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1. (WO2019047846) DERIVATIVES OF HYPOCRELLIN WITH PERI-POSITION AND 2-POSITION SIMULTANEOUSLY SUBSTITUTED BY AMINO GROUPS
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Pub. No.: WO/2019/047846 International Application No.: PCT/CN2018/104124
Publication Date: 14.03.2019 International Filing Date: 05.09.2018
IPC:
C07C 221/00 (2006.01) ,C07C 225/32 (2006.01) ,C07C 249/02 (2006.01) ,C07C 251/24 (2006.01) ,A61K 41/00 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
221
Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
225
Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a -CHO group, e.g. amino ketones
24
the carbon skeleton containing carbon atoms of quinone rings
26
having amino groups bound to carbon atoms of quinone rings or of condensed ring systems containing quinone rings
32
of condensed quinone ring systems formed by at least three rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
249
Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton
02
of compounds containing imino groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
251
Compounds containing nitrogen atoms doubly- bound to a carbon skeleton
02
containing imino groups
24
having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
41
Medicinal preparations obtained by treating materials with wave energy or particle radiation
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
中国科学院理化技术研究所 TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY OF THE CHINESE ACADEMY OF SCIENCES [CN/CN]; 中国北京市 海淀区中关村东路29号 29 Zhongguancun East Road, Haidian District Beijing 100190, CN
Inventors:
汪鹏飞 WANG, Pengfei; CN
吴加胜 WU, Jiasheng; CN
刘卫敏 LIU, Weimin; CN
郑秀丽 ZHENG, Xiuli; CN
顾瑛 GU, Ying; CN
Agent:
北京正理专利代理有限公司 BEIJING JANLEA PATENT AGENCY CO., LTD.; 中国北京市 西城区车公庄大街甲4号物华大厦A座1503室 Room 1503, 15th Floor, Tower A, Wuhua Mansion, A4 Chegongzhuang Avenue Xicheng District Beijing 100044, CN
Priority Data:
201710794566.X06.09.2017CN
201811020381.403.09.2018CN
Title (EN) DERIVATIVES OF HYPOCRELLIN WITH PERI-POSITION AND 2-POSITION SIMULTANEOUSLY SUBSTITUTED BY AMINO GROUPS
(FR) DÉRIVÉS D'HYPOCRELLINE AYANT UNE PÉRI-POSITION ET UNE POSITION 2 SIMULTANÉMENT SUBSTITUÉS PAR DES GROUPES AMINO
(ZH) 一种竹红菌素迫位和2-位同时氨基取代的衍生物及其制备方法和应用
Abstract:
(EN) Derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups and a preparation method and application thereof are disclosed. The structural formula of the derivatives is as shown in the formulae I-a to I-d. The prepared derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups have a maximum absorption wavelength of 600-650nm, and a molar extinction coefficient of about 20000-40000M -1cm -1. Compared with unmodified hypocrellin or hypocrellin only modified at 2-position, the prepared derivatives of hypocrellin have a significantly red-shifted absorption spectrum and a greatly enhanced molar extinction coefficient, and can efficiently produce reactive oxygen species such as singlet oxygen under a photosensitive condition. Under the same condition, the derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups act as photosensitizers, and have higher photodynamic inactivation of tumor cells than the first and second generations of commercial photosensitizers.
(FR) L'invention concerne des dérivés d'hypocrelline ayant une péri-position et une position 2 simultanément substitués par des groupes amino, ainsi qu'un procédé de préparation et une application de ceux-ci. La formule structurale des dérivés est telle que représentée par les formules I-a à I-d. Les dérivés préparés de l'hypocrelline ayant une péri-position et une position 2 simultanément substitués par des groupes amino ont une longueur d'onde d'absorption maximale de 600 à 650 nm, et un coefficient d'extinction molaire d'environ 20000 à 40000 M-1cm -1. Par comparaison avec l'hypocrelline non modifiée ou l'hypocrelline modifiée uniquement à la position 2, les dérivés préparés d'hypocrelline ont un spectre d'absorption significativement décalé vers le rouge et un coefficient d'extinction molaire amélioré de manière considérable, et peuvent produire efficacement des espèces réactives de l'oxygène telles que l'oxygène singulet dans une condition photosensible. Les dérivés d'hypocrelline ayant une péri-position et une position 2 simultanément substitués par des groupes amino agissent, dans la même condition, en tant que photosensibilisateurs, et ont une inactivation photodynamique plus élevée des cellules tumorales que les première et seconde générations des photosensibilisateurs de type commercial.
(ZH) 公开了一种竹红菌素迫位和2-位同时氨基取代的衍生物及其制备方法和应用。该衍生物的结构通式如式I-a~I-d所示。所制备的竹红菌素的迫位和2-位两个位置同时氨基取代的衍生物,其最大吸收波长在600-650nm,摩尔消光系数可达到20000-40000M -1cm -1左右。与未修饰的竹红菌素或仅2-位修饰的竹红菌素相比较,其吸收光谱显著红移且摩尔消光系数大大增强,光敏条件下能高效产生单重态氧等活性氧物种。相同条件下,竹红菌素的迫位和2-位同时氨基取代的衍生物作为光敏剂,比第一代和第二代商用光敏剂具有更高的光动力灭活肿瘤细胞的能力。
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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)