CN104321058A - 用于治疗低磷血性疾病的fgfr抑制剂 - Google Patents
用于治疗低磷血性疾病的fgfr抑制剂 Download PDFInfo
- Publication number
- CN104321058A CN104321058A CN201380015597.0A CN201380015597A CN104321058A CN 104321058 A CN104321058 A CN 104321058A CN 201380015597 A CN201380015597 A CN 201380015597A CN 104321058 A CN104321058 A CN 104321058A
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- Prior art keywords
- dimethoxy
- methyl
- ethyl
- piperazin
- phenylf
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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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/42—Phosphorus; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/29—Parathyroid hormone, i.e. parathormone; Parathyroid hormone-related peptides
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
-
- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- 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
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Inorganic Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Zoology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Marine Sciences & Fisheries (AREA)
- Toxicology (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811194059.3A CN109718239B (zh) | 2012-03-30 | 2013-03-29 | 用于治疗低磷血性疾病的fgfr抑制剂 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261617889P | 2012-03-30 | 2012-03-30 | |
| US61/617,889 | 2012-03-30 | ||
| PCT/EP2013/056811 WO2013144339A1 (en) | 2012-03-30 | 2013-03-29 | Fgfr inhibitor for use in the treatment of hypophosphatemic disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811194059.3A Division CN109718239B (zh) | 2012-03-30 | 2013-03-29 | 用于治疗低磷血性疾病的fgfr抑制剂 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104321058A true CN104321058A (zh) | 2015-01-28 |
Family
ID=47998482
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811194059.3A Active CN109718239B (zh) | 2012-03-30 | 2013-03-29 | 用于治疗低磷血性疾病的fgfr抑制剂 |
| CN201380015597.0A Pending CN104321058A (zh) | 2012-03-30 | 2013-03-29 | 用于治疗低磷血性疾病的fgfr抑制剂 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811194059.3A Active CN109718239B (zh) | 2012-03-30 | 2013-03-29 | 用于治疗低磷血性疾病的fgfr抑制剂 |
Country Status (11)
| Country | Link |
|---|---|
| US (4) | US20150072019A1 (enExample) |
| EP (1) | EP2830626B1 (enExample) |
| JP (1) | JP6190871B2 (enExample) |
| KR (1) | KR102126092B1 (enExample) |
| CN (2) | CN109718239B (enExample) |
| AU (1) | AU2013241664B2 (enExample) |
| CA (1) | CA2866229C (enExample) |
| IN (1) | IN2014DN08969A (enExample) |
| MX (1) | MX354783B (enExample) |
| RU (1) | RU2643326C2 (enExample) |
| WO (1) | WO2013144339A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108026588A (zh) * | 2015-07-24 | 2018-05-11 | 德彪药业国际股份公司 | Fgfr表达以及对fgfr抑制剂的敏感性 |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| EA028614B1 (ru) * | 2014-05-22 | 2017-12-29 | Общество С Ограниченной Ответственностью "Русские Фармацевтические Технологии" | Селективные ингибиторы, нарушающие взаимодействие рецептора фактора роста фибробластов и frs2, для профилактики и лечения рака |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| EA038045B1 (ru) | 2015-02-20 | 2021-06-28 | Инсайт Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| WO2016189472A1 (en) * | 2015-05-28 | 2016-12-01 | Novartis Ag | Fgfr inhibitor for use in the treatment of the phosphaturic mesenchymal tumor |
| CN108348519A (zh) * | 2015-07-20 | 2018-07-31 | 台北医学大学 | 经氯苯取代的氮杂芳基化合物 |
| ES2932262T3 (es) | 2017-01-06 | 2023-01-17 | Lemonex Inc | Composición para la prevención o el tratamiento de cáncer de ovario metastásico, cáncer de endometrio o cáncer de mama |
| WO2018128510A1 (ko) * | 2017-01-06 | 2018-07-12 | 주식회사 레모넥스 | 전이성 난소암, 자궁내막암 또는 유방암의 예방 또는 치료용 조성물 |
| JP6387198B1 (ja) | 2017-04-14 | 2018-09-05 | 堺ディスプレイプロダクト株式会社 | 有機el表示装置の製造方法及び製造装置 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| US11174257B2 (en) | 2018-05-04 | 2021-11-16 | Incyte Corporation | Salts of an FGFR inhibitor |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| PH12022550892A1 (en) | 2019-10-14 | 2023-05-03 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| WO2021119108A1 (en) * | 2019-12-09 | 2021-06-17 | Cedars-Sinai Medical Center | Use of fgfr inhibitors for treatment of idiopathic short stature |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法 |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為fgfr抑制劑之三環雜環 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009133101A1 (en) * | 2008-04-29 | 2009-11-05 | Novartis Ag | Methods of monitoring the modulation of the kinase activity of fibroblast growth factor receptor and uses of said methods |
| WO2011051425A1 (en) * | 2009-10-30 | 2011-05-05 | Novartis Ag | N-oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2433171A1 (en) | 2000-12-26 | 2002-07-04 | Chugai Seiyaku Kabushiki Kaisha | Human fgf23 protein mutants decreasing blood phosphorus level |
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| EP1882475A1 (en) * | 2006-07-26 | 2008-01-30 | Novartis AG | Method of treating disorders mediated by the fibroblast growth factor receptor |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
| EP2512476A1 (en) * | 2009-12-18 | 2012-10-24 | Novartis AG | Method for treating haematological cancers |
| WO2013088191A1 (en) | 2011-12-12 | 2013-06-20 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3 |
-
2013
- 2013-03-29 US US14/388,978 patent/US20150072019A1/en not_active Abandoned
- 2013-03-29 CN CN201811194059.3A patent/CN109718239B/zh active Active
- 2013-03-29 WO PCT/EP2013/056811 patent/WO2013144339A1/en not_active Ceased
- 2013-03-29 IN IN8969DEN2014 patent/IN2014DN08969A/en unknown
- 2013-03-29 KR KR1020147026889A patent/KR102126092B1/ko active Active
- 2013-03-29 AU AU2013241664A patent/AU2013241664B2/en active Active
- 2013-03-29 EP EP13712589.4A patent/EP2830626B1/en active Active
- 2013-03-29 JP JP2015502373A patent/JP6190871B2/ja active Active
- 2013-03-29 CA CA2866229A patent/CA2866229C/en active Active
- 2013-03-29 CN CN201380015597.0A patent/CN104321058A/zh active Pending
- 2013-03-29 MX MX2014011841A patent/MX354783B/es active IP Right Grant
- 2013-03-29 RU RU2014143517A patent/RU2643326C2/ru active
-
2016
- 2016-09-22 US US15/272,633 patent/US10028955B2/en active Active
-
2018
- 2018-06-12 US US16/005,966 patent/US20210308132A1/en not_active Abandoned
-
2024
- 2024-01-09 US US18/407,729 patent/US20240398798A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009133101A1 (en) * | 2008-04-29 | 2009-11-05 | Novartis Ag | Methods of monitoring the modulation of the kinase activity of fibroblast growth factor receptor and uses of said methods |
| CN102016592A (zh) * | 2008-04-29 | 2011-04-13 | 诺瓦提斯公司 | 监测成纤维细胞生长因子受体的激酶活性的调节的方法及所述方法的应用 |
| WO2011051425A1 (en) * | 2009-10-30 | 2011-05-05 | Novartis Ag | N-oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108026588A (zh) * | 2015-07-24 | 2018-05-11 | 德彪药业国际股份公司 | Fgfr表达以及对fgfr抑制剂的敏感性 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20210308132A1 (en) | 2021-10-07 |
| US10028955B2 (en) | 2018-07-24 |
| IN2014DN08969A (enExample) | 2015-05-22 |
| JP6190871B2 (ja) | 2017-08-30 |
| EP2830626A1 (en) | 2015-02-04 |
| CA2866229C (en) | 2020-09-15 |
| US20170007606A1 (en) | 2017-01-12 |
| RU2643326C2 (ru) | 2018-01-31 |
| US20240398798A1 (en) | 2024-12-05 |
| MX354783B (es) | 2018-03-21 |
| AU2013241664B2 (en) | 2016-05-19 |
| CA2866229A1 (en) | 2013-10-03 |
| AU2013241664A1 (en) | 2014-10-02 |
| JP2015511621A (ja) | 2015-04-20 |
| CN109718239A (zh) | 2019-05-07 |
| CN109718239B (zh) | 2024-09-10 |
| RU2014143517A (ru) | 2016-05-27 |
| KR20140145133A (ko) | 2014-12-22 |
| US20150072019A1 (en) | 2015-03-12 |
| EP2830626B1 (en) | 2019-01-02 |
| MX2014011841A (es) | 2015-02-10 |
| WO2013144339A1 (en) | 2013-10-03 |
| KR102126092B1 (ko) | 2020-06-24 |
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