AR097721A1 - Derivados de etinilo - Google Patents

Derivados de etinilo

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Publication number
AR097721A1
AR097721A1 ARP140103499A ARP140103499A AR097721A1 AR 097721 A1 AR097721 A1 AR 097721A1 AR P140103499 A ARP140103499 A AR P140103499A AR P140103499 A ARP140103499 A AR P140103499A AR 097721 A1 AR097721 A1 AR 097721A1
Authority
AR
Argentina
Prior art keywords
group
halogen
lower alkyl
hydrogen
pyridinyl
Prior art date
Application number
ARP140103499A
Other languages
English (en)
Inventor
Jaeschke Georg
Ricci Antonio
Rueher Daniel
Vieira Eric
Guba Wolfgang
Biemans Barbara
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR097721A1 publication Critical patent/AR097721A1/es

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    • 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
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96Two oxygen atoms
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/10Antiepileptics; Anticonvulsants for petit-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/91Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
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    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Epidemiology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

La presente se refiere a compuestos de fórmula (1), en la que: Y es N o C-R¹; G es un anillo aromático o heteroaromático de 5 ó 6 elementos que contiene 0, 1, 2 ó 3 heteroátomos, seleccionado de entre el grupo que consiste de fenilo, piridinilo con diferentes posiciones de N, imidazolilo, pirazinilo, pirimidinilo, tiofenilo, tiazolilo, pirazolilo o tiadiazolilo, que se sustituyen opcionalmente con 1, 2 ó 3 sustituyentes, seleccionados de entre el grupo que consiste de halógeno, alquilo inferior, alcoxi inferior, alcoxi inferior sustituido con halógeno o NRR, R y R son, independientemente uno de otro, hidrógeno o alquilo inferior, o pueden formar conjuntamente con el átomo de N al que se encuentran unidos un grupo heterocíclico saturado de cinco o seis elementos que puede contener un oxígeno adicional, NH o un grupo N-alquilo inferior; R¹ es hidrógeno, halógeno o alquilo inferior sustituido con halógeno; R¹ es hidrógeno, halógeno o alquilo inferior sustituido con halógeno; R² es hidrógeno, alquilo inferior, alcoxialquilo inferior, cicloalquilo o heterocicloalquilo, o R² puede formar conjuntamente con el átomo de carbono más próximo en el grupo G un grupo de la fórmula (2) en el que A es -CH₂-, -CH₂CH₂ o -C(CH₃)₂-; R³ es fenilo o piridinilo, en el que el átomo de N en el grupo piridinilo puede encontrarse en posiciones diferentes; o a una sal o sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o a su enantiómero y/o isómero óptico y/o estereoisómero correspondiente de los mismos. Inesperadamente se ha encontrado que los compuestos de fórmula general (1) son moduladores alostéricos positivos (MAP) del receptor metabotrópico del glutamato 4 (mGluR4) que resultan útiles para el tratamiento de la enfermedad de Parkinson, la ansiedad, la emesis, el trastorno obsesivo-compulsivo, el autismo, la neuroprotección, el cáncer, la depresión y la diabetes de tipo 2.
ARP140103499A 2013-09-25 2014-09-22 Derivados de etinilo AR097721A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13185856 2013-09-25

Publications (1)

Publication Number Publication Date
AR097721A1 true AR097721A1 (es) 2016-04-13

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ID=49230629

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Application Number Title Priority Date Filing Date
ARP140103499A AR097721A1 (es) 2013-09-25 2014-09-22 Derivados de etinilo

Country Status (28)

Country Link
US (2) US20160207890A1 (es)
EP (1) EP3049409B1 (es)
JP (1) JP6134441B2 (es)
KR (1) KR101757603B1 (es)
CN (1) CN105579447B (es)
AR (1) AR097721A1 (es)
AU (1) AU2014327504B2 (es)
BR (1) BR112016005994A2 (es)
CA (1) CA2924376A1 (es)
CL (1) CL2016000677A1 (es)
CR (1) CR20160075A (es)
DK (1) DK3049409T3 (es)
EA (1) EA029352B1 (es)
ES (1) ES2630319T3 (es)
HK (1) HK1220200A1 (es)
HU (1) HUE034849T2 (es)
IL (1) IL244039B (es)
MA (1) MA38885B1 (es)
MX (1) MX370341B (es)
MY (1) MY183953A (es)
PE (1) PE20160666A1 (es)
PH (1) PH12016500427A1 (es)
PL (1) PL3049409T3 (es)
SG (1) SG11201602029VA (es)
SI (1) SI3049409T1 (es)
TW (1) TWI527801B (es)
UA (1) UA116277C2 (es)
WO (1) WO2015044075A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3110802T3 (pl) * 2014-02-25 2019-03-29 F. Hoffmann-La Roche Ag Pochodne etynylowe
JP6539749B2 (ja) * 2015-03-19 2019-07-03 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft mGluR4のモジュレーターとしての3−(4−エチニルフェニル)ヘキサヒドロピリミジン−2,4−ジオン誘導体
DK3322701T3 (da) 2015-07-15 2019-07-08 H Hoffmann La Roche Ag Ethynylderivater som metabotropiske glutamatreceptormodulatorer
AR105556A1 (es) * 2015-08-03 2017-10-18 Hoffmann La Roche Derivados de etinilo
WO2017031116A1 (en) * 2015-08-18 2017-02-23 The Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of ku70/80 and uses thereof
HUE051006T2 (hu) * 2016-07-18 2021-01-28 Hoffmann La Roche Etinil-származékok
WO2020021064A1 (en) 2018-07-26 2020-01-30 Domain Therapeutics Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10330359A (ja) * 1997-03-31 1998-12-15 Nippon Bayeragrochem Kk フエニルアセチレン誘導体及び除草剤
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
EA200971143A1 (ru) * 2007-06-03 2010-06-30 Вандербилт Юниверсити Бензамидные mglur5 позитивные аллостерические модуляторы и способы их получения и применения
WO2011029104A1 (en) * 2009-09-04 2011-03-10 Vanderbilt University Mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
KR20120120416A (ko) * 2010-02-11 2012-11-01 벤더르빌트 유니버시티 Mglur4 알로스테릭 강화제로서 벤즈이속사졸 및 아자벤즈이속사졸, 조성물, 및 신경 기능이상을 치료하는 방법
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
BR112012028894A2 (pt) * 2010-05-12 2019-09-24 Univ Vanderbilt sulfona heterocíclica como potenciadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
CN102503888A (zh) * 2011-10-08 2012-06-20 西安交通大学 2-芳基-1,3-异喹啉二酮类抗肿瘤化合物及其合成方法和用途

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Publication number Publication date
PL3049409T3 (pl) 2017-09-29
US20170114028A1 (en) 2017-04-27
CN105579447A (zh) 2016-05-11
KR20160044581A (ko) 2016-04-25
US20160207890A1 (en) 2016-07-21
CA2924376A1 (en) 2015-04-02
EP3049409B1 (en) 2017-05-03
EP3049409A1 (en) 2016-08-03
WO2015044075A1 (en) 2015-04-02
CN105579447B (zh) 2018-11-13
SI3049409T1 (sl) 2017-08-31
IL244039A0 (en) 2016-04-21
TWI527801B (zh) 2016-04-01
BR112016005994A2 (pt) 2017-08-01
EA201690408A1 (ru) 2016-07-29
DK3049409T3 (en) 2017-07-10
HUE034849T2 (en) 2018-03-28
ES2630319T3 (es) 2017-08-21
MX370341B (es) 2019-12-10
AU2014327504B2 (en) 2018-01-04
TW201524963A (zh) 2015-07-01
UA116277C2 (uk) 2018-02-26
JP6134441B2 (ja) 2017-05-24
PE20160666A1 (es) 2016-07-09
HK1220200A1 (zh) 2017-04-28
JP2016531869A (ja) 2016-10-13
MA38885A1 (fr) 2017-12-29
AU2014327504A1 (en) 2016-02-18
EA029352B1 (ru) 2018-03-30
MY183953A (en) 2021-03-17
SG11201602029VA (en) 2016-04-28
MX2016002717A (es) 2016-06-08
PH12016500427A1 (en) 2016-05-16
US9676732B2 (en) 2017-06-13
CR20160075A (es) 2016-05-04
MA38885B1 (fr) 2018-11-30
KR101757603B1 (ko) 2017-07-12
IL244039B (en) 2019-06-30
CL2016000677A1 (es) 2016-11-04

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