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1. (WO2019031754) SUGAR-ADDED OSPEMIFENE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
Latest bibliographic data on file with the International BureauSubmit observation

Pub. No.: WO/2019/031754 International Application No.: PCT/KR2018/008662
Publication Date: 14.02.2019 International Filing Date: 31.07.2018
IPC:
C07H 15/203 (2006.01) ,C12P 19/18 (2006.01) ,C12P 19/46 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15
Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
20
Carbocyclic rings
203
Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
P
FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
19
Preparation of compounds containing saccharide radicals
18
produced by the action of a glycosyl transferase, e.g. alpha-, beta- or gamma-cyclodextrins
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
P
FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
19
Preparation of compounds containing saccharide radicals
44
Preparation of O-glycosides, e.g. glucosides
46
having an oxygen atom of the saccharide radical bound to a cyclohexyl radical, e.g. kasugamycin
Applicants:
고려대학교 산학협력단 KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION [KR/KR]; 서울시 성북구 안암로 145 145, Anam-ro Seongbuk-gu Seoul 02841, KR
Inventors:
박제원 PARK, Je Won; KR
Agent:
이처영 LEE, Cheo Young; KR
장제환 CHANG, Je Hwan; KR
Priority Data:
10-2017-010157410.08.2017KR
Title (EN) SUGAR-ADDED OSPEMIFENE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
(FR) OSPÉMIFÈNE À SUCRE AJOUTE, PROCÉDÉ DE PRÉPARATION S'Y RAPPORTANT ET COMPOSITION PHARMACEUTIQUE CONTENANT CELUI-CI EN TANT QUE PRINCIPE ACTIF
(KO) 당 부가된 오스페미펜, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
Abstract:
(EN) The present invention relates to a novel ospemifene derivative compound in which a sugar is added to ospemifene as one kind of selective estrogen receptor modulator (hereinafter, SERM), and to a preparation method for the compound. The ospemifene derivative compound has improved bioavailability compared with existing ospemifene, and also has partially improved bioavailability compared with the original compound ospemifene, which provides a disease treatment effect for dyspareunia, vaginal dryness, and the like appearing in menopausal women, and thus can be favorably used as a modified dosage form.
(FR) La présente invention concerne un nouveau composé dérivé d'ospémifène dans lequel un sucre est ajouté à l'ospémifène en tant qu'un type de modulateur sélectif du récepteur des oestrogènes (ci-après SERM) et un procédé de préparation pour le composé. Le composé dérivé d'ospémifène présente une biodisponibilité améliorée par comparaison avec l'ospémifène existant et présente également une biodisponibilité partiellement améliorée par comparaison avec le composé ospémifène d'origine, ce qui assure un effet de traitement de maladie pour la dyspareunie, la sécheresse vaginale et similaires apparaissant chez les femmes ménopausées, et il peut ainsi être avantageusement utilisé en tant que forme pharmaceutique modifiée.
(KO) 본 발명은 선택적 에스트로겐 수용체 조절제(selective estrogen receptor modulator; 이하 SERM)의 일종인 오스페미펜(ospemifene)에 당이 부가된 신규 오스페미펜 유도체 화합물 및 상기 화합물의 제조방법에 관한 것으로, 기존의 오스페미펜에 비하여 생체이용율이 향상되어, 폐경기 여성들에 있어서 나타나는 성교통(dyspareunia) 및 질 건조증(vaginal dryness) 등의 질환 치료 효과를 제공하고 있는 원래 화합물인 오스페미펜에 비하여 생체이용률 또한 일부 향상시키고 있는 바, 개량 제형으로서 유용하게 사용될 수 있다.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Korean (KO)
Filing Language: Korean (KO)