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1. (WO2018066947) ENTECAVIR DERIVATIVE COMPOUND BOUND WITH FATTY ACID AND PHARMACEUTICAL USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.:    WO/2018/066947    International Application No.:    PCT/KR2017/011022
Publication Date: 12.04.2018 International Filing Date: 29.09.2017
IPC:
C07D 473/18 (2006.01), A61K 31/522 (2006.01), A61K 9/00 (2006.01), A61K 9/16 (2006.01), A61K 9/20 (2006.01), A61K 9/48 (2006.01)
Applicants: DANKOOK UNIVERSITY CHEONAN CAMPUS INDUSTRY ACADEMIC COOPERATION FOUNDATION [KR/KR]; (Anseo-dong), Dankook University Cheonan Campus, 119, Dandae-ro, Dongnam-gu Cheonan-si Chungcheongnam-do 31116 (KR)
Inventors: KANG, Myung Joo; (KR).
HAN, Young Taek; (KR).
LEE, Dae Ro; (KR).
HO, Myoung Jin; (KR)
Agent: TAEBAEK INTELLECTUAL PROPERTY LAW FIRM; #601 Innoplex 1 cha, 151Gasandigital 1-ro Geumcheon-gu Seoul 08506 (KR)
Priority Data:
10-2016-0129647 07.10.2016 KR
Title (EN) ENTECAVIR DERIVATIVE COMPOUND BOUND WITH FATTY ACID AND PHARMACEUTICAL USE THEREOF
(FR) COMPOSÉ DÉRIVÉ D'ENTÉCAVIR LIÉ À UN ACIDE GRAS ET SON UTILISATION PHARMACEUTIQUE
(KO) 지방산이 결합된 엔테카비어 유도체 화합물 및 이의 약학적 용도
Abstract: front page image
(EN)The present invention relates to an entecavir derivative compound bound with a fatty acid and a pharmaceutical use thereof. The entecavir derivative covalently bound with a fatty acid according to the present invention exhibits a significantly lower solubility and dissolution rate than entecavir. The fatty acid polymer of entecavir according to the present invention can exert a sustained effect for several weeks or more after a single administration when a preparation is made for parenteral administration such as an injection, and can drastically improve patient medication compliance .
(FR)La présente invention concerne un composé dérivé d'entécavir lié à un acide gras et une utilisation pharmaceutique de celui-ci. Le dérivé d'entécavir lié de manière covalente à un acide gras selon la présente invention présente une solubilité et un taux de dissolution significativement inférieurs à celui de l'entécavir. Le polymère d'acide gras d'entécavir selon la présente invention peut exercer un effet prolongé pendant plusieurs semaines ou plus après une administration unique lorsqu'une préparation est réalisée pour une administration parentérale telle qu'une injection, et peut considérablement améliorer la conformité de médication du patient.
(KO)본 발명은 지방산이 결합된 엔테카비어 유도체 화합물 및 이의 약학적 용도에 대한 것으로서, 본 발명에 의한 지방산이 공유결합된 엔테카비어 유도체는 엔테카비어에 비해 현저하게 낮은 용해도와 용출속도를 나타낸다. 본 발명에 의한 엔테카비어의 지방산 중합체는 주사제 등의 비경구투여용 제제로 제조할 경우 단회투여 후 수 주 이상의 지속적인 효과를 발현할 수 있으며, 환자의 복약 순응도를 획기적으로 개선할 수 있다.
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 (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)