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1. (WO2018205286) CONJUGATE AND BLOCK COPOLYMER CONTAINING FLUORESCENT CHROMOPHORE AND PREPARATION METHOD THEREFOR AND USE THEREOF
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Pub. No.: WO/2018/205286 International Application No.: PCT/CN2017/084503
Publication Date: 15.11.2018 International Filing Date: 16.05.2017
IPC:
C07D 311/16 (2006.01) ,C07D 405/06 (2006.01) ,C07H 15/252 (2006.01) ,C09K 11/06 (2006.01) ,C07K 14/765 (2006.01) ,C07K 14/585 (2006.01) ,A61K 47/62 (2017.01) ,A61K 47/54 (2017.01) ,A61K 49/00 (2006.01) ,A61K 31/704 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
311
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02
ortho- or peri-condensed with carbocyclic rings or ring systems
04
Benzo [b] pyrans, not hydrogenated in the carbocyclic ring
06
with oxygen or sulfur atoms directly attached in position 2
08
not hydrogenated in the hetero ring
16
substituted in position 7
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
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
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
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
24
Condensed ring systems having three or more rings
252
Naphthacene radicals, e.g. daunomycins, adriamycins
C CHEMISTRY; METALLURGY
09
DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
K
MATERIALS FOR APPLICATIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
11
Luminescent, e.g. electroluminescent, chemiluminescent, materials
06
containing organic luminescent materials
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
76
Albumins
765
Serum albumin, e.g. HSA
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
575
Hormones
585
Calcitonins
[IPC code unknown for A61K 47/62][IPC code unknown for A61K 47/54]
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49
Preparations for testing in vivo
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
Applicants:
中国科学技术大学 UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA [CN/CN]; 中国安徽省合肥市 金寨路96号 No.96 JinZhai Road Baohe District Hefei, Anhui 230026, CN
Inventors:
刘世勇 LIU, Shiyong; CN
刘固寰 LIU, Guhuan; CN
姜琰琰 JIANG, Yanyan; CN
Agent:
北京集佳知识产权代理有限公司 UNITALEN ATTORNEYS AT LAW; 中国北京市 朝阳区建国门外大街22号赛特广场7层 7th Floor, Scitech Place No.22, Jian Guo Men Wai Ave. Chao Yang District Beijing 100004, CN
Priority Data:
201710316952.808.05.2017CN
201710317186.708.05.2017CN
201710317704.508.05.2017CN
Title (EN) CONJUGATE AND BLOCK COPOLYMER CONTAINING FLUORESCENT CHROMOPHORE AND PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) CONJUGUÉ ET COPOLYMÈRE SÉQUENCÉ CONTENANT UN CHROMOPHORE FLUORESCENT, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 含荧光发色团的缀合物、嵌段共聚物及其制备方法和应用
Abstract:
(EN) Provided is a conjugate containing a fluorescent chromophore, which has any structure selected from C1 to C3. The conjugate containing the fluorescent chromophore provided by the present invention comprises one fluorescent chromophore and two highly reactive groups R1 and R2 linked to the fluorescent chromophore by a covalent bond. The fluorescent chromophore in the conjugate initially has no or only weak fluorescence emission capability, and only after the two highly reactive groups react together with the corresponding molecule, the fluorescent chromophore has strong fluorescence emission. Therefore, the efficiency of conjugation of drug molecules to targeting molecules can be monitored in situ by the infrared fluorescence emission intensity and applied to the target-mediated drug delivery.
(FR) L'invention concerne un conjugué contenant un chromophore fluorescent, qui a une structure quelconque choisie parmi C1 à C3. Le conjugué contenant le chromophore fluorescent fourni par la présente invention comprend un chromophore fluorescent et deux groupes hautement réactifs R1 et R2 liés au chromophore fluorescent par une liaison covalente. Le chromophore fluorescent contenu dans le conjugué ne possède initialement pas, ou a seulement une faible capacité d'émission de fluorescence, et seulement après que les deux groupes hautement réactifs réagissent ensemble avec la molécule correspondante, le chromophore fluorescent a une forte émission de fluorescence. Par conséquent, l'efficacité de conjugaison de molécules médicamenteuses à des molécules de ciblage peut être surveillée in situ par l'intensité d'émission de fluorescence infrarouge et appliquée à l'administration de médicament à médiation par cible.
(ZH) 本发明提供了一种含荧光发色团的缀合物,具有C1~C3任一结构。本发明提供的上述含荧光发色团的缀合物,包含一个荧光发色团和通过共价键连接在荧光发色团上的两个高反应活性基团R1与R2,所述缀合物中的荧光发色团初始不具有或者仅具有弱的荧光发射能力,仅当两个高反应活性基团共同与相应分子反应后,荧光发色团才具有强的荧光发射,因此可以通过红外荧光发射强度原位监控药物分子与靶向分子缀合效率,并应用于靶向介导的药物传输。
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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, 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)