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1. (WO2019062665) LINKER COMPOUND, POLYETHYLENE GLYCOL-LINKER CONJUGATE AND DERIVATIVE THEREOF, AND POLYETHYLENE GLYCOL-LINKER-DRUG CONJUGATE
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Pub. No.: WO/2019/062665 International Application No.: PCT/CN2018/106972
Publication Date: 04.04.2019 International Filing Date: 21.09.2018
IPC:
A61K 47/54 (2017.01) ,A61K 47/60 (2017.01) ,A61K 31/704 (2006.01) ,A61P 35/00 (2006.01) ,C07C 229/08 (2006.01) ,C07C 215/08 (2006.01) ,C07D 249/04 (2006.01) ,C08G 65/333 (2006.01) ,C08G 65/48 (2006.01)
[IPC code unknown for A61K 47/54][IPC code unknown for A61K 47/60]
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7028
Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
7034
attached to a carbocyclic compound, e.g. phloridzin
704
attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02
having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
06
having only one amino and one carboxyl group bound to the carbon skeleton
08
the nitrogen atom of the amino group being further bound to hydrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
215
Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02
having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being saturated
06
and acyclic
08
with only one hydroxy group and one amino group bound to the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
04
1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
G
MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
65
Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
02
from cyclic ethers by opening of the heterocyclic ring
32
Polymers modified by chemical after-treatment
329
with organic compounds
333
containing nitrogen
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
G
MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
65
Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
34
from hydroxy compounds or their metallic derivatives
48
Polymers modified by chemical after-treatment
Applicants:
天津键凯科技有限公司 JENKEM TECHNOLOGY CO., LTD. (TIANJIN) [CN/CN]; 中国天津市 经济技术开发区西区康诚街9号 No.9 Kangcheng Street, West Zone of TEDA Tianjin 300462, CN
Inventors:
冯泽旺 FENG, Zewang; CN
王庆彬 WANG, Qingbin; CN
汪进良 WANG, Jinliang; CN
宋艳萍 SONG, Yanping; CN
熊艳丽 XIONG, Yanli; CN
王雷敏 WANG, Leimin; CN
杜景辉 DU, Jinghui; CN
赵宣 ZHAO, Xuan; CN
Agent:
北京布瑞知识产权代理有限公司 BEIJING BRIGHT IP AGENCY CO., LTD.; 中国北京市 朝阳区广顺北大街5号院内32号B228 B228 No. 32, Inside the No. 5 Yard, Guangshun North Street, Chaoyang District Beijing 100102, CN
Priority Data:
201710919466.530.09.2017CN
201810186781.607.03.2018CN
201811043884.307.09.2018CN
Title (EN) LINKER COMPOUND, POLYETHYLENE GLYCOL-LINKER CONJUGATE AND DERIVATIVE THEREOF, AND POLYETHYLENE GLYCOL-LINKER-DRUG CONJUGATE
(FR) COMPOSÉ DE LIEUR, CONJUGUÉ POLYÉTHYLÈNE GLYCOL-LIEUR ET DÉRIVÉ DE CELUI-CI, ET CONJUGUÉ POLYÉTHYLÈNE GLYCOL-LIEUR-MÉDICAMENT
(ZH) 一种连接子化合物、聚乙二醇-连接子结合物及其衍生物和聚乙二醇-连接子-药物结合物
Abstract:
(EN) The present invention discloses a linker compound, a polyethylene glycol-linker conjugate and a derivative thereof, and a polyethylene glycol-linker drug conjugate. The linker compound and the polyethylene glycol conjugate and a derivative thereof can be used for drug modification, and the modification reaction is simple and easy to carry out and has a high reaction yield, and the modified drugs have a wide application range. The modified drugs gradually degrade from a conjugate chain in the body, and can stay in a lesion (such as a cancer site) for a longer period of time, achieving the purpose of sustained and controlled release, reducing frequency of administration, and greatly improving drug bioavailability and drug compliance of patients.
(FR) La présente invention concerne un composé de lieur, un conjugué polyéthylène glycol-lieur et un dérivé de celui-ci, et un conjugué polyéthylène glycol-lieur-médicament. Le composé de lieur et le conjugué polyéthylène glycol et un dérivé de celui-ci peuvent être utilisés pour une modification de médicament, et la réaction de modification est simple et facile à mettre en oeuvre et a un rendement de réaction élevé, et les médicaments modifiés ont une large gamme d'applications. Les médicaments modifiés se dégradent progressivement à partir d'une chaîne conjuguée dans le corps, et peuvent rester dans une lésion (telle qu'un site cancéreux) pendant une plus longue période de temps, ce qui permet d'obtenir une libération prolongée et contrôlée, de réduire la fréquence d'administration, et d'améliorer considérablement la biodisponibilité des médicaments et l'observance médicamenteuse des patients.
(ZH) 本发明公开了一种连接子化合物、聚乙二醇-连接子结合物及其衍生物和聚乙二醇-连接子-药物结合物。所述的连接子化合物及其与聚乙二醇的结合物及其衍生物,可用于修饰药物,且修饰反应简单,容易进行,反应产率较高,修饰药物的适用范围较宽。修饰后的药物在体内从结合物链上逐渐降解,可在病灶(例如患癌)部位停留更长时间,达到缓释和控释的目的,可降低给药频率,大大提高药物的生物利用度和病人的依从性。
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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)