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1. (WO2019062924) LONG-ACTING PRODRUG OF ENTECAVIR AND PREPARATION METHOD AND APPLICATION THEREOF
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Pub. No.: WO/2019/062924 International Application No.: PCT/CN2018/108663
Publication Date: 04.04.2019 International Filing Date: 29.09.2018
IPC:
C07D 473/18 (2006.01) ,C07J 43/00 (2006.01) ,A61K 31/522 (2006.01) ,A61K 31/58 (2006.01) ,A61P 31/20 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
18
one oxygen and one nitrogen atom, e.g. guanine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
43
Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
52
Purines, e.g. adenine
522
having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
58
containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
20
for DNA viruses
Applicants:
广州市恒诺康医药科技有限公司 GUANGZHOU HENOVCOM BIOSCIENCE CO., LTD [CN/CN]; 中国广东省广州市 黄埔区开源大道11号C4栋第九层 9F, Zone C4, 11 Kaiyuan Road, HuangPu District Guangzhou City, Guangdong 510535, CN
Inventors:
张健存 ZHANG, Jiancun; CN
李德耀 LI, Deyao; CN
周溢谦 ZHOU, Yiqian; CN
吴毅武 WU, Yiwu; CN
刘燕 LIU, Yan; CN
Agent:
北京瑞恒信达知识产权代理事务所(普通合伙) LEADING INTELLECTUAL PROPERTY FIRM; 中国北京市 海淀区大柳树路17号富海中心2号楼9层909房间 Room 909,9th Floor, Tower B,Fortune Building, No.17,Daliushu Road,Haidian District Beijing 100081, CN
Priority Data:
201710903592.129.09.2017CN
Title (EN) LONG-ACTING PRODRUG OF ENTECAVIR AND PREPARATION METHOD AND APPLICATION THEREOF
(FR) PROMÉDICAMENT À ACTION PROLONGÉE D'ENTÉCAVIR, SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION
(ZH) 长效恩替卡韦前药及其制备方法和应用
Abstract:
(EN) Provided are a long-acting prodrug of entecavir and a preparation method and application thereof. The prodrug of entecavir has the structure shown in formula I, and the compound can be released slowly, continuously, and stably and converted into an active drug, entecavir, in the body, thereby achieving the purpose of long-acting. The definitions of R1, R2, and R3 in formula I are as described in the specification.
(FR) L'invention concerne un promédicament à action prolongée d'entécavir, son procédé de préparation et son application. Le promédicament d'entécavir a la structure représentée par la formule I, et le composé peut être libéré lentement, de manière continue et de façon stable et converti en un médicament actif, entécavir, dans le corps, ce qui permet d'atteindre l'objectif de l'action prolongée. Les définitions de R1, R2 et R3 dans la formule I sont telles que indiquées dans la description.
(ZH) 提供了一种长效恩替卡韦前药及其制备方法和应用。该恩替卡韦前药具有式I所示的结构,该化合物在体内能缓慢、持续、稳定地释放并转化为恩替卡韦原药,达到长效的目的。在式I中,R1、R2和R3的定义如说明书所述。
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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, KR, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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: Chinese (ZH)
Filing Language: Chinese (ZH)