CU20140066A7 - Compuestos novedosos de benzopirano, composiciones y usos de los mismos - Google Patents
Compuestos novedosos de benzopirano, composiciones y usos de los mismosInfo
- Publication number
- CU20140066A7 CU20140066A7 CU2014000066A CU20140066A CU20140066A7 CU 20140066 A7 CU20140066 A7 CU 20140066A7 CU 2014000066 A CU2014000066 A CU 2014000066A CU 20140066 A CU20140066 A CU 20140066A CU 20140066 A7 CU20140066 A7 CU 20140066A7
- Authority
- CU
- Cuba
- Prior art keywords
- compounds
- methyl
- benzopiran
- compositions
- new
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- 230000001833 anti-estrogenic effect Effects 0.000 abstract 3
- KDVXAPCZVZMPMU-XBBWARJSSA-N (2s)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C([C@H]2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-XBBWARJSSA-N 0.000 abstract 2
- 229940046836 anti-estrogen Drugs 0.000 abstract 2
- 239000000328 estrogen antagonist Substances 0.000 abstract 2
- KDVXAPCZVZMPMU-COBFLCELSA-N 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C(C2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-COBFLCELSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000001562 benzopyrans Chemical class 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 230000001076 estrogenic effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
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- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se preveen compuestos de benzopirano con fuerte actividad anti- estrogénica y en esencia ninguna actividad estrogénica, que son OP-1038, que es 3-(4- hidroxifenil)-4- metil-2-(4-{2-[(3R)- 3- metil- pirrolidin-1-il]etoxi} fenil)-2H- cromen-7-ol, y OP -1074, que es (2S)-3-(4- hidroxifenil)-4- metil-2-(4-{2-[(3R)-3- metilpirrolidin -1- il]etoxi} fenil)- 2H-cromen-7-ol. OP-1074 es un anti- estrógeno puro cuando es probado en el modo agonista y un anti-estrógeno completo cuando se prueba en el modo antagonista. Estos compuestos son útiles para el tratamiento o prevención de una variedad de condiciones que son modulados a través del receptor de estrógeno en mamíferos incluyendo humanos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161576890P | 2011-12-16 | 2011-12-16 | |
| PCT/US2012/070168 WO2013090921A1 (en) | 2011-12-16 | 2012-12-17 | Novel benzopyran compounds, compositions and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CU20140066A7 true CU20140066A7 (es) | 2014-10-02 |
Family
ID=48613277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CU2014000066A CU20140066A7 (es) | 2011-12-16 | 2014-06-11 | Compuestos novedosos de benzopirano, composiciones y usos de los mismos |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9018244B2 (es) |
| EP (1) | EP2791128A4 (es) |
| JP (1) | JP2015505856A (es) |
| KR (1) | KR20140103335A (es) |
| CN (1) | CN104169266A (es) |
| AP (1) | AP2014007657A0 (es) |
| AU (1) | AU2012353660A1 (es) |
| BR (1) | BR112014014767A2 (es) |
| CA (1) | CA2857061A1 (es) |
| CL (1) | CL2014001533A1 (es) |
| CR (1) | CR20140259A (es) |
| CU (1) | CU20140066A7 (es) |
| DO (1) | DOP2014000135A (es) |
| EA (1) | EA201490897A1 (es) |
| EC (1) | ECSP14009619A (es) |
| HK (1) | HK1199246A1 (es) |
| IL (1) | IL233118A0 (es) |
| MA (1) | MA35722B1 (es) |
| MD (1) | MD20140054A2 (es) |
| MX (1) | MX2014007198A (es) |
| NI (1) | NI201400057A (es) |
| PE (1) | PE20150099A1 (es) |
| PH (1) | PH12014501237A1 (es) |
| SG (1) | SG11201402564QA (es) |
| TN (1) | TN2014000243A1 (es) |
| WO (1) | WO2013090921A1 (es) |
| ZA (1) | ZA201404733B (es) |
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| RS56042B1 (sr) | 2010-06-10 | 2017-09-29 | Seragon Pharmaceuticals Inc | Modulatori estrogenih receptora i njihove upotrebe |
| WO2013090829A1 (en) | 2011-12-14 | 2013-06-20 | Aragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
| WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
| CN104725333A (zh) * | 2013-12-20 | 2015-06-24 | 北京蓝贝望生物医药科技股份有限公司 | 一种新的氮杂环庚烷衍生物的制备方法 |
| SG11201607339VA (en) * | 2014-03-13 | 2016-10-28 | Hoffmann La Roche | Methods and compositions for modulating estrogen receptor mutants |
| WO2015136016A2 (en) * | 2014-03-13 | 2015-09-17 | F. Hoffmann-La Roche Ag | Therapeutic combinations with estrogen receptor modulators |
| WO2017024318A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| KR20240142622A (ko) | 2015-10-01 | 2024-09-30 | 올레마 파마슈티컬스 인코포레이티드 | 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물 |
| WO2017072792A1 (en) | 2015-10-27 | 2017-05-04 | Sun Pharma Advanced Research Company Limited | Novel heterocyclic antiestrogens |
| LT3386500T (lt) | 2015-12-09 | 2022-12-27 | The Board Of Trustees Of The University Of Illinois | Selektyvūs estrogenų receptorių slopintojai benzotiofeno pagrindu |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| RU2019102647A (ru) | 2016-07-01 | 2020-08-03 | Г1 Терапьютикс, Инк. | Антипролиферационные средства на основе пиримидина |
| ES2909576T3 (es) | 2016-10-11 | 2022-05-09 | Univ Duke | Tratamiento con lasofoxifeno del cáncer de mama ER+ |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
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| KR20190117582A (ko) | 2017-02-10 | 2019-10-16 | 쥐원 쎄라퓨틱스, 인크. | 벤조티오펜 에스트로겐 수용체 조정제 |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| WO2019006393A1 (en) | 2017-06-29 | 2019-01-03 | G1 Therapeutics, Inc. | Morphic forms of git38 and methods of manufacture thereof |
| AU2018351050B2 (en) | 2017-10-18 | 2025-09-18 | Novartis Ag | Compositions and methods for selective protein degradation |
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| US11497730B2 (en) | 2018-04-10 | 2022-11-15 | Duke University | Lasofoxifene treatment of breast cancer |
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-
2012
- 2012-12-17 EP EP20120858374 patent/EP2791128A4/en not_active Withdrawn
- 2012-12-17 AU AU2012353660A patent/AU2012353660A1/en not_active Abandoned
- 2012-12-17 MD MDA20140054A patent/MD20140054A2/ro not_active Application Discontinuation
- 2012-12-17 BR BR112014014767A patent/BR112014014767A2/pt not_active IP Right Cessation
- 2012-12-17 EA EA201490897A patent/EA201490897A1/ru unknown
- 2012-12-17 MX MX2014007198A patent/MX2014007198A/es unknown
- 2012-12-17 WO PCT/US2012/070168 patent/WO2013090921A1/en not_active Ceased
- 2012-12-17 US US13/717,326 patent/US9018244B2/en not_active Expired - Fee Related
- 2012-12-17 JP JP2014547552A patent/JP2015505856A/ja active Pending
- 2012-12-17 PE PE2014000963A patent/PE20150099A1/es not_active Application Discontinuation
- 2012-12-17 AP AP2014007657A patent/AP2014007657A0/xx unknown
- 2012-12-17 SG SG11201402564QA patent/SG11201402564QA/en unknown
- 2012-12-17 CA CA2857061A patent/CA2857061A1/en not_active Abandoned
- 2012-12-17 HK HK14112731.3A patent/HK1199246A1/xx unknown
- 2012-12-17 KR KR1020147019676A patent/KR20140103335A/ko not_active Ceased
- 2012-12-17 CN CN201280062009.4A patent/CN104169266A/zh active Pending
-
2014
- 2014-05-28 CR CR20140259A patent/CR20140259A/es unknown
- 2014-06-02 PH PH12014501237A patent/PH12014501237A1/en unknown
- 2014-06-02 MA MA37096A patent/MA35722B1/fr unknown
- 2014-06-03 TN TNP2014000243A patent/TN2014000243A1/fr unknown
- 2014-06-11 CL CL2014001533A patent/CL2014001533A1/es unknown
- 2014-06-11 CU CU2014000066A patent/CU20140066A7/es unknown
- 2014-06-12 IL IL233118A patent/IL233118A0/en unknown
- 2014-06-13 NI NI201400057A patent/NI201400057A/es unknown
- 2014-06-16 DO DO2014000135A patent/DOP2014000135A/es unknown
- 2014-06-26 ZA ZA2014/04733A patent/ZA201404733B/en unknown
- 2014-07-16 EC ECIEPI20149619A patent/ECSP14009619A/es unknown
-
2015
- 2015-03-17 US US14/660,248 patent/US20150197506A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| BR112014014767A2 (pt) | 2017-06-13 |
| MX2014007198A (es) | 2014-10-13 |
| SG11201402564QA (en) | 2014-09-26 |
| CR20140259A (es) | 2014-08-21 |
| AP2014007657A0 (en) | 2014-05-31 |
| HK1199246A1 (en) | 2015-06-26 |
| WO2013090921A1 (en) | 2013-06-20 |
| PH12014501237A1 (en) | 2014-09-08 |
| AU2012353660A1 (en) | 2014-06-12 |
| PE20150099A1 (es) | 2015-01-30 |
| ZA201404733B (en) | 2016-04-28 |
| CA2857061A1 (en) | 2013-06-20 |
| EP2791128A4 (en) | 2015-04-22 |
| NI201400057A (es) | 2014-10-01 |
| IL233118A0 (en) | 2014-08-03 |
| EP2791128A1 (en) | 2014-10-22 |
| US9018244B2 (en) | 2015-04-28 |
| CL2014001533A1 (es) | 2014-10-17 |
| TN2014000243A1 (fr) | 2015-09-30 |
| EA201490897A1 (ru) | 2015-03-31 |
| MA35722B1 (fr) | 2014-12-01 |
| DOP2014000135A (es) | 2014-08-31 |
| JP2015505856A (ja) | 2015-02-26 |
| US20150197506A1 (en) | 2015-07-16 |
| MD20140054A2 (ro) | 2014-10-31 |
| CN104169266A (zh) | 2014-11-26 |
| US20130178445A1 (en) | 2013-07-11 |
| ECSP14009619A (es) | 2015-09-30 |
| KR20140103335A (ko) | 2014-08-26 |
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