EA201792517A1 - Производные бензоимидазола в качестве ингибиторов pad4 - Google Patents
Производные бензоимидазола в качестве ингибиторов pad4Info
- Publication number
- EA201792517A1 EA201792517A1 EA201792517A EA201792517A EA201792517A1 EA 201792517 A1 EA201792517 A1 EA 201792517A1 EA 201792517 A EA201792517 A EA 201792517A EA 201792517 A EA201792517 A EA 201792517A EA 201792517 A1 EA201792517 A1 EA 201792517A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- benzoimidazole
- derivatives
- pad4 inhibitors
- lupus erythematosus
- pad4
- Prior art date
Links
Classifications
-
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D498/06—Peri-condensed systems
Abstract
Соединение формулы (I)где X, Y, Rи R-Rимеют значение, определённое в данной заявке, и его соли являются ингибиторами PAD4 и могут применяться в лечении различных заболеваний, например ревматоидного артрита, васкулита, системной красной волчанки, язвенного колита, ракового заболевания, муковисцидоза, астмы, кожной формы красной волчанки и псориаза.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562164906P | 2015-05-21 | 2015-05-21 | |
PCT/IB2016/000761 WO2016185279A1 (en) | 2015-05-21 | 2016-05-19 | Benzoimidazole derivatives as pad4 inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201792517A1 true EA201792517A1 (ru) | 2018-04-30 |
EA033680B1 EA033680B1 (ru) | 2019-11-15 |
Family
ID=56235853
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201792517A EA033680B1 (ru) | 2015-05-21 | 2016-05-19 | Производные бензоимидазола в качестве ингибиторов pad4 |
Country Status (15)
Country | Link |
---|---|
US (2) | US10407407B2 (ru) |
EP (1) | EP3298003B1 (ru) |
JP (1) | JP6703553B2 (ru) |
KR (1) | KR20180005250A (ru) |
CN (1) | CN107849015B (ru) |
AR (1) | AR106863A1 (ru) |
AU (1) | AU2016264958B2 (ru) |
BR (1) | BR112017024678A2 (ru) |
CA (2) | CA2986199C (ru) |
EA (1) | EA033680B1 (ru) |
ES (1) | ES2945314T3 (ru) |
IL (2) | IL255666A (ru) |
MX (1) | MX2017014714A (ru) |
TW (1) | TW201706263A (ru) |
WO (1) | WO2016185279A1 (ru) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
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AR107032A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
EP3419969B1 (en) * | 2016-02-23 | 2019-12-18 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
EP3490989B1 (en) | 2016-07-27 | 2020-09-09 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
JP7118951B2 (ja) | 2016-09-12 | 2022-08-16 | パドロック・セラピューティクス・インコーポレイテッド | Pad4のヘテロアリール阻害剤 |
NZ762985A (en) * | 2017-09-22 | 2024-03-22 | Jubilant Epipad LLC | Heterocyclic compounds as pad inhibitors |
HUE061607T2 (hu) * | 2017-10-18 | 2023-07-28 | Jubilant Epipad LLC | Imidazopiridin vegyületek mint PAD inhibitorok |
CN111386265A (zh) | 2017-11-06 | 2020-07-07 | 朱比连特普罗德尔有限责任公司 | 作为pd1/pd-l1活化的抑制剂的嘧啶衍生物 |
EP3704120B1 (en) | 2017-11-24 | 2024-03-06 | Jubilant Episcribe LLC | Heterocyclic compounds as prmt5 inhibitors |
WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
EP3746430A4 (en) | 2018-02-02 | 2021-11-03 | Padforward LLC | INHIBITORS OF PROTEIN ARGININE DEIMINASES |
BR112020018610A2 (pt) | 2018-03-13 | 2020-12-29 | Jubilant Prodel LLC | Compostos de fórmula i, fórmula ii, fórmula iii, fórmula iv, fórmula v, fórmula vi, ou seus polimorfos, estereoisômeros, tautômeros, profármacos, solvatos e sais farmaceuticamente aceitáveis dos mesmos e uso dos mesmos; processo de preparação; composição farmacêutica; e método para o tratamento e/ou prevenção de várias doenças, que incluem câncer e doenças infecciosas |
HRP20230388T1 (hr) | 2018-03-22 | 2023-06-23 | F. Hoffmann - La Roche Ag | Inhibitori oksazin monoacilglicerol lipaze (magl) |
CN112789087A (zh) * | 2018-08-08 | 2021-05-11 | 百时美施贵宝公司 | Pad酶的苯并咪唑抑制剂 |
MX2021001471A (es) * | 2018-08-08 | 2021-04-28 | Bristol Myers Squibb Co | Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4). |
EA202190462A1 (ru) | 2018-08-08 | 2021-06-03 | Бристол-Маерс Сквибб Компани | Индольные и азаиндольные ингибиторы ферментов pad |
EP3837263A1 (en) | 2018-08-13 | 2021-06-23 | F. Hoffmann-La Roche AG | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
MA53220A (fr) | 2018-08-13 | 2021-11-17 | Hoffmann La Roche | Nouveaux composés hétérocycliques utilisés en tant qu'inhibiteurs de monoacylglycérol lipase |
EP3883936B1 (en) | 2018-11-22 | 2023-07-12 | F. Hoffmann-La Roche AG | New heterocyclic compounds |
US20210094971A1 (en) | 2019-09-09 | 2021-04-01 | Hoffmann-La Roche Inc. | Heterocyclic compounds |
EP4028403B1 (en) | 2019-09-12 | 2023-11-22 | F. Hoffmann-La Roche AG | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
AU2020354414A1 (en) | 2019-09-24 | 2022-02-17 | F. Hoffmann-La Roche Ag | New heterocyclic monoacylglycerol lipase (MAGL) inhibitors |
AR120029A1 (es) | 2019-09-24 | 2022-01-26 | Hoffmann La Roche | Compuestos heterocíclicos |
CN114514233A (zh) | 2019-09-24 | 2022-05-17 | 豪夫迈·罗氏有限公司 | 用于单酰基甘油脂肪酶(magl)的荧光探针 |
TW202115083A (zh) * | 2019-09-27 | 2021-04-16 | 大陸商南京藥捷安康生物科技有限公司 | 肽醯精胺酸脫亞胺酶抑制劑及其用途 |
JP2023512557A (ja) * | 2020-02-06 | 2023-03-27 | ブリストル-マイヤーズ スクイブ カンパニー | 免疫抑制剤として有用な大環状pad4阻害剤 |
TW202140477A (zh) * | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環pad4抑制劑 |
US20230107927A1 (en) | 2020-02-28 | 2023-04-06 | First Wave Bio, Inc. | Methods of treating iatrogenic autoimmune colitis |
PE20230488A1 (es) * | 2020-04-30 | 2023-03-21 | Gilead Sciences Inc | Inhibidores macrociclicos de las peptidilarginina deiminasas |
WO2022034616A1 (en) * | 2020-08-12 | 2022-02-17 | Jubilant Epipad LLC | Method and compound for use, in treating and/or preventing netosis |
WO2022140390A1 (en) | 2020-12-22 | 2022-06-30 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
WO2023083365A1 (en) * | 2021-11-15 | 2023-05-19 | Qilu Regor Therapeutics Inc. | Pad4 inhibitors and use thereof |
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AU570439B2 (en) | 1983-03-28 | 1988-03-17 | Compression Labs, Inc. | A combined intraframe and interframe transform coding system |
US5776963A (en) | 1989-05-19 | 1998-07-07 | Hoechst Marion Roussel, Inc. | 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility |
CA2361954C (en) | 1995-04-14 | 2003-07-08 | Smithkline Beecham Corporation | Metered dose inhaler for albuterol |
TW533865U (en) | 1997-06-10 | 2003-05-21 | Glaxo Group Ltd | Dispenser for dispensing medicament and actuation indicating device |
US6315112B1 (en) | 1998-12-18 | 2001-11-13 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
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US6352152B1 (en) | 1998-12-18 | 2002-03-05 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
US6390291B1 (en) | 1998-12-18 | 2002-05-21 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
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JP5039268B2 (ja) * | 2001-10-26 | 2012-10-03 | アベンティス・ファーマスーティカルズ・インコーポレイテツド | ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用 |
EP1699512B1 (en) | 2003-11-03 | 2012-06-20 | Glaxo Group Limited | A fluid dispensing device |
US7429611B2 (en) * | 2004-09-23 | 2008-09-30 | Bristol-Myers Squibb Company | Indole inhibitors of 15-lipoxygenase |
UY32138A (es) | 2008-09-25 | 2010-04-30 | Boehringer Ingelheim Int | Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables |
ES2882797T3 (es) * | 2009-04-02 | 2021-12-02 | Merck Serono Sa | Inhibidores de dihidroorotato deshidrogenasa |
PL3001903T3 (pl) * | 2009-12-21 | 2018-03-30 | Samumed, Llc | 1H-pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne |
PL2877467T3 (pl) * | 2012-07-26 | 2017-08-31 | Glaxo Group Limited | 2-(azaindolo-2-ylo)benzoimidazole jako inhibitory pad4 |
AR107032A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
-
2016
- 2016-05-19 CN CN201680042358.8A patent/CN107849015B/zh active Active
- 2016-05-19 US US15/575,583 patent/US10407407B2/en active Active
- 2016-05-19 KR KR1020177036327A patent/KR20180005250A/ko not_active Application Discontinuation
- 2016-05-19 EP EP16732332.8A patent/EP3298003B1/en active Active
- 2016-05-19 ES ES16732332T patent/ES2945314T3/es active Active
- 2016-05-19 WO PCT/IB2016/000761 patent/WO2016185279A1/en active Application Filing
- 2016-05-19 EA EA201792517A patent/EA033680B1/ru not_active IP Right Cessation
- 2016-05-19 MX MX2017014714A patent/MX2017014714A/es unknown
- 2016-05-19 CA CA2986199A patent/CA2986199C/en active Active
- 2016-05-19 CA CA3199601A patent/CA3199601A1/en active Pending
- 2016-05-19 JP JP2017560547A patent/JP6703553B2/ja active Active
- 2016-05-19 AU AU2016264958A patent/AU2016264958B2/en active Active
- 2016-05-19 BR BR112017024678-3A patent/BR112017024678A2/pt not_active Application Discontinuation
- 2016-05-20 TW TW105115842A patent/TW201706263A/zh unknown
- 2016-05-20 AR ARP160101486A patent/AR106863A1/es unknown
-
2017
- 2017-11-14 IL IL255666A patent/IL255666A/en active IP Right Grant
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2019
- 2019-07-18 US US16/515,735 patent/US10815218B2/en active Active
-
2020
- 2020-11-23 IL IL278916A patent/IL278916A/en unknown
Also Published As
Publication number | Publication date |
---|---|
EP3298003B1 (en) | 2023-04-19 |
AU2016264958B2 (en) | 2020-10-29 |
IL255666A (en) | 2018-01-31 |
MX2017014714A (es) | 2018-01-25 |
US20180297983A1 (en) | 2018-10-18 |
BR112017024678A2 (pt) | 2018-07-31 |
AU2016264958A1 (en) | 2017-12-07 |
ES2945314T3 (es) | 2023-06-30 |
JP6703553B2 (ja) | 2020-06-03 |
EP3298003A1 (en) | 2018-03-28 |
CA2986199A1 (en) | 2016-11-24 |
EA033680B1 (ru) | 2019-11-15 |
CN107849015B (zh) | 2021-03-19 |
US20200095227A1 (en) | 2020-03-26 |
US10407407B2 (en) | 2019-09-10 |
CA2986199C (en) | 2023-07-18 |
AR106863A1 (es) | 2018-02-28 |
CA3199601A1 (en) | 2016-11-24 |
JP2018520105A (ja) | 2018-07-26 |
TW201706263A (zh) | 2017-02-16 |
WO2016185279A1 (en) | 2016-11-24 |
IL278916A (en) | 2021-01-31 |
US10815218B2 (en) | 2020-10-27 |
CN107849015A (zh) | 2018-03-27 |
KR20180005250A (ko) | 2018-01-15 |
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