AU2016377702B2 - Inhibitors of glucocorticoid receptor - Google Patents

Inhibitors of glucocorticoid receptor Download PDF

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Publication number
AU2016377702B2
AU2016377702B2 AU2016377702A AU2016377702A AU2016377702B2 AU 2016377702 B2 AU2016377702 B2 AU 2016377702B2 AU 2016377702 A AU2016377702 A AU 2016377702A AU 2016377702 A AU2016377702 A AU 2016377702A AU 2016377702 B2 AU2016377702 B2 AU 2016377702B2
Authority
AU
Australia
Prior art keywords
optionally substituted
alkyl
carbocyclyl
cancer
heterocyclyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2016377702A
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English (en)
Other versions
AU2016377702A1 (en
Inventor
Minna Delarae BALBAS
Xiaohui Du
John Eksterowicz
Valeria R. Fantin
Lawrence R. Mcgee
Julio C. Medina
Yosup Rew
Daqing Sun
Xuelei Yan
Haiying Zhou
Liusheng Zhu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Oric Pharmaceuticals Inc
Original Assignee
Oric Pharmaceuticals Inc
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 Oric Pharmaceuticals Inc filed Critical Oric Pharmaceuticals Inc
Publication of AU2016377702A1 publication Critical patent/AU2016377702A1/en
Application granted granted Critical
Publication of AU2016377702B2 publication Critical patent/AU2016377702B2/en
Priority to AU2021202019A priority Critical patent/AU2021202019B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • 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
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096—Alkynyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0088—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Toxicology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2016377702A 2015-12-23 2016-12-22 Inhibitors of glucocorticoid receptor Ceased AU2016377702B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2021202019A AU2021202019B2 (en) 2015-12-23 2021-03-31 Inhibitors of glucocorticoid receptor

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562387282P 2015-12-23 2015-12-23
US62/387,282 2015-12-23
PCT/US2016/068431 WO2017112902A1 (en) 2015-12-23 2016-12-22 Inhibitors of glucocorticoid receptor

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2021202019A Division AU2021202019B2 (en) 2015-12-23 2021-03-31 Inhibitors of glucocorticoid receptor

Publications (2)

Publication Number Publication Date
AU2016377702A1 AU2016377702A1 (en) 2018-07-19
AU2016377702B2 true AU2016377702B2 (en) 2021-03-11

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
AU2016377702A Ceased AU2016377702B2 (en) 2015-12-23 2016-12-22 Inhibitors of glucocorticoid receptor
AU2021202019A Ceased AU2021202019B2 (en) 2015-12-23 2021-03-31 Inhibitors of glucocorticoid receptor

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2021202019A Ceased AU2021202019B2 (en) 2015-12-23 2021-03-31 Inhibitors of glucocorticoid receptor

Country Status (7)

Country Link
US (2) US11124537B2 (OSRAM)
EP (1) EP3394078A4 (OSRAM)
JP (2) JP6906525B2 (OSRAM)
CN (1) CN108699102A (OSRAM)
AU (2) AU2016377702B2 (OSRAM)
CA (1) CA3009522A1 (OSRAM)
WO (1) WO2017112902A1 (OSRAM)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017112904A1 (en) 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
EP3394078A4 (en) 2015-12-23 2019-11-27 Oric Pharmaceuticals, Inc. INHIBITORS OF THE GLUCOCORTICIDE RECEPTOR
JP6995757B2 (ja) 2015-12-23 2022-01-17 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体の阻害剤
WO2018068021A1 (en) 2016-10-07 2018-04-12 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
US11998606B2 (en) 2018-04-13 2024-06-04 Board Of Regents, The University Of Texas System Compounds and methods for selective proteolysis of glucocorticoid receptors
CN116322694A (zh) * 2020-08-04 2023-06-23 欧瑞克制药公司 糖皮质激素受体(gr)拮抗剂和雄激素受体(ar)降解剂组合的用途
WO2022046870A1 (en) * 2020-08-31 2022-03-03 The Trustees Of Indiana University Methods to prevent high-grade serous ovarian cancer and breast cancer by administering antiprogestins
WO2023000135A1 (en) * 2021-07-19 2023-01-26 Context Biopharma Inc. Processes of making onapristone and intermediates thereof

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US4447424A (en) * 1981-01-09 1984-05-08 Roussel Uclaf Steroid derivatives
EP0369881A1 (fr) * 1988-11-16 1990-05-23 Roussel-Uclaf Nouveaux produits dérivés de la structure 3-céto delta-4,9 19-nor stéroides et leur application comme médicaments
US5006518A (en) * 1987-12-30 1991-04-09 Roussel Uclaf Novel 17β-hydroxy-19-nor-steroids
WO1998031702A1 (en) * 1997-01-15 1998-07-23 Akzo Nobel N.V. 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives
US20030064973A1 (en) * 2001-08-16 2003-04-03 Vladimir Patchev Methods and compositions for treating diseases due to androgen deficiency with glucocorticoid receptor antagonist compounds and new compounds
US20040180869A1 (en) * 2002-12-16 2004-09-16 Ulrich Bothe New glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility
WO2007098382A2 (en) * 2006-02-17 2007-08-30 Janssen Pharmaceutica N.V. 17-phosphorous steroid derivatives useful as progesterone receptor modulators
US20130029953A1 (en) * 2011-07-28 2013-01-31 Klaus Nickisch Progesterone antagonists
WO2014197653A2 (en) * 2013-06-05 2014-12-11 Evestra, Inc. Imidazolyl progesterone antagonists

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FR2522328B1 (fr) 1982-03-01 1986-02-14 Roussel Uclaf Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments
DE3921059A1 (de) 1989-06-23 1991-01-10 Schering Ag 11(beta)-aryl-4-estrene, verfahren zu ihrer herstellung sowie deren verwendung als arzneimittel
FR2651435A1 (fr) 1989-09-07 1991-03-08 Roussel Uclaf Nouvelle utilisation de composes anti-progestomimetiques.
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WO1995017192A1 (en) 1993-12-22 1995-06-29 The Salk Institute For Biological Studies Methods for reducing multidrug resistance
WO1996023503A1 (de) 1995-02-02 1996-08-08 Schering Aktiengesellschaft Progesteronantagonisten für die herstellung von arzneimitteln zur behandlung von dysfunktionellen uterinen blutungen
IL118974A (en) 1995-08-17 2001-09-13 Akzo Nobel Nv History 11 - (Transformed Phenyl) - Astra - 4, 9 - Diane, their preparation and pharmaceutical preparations containing them
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EP2545922A1 (en) 2011-07-12 2013-01-16 PregLem S.A. Treatment of excessive menstrual bleeding associated with uterine fibroids
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EP3394078A4 (en) 2015-12-23 2019-11-27 Oric Pharmaceuticals, Inc. INHIBITORS OF THE GLUCOCORTICIDE RECEPTOR
JP6995757B2 (ja) 2015-12-23 2022-01-17 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体の阻害剤
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Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4447424A (en) * 1981-01-09 1984-05-08 Roussel Uclaf Steroid derivatives
US5006518A (en) * 1987-12-30 1991-04-09 Roussel Uclaf Novel 17β-hydroxy-19-nor-steroids
EP0369881A1 (fr) * 1988-11-16 1990-05-23 Roussel-Uclaf Nouveaux produits dérivés de la structure 3-céto delta-4,9 19-nor stéroides et leur application comme médicaments
WO1998031702A1 (en) * 1997-01-15 1998-07-23 Akzo Nobel N.V. 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives
US20030064973A1 (en) * 2001-08-16 2003-04-03 Vladimir Patchev Methods and compositions for treating diseases due to androgen deficiency with glucocorticoid receptor antagonist compounds and new compounds
US20040180869A1 (en) * 2002-12-16 2004-09-16 Ulrich Bothe New glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility
WO2007098382A2 (en) * 2006-02-17 2007-08-30 Janssen Pharmaceutica N.V. 17-phosphorous steroid derivatives useful as progesterone receptor modulators
US20130029953A1 (en) * 2011-07-28 2013-01-31 Klaus Nickisch Progesterone antagonists
WO2014197653A2 (en) * 2013-06-05 2014-12-11 Evestra, Inc. Imidazolyl progesterone antagonists

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Title
CAS Registry Number 1060698-58-9; STN Entry Date 13 October 2008; Acetamide, N-[4-[(11β)-17-hydroxy-11-(3-methylphenyl)-3-oxo-19-norpregna-4,9-dien-20-yn-21-yl]phenyl]- *
CHEMICAL ABSTRACTS, (2004-10-10), Database accession no. 760141-59-1 *
GEBHARD, R. et al., "11,21-Bisphenyl-19-norpregnane derivatives are selective antiglucocorticoids", Bioorganic & Medicinal Chemistry Letters, (1997-09-09), vol. 7, no. 17, pages 2229 - 2234 *
HAZRA, B. G. ET AL, STEROIDS, 2000, vol. 65 (3), pages 157 - 162 *

Also Published As

Publication number Publication date
JP2021167323A (ja) 2021-10-21
EP3394078A4 (en) 2019-11-27
US20210395295A1 (en) 2021-12-23
US20210017220A1 (en) 2021-01-21
JP2019500374A (ja) 2019-01-10
EP3394078A1 (en) 2018-10-31
JP6906525B2 (ja) 2021-07-21
CA3009522A1 (en) 2017-06-29
AU2021202019B2 (en) 2022-01-27
AU2021202019A1 (en) 2021-04-29
US11124537B2 (en) 2021-09-21
AU2016377702A1 (en) 2018-07-19
CN108699102A (zh) 2018-10-23
WO2017112902A1 (en) 2017-06-29

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