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1. WO2019024339 - PHOTOSENSITIZER AND DERIVATIVES AND APPLICATION THEREOF

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Publication Number WO/2019/024339
Publication Date 07.02.2019
International Application No. PCT/CN2017/112765
International Filing Date 24.11.2017
IPC
C07D 279/36 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
279Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
101,4-Thiazines; Hydrogenated 1,4-thiazines
14condensed with carbocyclic rings or ring systems
36-condensed, at least one with a further condensed benzene ring
C07D 293/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
293Heterocyclic compounds containing rings having nitrogen and selenium or nitrogen and tellurium, with or without oxygen or sulfur atoms, as the ring hetero atoms
10condensed with carbocyclic rings or ring systems
12Selenazoles; Hydrogenated selenazoles
C07D 417/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic 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
14containing three or more hetero rings
C07D 417/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic 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
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61K 31/5415 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
5415ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/395 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
CPC
A61K 31/405
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
A61K 31/4188
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4188condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
A61K 31/5415
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
5415ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/55
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 41/0057
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
41Medicinal preparations obtained by treating materials with wave energy or particle radiation ; ; Therapies using these preparations
0057Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent
A61K 47/55
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
55the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
Applicants
  • 大连理工大学 DALIAN UNIVERSITY OF TECHNOLOGY [CN]/[CN]
  • 大连科荣生物技术有限公司 DALIAN CHROMAS BIOSCIENCE CO., LTD [CN]/[CN]
Inventors
  • 彭孝军 PENG, Xiaojun
  • 李明乐 LI, Mingle
  • 樊江莉 FAN, Jiangli
  • 姚起超 YAO, Qichao
  • 杜健军 DU, Jianjun
  • 龙飒然 LONG, Saran
  • 王静云 WANG, Jingyun
Agents
  • 大连格智知识产权代理有限公司 DALIAN GEZHI INTELLECTUAL PROPERTY AGENT LTD.
Priority Data
201710660846.104.08.2017CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
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
front page image
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 2） n1-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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