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1. (WO2019024339) PHOTOSENSITIZER AND DERIVATIVES AND APPLICATION THEREOF
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Pub. No.: WO/2019/024339 International Application No.: PCT/CN2017/112765
Publication Date: 07.02.2019 International Filing Date: 24.11.2017
IPC:
C07D 279/36 (2006.01) ,C07D 293/12 (2006.01) ,C07D 417/14 (2006.01) ,C07D 417/12 (2006.01) ,A61K 31/5415 (2006.01) ,A61K 31/395 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
279
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
10
1,4-Thiazines; Hydrogenated 1,4-thiazines
14
condensed with carbocyclic rings or ring systems
36
[b, e]-condensed, at least one with a further condensed benzene ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
293
Heterocyclic compounds containing rings having nitrogen and selenium or nitrogen and tellurium, with or without oxygen or sulfur atoms, as the ring hetero atoms
10
condensed with carbocyclic rings or ring systems
12
Selenazoles; Hydrogenated selenazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
5415
ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
大连理工大学 DALIAN UNIVERSITY OF TECHNOLOGY [CN/CN]; 中国辽宁省大连市 凌工路2号 No.2 Linggong Road Dalian, Liaoning 116024, CN
大连科荣生物技术有限公司 DALIAN CHROMAS BIOSCIENCE CO., LTD [CN/CN]; 中国辽宁省大连市 火炬路43号 No.43 Huoju Road Dalian, Liaoning 116024, CN
Inventors:
彭孝军 PENG, Xiaojun; CN
李明乐 LI, Mingle; CN
樊江莉 FAN, Jiangli; CN
姚起超 YAO, Qichao; CN
杜健军 DU, Jianjun; CN
龙飒然 LONG, Saran; CN
王静云 WANG, Jingyun; CN
Agent:
大连格智知识产权代理有限公司 DALIAN GEZHI INTELLECTUAL PROPERTY AGENT LTD.; 中国辽宁省大连市 长白街2号208室 Room 208 No.2 Changbai Street Dalian, Liaoning 116012, CN
Priority Data:
201710660846.104.08.2017CN
Title (EN) PHOTOSENSITIZER AND DERIVATIVES AND APPLICATION THEREOF
(FR) PHOTOSENSIBILISATEUR, DÉRIVÉS ET APPLICATION CORRESPONDANTE
(ZH) 一类光敏剂及其衍生物和应用
Abstract:
(EN) A photosensitizer and derivatives and an application thereof. The photosensitizer has the structure of general formula I, X is S or Se, Y is an organic or inorganic ion, R1 and R2 are respectively independently selected from H, alkyl, alkoxy, amido, alkyl azido and the like, R3 is selected from H, alkyl, alkoxy, amino, sulfonyl, hydroxyl, carboxyl and the like, and L1 is a linker selected from -(CH2)n1- or -(CH2CH2O)n2-; the derivatives are molecular medicines connected to an anti-cancer chemotherapy medicine molecule on the photosensitizer or having a tumor targeted function. The photosensitizer has excellent near infrared characteristic and low dark toxicity and is used for the field of photodynamic tumor treatment. The derivatives introduce the molecules having the tumor targeted function to a phenothiazide or phenoselazine structure, and the specific uptake of tumor tissues to the photosensitizer can be improved; or a clinic anti-cancer medicine is introduced into the phenothiazide or phenoselazine structure, so that the purpose of photodynamic therapy and chemotherapy synergy treatment can be achieved.
(FR) La présente invention concerne un photosensibilisateur, des dérivés et une application correspondante. Le photosensibilisateur selon l'invention est représenté par la structure de formule générale I, X représente S ou Se, Y représente un ion organique ou inorganique, R1 et R2 sont respectivement indépendamment choisis parmi H, alkyle, alcoxy, amido, alkyle azido et analogues, R3 est choisi parmi H, alkyle, alcoxy, amino, sulfonyle, hydroxyle, carboxyle et analogues, et L1 est un lieur choisi parmi -(CH2)n1- ou -(CH2CH2O)n2- ; les dérivés sont des médicaments moléculaires reliés à une molécule médicamenteuse de chimiothérapie anticancéreuse sur le photosensibilisateur ou ayant une fonction ciblant des tumeurs. Le photosensibilisateur présente une excellente caractéristique proche infrarouge et une faible toxicité en obscurité et peut être utilisé dans le domaine du traitement photodynamique de tumeurs. Les dérivés introduisent les molécules ayant la fonction ciblant des tumeurs à une structure phénothiazide ou phénoselazine, et l'absorption spécifique de tissus tumoraux au photosensibilisateur peut être améliorée ; ou un médicament anticancéreux clinique est introduit dans la structure de phénothiazide ou de phénoselazine, de sorte que l'objectif de thérapie photodynamique et de traitement de synergie chimio-thérapeutique peut être obtenu.
(ZH) 一类光敏剂及衍生物、应用,所述光敏剂具有通式I的结构,X为S或Se,Y为有机或无机离子,R 1和R 2各自独立地选自H、烷基、烷氧基、酰胺基、烷基叠氮基等,R 3选自H、烷基、烷氧基、氨基、磺酰基、羟基和羧基等;L 1为连接链,选自-(CH 2n1-或-(CH 2CH 2O) n2-。所述衍生物是在上述光敏剂上连接抗癌化疗药物分子或具有肿瘤靶向功能的分子药物。所述光敏剂具有优异的近红外特性,暗毒性低,用于光动力肿瘤治疗领域。所述衍生物引入具有肿瘤靶向功能的分子到苯并吩噻嗪或者苯并吩硒嗪结构上,可以提高肿瘤组织对光敏剂的特异性摄取;或者将临床用抗癌药物引入苯并吩噻嗪或者苯并吩硒嗪结构,可以达到光动力治疗和化疗协同治疗的目的。
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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)