SG10201604799TA - Novel heterocyclic carboxamides as modulators of kinase activity. - Google Patents

Novel heterocyclic carboxamides as modulators of kinase activity.

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Publication number
SG10201604799TA
SG10201604799TA SG10201604799TA SG10201604799TA SG10201604799TA SG 10201604799T A SG10201604799T A SG 10201604799TA SG 10201604799T A SG10201604799T A SG 10201604799TA SG 10201604799T A SG10201604799T A SG 10201604799TA SG 10201604799T A SG10201604799T A SG 10201604799TA
Authority
SG
Singapore
Prior art keywords
modulators
kinase activity
novel heterocyclic
heterocyclic carboxamides
carboxamides
Prior art date
Application number
SG10201604799TA
Other languages
English (en)
Inventor
Bayard R Huck
Xiaoling Chen
Yufang Xiao
Ruoxi Lan
Selm Lizbeth Celeste De
Constantin Neagu
Justin Potnick
Srinivasa R Karra
Theresa L Johnson
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of SG10201604799TA publication Critical patent/SG10201604799TA/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
SG10201604799TA 2011-12-22 2012-12-17 Novel heterocyclic carboxamides as modulators of kinase activity. SG10201604799TA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161579377P 2011-12-22 2011-12-22

Publications (1)

Publication Number Publication Date
SG10201604799TA true SG10201604799TA (en) 2016-07-28

Family

ID=47459185

Family Applications (2)

Application Number Title Priority Date Filing Date
SG10201604799TA SG10201604799TA (en) 2011-12-22 2012-12-17 Novel heterocyclic carboxamides as modulators of kinase activity.
SG11201402387WA SG11201402387WA (en) 2011-12-22 2012-12-17 Novel heterocyclic carboxamides as modulators of kinase activity

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG11201402387WA SG11201402387WA (en) 2011-12-22 2012-12-17 Novel heterocyclic carboxamides as modulators of kinase activity

Country Status (24)

Country Link
US (3) US9139568B2 (zh)
EP (1) EP2794571B1 (zh)
JP (2) JP6193880B2 (zh)
KR (1) KR102098358B1 (zh)
CN (1) CN104169258B (zh)
AU (2) AU2012355494B2 (zh)
BR (1) BR112014015327B1 (zh)
CA (1) CA2856448C (zh)
DK (1) DK2794571T3 (zh)
EA (2) EA027968B1 (zh)
ES (1) ES2614232T3 (zh)
HK (1) HK1201829A1 (zh)
HR (1) HRP20170099T1 (zh)
HU (1) HUE032918T2 (zh)
IL (1) IL233199B (zh)
LT (1) LT2794571T (zh)
MX (1) MX353062B (zh)
PL (1) PL2794571T3 (zh)
PT (1) PT2794571T (zh)
RS (1) RS55621B1 (zh)
SG (2) SG10201604799TA (zh)
SI (1) SI2794571T1 (zh)
WO (1) WO2013096194A1 (zh)
ZA (1) ZA201403517B (zh)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA028012B1 (ru) 2010-07-29 2017-09-29 Мерк Патент Гмбх Циклический амин-азагетероциклический карбоксамид
SG10201604799TA (en) * 2011-12-22 2016-07-28 Merck Patent Gmbh Novel heterocyclic carboxamides as modulators of kinase activity.
AU2014228385B2 (en) * 2013-03-11 2018-08-09 Merck Patent Gmbh 6-[4-(1-H-imidazol-2-yl]piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
JP2021515767A (ja) 2018-03-07 2021-06-24 バイエル・アクチエンゲゼルシヤフト Erk5阻害剤の同定及び使用
CN115073369A (zh) * 2022-05-31 2022-09-20 汉瑞药业(荆门)有限公司 一种5-溴喹啉-8-甲醛的制备方法

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GB1465651A (en) * 1974-04-19 1977-02-23 Wyeth John & Brother Ltd Carbocyclic-fused ring pyridine derivatives
US4933447A (en) 1987-09-24 1990-06-12 Ss Pharmaceutical Co., Ltd. Quinoline derivatives
JPH01156960A (ja) * 1987-09-24 1989-06-20 Ss Pharmaceut Co Ltd キノリン誘導体
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
TW200407324A (en) * 2002-05-17 2004-05-16 Bristol Myers Squibb Co Bicyclic modulators of androgen receptor function
EP1615906A1 (en) 2003-04-03 2006-01-18 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
MXPA06003557A (es) 2003-09-30 2006-06-20 Irm Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
AU2004283751B2 (en) 2003-10-24 2011-05-19 Exelixis, Inc. p70S6 kinase modulators and method of use
EP1687305B1 (en) 2003-11-21 2008-07-09 Novartis AG 1h-imidazoquinoline derivatives as protein kinase inhibitors
BRPI0417498A (pt) 2003-12-09 2007-05-29 Us Gov Health & Human Serv método para suprimir uma resposta imune em um indivìduo; método de inibição da proliferação de um célula; método de tratamento de um distúrbio proliferativo em um indivìduo; método para selecionar um agente imunossupressor ou anti-proliferativo; composição farmacêutica e estente vascular
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
US7994172B2 (en) 2004-12-28 2011-08-09 Exelixis, Inc. [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
US8343953B2 (en) 2005-06-22 2013-01-01 Astex Therapeutics Limited Pharmaceutical compounds
WO2010093419A1 (en) * 2009-02-11 2010-08-19 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides
SG10201604799TA (en) * 2011-12-22 2016-07-28 Merck Patent Gmbh Novel heterocyclic carboxamides as modulators of kinase activity.
BR112016008378B1 (pt) * 2013-10-14 2022-11-08 Eisai R&D Management Co., Ltd Compostos de quinolina seletivamente substituídos ou sal dos mesmos, e composição farmacêutica contendo os ditos compostos
MY192489A (en) * 2013-10-14 2022-08-23 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds

Also Published As

Publication number Publication date
JP6553686B2 (ja) 2019-07-31
BR112014015327B1 (pt) 2020-10-27
EA027968B1 (ru) 2017-09-29
US10080753B2 (en) 2018-09-25
MX353062B (es) 2017-12-19
KR20140107317A (ko) 2014-09-04
DK2794571T3 (en) 2017-02-06
EP2794571B1 (en) 2016-11-02
ZA201403517B (en) 2018-07-25
EP2794571A1 (en) 2014-10-29
CN104169258A (zh) 2014-11-26
US20140309245A1 (en) 2014-10-16
AU2012355494A1 (en) 2014-06-05
US20160339028A1 (en) 2016-11-24
PL2794571T3 (pl) 2017-04-28
IL233199B (en) 2019-03-31
BR112014015327A2 (pt) 2017-06-13
AU2017239625B2 (en) 2019-07-11
BR112014015327A8 (pt) 2017-06-13
JP2017197587A (ja) 2017-11-02
HK1201829A1 (zh) 2015-09-11
EA201400736A1 (ru) 2015-01-30
CA2856448C (en) 2020-03-24
RS55621B1 (sr) 2017-06-30
JP2015503521A (ja) 2015-02-02
EA201791073A1 (ru) 2017-09-29
US20160058763A1 (en) 2016-03-03
AU2012355494B2 (en) 2017-07-13
SI2794571T1 (sl) 2017-03-31
LT2794571T (lt) 2017-02-10
CN104169258B (zh) 2017-03-01
WO2013096194A1 (en) 2013-06-27
KR102098358B1 (ko) 2020-04-08
HUE032918T2 (hu) 2017-11-28
ES2614232T3 (es) 2017-05-30
IL233199A0 (en) 2014-08-03
MX2014007364A (es) 2014-08-01
SG11201402387WA (en) 2014-09-26
PT2794571T (pt) 2017-02-07
US9139568B2 (en) 2015-09-22
JP6193880B2 (ja) 2017-09-06
AU2017239625A1 (en) 2017-10-26
CA2856448A1 (en) 2013-06-27
HRP20170099T1 (hr) 2017-03-24

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