UA121255C2 - Сполуки як модулятори ror-гамма - Google Patents

Сполуки як модулятори ror-гамма Download PDF

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Publication number
UA121255C2
UA121255C2 UAA201803569A UAA201803569A UA121255C2 UA 121255 C2 UA121255 C2 UA 121255C2 UA A201803569 A UAA201803569 A UA A201803569A UA A201803569 A UAA201803569 A UA A201803569A UA 121255 C2 UA121255 C2 UA 121255C2
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Ukraine
Prior art keywords
mmol
mach
compound
mixture
stirred
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UAA201803569A
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English (en)
Ukrainian (uk)
Inventor
Йоханна Баконі
Йоханна Бакони
Стівен Річард Брюнетт
Стивен Ричард Брюнетт
Дельфін Коллін
Дельфин Коллин
Роберт Оуен Хьюз
Роберт Оуэн Хьюз
Сян Лі
Сян Ли
Шуан Лян
Роберт Сіблі
Роберт СИБЛИ
Майкл Роберт Тьорнер
Майкл Роберт Тёрнер
Ліфень У
Лифень У
Цян Чжан
Original Assignee
Бьорінгер Інгельхайм Інтернаціональ Гмбх
Бёрингер Ингельхайм Интернациональ Гмбх
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Publication of UA121255C2 publication Critical patent/UA121255C2/uk

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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
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    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Otolaryngology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
UAA201803569A 2014-04-14 2015-04-10 Сполуки як модулятори ror-гамма UA121255C2 (uk)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461979231P 2014-04-14 2014-04-14

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UA121255C2 true UA121255C2 (uk) 2020-04-27

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UAA201803569A UA121255C2 (uk) 2014-04-14 2015-04-10 Сполуки як модулятори ror-гамма
UAA201610804A UA120094C2 (uk) 2014-04-14 2015-04-10 Сполуки як модулятори ror-гамма

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UAA201610804A UA120094C2 (uk) 2014-04-14 2015-04-10 Сполуки як модулятори ror-гамма

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JP (2) JP6282759B2 (enExample)
KR (2) KR102410069B1 (enExample)
CN (3) CN107266450B (enExample)
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TW (2) TWI652268B (enExample)
UA (2) UA121255C2 (enExample)
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BR122020020657B1 (pt) * 2014-04-14 2022-12-20 Boehringer Ingelheim International Gmbh Compostos, composição farmacêutica e seus usos como moduladores de ror gama
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)
KR102702236B1 (ko) 2015-05-15 2024-09-04 오리진 온콜로지 리미티드 Ror 감마 조절제로서의 치환된 테트라하이드로퀴놀리논 화합물
US10450314B2 (en) 2015-10-01 2019-10-22 Boehringer Ingelheim International Gmbh Pteridine derivatives as modulators of ROR gamma
KR101947976B1 (ko) 2015-12-15 2019-02-13 아스트라제네카 아베 이소인돌 화합물
EP3405470B1 (en) * 2016-01-20 2020-07-15 Boehringer Ingelheim International GmbH Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma
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
EP3638661A1 (en) 2017-06-14 2020-04-22 Astrazeneca AB 2,3-dihydroisoindole-1-carboxamides useful as ror-gamma modulators
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
SMT202300212T1 (it) 2018-05-03 2023-09-06 Shanghai hengrui pharmaceutical co ltd Derivati di benzimidazolo come modulatori del recettore gamma orfano correlato al retinoide (rory) e usi farmaceutici di essi
US20210395185A1 (en) 2018-10-18 2021-12-23 Boehringer Ingelheim International Gmbh Scalable synthesis of optically active 1-cyclopropylalkyl-1-amines
WO2021061803A1 (en) 2019-09-23 2021-04-01 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
US20230014730A1 (en) 2019-09-23 2023-01-19 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
BR112022008293A2 (pt) 2019-10-31 2022-07-26 Jiangsu Hengrui Medicine Co Sal de adição de ácido de regulador de ror?, composições farmacêuticas, uso dos mesmos e métodos para preparar forma cristalina e composição farmacêutica
WO2022106548A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Solid forms of a ror gamma inhibitor
WO2022106549A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline salts of a ror gamma inhibitor
WO2022106547A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Process for synthesising a ror gamma inhibitor
WO2022106550A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline polymorphic form of a ror gamma inhibitor
WO2022106551A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Co-crystals of 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
AU2024267864A1 (en) * 2023-05-09 2025-11-06 11949098 Canada Inc. Inverse agonists of rar related orphan receptors (rors)

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WO2009022185A2 (en) * 2007-08-16 2009-02-19 Astrazeneca Ab 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use
PE20110854A1 (es) 2008-09-26 2011-12-23 Boehringer Ingelheim Int DERIVADOS DE 1-FENIL-1H-PIRAZOLO[3,4-c]PIRIDINA-4-CARBONILAMINA COMO ANTAGONISTAS DE LOS RECEPTORES CCR1
AP2012006204A0 (en) 2009-10-21 2012-04-30 Boehringer Ingelheim Int Indazole and pyrazolopyridine compounds as CCR1 receptor antagonists.
BR112013030894A2 (pt) * 2011-06-01 2016-08-16 Janus Biotherapeutics Inc moduladores do sistema imune
CN106008511B (zh) * 2012-05-14 2018-08-14 华东理工大学 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
BR122020020657B1 (pt) * 2014-04-14 2022-12-20 Boehringer Ingelheim International Gmbh Compostos, composição farmacêutica e seus usos como moduladores de ror gama
US10450314B2 (en) * 2015-10-01 2019-10-22 Boehringer Ingelheim International Gmbh Pteridine derivatives as modulators of ROR gamma
EP3405470B1 (en) * 2016-01-20 2020-07-15 Boehringer Ingelheim International GmbH Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma

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AU2015247983A1 (en) 2016-09-08
PE20211002A1 (es) 2021-06-01
BR112016021962A2 (pt) 2023-01-20
MX370780B (es) 2020-01-03
US20160075706A1 (en) 2016-03-17
EP3418280B1 (en) 2023-07-12
AR100058A1 (es) 2016-09-07
JP2017511357A (ja) 2017-04-20
KR102410069B1 (ko) 2022-06-20
US9242989B2 (en) 2016-01-26
HK1244800A1 (zh) 2018-08-17
CA2944787A1 (en) 2015-10-22
CY1122012T1 (el) 2020-10-14
UY36077A (es) 2015-10-30
CA2944787C (en) 2023-03-14
US20170008894A1 (en) 2017-01-12
HRP20191579T1 (hr) 2019-11-29
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
JP2018065874A (ja) 2018-04-26
PH12016502019B1 (en) 2020-10-23
PL3131902T3 (pl) 2019-11-29
CN107266450B (zh) 2020-07-24
JP6282759B2 (ja) 2018-02-21
LT3131902T (lt) 2019-09-25
MY182834A (en) 2021-02-05
CN107266450A (zh) 2017-10-20
JP6463855B2 (ja) 2019-02-06
IL263878B (en) 2019-11-28
TW201625622A (zh) 2016-07-16
ES2744299T3 (es) 2020-02-24
US20180022749A1 (en) 2018-01-25
PH12016502019A1 (en) 2017-01-09
TWI655192B (zh) 2019-04-01
PH12020500252A1 (en) 2021-07-26
CN107266454A (zh) 2017-10-20
HK1244801A1 (zh) 2018-08-17
CN106132965A (zh) 2016-11-16
TWI652268B (zh) 2019-03-01
AU2015247983B2 (en) 2019-05-16
EA035063B1 (ru) 2020-04-23
EA031351B1 (ru) 2018-12-28
KR20200040917A (ko) 2020-04-20
KR20160142396A (ko) 2016-12-12
EA201890329A1 (ru) 2018-07-31
AU2019203027B2 (en) 2020-07-09
EP3418280A1 (en) 2018-12-26
HUE045847T2 (hu) 2020-01-28
EP3131902B1 (en) 2019-06-12
MA46373A (fr) 2019-08-07
SI3131902T1 (sl) 2019-10-30
MX2016013342A (es) 2017-01-26
US9598415B2 (en) 2017-03-21
NZ723530A (en) 2023-05-26
TW201841915A (zh) 2018-12-01
ME03513B (me) 2020-04-20
WO2015160654A1 (en) 2015-10-22
PE20161572A1 (es) 2017-02-01
CN106132965B (zh) 2020-02-07
AP2016009403A0 (en) 2016-08-31
DK3131902T3 (da) 2019-09-02
EP3131902A1 (en) 2017-02-22
BR112016021962B1 (pt) 2022-12-13
AR119454A2 (es) 2021-12-22
US20150291607A1 (en) 2015-10-15
EA201691978A1 (ru) 2017-02-28
CN107266454B (zh) 2019-08-09
AU2019203027A1 (en) 2019-05-23
CL2016002421A1 (es) 2017-03-24
UA120094C2 (uk) 2019-10-10
SG11201608537SA (en) 2016-11-29
RS59170B1 (sr) 2019-10-31
PT3131902T (pt) 2019-09-17
BR122020020657B1 (pt) 2022-12-20
KR102410076B1 (ko) 2022-06-22
US20190002465A1 (en) 2019-01-03

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