CA2930232C - Aramchol salts - Google Patents

Aramchol salts Download PDF

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Publication number
CA2930232C
CA2930232C CA2930232A CA2930232A CA2930232C CA 2930232 C CA2930232 C CA 2930232C CA 2930232 A CA2930232 A CA 2930232A CA 2930232 A CA2930232 A CA 2930232A CA 2930232 C CA2930232 C CA 2930232C
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CA
Canada
Prior art keywords
beta
alpha
amine
salt
cholan
Prior art date
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Active
Application number
CA2930232A
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English (en)
French (fr)
Other versions
CA2930232A1 (en
Inventor
Allen BAHARAFF
Idit Eshkar-Oren
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Galmed Research and Development Ltd
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Galmed Research and Development Ltd
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Publication of CA2930232A1 publication Critical patent/CA2930232A1/en
Application granted granted Critical
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/03—Monoamines
    • C07C211/05—Mono-, di- or tri-ethylamine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CA2930232A 2013-12-04 2014-12-04 Aramchol salts Active CA2930232C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361911478P 2013-12-04 2013-12-04
US61/911,478 2013-12-04
PCT/IL2014/051052 WO2015083164A1 (en) 2013-12-04 2014-12-04 Aramchol salts

Publications (2)

Publication Number Publication Date
CA2930232A1 CA2930232A1 (en) 2015-06-11
CA2930232C true CA2930232C (en) 2020-09-15

Family

ID=53272986

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2930232A Active CA2930232C (en) 2013-12-04 2014-12-04 Aramchol salts

Country Status (21)

Country Link
US (1) US20160304553A1 (https=)
EP (1) EP3077047B1 (https=)
JP (2) JP6675310B2 (https=)
KR (1) KR102320191B1 (https=)
CN (2) CN110437298A (https=)
AU (2) AU2014358668B2 (https=)
BR (1) BR112016012465B1 (https=)
CA (1) CA2930232C (https=)
CY (1) CY1121736T1 (https=)
DK (1) DK3077047T3 (https=)
ES (1) ES2732845T3 (https=)
HR (1) HRP20191023T1 (https=)
HU (1) HUE045209T2 (https=)
LT (1) LT3077047T (https=)
PL (1) PL3077047T3 (https=)
PT (1) PT3077047T (https=)
RS (1) RS59067B1 (https=)
SI (1) SI3077047T1 (https=)
SM (1) SMT201900363T1 (https=)
TR (1) TR201909447T4 (https=)
WO (1) WO2015083164A1 (https=)

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Publication number Priority date Publication date Assignee Title
IL227890A0 (en) * 2013-08-08 2014-01-30 Galderm Therapeutics Ltd Antiaging compounds containing bile acid and fatty acid conjugates
SI3077047T1 (sl) * 2013-12-04 2019-09-30 Galmed Research & Development Ltd. Soli aramchola
US10849911B2 (en) 2015-06-10 2020-12-01 Galmed Research And Development Ltd. Low dose compositions of Aramachol salts
CN108337879B (zh) * 2015-07-12 2021-01-19 西夫索有限公司 硫酸胆钙化醇的盐及其用于治疗维生素d3缺乏的用途
WO2017017677A1 (en) * 2015-07-27 2017-02-02 Galmed Research And Development Ltd. Combination treatment for liver disease
IL243707A0 (en) 2016-01-20 2016-05-01 Galmed Res And Dev Ltd Treatment to regulate the microbiota in the intestine
FR3050112B1 (fr) 2016-04-15 2020-09-04 Soc Civ Immobiliere Gecinq Utilisation de l'acide fenofibrique dans le traitement des maladies hepatiques
EP3518918A4 (en) * 2016-09-28 2020-04-22 Eiger Biopharmaceuticals, Inc. METHOD AND PHARMACEUTICAL COMPOSITIONS FOR TREATING NON-ALCOHOLIC STEATOHEPATITIS
US11197870B2 (en) 2016-11-10 2021-12-14 Galmed Research And Development Ltd Treatment for hepatic fibrosis
MA46786A (fr) * 2016-11-10 2019-09-18 Galmed Res And Development Ltd Inhibition de la fibrose chez des patients atteints d'une stéatose hépatique non alcoolique
US11136347B2 (en) 2017-06-07 2021-10-05 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystalline forms of a fatty acid bile acid conjugate, preparation method thereof and use thereof
WO2019055280A1 (en) 2017-09-13 2019-03-21 Emmyon, Inc. DIETHANOLAMINE SALTS AND URSOLIC ACID MORPHOLIN
US20190183832A1 (en) * 2017-12-20 2019-06-20 Michael Guarnieri Nutritional bolus for animals
WO2020026471A1 (ja) * 2018-07-31 2020-02-06 株式会社親広産業 グルコース消費促進剤および解糖系促進剤
JP6612004B1 (ja) * 2018-07-31 2019-11-27 株式会社親広産業 グルコース消費促進剤および解糖系促進剤
CN117769561A (zh) * 2021-04-19 2024-03-26 神经创伤科学有限责任公司 (3E)3-[o-[(膦酰氧基)甲基]肟]-孕烯-4-烯-3,20-二酮的盐和晶型及相关用途
US20260062432A1 (en) * 2022-09-02 2026-03-05 Rexpharmtech Co., Ltd Novel benfotiamine choline salt
US12090151B1 (en) 2023-05-12 2024-09-17 Michael Guarnieri Injectable sustained release buprenorphine formulation

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GB1532413A (en) * 1974-12-23 1978-11-15 Union International Co Ltd Chenodeoxycholic acid
IL123998A (en) * 1998-04-08 2004-09-27 Galmed Int Ltd Conjugates of bile salts and pharmaceutical preparations containing them
IL142650A (en) * 1998-04-08 2007-06-03 Galmed Int Ltd Use of bile acid conjugates or bile salts and fatty acids or fatty acids in the preparation of pharmaceuticals for lowering cholesterol, for the treatment of fatty liver and for the treatment of hyperglycemia and diabetes
CA2386190C (en) * 1999-10-13 2009-04-14 Johns Hopkins University School Of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
US8975246B2 (en) * 2001-04-17 2015-03-10 Galmed Research And Development Ltd. Bile acid or bile salt fatty acid conjugates
CN1950086A (zh) * 2004-04-28 2007-04-18 默克公司 作为雄激素受体调节剂的氟化的4－氮杂甾族化合物
ITMI20061735A1 (it) * 2006-09-12 2008-03-13 Dipharma Spa Procedimento per la preparazione di acidi colanici
DE102007032507A1 (de) * 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
US20120157419A1 (en) * 2009-02-02 2012-06-21 Tuvia Gilat Methods and compositions for treating alzheimer's disease
US20120251492A1 (en) * 2009-12-15 2012-10-04 Meiji Seika Pharma Co., Ltd. Triterpene derivative and agent for preventing or treating chronic hepatitis c
CN102115486B (zh) * 2009-12-30 2015-06-03 上海特化医药科技有限公司 一种3-β-花生酰胺基-7α,12α,5β-胆烷-24-羧酸的制备方法
BR112012018913A2 (pt) * 2010-01-28 2017-06-20 Merck Sharp & Dohme "composição farmacêutica, e, uso da composição"
PL2531501T3 (pl) * 2010-02-03 2014-05-30 Takeda Pharmaceuticals Co Inhibitory kinazy 1 regulującej sygnał apoptotyczny
EP3360552A1 (en) * 2010-12-07 2018-08-15 Amira Pharmaceuticals, Inc. Polycyclic lpa1 antagonist and uses thereof
SI3077047T1 (sl) * 2013-12-04 2019-09-30 Galmed Research & Development Ltd. Soli aramchola

Also Published As

Publication number Publication date
JP2020111584A (ja) 2020-07-27
TR201909447T4 (tr) 2019-07-22
WO2015083164A1 (en) 2015-06-11
JP2016539131A (ja) 2016-12-15
EP3077047A1 (en) 2016-10-12
BR112016012465A8 (pt) 2020-05-05
PL3077047T3 (pl) 2019-10-31
RS59067B1 (sr) 2019-09-30
AU2014358668B2 (en) 2019-10-24
ES2732845T3 (es) 2019-11-26
HRP20191023T1 (hr) 2019-09-06
AU2014358668A1 (en) 2016-06-02
CA2930232A1 (en) 2015-06-11
SI3077047T1 (sl) 2019-09-30
EP3077047B1 (en) 2019-04-24
PT3077047T (pt) 2019-07-11
HK1226347A1 (zh) 2017-09-29
BR112016012465B1 (pt) 2023-04-18
EP3077047A4 (en) 2017-05-03
JP6675310B2 (ja) 2020-04-01
KR20160093051A (ko) 2016-08-05
SMT201900363T1 (it) 2019-09-09
CN105848718A (zh) 2016-08-10
AU2019275638B2 (en) 2021-05-06
AU2019275638A1 (en) 2020-01-23
HUE045209T2 (hu) 2019-12-30
CN105848718B (zh) 2019-07-30
US20160304553A1 (en) 2016-10-20
CN110437298A (zh) 2019-11-12
DK3077047T3 (da) 2019-07-15
CY1121736T1 (el) 2020-07-31
KR102320191B1 (ko) 2021-11-03
LT3077047T (lt) 2019-08-26

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