EA201691046A1 - Производные этинилимидазолин-2,4-диона в качестве модуляторов метаботропного глутаматного рецептора 4 (mglur4) - Google Patents
Производные этинилимидазолин-2,4-диона в качестве модуляторов метаботропного глутаматного рецептора 4 (mglur4)Info
- Publication number
- EA201691046A1 EA201691046A1 EA201691046A EA201691046A EA201691046A1 EA 201691046 A1 EA201691046 A1 EA 201691046A1 EA 201691046 A EA201691046 A EA 201691046A EA 201691046 A EA201691046 A EA 201691046A EA 201691046 A1 EA201691046 A1 EA 201691046A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- hydrogen
- lower alkyl
- ethylimidazoline
- mglur4
- dion
- Prior art date
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- C—CHEMISTRY; METALLURGY
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B55/00—Racemisation; Complete or partial inversion
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/04—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
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- 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
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic 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 three hetero rings
- C07D487/14—Ortho-condensed systems
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- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Otolaryngology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Настоящее изобретение относится к соединениям формулы Iгде Y представляет собой C-R; Rявляется водородом или галогеном; Rявляется водородом или галогеном; Rявляется водородом, низшим алкилом или фенилом; Rявляется водородом или низшим алкилом; или Rи Rмогут образовывать вместе с соответствующими атомами, к которым они присоединены, следующие кольцаRявляется водородом или низшим алкилом; и если Rи Rобразуют кольцо, такое как описано выше, то Rявляется водородом; или Rи Rвместе с атомом углерода, к которому они присоединены, могут образовывать гетероциклоалкильное кольцо; Rявляется фенилом или пиридинилом, где атом N пиридинильной группы может находиться в разных положениях; или к их фармацевтически приемлемой соли или соли присоединения кислоты, к рацемической смеси или ее соответствующему энантиомеру, и/или оптическому изомеру, и/или стереоизомеру. Соединения могут применяться для лечения болезни Паркинсона, тревожного расстройства, тошноты и рвоты, обессивно-компульсивного расстройства, аутизма, при нейропротекции, лечении онкологического заболевания, депрессивного синдрома и диабета 2 типа.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP14150700 | 2014-01-10 | ||
PCT/EP2015/050127 WO2015104271A1 (en) | 2014-01-10 | 2015-01-07 | Ethynyl-imidazolin-2,4-dione derivatives as mglur4 modulators |
Publications (2)
Publication Number | Publication Date |
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EA201691046A1 true EA201691046A1 (ru) | 2016-12-30 |
EA029967B1 EA029967B1 (ru) | 2018-06-29 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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EA201691046A EA029967B1 (ru) | 2014-01-10 | 2015-01-07 | Производные этинилимидазолин-2,4-диона в качестве модуляторов метаботропного глутаматного рецептора 4 (mglur4) |
Country Status (22)
Country | Link |
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US (1) | US9695128B2 (ru) |
EP (1) | EP3092219B1 (ru) |
JP (1) | JP6263633B2 (ru) |
KR (1) | KR101868248B1 (ru) |
CN (1) | CN106170479B (ru) |
AR (1) | AR099047A1 (ru) |
AU (1) | AU2015205661B2 (ru) |
BR (1) | BR112016010168A2 (ru) |
CA (1) | CA2934768A1 (ru) |
CL (1) | CL2016001739A1 (ru) |
CR (1) | CR20160198A (ru) |
EA (1) | EA029967B1 (ru) |
HK (1) | HK1226054A1 (ru) |
IL (1) | IL245327B (ru) |
MX (1) | MX369820B (ru) |
PE (1) | PE20160860A1 (ru) |
PH (1) | PH12016501100A1 (ru) |
SG (1) | SG11201605557TA (ru) |
TW (1) | TWI649310B (ru) |
UA (1) | UA119053C2 (ru) |
WO (1) | WO2015104271A1 (ru) |
ZA (1) | ZA201602890B (ru) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI3110802T1 (sl) * | 2014-02-25 | 2019-01-31 | F. Hoffmann-La Roche Ag | Derivati etinila |
RS58929B1 (sr) | 2015-07-15 | 2019-08-30 | Hoffmann La Roche | Derivati etinila kao modulatori metabotropnih glutamatnih receptora |
AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
RU2745068C2 (ru) | 2016-07-18 | 2021-03-18 | Ф. Хоффманн-Ля Рош Аг | Производные этинила |
JP7364553B2 (ja) * | 2017-08-17 | 2023-10-18 | エフ. ホフマン-ラ ロシュ アーゲー | パーキンソン病等の疾患を処置するためのイミダゾ[1,2-a]イミダゾール-2-オン誘導体 |
US10893929B2 (en) | 2018-01-10 | 2021-01-19 | Cook Medical Technologies Llc | Vascular graft with compartments for compliance matching |
US10517713B2 (en) | 2018-01-10 | 2019-12-31 | Cook Medical Technologies Llc | Vascular graft with helical flow compliance compartments |
AU2019309448A1 (en) | 2018-07-26 | 2021-01-14 | Domain Therapeutics | Substituted quinazolinone derivatives and their use as positive allosteric modulators of mGluR4 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX2009013169A (es) * | 2007-06-03 | 2010-04-30 | Univ Vanderbilt | Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos. |
CN102740699A (zh) * | 2009-09-04 | 2012-10-17 | 范德比尔特大学 | 用于治疗神经学上的功能失调的mglur4变构增效剂、组合物和方法 |
US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
US10533000B2 (en) * | 2011-05-26 | 2020-01-14 | Sunovion Pharmaceuticals, Inc. | Metabotrophic glutamate receptor 5 modulators and methods of use thereof |
-
2015
- 2015-01-06 TW TW104100333A patent/TWI649310B/zh not_active IP Right Cessation
- 2015-01-07 CN CN201580002922.9A patent/CN106170479B/zh active Active
- 2015-01-07 EA EA201691046A patent/EA029967B1/ru not_active IP Right Cessation
- 2015-01-07 WO PCT/EP2015/050127 patent/WO2015104271A1/en active Application Filing
- 2015-01-07 EP EP15700850.9A patent/EP3092219B1/en active Active
- 2015-01-07 BR BR112016010168A patent/BR112016010168A2/pt not_active IP Right Cessation
- 2015-01-07 KR KR1020167018069A patent/KR101868248B1/ko active IP Right Grant
- 2015-01-07 CA CA2934768A patent/CA2934768A1/en not_active Abandoned
- 2015-01-07 MX MX2016008887A patent/MX369820B/es active IP Right Grant
- 2015-01-07 JP JP2016545871A patent/JP6263633B2/ja active Active
- 2015-01-07 AU AU2015205661A patent/AU2015205661B2/en not_active Ceased
- 2015-01-07 SG SG11201605557TA patent/SG11201605557TA/en unknown
- 2015-01-07 PE PE2016000958A patent/PE20160860A1/es unknown
- 2015-01-08 AR ARP150100038A patent/AR099047A1/es unknown
- 2015-07-01 UA UAA201608260A patent/UA119053C2/uk unknown
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2016
- 2016-04-27 IL IL245327A patent/IL245327B/en active IP Right Grant
- 2016-04-28 CR CR20160198A patent/CR20160198A/es unknown
- 2016-04-28 ZA ZA2016/02890A patent/ZA201602890B/en unknown
- 2016-06-09 PH PH12016501100A patent/PH12016501100A1/en unknown
- 2016-07-07 CL CL2016001739A patent/CL2016001739A1/es unknown
- 2016-07-08 US US15/205,466 patent/US9695128B2/en active Active
- 2016-12-14 HK HK16114239A patent/HK1226054A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
PE20160860A1 (es) | 2016-09-03 |
AR099047A1 (es) | 2016-06-22 |
ZA201602890B (en) | 2017-07-26 |
US20170008854A1 (en) | 2017-01-12 |
SG11201605557TA (en) | 2016-08-30 |
PH12016501100B1 (en) | 2016-07-11 |
CL2016001739A1 (es) | 2017-05-12 |
TWI649310B (zh) | 2019-02-01 |
MX2016008887A (es) | 2016-10-04 |
MX369820B (es) | 2019-11-22 |
EP3092219B1 (en) | 2018-09-19 |
AU2015205661B2 (en) | 2018-08-23 |
UA119053C2 (uk) | 2019-04-25 |
CR20160198A (es) | 2016-06-17 |
HK1226054A1 (zh) | 2017-09-22 |
KR101868248B1 (ko) | 2018-06-15 |
IL245327A0 (en) | 2016-06-30 |
CA2934768A1 (en) | 2015-07-16 |
US9695128B2 (en) | 2017-07-04 |
JP2017502066A (ja) | 2017-01-19 |
IL245327B (en) | 2018-12-31 |
KR20160095099A (ko) | 2016-08-10 |
TW201531464A (zh) | 2015-08-16 |
BR112016010168A2 (pt) | 2017-08-08 |
CN106170479B (zh) | 2019-02-12 |
EA029967B1 (ru) | 2018-06-29 |
JP6263633B2 (ja) | 2018-01-17 |
PH12016501100A1 (en) | 2016-07-11 |
CN106170479A (zh) | 2016-11-30 |
EP3092219A1 (en) | 2016-11-16 |
WO2015104271A1 (en) | 2015-07-16 |
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