DK3131902T3 - Forbindelser som ROR-gamma-modulatorer - Google Patents

Forbindelser som ROR-gamma-modulatorer Download PDF

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Publication number
DK3131902T3
DK3131902T3 DK15718330.2T DK15718330T DK3131902T3 DK 3131902 T3 DK3131902 T3 DK 3131902T3 DK 15718330 T DK15718330 T DK 15718330T DK 3131902 T3 DK3131902 T3 DK 3131902T3
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DK
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Prior art keywords
ror
compounds
gamma modulators
modulators
gamma
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DK15718330.2T
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English (en)
Inventor
Johanna Bakonyi
Steven Richard Brunette
Delphine Collin
Robert Owen Hughes
Xiang Li
Robert Sibley
Michael Robert Turner
Lifen Wu
Qiang Zhang
Shuang Liang
Original Assignee
Boehringer Ingelheim Int
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Publication of DK3131902T3 publication Critical patent/DK3131902T3/da

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/08—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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/10—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with an aromatic or hetero-aromatic ring directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
DK15718330.2T 2014-04-14 2015-04-10 Forbindelser som ROR-gamma-modulatorer DK3131902T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461979231P 2014-04-14 2014-04-14
PCT/US2015/025328 WO2015160654A1 (en) 2014-04-14 2015-04-10 Compounds as modulators of ror gamma

Publications (1)

Publication Number Publication Date
DK3131902T3 true DK3131902T3 (da) 2019-09-02

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
DK15718330.2T DK3131902T3 (da) 2014-04-14 2015-04-10 Forbindelser som ROR-gamma-modulatorer

Country Status (36)

Country Link
US (5) US9242989B2 (da)
EP (2) EP3418280B1 (da)
JP (2) JP6282759B2 (da)
KR (2) KR102410076B1 (da)
CN (3) CN106132965B (da)
AP (1) AP2016009403A0 (da)
AR (2) AR100058A1 (da)
AU (2) AU2015247983B2 (da)
BR (2) BR122020020657B1 (da)
CA (1) CA2944787C (da)
CL (1) CL2016002421A1 (da)
CY (1) CY1122012T1 (da)
DK (1) DK3131902T3 (da)
EA (2) EA035063B1 (da)
ES (1) ES2744299T3 (da)
HK (2) HK1244800A1 (da)
HR (1) HRP20191579T1 (da)
HU (1) HUE045847T2 (da)
IL (2) IL247419B (da)
LT (1) LT3131902T (da)
MA (1) MA46373A (da)
ME (1) ME03513B (da)
MX (1) MX370780B (da)
MY (1) MY182834A (da)
NZ (1) NZ723530A (da)
PE (2) PE20211002A1 (da)
PH (2) PH12016502019A1 (da)
PL (1) PL3131902T3 (da)
PT (1) PT3131902T (da)
RS (1) RS59170B1 (da)
SG (1) SG11201608537SA (da)
SI (1) SI3131902T1 (da)
TW (2) TWI652268B (da)
UA (2) UA120094C2 (da)
UY (1) UY36077A (da)
WO (1) WO2015160654A1 (da)

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JP6282759B2 (ja) 2014-04-14 2018-02-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｒｏｒガンマのモジュレーターとしての化合物
FR3030518B1 (fr) * 2014-12-19 2018-03-23 Galderma Research & Development Derives sulfonamides en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t)
CN108026045B (zh) 2015-05-15 2021-04-27 奥瑞基尼探索技术有限公司 用作RORγ调节剂的经过取代的四氢喹啉酮化合物
US10450314B2 (en) 2015-10-01 2019-10-22 Boehringer Ingelheim International Gmbh Pteridine derivatives as modulators of ROR gamma
MX2018007296A (es) 2015-12-15 2019-01-10 Astrazeneca Ab Compuestos de isoindol.
JP6899391B2 (ja) * 2016-01-20 2021-07-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ガンマのモジュレータとしての化合物
AR110481A1 (es) 2016-12-05 2019-04-03 Lead Pharma Holding Bv MODULADORES DE ROR g (RORg)
US20200031753A1 (en) 2017-04-06 2020-01-30 Boehringer Ingelheim International Gmbh Cyclopropyl alkyl amines and process for their preparation
CN110730780A (zh) 2017-06-14 2020-01-24 阿斯利康(瑞典)有限公司 用作ROR-γ调节剂的2，3-二氢异吲哚-1-甲酰胺
CN109206346A (zh) * 2017-07-01 2019-01-15 复旦大学 叔胺类衍生物或其盐及其制备方法和用途
CN107903263B (zh) * 2017-12-28 2019-11-12 山东铂源药业有限公司 一种帕布昔利布中间体的合成方法
TWI818985B (zh) 2018-05-03 2023-10-21 中國大陸商江蘇恒瑞醫藥股份有限公司 作為類視色素相關孤兒受體γ（ＲＯＲγ）調節劑之苯并咪唑衍生物及其醫藥用途
WO2020079145A1 (en) 2018-10-18 2020-04-23 Boehringer Ingelheim International Gmbh Scalable synthesis of optically active 1-cyclopropylalkyl-1-amines
US20230014730A1 (en) 2019-09-23 2023-01-19 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
CN114502535B (zh) 2019-10-31 2024-04-12 江苏恒瑞医药股份有限公司 一种RORγ调节剂的酸加成盐
WO2022106549A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline salts of a ror gamma inhibitor
WO2022106551A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Co-crystals of a ror gamma inhibitor
WO2022106550A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline polymorphic form of a ror gamma inhibitor
WO2022106548A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Solid forms of a ror gamma inhibitor
WO2022106547A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Process for synthesising a ror gamma inhibitor
CN117003757A (zh) * 2022-05-07 2023-11-07 苏州浦合医药科技有限公司 取代的双环杂芳基化合物作为usp1抑制剂
WO2023232870A1 (en) 2022-05-31 2023-12-07 Immunic Ag Rorg/rorgt modulators for the treatment of virus infections like covid-19
CN116178279A (zh) * 2023-03-15 2023-05-30 上海药坦药物研究开发有限公司 一种5-溴-4-环丙基-6-甲氧基嘧啶及其中间体的制备方法

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SE0102716D0 (sv) * 2001-08-14 2001-08-14 Astrazeneca Ab Novel compounds
WO2009022185A2 (en) * 2007-08-16 2009-02-19 Astrazeneca Ab 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use
CA2737472A1 (en) 2008-09-26 2010-04-01 Boehringer Ingelheim International Gmbh Azaindazole compounds as ccr1 receptor antagonists
IN2012DN03449A (da) 2009-10-21 2015-10-23 Boehringer Ingelheim Int
JP6093759B2 (ja) * 2011-06-01 2017-03-08 ジャナス バイオセラピューティクス，インク． 新規の免疫系調節剤
DE112013002484B4 (de) * 2012-05-14 2023-05-04 Shanghai Yidian Pharmaceutical Technology Development Co., Ltd. Pteridinketon-Derivat und Anwendungen desselben als EGFR-, BLK- und FLT3-Inhibitor
JP6282759B2 (ja) * 2014-04-14 2018-02-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｒｏｒガンマのモジュレーターとしての化合物
US10450314B2 (en) * 2015-10-01 2019-10-22 Boehringer Ingelheim International Gmbh Pteridine derivatives as modulators of ROR gamma
JP6899391B2 (ja) * 2016-01-20 2021-07-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ガンマのモジュレータとしての化合物

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AU2019203027B2 (en) 2020-07-09
UY36077A (es) 2015-10-30
LT3131902T (lt) 2019-09-25
MY182834A (en) 2021-02-05
EP3131902A1 (en) 2017-02-22
BR112016021962A2 (pt) 2023-01-20
US20190002465A1 (en) 2019-01-03
US20180022749A1 (en) 2018-01-25
US9598415B2 (en) 2017-03-21
AR119454A2 (es) 2021-12-22
EA031351B1 (ru) 2018-12-28
CN106132965A (zh) 2016-11-16
HK1244800A1 (zh) 2018-08-17
TW201625622A (zh) 2016-07-16
BR112016021962B1 (pt) 2022-12-13
AP2016009403A0 (en) 2016-08-31
AU2019203027A1 (en) 2019-05-23
KR102410069B1 (ko) 2022-06-20
EA201890329A1 (ru) 2018-07-31
CN107266454B (zh) 2019-08-09
AU2015247983A1 (en) 2016-09-08
EA201691978A1 (ru) 2017-02-28
KR20160142396A (ko) 2016-12-12
PH12020500252A1 (en) 2021-07-26
AR100058A1 (es) 2016-09-07
KR102410076B1 (ko) 2022-06-22
JP2017511357A (ja) 2017-04-20
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
KR20200040917A (ko) 2020-04-20
TWI655192B (zh) 2019-04-01
PH12016502019B1 (en) 2017-01-09
NZ723530A (en) 2023-05-26
PT3131902T (pt) 2019-09-17
UA120094C2 (uk) 2019-10-10
UA121255C2 (uk) 2020-04-27
MX2016013342A (es) 2017-01-26
MX370780B (es) 2020-01-03
US20160075706A1 (en) 2016-03-17
EP3131902B1 (en) 2019-06-12
EA035063B1 (ru) 2020-04-23
CN107266450A (zh) 2017-10-20
US20150291607A1 (en) 2015-10-15
CL2016002421A1 (es) 2017-03-24
PE20161572A1 (es) 2017-02-01
HK1244801A1 (zh) 2018-08-17
AU2015247983B2 (en) 2019-05-16
EP3418280A1 (en) 2018-12-26
PL3131902T3 (pl) 2019-11-29
BR122020020657B1 (pt) 2022-12-20
PE20211002A1 (es) 2021-06-01
CN107266454A (zh) 2017-10-20
HRP20191579T1 (hr) 2019-11-29
TWI652268B (zh) 2019-03-01
CY1122012T1 (el) 2020-10-14
ME03513B (me) 2020-04-20
RS59170B1 (sr) 2019-10-31
TW201841915A (zh) 2018-12-01
JP6463855B2 (ja) 2019-02-06
US9242989B2 (en) 2016-01-26
SI3131902T1 (sl) 2019-10-30
JP6282759B2 (ja) 2018-02-21
WO2015160654A1 (en) 2015-10-22
CA2944787A1 (en) 2015-10-22
CN107266450B (zh) 2020-07-24
JP2018065874A (ja) 2018-04-26
MA46373A (fr) 2019-08-07
EP3418280B1 (en) 2023-07-12
SG11201608537SA (en) 2016-11-29
CA2944787C (en) 2023-03-14
CN106132965B (zh) 2020-02-07
IL263878B (en) 2019-11-28
HUE045847T2 (hu) 2020-01-28
ES2744299T3 (es) 2020-02-24
US20170008894A1 (en) 2017-01-12
PH12016502019A1 (en) 2017-01-09

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