho de um tumor pituitário visível em um paciente
AU2019404026B2 (en) * 2018-12-19 2023-06-08 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
US11234971B2 (en) 2018-12-19 2022-02-01 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
WO2020132046A1 (en) 2018-12-19 2020-06-25 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
WO2020132171A1 (en) * 2018-12-20 2020-06-25 Corcept Therapeutics Incorporated Methods for imaging and treatment of somatostatin-receptor positive tumors
CA3131263C (en) * 2019-02-22 2024-01-02 Corcept Therapeutics Incorporated Therapeutic uses of relacorilant, a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator
CN114650820A (zh) * 2019-10-16 2022-06-21 科赛普特治疗学股份有限公司 通过选择性糖皮质激素受体拮抗剂使癌症患者的中性粒细胞对淋巴细胞比例正常化的方法
US11903945B2 (en) 2019-12-11 2024-02-20 Corcept Therapeutics Incorporated Methods of treating antipsychotic-induced weight gain with miricorilant
WO2021127376A1 (en) 2019-12-21 2021-06-24 Corcept Therapeutics Incorporated Treatment of, and differential diagnosis between, acth-dependent cushing's syndrome and acth-independent cushing's syndrome
EP4103180A4 (en) * 2020-02-10 2024-03-13 Corcept Therapeutics Incorporated METHOD FOR STIMULATING AN ANTI-TUMOR RESPONSE USING A SELECTIVE GLUCOCORTICOID RECEPTOR MODULATOR
CN115916202A (zh) 2020-05-27 2023-04-04 科赛普特治疗学股份有限公司 糖皮质激素受体调节剂瑞拉可兰和cyp2c9底物的并行给药
KR20230017829A (ko) 2020-05-27 2023-02-06 코어셉트 쎄라퓨틱스 인코포레이티드 글루코코르티코이드 수용체 조절제 렐라코릴란트 및 cyp2c8과 cyp3a4의 이중 기질인 파클리탁셀의 병용 투여
WO2022134033A1 (en) * 2020-12-25 2022-06-30 Corcept Therapeutics Incorporated Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
WO2022166810A1 (zh) * 2021-02-03 2022-08-11 江苏恒瑞医药股份有限公司 稠合的氮杂三环类衍生物、其制备方法及其在医药上的应用
CN114907340A (zh) * 2021-02-09 2022-08-16 江苏恒瑞医药股份有限公司 稠合的氮杂三环类衍生物、其制备方法及其在医药上的应用
CN114907349A (zh) * 2021-02-10 2022-08-16 江苏恒瑞医药股份有限公司 稠合的氮杂三环类衍生物、其制备方法及其在医药上的应用
US12616698B2 (en) 2021-05-05 2026-05-05 Corcept Therapeutics Incorporated Methods for reducing liver fat and for treating fatty liver disorders
CN117510490A (zh) * 2022-08-03 2024-02-06 江苏恒瑞医药股份有限公司 一种稠合氮杂萘烷类衍生物的晶型及其制备方法
WO2024077169A1 (en) * 2022-10-06 2024-04-11 Corcept Therapeutics Incorporated Formulations of glucocorticoid receptor modulators
US12433882B2 (en) 2022-10-28 2025-10-07 Corcept Therapeutics Incorporated Treatments for amyotrophic lateral sclerosis using dazucorilant
WO2024173745A1 (en) * 2023-02-17 2024-08-22 Corcept Therapeutics Incorporated Methods and compositions for treating huntington's disease and its symptoms

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AU2005222421B2 (en) 2004-03-09 2010-09-23 Corcept Therapeutics, Inc. Fused ring azadecalin glucocorticoid receptor modulators
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EP1932843A1 (en) * 2006-12-14 2008-06-18 sanofi-aventis Sulfonyl-phenyl-2H-(1,2,4) oxadiazole-5-one derivatives, processes for their preparation and their use as pharmaceuticals
MX2013002186A (es) * 2010-08-27 2013-06-28 Corcept Therapeutics Inc Moduladores de azadecalina de piridil-amina fusionada.

Also Published As

Publication number Publication date
PL3590517T3 (pl) 2021-09-20
KR20150021955A (ko) 2015-03-03
AU2013266110C1 (en) 2018-07-12
SG11201407682TA (en) 2014-12-30
CL2014003173A1 (es) 2015-02-27
DK3338781T3 (da) 2019-12-09
JP6172871B2 (ja) 2017-08-02
ES2753816T3 (es) 2020-04-14
MY172739A (en) 2019-12-11
WO2013177559A3 (en) 2014-01-16
CN104619328A (zh) 2015-05-13
PL4119561T3 (pl) 2024-11-25
AU2013266110A1 (en) 2014-11-20
ES2665338T3 (es) 2018-04-25
RU2639867C2 (ru) 2017-12-25
EP2854814A2 (en) 2015-04-08
PT3338781T (pt) 2019-11-29
DK2854814T3 (en) 2018-03-12
MX365423B (es) 2019-06-03
IL235868A0 (en) 2015-01-29
FI4119561T3 (fi) 2024-11-01
HK1250014B (en) 2020-06-12
IL235868A (en) 2017-12-31
BR112014028857A2 (pt) 2017-08-15
AU2013266110B2 (en) 2017-04-20
PH12014502584B1 (en) 2015-01-21
RU2014152625A (ru) 2016-07-20
EP3590517B1 (en) 2021-03-17
EP4434584A2 (en) 2024-09-25
PL3338781T3 (pl) 2020-03-31
CN104619328B (zh) 2018-10-02
KR102062640B1 (ko) 2020-01-06
EP3851107A1 (en) 2021-07-21
PE20150352A1 (es) 2015-03-16
MX2014014239A (es) 2015-08-05
CA2872260A1 (en) 2013-11-28
EP3851107B1 (en) 2022-10-19
PL3851107T3 (pl) 2023-03-06
EP3590517A1 (en) 2020-01-08
CA2872260C (en) 2020-12-22
JP2015517580A (ja) 2015-06-22
EP4119561A1 (en) 2023-01-18
DK3851107T3 (da) 2022-11-21
EP2854814B1 (en) 2018-01-31
ES2873949T3 (es) 2021-11-04
HK1208818A1 (en) 2016-03-18
EP3338781B1 (en) 2019-09-11
PL2854814T3 (pl) 2018-07-31
ES2930298T3 (es) 2022-12-09
EP2854814A4 (en) 2016-01-27
EP4434584A3 (en) 2024-11-20
PH12014502584A1 (en) 2015-01-21
EP4119561B1 (en) 2024-09-11
PT2854814T (pt) 2018-03-15
BR112014028857B1 (pt) 2021-09-28
DK4119561T3 (da) 2024-09-30
NZ701469A (en) 2017-06-30
ES2995026T3 (en) 2025-02-05
PT3590517T (pt) 2021-04-07
PT3851107T (pt) 2022-10-28
WO2013177559A2 (en) 2013-11-28
PT4119561T (pt) 2024-09-30
ZA201408182B (en) 2017-09-27
EP3338781A1 (en) 2018-06-27

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