PE20160802A1 - Inhibidores de dgat1 de eter ciclico de cabeza de puente - Google Patents

Inhibidores de dgat1 de eter ciclico de cabeza de puente

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Publication number
PE20160802A1
PE20160802A1 PE2016000359A PE2016000359A PE20160802A1 PE 20160802 A1 PE20160802 A1 PE 20160802A1 PE 2016000359 A PE2016000359 A PE 2016000359A PE 2016000359 A PE2016000359 A PE 2016000359A PE 20160802 A1 PE20160802 A1 PE 20160802A1
Authority
PE
Peru
Prior art keywords
cyclic ether
treatment
bridge head
disorders
dgat1 inhibitors
Prior art date
Application number
PE2016000359A
Other languages
English (en)
Inventor
Xuchun Zheng
Frederic Zecri
Jiong Ye
Sejal Patel
Justin Yik Ching Mao
Jay Larrow
Qian Liu
Tyler Harrison
Yu Gai
Rohit Duvadie
Yiping Ding
Xin Chen
Yizong Zhou
Rui Zheng
Original Assignee
Novartis Ag
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48577190&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20160802(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20160802A1 publication Critical patent/PE20160802A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed 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
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La invencion se refiere a los compuestos de la formula (I); donde p es 1, 2 o 3; X es O o CH2; Y es O, CH2 o esta ausente; Z1, Z2, Z3 y Z4 son cada independientemente N o CH; A es entre otros oxazol, tiazol; utiles para el tratamiento de los trastornos mediados por acil-transferasa de acil-CoA-diacil-glicerol 1 (DGAT1), por ejemplo, los trastornos metabolicos. La invencion tambien proporciona metodos para el tratamiento de los trastornos, y las composiciones para su tratamiento Son compuestos especificos: Acido 2-(4-(4-(5-(5-tert-butil-1 ,3,4-oxadiazol-2-ilamino)piridin-2-il)fenil)-2- oxabiciclo[2.2.2]octan-1-il)acetico; Acido 2-(4-(4-(5-((5-ciclobutil-1 ,3,4-oxadiazol-2-il)amino)piridin-2-il)fenil)-2- oxabiciclo[2.2.2]octan-1-il)acetico; entre otros.
PE2016000359A 2012-04-27 2013-04-25 Inhibidores de dgat1 de eter ciclico de cabeza de puente PE20160802A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261639341P 2012-04-27 2012-04-27
US201361787695P 2013-03-15 2013-03-15
CN2013072735 2013-03-15

Publications (1)

Publication Number Publication Date
PE20160802A1 true PE20160802A1 (es) 2016-09-03

Family

ID=48577190

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2014001902A PE20150724A1 (es) 2012-04-27 2013-04-25 Inhibidores de dgat1 de eter ciclico de cabeza de puente
PE2016000359A PE20160802A1 (es) 2012-04-27 2013-04-25 Inhibidores de dgat1 de eter ciclico de cabeza de puente

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2014001902A PE20150724A1 (es) 2012-04-27 2013-04-25 Inhibidores de dgat1 de eter ciclico de cabeza de puente

Country Status (26)

Country Link
US (2) US8993619B2 (es)
EP (1) EP2852590B1 (es)
JP (1) JP6042529B2 (es)
KR (1) KR20150013194A (es)
CN (1) CN104395309B (es)
AP (1) AP3592A (es)
AR (1) AR090859A1 (es)
AU (1) AU2013254307B2 (es)
BR (1) BR112014026760A8 (es)
CA (1) CA2870336A1 (es)
CL (1) CL2014002822A1 (es)
CO (1) CO7111275A2 (es)
CR (1) CR20140494A (es)
EA (1) EA025050B1 (es)
EC (1) ECSP14030538A (es)
ES (1) ES2624291T3 (es)
IL (1) IL235313A0 (es)
MA (1) MA37439B1 (es)
MX (1) MX357768B (es)
PE (2) PE20150724A1 (es)
PH (1) PH12014502413A1 (es)
SG (1) SG11201406526WA (es)
TN (1) TN2014000425A1 (es)
TW (1) TW201348239A (es)
UY (1) UY34767A (es)
WO (1) WO2013160873A1 (es)

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CN104583218B (zh) 2012-04-26 2018-04-24 百时美施贵宝公司 作为蛋白酶活化受体4(par4)抑制剂用于治疗血小板聚集的咪唑并噻二唑和咪唑并吡嗪的衍生物
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲mPGES-1抑制劑之三唑酮化合物
WO2014110574A1 (en) 2013-01-14 2014-07-17 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
KR102403306B1 (ko) 2013-01-15 2022-06-02 인사이트 홀딩스 코포레이션 Pim 키나제 저해제로서 유용한 티아졸카복스아마이드 및 피리딘카복스아마이드 화합물
US8962660B2 (en) * 2013-03-14 2015-02-24 Bristol-Myers Squibb Company Oxabicyclo [2.2.2] acid GPR120 modulators
US9556197B2 (en) 2013-08-23 2017-01-31 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
CN104292190B (zh) * 2014-09-03 2016-05-04 哈尔滨工业大学 一种β-溴代四氢呋喃类化合物的合成方法
CN104292189B (zh) * 2014-09-03 2016-05-04 哈尔滨工业大学 一种β-丙二酸二乙酯取代四氢呋喃类化合物的合成方法
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
CN113366000A (zh) * 2018-09-18 2021-09-07 百时美施贵宝公司 作为lpa拮抗剂的氧杂双环酸

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
EP1638963B1 (en) 2003-05-20 2009-09-09 Novartis AG N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
DE602005022089D1 (de) * 2004-08-06 2010-08-12 Merck Sharp & Dohme Sulfonylverbindungen als hemmer von 11-beta-hydroxysteroiddehydrogenase-1
UA97474C2 (ru) * 2006-03-31 2012-02-27 Новартис Аг Соединения для лечения нарушений, связанных с активностью dgat1
CN101932562B (zh) * 2007-12-20 2013-06-12 阿斯利康(瑞典)有限公司 作为dgat1抑制剂190的氨基甲酰基化合物
SG188586A1 (en) * 2010-10-07 2013-04-30 Novartis Ag New crystalline forms of the sodium salt of (4- {4- [5- ( 6 - trifluoromethyl - pyridin- 3 - ylamino ) - pyridin- 2 -yl] -phenyl} - cyclohexyl) -acetic acid
US8962660B2 (en) * 2013-03-14 2015-02-24 Bristol-Myers Squibb Company Oxabicyclo [2.2.2] acid GPR120 modulators

Also Published As

Publication number Publication date
CA2870336A1 (en) 2013-10-31
WO2013160873A1 (en) 2013-10-31
AP3592A (en) 2016-02-15
MA37439A1 (fr) 2016-07-29
ECSP14030538A (es) 2015-11-30
AU2013254307A1 (en) 2014-10-30
ES2624291T3 (es) 2017-07-13
CL2014002822A1 (es) 2015-04-24
UY34767A (es) 2013-11-29
TN2014000425A1 (en) 2016-03-30
CN104395309B (zh) 2016-09-28
US8993619B2 (en) 2015-03-31
IL235313A0 (en) 2014-12-31
AU2013254307B2 (en) 2016-05-26
US20130289058A1 (en) 2013-10-31
CR20140494A (es) 2015-03-13
EP2852590B1 (en) 2017-02-01
JP2015514798A (ja) 2015-05-21
CO7111275A2 (es) 2014-11-10
EA201491970A1 (ru) 2015-03-31
SG11201406526WA (en) 2014-11-27
MA37439B1 (fr) 2017-02-28
PE20150724A1 (es) 2015-05-17
KR20150013194A (ko) 2015-02-04
PH12014502413A1 (en) 2015-01-12
US20150166563A1 (en) 2015-06-18
EP2852590A1 (en) 2015-04-01
MX2014013002A (es) 2015-01-22
JP6042529B2 (ja) 2016-12-14
TW201348239A (zh) 2013-12-01
CN104395309A (zh) 2015-03-04
EA025050B1 (ru) 2016-11-30
BR112014026760A8 (pt) 2018-01-16
AR090859A1 (es) 2014-12-10
MX357768B (es) 2018-07-24
BR112014026760A2 (pt) 2017-06-27
AP2014008018A0 (en) 2014-10-31

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