HRP20170099T1 - Novi heterociklički karboksamidi kao modulatori aktivnosti kinaze - Google Patents

Novi heterociklički karboksamidi kao modulatori aktivnosti kinaze Download PDF

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Publication number
HRP20170099T1
HRP20170099T1 HRP20170099TT HRP20170099T HRP20170099T1 HR P20170099 T1 HRP20170099 T1 HR P20170099T1 HR P20170099T T HRP20170099T T HR P20170099TT HR P20170099 T HRP20170099 T HR P20170099T HR P20170099 T1 HRP20170099 T1 HR P20170099T1
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HR
Croatia
Prior art keywords
hal
atoms
group
replaced
monocyclic alkyl
Prior art date
Application number
HRP20170099TT
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English (en)
Croatian (hr)
Inventor
Bayard R. Huck
Xiaoling Chen
Yufang Xiao
Ruoxi Lan
Lizbeth Celeste De Selm
Constantin Neagu
Justin Potnick
Srinivasa R. Karra
Theresa L. Johnson
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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 HRP20170099T1 publication Critical patent/HRP20170099T1/hr

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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
    • 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
    • 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

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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)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
HRP20170099TT 2011-12-22 2012-12-17 Novi heterociklički karboksamidi kao modulatori aktivnosti kinaze HRP20170099T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161579377P 2011-12-22 2011-12-22
PCT/US2012/070085 WO2013096194A1 (en) 2011-12-22 2012-12-17 Novel heterocyclic carboxamides as modulators of kinase activity
EP12808640.2A EP2794571B1 (en) 2011-12-22 2012-12-17 Novel heterocyclic carboxamides as modulators of kinase activity

Publications (1)

Publication Number Publication Date
HRP20170099T1 true HRP20170099T1 (hr) 2017-03-24

Family

ID=47459185

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20170099TT HRP20170099T1 (hr) 2011-12-22 2012-12-17 Novi heterociklički karboksamidi kao modulatori aktivnosti kinaze

Country Status (23)

Country Link
US (3) US9139568B2 (https=)
EP (1) EP2794571B1 (https=)
JP (2) JP6193880B2 (https=)
KR (1) KR102098358B1 (https=)
CN (1) CN104169258B (https=)
AU (2) AU2012355494B2 (https=)
BR (1) BR112014015327B1 (https=)
CA (1) CA2856448C (https=)
DK (1) DK2794571T3 (https=)
EA (2) EA027968B1 (https=)
ES (1) ES2614232T3 (https=)
HR (1) HRP20170099T1 (https=)
HU (1) HUE032918T2 (https=)
IL (1) IL233199B (https=)
LT (1) LT2794571T (https=)
MX (1) MX353062B (https=)
PL (1) PL2794571T3 (https=)
PT (1) PT2794571T (https=)
RS (1) RS55621B1 (https=)
SG (2) SG11201402387WA (https=)
SI (1) SI2794571T1 (https=)
WO (1) WO2013096194A1 (https=)
ZA (1) ZA201403517B (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9586938B2 (en) 2010-07-29 2017-03-07 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
SG11201402387WA (en) * 2011-12-22 2014-09-26 Merck Patent Gmbh Novel heterocyclic carboxamides as modulators of kinase activity
SG11201505999VA (en) 2013-03-11 2015-08-28 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
WO2004092154A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2004278413B2 (en) 2003-09-30 2008-07-31 Irm Llc Compounds and compositions as protein kinase inhibitors
JP4800216B2 (ja) 2003-10-24 2011-10-26 エグゼリクシス, インコーポレイテッド p70S6キナーゼモジュレーターおよび使用方法
DE602004014969D1 (de) 2003-11-21 2008-08-21 Novartis Ag 1h-imidazochinolinderivate als proteinkinaseinhibitoren
CN1889958A (zh) 2003-12-09 2007-01-03 美国政府健康及人类服务部 抑制免疫应答或治疗增生性疾病的方法
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
CA2590961C (en) 2004-12-28 2013-11-26 Exelixis, Inc. [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine 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
EP1902032A1 (en) 2005-06-22 2008-03-26 Astex Therapeutics Limited Pharmaceutical compounds
NZ595087A (en) 2009-02-11 2013-03-28 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides
SG11201402387WA (en) * 2011-12-22 2014-09-26 Merck Patent Gmbh Novel heterocyclic carboxamides as modulators of kinase activity
JP6223563B2 (ja) * 2013-10-14 2017-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的に置換されたキノリン化合物
CN105636945B (zh) * 2013-10-14 2017-11-17 卫材R&D管理有限公司 选择性取代的喹啉化合物

Also Published As

Publication number Publication date
ZA201403517B (en) 2018-07-25
EP2794571A1 (en) 2014-10-29
SG11201402387WA (en) 2014-09-26
JP6193880B2 (ja) 2017-09-06
EA201791073A1 (ru) 2017-09-29
US20160058763A1 (en) 2016-03-03
PT2794571T (pt) 2017-02-07
CN104169258A (zh) 2014-11-26
BR112014015327A2 (pt) 2017-06-13
IL233199B (en) 2019-03-31
US20140309245A1 (en) 2014-10-16
DK2794571T3 (en) 2017-02-06
AU2017239625B2 (en) 2019-07-11
WO2013096194A1 (en) 2013-06-27
AU2012355494A1 (en) 2014-06-05
EA201400736A1 (ru) 2015-01-30
EA027968B1 (ru) 2017-09-29
CA2856448C (en) 2020-03-24
MX2014007364A (es) 2014-08-01
AU2017239625A1 (en) 2017-10-26
HUE032918T2 (hu) 2017-11-28
HK1201829A1 (en) 2015-09-11
BR112014015327B1 (pt) 2020-10-27
KR20140107317A (ko) 2014-09-04
SI2794571T1 (sl) 2017-03-31
CN104169258B (zh) 2017-03-01
AU2012355494B2 (en) 2017-07-13
ES2614232T3 (es) 2017-05-30
CA2856448A1 (en) 2013-06-27
KR102098358B1 (ko) 2020-04-08
JP6553686B2 (ja) 2019-07-31
MX353062B (es) 2017-12-19
US20160339028A1 (en) 2016-11-24
PL2794571T3 (pl) 2017-04-28
SG10201604799TA (en) 2016-07-28
EP2794571B1 (en) 2016-11-02
RS55621B1 (sr) 2017-06-30
US9139568B2 (en) 2015-09-22
LT2794571T (lt) 2017-02-10
BR112014015327A8 (pt) 2017-06-13
IL233199A0 (en) 2014-08-03
JP2017197587A (ja) 2017-11-02
US10080753B2 (en) 2018-09-25
JP2015503521A (ja) 2015-02-02

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