RU2639867C2 - Конденсированные с гетероарилкетонами азадекалины - модуляторы глюкокортикоидных рецепторов - Google Patents

Конденсированные с гетероарилкетонами азадекалины - модуляторы глюкокортикоидных рецепторов Download PDF

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RU2639867C2
RU2639867C2 RU2014152625A RU2014152625A RU2639867C2 RU 2639867 C2 RU2639867 C2 RU 2639867C2 RU 2014152625 A RU2014152625 A RU 2014152625A RU 2014152625 A RU2014152625 A RU 2014152625A RU 2639867 C2 RU2639867 C2 RU 2639867C2
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fluorophenyl
pyrazolo
isoquinolin
hexahydro
methanone
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RU2014152625A
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Russian (ru)
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RU2014152625A (ru
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Хейзел ХАНТ
Тони ДЖОНСОН
Николас РЭЙ
Айэйн УОЛТЕРС
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Корсепт Терапьютикс, Инк.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/495—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
    • A61K31/535—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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • 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
    • C07D498/04—Ortho-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)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (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)
  • Electroluminescent Light Sources (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2014152625A 2012-05-25 2013-05-24 Конденсированные с гетероарилкетонами азадекалины - модуляторы глюкокортикоидных рецепторов RU2639867C2 (ru)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US201261651669P 2012-05-25 2012-05-25
US61/651,669 2012-05-25
US201261691083P 2012-08-20 2012-08-20
US61/691,083 2012-08-20
US201261715907P 2012-10-19 2012-10-19
US61/715,907 2012-10-19
US201361759520P 2013-02-01 2013-02-01
US61/759,520 2013-02-01
US201361781629P 2013-03-14 2013-03-14
US61/781,629 2013-03-14
PCT/US2013/042732 WO2013177559A2 (en) 2012-05-25 2013-05-24 Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

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RU2014152625A RU2014152625A (ru) 2016-07-20
RU2639867C2 true RU2639867C2 (ru) 2017-12-25

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JP (1) JP6172871B2 (enExample)
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AU (1) AU2013266110C1 (enExample)
BR (1) BR112014028857B1 (enExample)
CA (1) CA2872260C (enExample)
CL (1) CL2014003173A1 (enExample)
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ES (5) ES2995026T3 (enExample)
FI (1) FI4119561T3 (enExample)
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PL (5) PL3851107T3 (enExample)
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RU (1) RU2639867C2 (enExample)
SG (1) SG11201407682TA (enExample)
WO (1) WO2013177559A2 (enExample)
ZA (1) ZA201408182B (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11648245B2 (en) 2012-05-25 2023-05-16 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US11925626B2 (en) 2018-12-19 2024-03-12 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
US12226412B2 (en) 2012-05-25 2025-02-18 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US12433882B2 (en) 2022-10-28 2025-10-07 Corcept Therapeutics Incorporated Treatments for amyotrophic lateral sclerosis using dazucorilant
US12589094B2 (en) 2020-05-27 2026-03-31 Corcept Therapeutics Incorporated Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of CYP2C8 and CYP3A4

Families Citing this family (30)

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ES2943542T3 (es) * 2013-11-25 2023-06-14 Corcept Therapeutics Inc Moduladores del receptor de glucocorticoides de azadecalina condensada con octahidro
JP6821582B2 (ja) * 2015-03-02 2021-01-27 コーセプト セラピューティクス, インコーポレイテッド Acth分泌腫瘍を処置するための糖質コルチコイドレセプターアンタゴニストおよびソマトスタチンアナログの使用
JP6754533B2 (ja) 2015-03-30 2020-09-16 コーセプト セラピューティクス, インコーポレイテッド 副腎機能不全を処置するための糖質コルチコイドと組み合わせた糖質コルチコイドレセプターアンタゴニストの使用
US10604807B2 (en) 2015-05-18 2020-03-31 Corcept Therapeutics, Inc. Methods for diagnosing and assessing treatment for Cushing's syndrome
MX383318B (es) * 2015-08-13 2025-03-13 Corcept Therapeutics Inc Metodo para diagnosticar de manera diferencial el sindrome de cushing dependiente de la corticotropina.
AU2017228329B2 (en) * 2016-03-01 2021-03-11 Corcept Therapeutics, Inc. The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors
US9943505B2 (en) * 2016-09-09 2018-04-17 Corcept Therapeutics, Inc. Glucocorticoid receptor modulators to treat pancreatic cancer
AU2018244928B2 (en) 2017-03-31 2023-10-19 Corcept Therapeutics, Inc. Glucocorticoid receptor modulators to treat cervical cancer
WO2018236749A2 (en) 2017-06-20 2018-12-27 Corcept Therapeutics, Inc. Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators
IL278125B (en) * 2018-04-23 2022-09-01 Corcept Therapeutics Inc Methods for the preparation of regioselective n-alkyl triazoles
SG11202104732UA (en) 2018-11-09 2021-06-29 Corcept Therapeutics Inc Methods for shrinking pituitary tumors
US11389432B2 (en) 2018-12-19 2022-07-19 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
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
MX2021007402A (es) * 2018-12-20 2021-07-15 Corcept Therapeutics Inc Metodos para la toma de imagenes y el tratamiento de tumores positivos para el receptor de somatostatina.
NZ778399A (en) 2019-02-22 2024-11-29 Corcept Therapeutics Inc Therapeutic uses of relacorilant, a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator
AU2020367769B2 (en) * 2019-10-16 2023-10-12 Corcept Therapeutics Incorporated Method of normalizing the neutrophil to lymphocyte ratio in cancer patients with a selective glucocorticoid receptor antagonist
JP7569492B2 (ja) 2019-12-11 2024-10-18 コーセプト セラピューティクス, インコーポレイテッド 抗精神病薬誘発性体重増加のミリコリラントによる治療方法
AU2020408057B2 (en) * 2019-12-21 2026-01-29 Corcept Therapeutics Incorporated Treatment of, and differential diagnosis between, ACTH-Dependent Cushing's syndrome and ACTH-Independent Cushing's syndrome
AU2021214938B2 (en) 2020-01-29 2024-02-08 Corcept Therapeutics Incorporated Treatment of adrenocortical carcinoma with selective glucocorticoid receptor modulators (SGRMs) and antibody checkpoint inhibitors
JP2023515781A (ja) * 2020-02-10 2023-04-14 コーセプト セラピューティクス, インコーポレイテッド 選択的グルココルチコイド受容体モジュレーターを使用して抗腫瘍応答を刺激する方法
MX2022014923A (es) 2020-05-27 2023-01-04 Corcept Therapeutics Inc Administracion concomitante del modulador del receptor de glucocorticoides relacorilant y sustratos cyp2c9.
WO2022134033A1 (en) * 2020-12-25 2022-06-30 Corcept Therapeutics Incorporated Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
TW202246260A (zh) * 2021-02-03 2022-12-01 大陸商江蘇恆瑞醫藥股份有限公司 稠合的氮雜三環類衍生物、其製備方法及其在醫藥上的應用
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
CN114907349B (zh) * 2021-02-10 2026-06-12 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
AU2024223250A1 (en) * 2023-02-17 2025-08-14 Corcept Therapeutics Incorporated Methods and compositions for treating huntington's disease and its symptoms
WO2026132432A1 (en) 2024-12-20 2026-06-25 Curia Spain, S.A.U. Relacorilant crystalline forms

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WO2005087769A1 (en) * 2004-03-09 2005-09-22 Corcept Therapeutics, Inc. Fused ring azadecalin glucocorticoid receptor modulators
RU2009126745A (ru) * 2006-12-14 2011-01-20 Санофи-Авентис (Fr) Производные сульфонилфенил-2н-{1,2,4}оксадиазол-5-она, способы их получения и их применение в качестве фармацевтических средств
WO2012027702A1 (en) * 2010-08-27 2012-03-01 Corcept Therapeutics, Inc. Pyridyl-amine fused azadecalin modulators

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11648245B2 (en) 2012-05-25 2023-05-16 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
US11925626B2 (en) 2018-12-19 2024-03-12 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
US12514849B2 (en) 2018-12-19 2026-01-06 Corcept Therapeutics Incorporated Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
US12589094B2 (en) 2020-05-27 2026-03-31 Corcept Therapeutics Incorporated Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of CYP2C8 and CYP3A4
US12433882B2 (en) 2022-10-28 2025-10-07 Corcept Therapeutics Incorporated Treatments for amyotrophic lateral sclerosis using dazucorilant

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ZA201408182B (en) 2017-09-27
MX2014014239A (es) 2015-08-05
PT3851107T (pt) 2022-10-28
EP4434584A3 (en) 2024-11-20
JP2015517580A (ja) 2015-06-22
KR102062640B1 (ko) 2020-01-06
EP4119561B1 (en) 2024-09-11
KR20150021955A (ko) 2015-03-03
BR112014028857B1 (pt) 2021-09-28
EP2854814B1 (en) 2018-01-31
ES2873949T3 (es) 2021-11-04
ES2930298T3 (es) 2022-12-09
BR112014028857A2 (pt) 2017-08-15
EP3590517B1 (en) 2021-03-17
PT3590517T (pt) 2021-04-07
AU2013266110C1 (en) 2018-07-12
PL3590517T3 (pl) 2021-09-20
WO2013177559A3 (en) 2014-01-16
NZ701469A (en) 2017-06-30
PL4119561T3 (pl) 2024-11-25
JP6172871B2 (ja) 2017-08-02
EP3851107B1 (en) 2022-10-19
PT3338781T (pt) 2019-11-29
AU2013266110B2 (en) 2017-04-20
WO2013177559A2 (en) 2013-11-28
PH12014502584A1 (en) 2015-01-21
MX365423B (es) 2019-06-03
CL2014003173A1 (es) 2015-02-27
DK2854814T3 (en) 2018-03-12
EP3851107A1 (en) 2021-07-21
AU2013266110A1 (en) 2014-11-20
IL235868A0 (en) 2015-01-29
PH12014502584B1 (en) 2015-01-21
DK3338781T3 (da) 2019-12-09
IL235868A (en) 2017-12-31
PL3851107T3 (pl) 2023-03-06
ES2753816T3 (es) 2020-04-14
EP2854814A2 (en) 2015-04-08
ES2665338T3 (es) 2018-04-25
EP3338781A1 (en) 2018-06-27
EP2854814A4 (en) 2016-01-27
DK3590517T3 (da) 2021-05-03
CN104619328B (zh) 2018-10-02
MY172739A (en) 2019-12-11
CA2872260A1 (en) 2013-11-28
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