AR106987A1 - Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje - Google Patents
Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltajeInfo
- Publication number
- AR106987A1 AR106987A1 ARP160103829A ARP160103829A AR106987A1 AR 106987 A1 AR106987 A1 AR 106987A1 AR P160103829 A ARP160103829 A AR P160103829A AR P160103829 A ARP160103829 A AR P160103829A AR 106987 A1 AR106987 A1 AR 106987A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- branched
- linear
- cyclic alkyl
- formula
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 108010052164 Sodium Channels Proteins 0.000 title 1
- 102000018674 Sodium Channels Human genes 0.000 title 1
- 150000003385 sodium Chemical class 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 10
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001721 carbon Chemical group 0.000 abstract 3
- 102220531732 Piwi-like protein 1_R10A_mutation Human genes 0.000 abstract 2
- 102220531498 Piwi-like protein 1_R11A_mutation Human genes 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102220497245 Serine-tRNA ligase, cytoplasmic_R9A_mutation Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
- C07D277/38—Nitrogen atoms
- C07D277/50—Nitrogen atoms bound to hetero atoms
- C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cephalosporin Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Reivindicación 1: Un compuesto, o una sal farmacéuticamente aceptable del mismo, que tiene la estructura de fórmula (1), en la que: R¹ es: -Cl, -Br, o alquilo lineal, ramificado o cíclico de hasta 3 átomos de carbono; R² es: (a) un resto de la fórmula (2), en la que, uno de R³ᵃ y R³ᵇ es -H y el otro es -H, -F, CH₃; o (b) un resto de la fórmula (3); y E es: (I) un resto de fórmula (4), en la que: R⁶ es -H o un alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono; y B es: (a) un resto de la fórmula (5), resto que se une a nitrógeno en uno de R⁷A, R⁷B, o R⁷C por medio de -CH₂-, o se une a nitrógeno directamente en uno de R⁷C, y en la que: m es 0, 1 ó 2; R⁷A y R⁷B son independientemente para cada aparición -H, o un alquilo lineal, ramificado o cíclico de hasta 3 átomos de carbono cuando no se selecciona para unirse al nitrógeno por medio de metileno; R⁷C cuando no se selecciona para unirse al nitrógeno directamente o por medio de metileno es independientemente para cada aparición (i) -H; (ii) alquilo lineal, ramificado o cíclico de hasta tres carbonos; y R⁷D es: (ai) -H; o (aii) un alquilo lineal, ramificado o cíclico de hasta 5 átomos de carbono; o (b) un resto de la fórmula (6), en la que: R⁷ʰ es -H o un alquilo lineal, ramificado o cíclico de hasta 3 átomos de carbono; y R⁷ᵍ y R⁷ᶠ se seleccionan como sigue: (i) R⁷ᵍ es un alquilo lineal de al menos 2, hasta 4 átomos de carbono, un alquilo ramificado de al menos 3 hasta 6 átomos de carbono o alquilo cíclico de hasta 6 átomos de carbono y R⁷ᶠ es un alquilo lineal de al menos 2 átomos de carbono hasta 4 átomos de carbono, o un alquilo ramificado o cíclico de hasta 6 átomos de carbono que está sustituido con -OH en un átomo de carbono del mismo que está unido en beta, o más lejos, al nitrógeno al que está unido; o (ii) R⁷ᶠ es -H o un alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono o y R⁷ᵍ es -(CH₂)₁₋₂-(HC(OH))-(CH₂)₁₋₂; (II) un resto de fórmula (7), en la que cada R⁸ es independientemente -H o alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono; o (III) un resto de fórmula (8), en la que: R⁹A es independientemente para cada aparición (i) -H; (ii) -OH; o (iii) un alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono que está opcionalmente sustituido en un átomo de carbono del mismo con un -OH; R¹⁰A es independientemente para cada aparición (i) -H; o (ii) alquilo lineal, ramificado o cíclico de hasta 6 átomos de carbono que está opcionalmente sustituido en un átomo de carbono del mismo con un -OH; R¹¹A es -H o un, alquilo de 2 ó 3 carbonos que está opcionalmente sustituido en un carbono b o g con un -OH, con la condición de que únicamente un sustituyente -OH esté presente entre todos de R⁹A, R¹⁰A y R¹¹A.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562269327P | 2015-12-18 | 2015-12-18 | |
| US201662290235P | 2016-02-02 | 2016-02-02 | |
| US201662420956P | 2016-11-11 | 2016-11-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR106987A1 true AR106987A1 (es) | 2018-03-07 |
Family
ID=57708830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160103829A AR106987A1 (es) | 2015-12-18 | 2016-12-14 | Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US10221167B2 (es) |
| EP (1) | EP3390374B1 (es) |
| JP (1) | JP6572392B2 (es) |
| KR (1) | KR20180095598A (es) |
| CN (1) | CN108699015A (es) |
| AR (1) | AR106987A1 (es) |
| AU (1) | AU2016370554B2 (es) |
| BR (1) | BR112018012327A2 (es) |
| CA (1) | CA3008611A1 (es) |
| CL (1) | CL2018001640A1 (es) |
| CO (1) | CO2018006137A2 (es) |
| CR (1) | CR20180322A (es) |
| DO (1) | DOP2018000150A (es) |
| EA (1) | EA201891313A1 (es) |
| EC (1) | ECSP18052850A (es) |
| HK (1) | HK1255027A1 (es) |
| IL (1) | IL260052A (es) |
| MX (1) | MX2018007450A (es) |
| NI (1) | NI201800067A (es) |
| PE (1) | PE20181495A1 (es) |
| PH (1) | PH12018501288A1 (es) |
| SG (1) | SG11201804936UA (es) |
| SV (1) | SV2018005708A (es) |
| TN (1) | TN2018000195A1 (es) |
| TW (1) | TW201726637A (es) |
| WO (1) | WO2017106226A1 (es) |
| ZA (1) | ZA201803591B (es) |
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| TWI773657B (zh) | 2015-12-18 | 2022-08-11 | 美商亞德利克斯公司 | 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物 |
| CN108699015A (zh) * | 2015-12-18 | 2018-10-23 | 默沙东公司 | 对电压门控性钠通道具有选择性活性的羟基烷基胺-和羟基环烷基胺-取代的二胺-芳基磺胺化合物 |
| BR112019007763A2 (pt) | 2016-10-17 | 2019-07-02 | Genentech Inc | composto de fórmula, composição farmacêutica, métodos para tratar uma doença ou condição, para tratar dores, para diminuir o fluxo de íons e para tratar prurido, uso de um composto e invenção |
| ES2897998T3 (es) * | 2016-10-27 | 2022-03-03 | Bristol Myers Squibb Co | Inhibidores de la acilsulfonamida del NaV1.7 |
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| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
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| CN111285825B (zh) * | 2018-12-10 | 2023-02-17 | 中国科学院上海药物研究所 | 一类苯磺酰胺取代的衍生物，其制法及其用途 |
| WO2020248123A1 (en) | 2019-06-11 | 2020-12-17 | Merck Sharp & Dohme Corp. | Hydroxypyrrolidine-substituted arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| CN113527281B (zh) * | 2020-04-20 | 2023-12-22 | 昆山彭济凯丰生物科技有限公司 | 杂环化合物及其制备方法和应用 |
| CN117362206B (zh) * | 2023-12-08 | 2024-02-20 | 四川大学华西第二医院 | 一类芳基磺酰胺类化合物、合成方法及用途 |
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-
2016
- 2016-12-14 CN CN201680081234.0A patent/CN108699015A/zh active Pending
- 2016-12-14 CR CR20180322A patent/CR20180322A/es unknown
- 2016-12-14 AR ARP160103829A patent/AR106987A1/es unknown
- 2016-12-14 US US15/378,465 patent/US10221167B2/en active Active
- 2016-12-14 CA CA3008611A patent/CA3008611A1/en not_active Abandoned
- 2016-12-14 WO PCT/US2016/066445 patent/WO2017106226A1/en not_active Ceased
- 2016-12-14 BR BR112018012327A patent/BR112018012327A2/pt not_active Application Discontinuation
- 2016-12-14 PE PE2018001100A patent/PE20181495A1/es unknown
- 2016-12-14 TN TNP/2018/000195A patent/TN2018000195A1/en unknown
- 2016-12-14 EA EA201891313A patent/EA201891313A1/ru unknown
- 2016-12-14 JP JP2018531094A patent/JP6572392B2/ja not_active Expired - Fee Related
- 2016-12-14 MX MX2018007450A patent/MX2018007450A/es unknown
- 2016-12-14 HK HK18114148.2A patent/HK1255027A1/zh unknown
- 2016-12-14 AU AU2016370554A patent/AU2016370554B2/en not_active Ceased
- 2016-12-14 KR KR1020187020090A patent/KR20180095598A/ko not_active Abandoned
- 2016-12-14 TW TW105141337A patent/TW201726637A/zh unknown
- 2016-12-14 SG SG11201804936UA patent/SG11201804936UA/en unknown
- 2016-12-14 EP EP16820497.2A patent/EP3390374B1/en active Active
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2018
- 2018-05-30 ZA ZA2018/03591A patent/ZA201803591B/en unknown
- 2018-06-12 NI NI201800067A patent/NI201800067A/es unknown
- 2018-06-13 SV SV2018005708A patent/SV2018005708A/es unknown
- 2018-06-14 PH PH12018501288A patent/PH12018501288A1/en unknown
- 2018-06-14 IL IL260052A patent/IL260052A/en unknown
- 2018-06-15 CO CONC2018/0006137A patent/CO2018006137A2/es unknown
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- 2018-06-18 DO DO2018000150A patent/DOP2018000150A/es unknown
- 2018-07-12 EC ECSENADI201852850A patent/ECSP18052850A/es unknown
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2019
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|---|---|
| MX2018007450A (es) | 2018-11-14 |
| CO2018006137A2 (es) | 2018-07-10 |
| EA201891313A1 (ru) | 2018-11-30 |
| CR20180322A (es) | 2018-08-21 |
| US10221167B2 (en) | 2019-03-05 |
| AU2016370554B2 (en) | 2018-11-29 |
| PE20181495A1 (es) | 2018-09-18 |
| EP3390374B1 (en) | 2020-08-26 |
| CN108699015A (zh) | 2018-10-23 |
| SG11201804936UA (en) | 2018-07-30 |
| CA3008611A1 (en) | 2017-06-22 |
| DOP2018000150A (es) | 2018-07-31 |
| ECSP18052850A (es) | 2018-12-31 |
| US20170174674A1 (en) | 2017-06-22 |
| SV2018005708A (es) | 2018-12-14 |
| IL260052A (en) | 2018-07-31 |
| WO2017106226A1 (en) | 2017-06-22 |
| PH12018501288A1 (en) | 2019-01-28 |
| CL2018001640A1 (es) | 2018-08-03 |
| BR112018012327A2 (pt) | 2018-12-04 |
| EP3390374A1 (en) | 2018-10-24 |
| AU2016370554A1 (en) | 2018-06-14 |
| JP2019502681A (ja) | 2019-01-31 |
| US20190233406A1 (en) | 2019-08-01 |
| ZA201803591B (en) | 2019-04-24 |
| KR20180095598A (ko) | 2018-08-27 |
| JP6572392B2 (ja) | 2019-09-11 |
| HK1255027A1 (zh) | 2019-08-02 |
| TW201726637A (zh) | 2017-08-01 |
| TN2018000195A1 (en) | 2019-10-04 |
| NI201800067A (es) | 2018-07-24 |
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