ES2670984T3 - Composiciones y métodos para modular receptores X farnesoides - Google Patents

Composiciones y métodos para modular receptores X farnesoides Download PDF

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Publication number
ES2670984T3
ES2670984T3 ES14803001.8T ES14803001T ES2670984T3 ES 2670984 T3 ES2670984 T3 ES 2670984T3 ES 14803001 T ES14803001 T ES 14803001T ES 2670984 T3 ES2670984 T3 ES 2670984T3
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ES
Spain
Prior art keywords
methyl
carboxamido
pyrazol
dihydrochromen
acid
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ES14803001.8T
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English (en)
Spanish (es)
Inventor
David Tully
Donatella Chianelli
Xiaodong Liu
Valentina Molteni
John Nelson
Jason ROLAND
Paul Rucker
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • 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
    • C07D471/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
ES14803001.8T 2013-11-05 2014-11-04 Composiciones y métodos para modular receptores X farnesoides Active ES2670984T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361900013P 2013-11-05 2013-11-05
US201361900013P 2013-11-05
PCT/US2014/063948 WO2015069666A1 (en) 2013-11-05 2014-11-04 Compositions and methods for modulating farnesoid x receptors

Publications (1)

Publication Number Publication Date
ES2670984T3 true ES2670984T3 (es) 2018-06-04

Family

ID=51982773

Family Applications (1)

Application Number Title Priority Date Filing Date
ES14803001.8T Active ES2670984T3 (es) 2013-11-05 2014-11-04 Composiciones y métodos para modular receptores X farnesoides

Country Status (42)

Country Link
US (5) US9682939B2 (enExample)
EP (1) EP3065738B1 (enExample)
JP (1) JP6424231B2 (enExample)
KR (1) KR102350357B1 (enExample)
CN (1) CN105682656B (enExample)
AP (1) AP2016009165A0 (enExample)
AR (1) AR098316A1 (enExample)
AU (1) AU2014346919B2 (enExample)
BR (1) BR112016009630B1 (enExample)
CA (1) CA2927705C (enExample)
CL (1) CL2016000982A1 (enExample)
CR (1) CR20160212A (enExample)
CU (1) CU24375B1 (enExample)
CY (1) CY1120273T1 (enExample)
DK (1) DK3065738T3 (enExample)
EA (1) EA030430B1 (enExample)
ES (1) ES2670984T3 (enExample)
GT (1) GT201600085A (enExample)
HR (1) HRP20180817T1 (enExample)
HU (1) HUE039155T2 (enExample)
IL (1) IL245242B (enExample)
JO (1) JO3454B1 (enExample)
LT (1) LT3065738T (enExample)
MA (1) MA39088B1 (enExample)
MX (1) MX364834B (enExample)
MY (1) MY175903A (enExample)
NO (1) NO3105103T3 (enExample)
NZ (1) NZ719078A (enExample)
PE (1) PE20160682A1 (enExample)
PH (1) PH12016500777B1 (enExample)
PL (1) PL3065738T3 (enExample)
PT (1) PT3065738T (enExample)
RS (1) RS57179B1 (enExample)
SG (1) SG11201603026PA (enExample)
SI (1) SI3065738T1 (enExample)
SV (1) SV2016005192A (enExample)
TN (1) TN2016000143A1 (enExample)
TR (1) TR201807321T4 (enExample)
TW (1) TWI662027B (enExample)
UY (1) UY35818A (enExample)
WO (1) WO2015069666A1 (enExample)
ZA (1) ZA201602555B (enExample)

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EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
SG11201603026PA (en) 2013-11-05 2016-05-30 Novartis Ag Compositions and methods for modulating farnesoid x receptors
TWI698430B (zh) 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 三環化合物及其在藥物中的應用
US10351576B2 (en) 2015-04-30 2019-07-16 Novartis Ag Fused tricyclic pyrazole derivatives useful for farnesoid X receptors
LT3419625T (lt) 2016-02-22 2021-07-26 Novartis Ag Fxr agonistų panaudojimo būdai
NZ748641A (en) 2016-06-13 2020-04-24 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (NR1H4)
JP6915050B2 (ja) * 2016-09-14 2021-08-04 ノバルティス アーゲー Fxrアゴニストの新規のレジーム
PE20190972A1 (es) * 2016-09-14 2019-07-09 Novartis Ag Combinacion de agonistas de fxr
MX2019003889A (es) * 2016-10-05 2019-08-12 Novartis Ag Composiciones de combinacion que comprenden agonistas de fxr para tratar o prevenir una enfermedad o trastorno fibrotico o cirrotico.
CN107973790A (zh) * 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
ES2982801T3 (es) 2017-03-28 2024-10-17 Gilead Sciences Inc Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas
WO2018226155A1 (en) * 2017-06-05 2018-12-13 National University Of Singapore Compounds useful in inhibiting human trefoil factor 3
TW201910317A (zh) 2017-08-15 2019-03-16 愛爾蘭商英弗雷佐姆有限公司 新穎化合物
MX2020001776A (es) 2017-08-15 2020-03-24 Inflazome Ltd Sulfonilureas y sulfoniltioureas como inhibidores de nlrp3.
WO2019034693A1 (en) 2017-08-15 2019-02-21 Inflazome Limited SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3
JP2020533339A (ja) * 2017-09-13 2020-11-19 ノバルティス アーゲー Fxrアゴニストを含む組合せ
WO2019092171A1 (en) 2017-11-09 2019-05-16 Inflazome Limited Novel sulfonamide carboxamide compounds
CN111315733A (zh) 2017-11-09 2020-06-19 英夫拉索姆有限公司 新颖磺酰胺甲酰胺化合物
CN110128432B (zh) * 2018-02-02 2021-03-02 广东东阳光药业有限公司 含氮三环化合物及其在药物中的应用
WO2019166619A1 (en) 2018-03-02 2019-09-06 Inflazome Limited Novel compounds
US12168012B2 (en) 2018-07-25 2024-12-17 Novartis Ag NLRP3 inflammasome inhibitors
KR102692309B1 (ko) 2019-01-15 2024-08-07 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
US10610280B1 (en) 2019-02-02 2020-04-07 Ayad K. M. Agha Surgical method and apparatus for destruction and removal of intraperitoneal, visceral, and subcutaneous fat
WO2020172075A1 (en) 2019-02-19 2020-08-27 Gilead Sciences, Inc. Solid forms of fxr agonists
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
WO2021009332A1 (en) 2019-07-18 2021-01-21 Enyo Pharma Method for decreasing adverse-effects of interferon
TW202122078A (zh) 2019-09-06 2021-06-16 瑞士商諾華公司 使用lta4h抑制劑治療肝臟疾病之方法
IL293892A (en) 2020-01-15 2022-08-01 Inserm Institut National De La Sant? Et De La Rech M?Dicale Use of fxr agonists for treating an infection by hepatitis d virus
CN113387828A (zh) * 2020-03-14 2021-09-14 江巨东 一种阿利克仑中间体的制备方法
WO2022037663A1 (zh) * 2020-08-21 2022-02-24 苏州晶云药物科技股份有限公司 苯甲酸衍生物的新晶型及其制备方法
MX2023008365A (es) 2021-01-14 2023-10-04 Enyo Pharma Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv.
TW202308629A (zh) 2021-04-28 2023-03-01 法商Enyo製藥公司 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
EP4577206A2 (en) * 2022-08-26 2025-07-02 Celmatix Inc. Novel modulators of fshr and uses thereof
WO2026133229A1 (en) 2024-12-20 2026-06-25 Novartis Ag Nlrp3 inflammasome inhibitors

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US20050143449A1 (en) * 2002-11-15 2005-06-30 The Salk Institute For Biological Studies Non-steroidal farnesoid X receptor modulators and methods for the use thereof
DK2029547T3 (da) * 2006-05-24 2010-07-26 Lilly Co Eli FXR-agonister
JP2010504032A (ja) * 2006-09-15 2010-02-04 タレス アビオニクス インコーポレイテッド 航空機との間でコンテンツを無線で転送するシステム及び方法
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
CU24152B1 (es) * 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
SG11201603026PA (en) 2013-11-05 2016-05-30 Novartis Ag Compositions and methods for modulating farnesoid x receptors
US10351576B2 (en) 2015-04-30 2019-07-16 Novartis Ag Fused tricyclic pyrazole derivatives useful for farnesoid X receptors

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Publication number Publication date
TWI662027B (zh) 2019-06-11
CA2927705C (en) 2021-09-21
US20210253534A1 (en) 2021-08-19
SV2016005192A (es) 2016-11-21
AU2014346919B2 (en) 2017-02-02
AP2016009165A0 (en) 2016-04-30
TN2016000143A1 (en) 2017-10-06
PH12016500777A1 (en) 2016-05-30
NZ719078A (en) 2018-07-27
KR20160079091A (ko) 2016-07-05
HUE039155T2 (hu) 2018-12-28
NO3105103T3 (enExample) 2018-05-12
MY175903A (en) 2020-07-15
CA2927705A1 (en) 2015-05-14
US11021446B2 (en) 2021-06-01
US10077240B2 (en) 2018-09-18
US20160340317A1 (en) 2016-11-24
CR20160212A (es) 2016-07-22
EA030430B1 (ru) 2018-08-31
EA201690930A1 (ru) 2016-08-31
IL245242A0 (en) 2016-06-30
BR112016009630B1 (pt) 2021-02-09
IL245242B (en) 2019-03-31
JO3454B1 (ar) 2020-07-05
US20200247757A1 (en) 2020-08-06
TW201612163A (en) 2016-04-01
CL2016000982A1 (es) 2016-10-07
US20170275256A1 (en) 2017-09-28
KR102350357B1 (ko) 2022-01-14
SI3065738T1 (en) 2018-06-29
RS57179B1 (sr) 2018-07-31
GT201600085A (es) 2019-07-19
SG11201603026PA (en) 2016-05-30
US9682939B2 (en) 2017-06-20
CU24375B1 (es) 2018-12-05
CN105682656A (zh) 2016-06-15
US20190062283A1 (en) 2019-02-28
AR098316A1 (es) 2016-05-26
CN105682656B (zh) 2019-11-05
PT3065738T (pt) 2018-06-04
CU20160063A7 (es) 2016-09-30
PE20160682A1 (es) 2016-07-23
CY1120273T1 (el) 2019-07-10
US10683271B2 (en) 2020-06-16
ZA201602555B (en) 2017-06-28
PH12016500777B1 (en) 2016-05-30
MA39088B1 (fr) 2018-06-29
MX2016005865A (es) 2016-07-13
JP2016535784A (ja) 2016-11-17
UY35818A (es) 2015-05-29
WO2015069666A1 (en) 2015-05-14
MA39088A1 (fr) 2017-07-31
TR201807321T4 (tr) 2018-06-21
MX364834B (es) 2019-05-08
AU2014346919A1 (en) 2016-05-12
JP6424231B2 (ja) 2018-11-14
LT3065738T (lt) 2018-05-10
BR112016009630A8 (pt) 2020-04-07
PL3065738T3 (pl) 2018-07-31
EP3065738A1 (en) 2016-09-14
HRP20180817T1 (hr) 2018-06-29
EP3065738B1 (en) 2018-02-28
DK3065738T3 (en) 2018-06-06

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