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CONJUGATE CONTAINING FOLIC ACID AND INDOLE-3-CARBINOL FOR MEDICAL USE
专利权人:
DOM TERRY INTERNATIONAL S.R.L.
发明人:
TERENZIO Domenico (IT),ТЕРЕНЦИО Доменико (IT),RASTRELLI Luca (IT),РАСТРЕЛЛИ Лука (IT)
申请号:
RU2016119036
公开号:
RU0002692078C2
申请日:
2014.11.19
申请国别(地区):
RU
年份:
2019
代理人:
摘要:
FIELD: pharmaceuticals.SUBSTANCE: invention relates to a compound of general formula Bx-(S)y-L-(S')z-Dn (I), in which B is a substance selected from vitamins, peptides, tumor-specific peptides, tumor cells-specific aptamers, tumor cells-specific carbohydrates, monoclonal or polyclonal antibodies, antibody fragments, proteins expressed on metastatic tumor cells; x is 0, 1 or 2; S is lysine or is a bifunctional carrier; y equals 0, or 1, or 2; L is a carrier – polyethylene glycol; S' is a bifunctional carrier selected from L-2-amino-adipic acid (AD) and β-glutamine acid (β – Glu); z is 0, or 1, or 2; D is indole-3-carbinol (I3C), wherein said compound is selected from: B-Lys-PEG-I3C, B-Lys-PEG-AD-(I3C)2, B-Lys-PEG-βGLU-(I3C)2, F-PEG-I3C, F-PEG-AD-(I3C)2, F-PEG-βGLU-(I3C)2, F-Lys-PEG-I3C, F-Lys-PEG-AD-(I3C)2, F-Lys-PEG-βGLU-(I3C)2, F2-AD-PEG-I3C, F2-AD-PEG-βGLU-(I3C)2, F2-AD-PEG-AD-(I3C)2, wherein F is folic acid; Lys is lysine; PEG is polyethylene glycol or monomethoxy-polyethylene glycol (mPEG), homobifunctional or heterobifunctional; AD is L-2-amino-adipic acid, β-GLU is β-glutamic acid and I3C is indole-3-carbinol (BC). Invention also relates to versions of a method of producing a compound, to the use of said compound, to pharmaceutical or nutraceutical preparations, to a method of treating or preventing a tumor, to a method of treating or preventing an inflammatory disease.EFFECT: proposed compound has anti-tumor activity, more selective, less toxic and is characterized by improved pharmacological properties.21 cl, 2 tbl, 8 exИзобретение относится к соединению с общей формулой , в котором В представляет собой вещество, выбранное из витаминов, пептидов, опухоль-специфических пептидов, опухолевые клетки-специфических аптамеров, опухолевые клетки-специфических углеводов, моноклональных или поликлональных антител, фрагментов антител, белков, экспрессированных на метастатических опухолевых клетках; х равно 0, 1 или 2; S представляет собой лизин или является бифункциона
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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