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КОНЪЮГАТ, СОДЕРЖАЩИЙ ЛИГАНД РЕЦЕПТОРОВ НЕЙРОТЕНЗИНА, И ЕГО ПРИМЕНЕНИЕ
专利权人:
3Б ФАРМАСЬЮТИКАЛЗ ГМБХ (DE)
发明人:
ОСТЕРКАМП Франк (DE),ХААЗЕ Кристиан (DE),РАЙНЕКЕ Ульрих (DE),СМЕРЛИНГ Кристиане (DE),ПАШКЕ Маттиас (DE),УНГЕВИСС Ян (DE)
申请号:
RU2016151310
公开号:
RU2016151310A
申请日:
2015.06.10
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
The present invention is related to a conjugate comprising a structure of general formula (1) [TM1] - [AD1] - [LM] - [AD2] - [TM2] (1), wherein TM1 is a first targeting moiety, wherein the first targeting moiety is capable of binding to a first target, AD1 is a first adapter moiety or is absent, LM is a linker moiety or is absent, AD2 is a second adapter moiety or is absent, and TM2 is a second targeting moiety, wherein the second targeting moiety is capable of binding to a second target wherein the first targeting moiety and/or the second targeting moiety is a compound of formula (2): wherein R1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl AA-COOH is an amino acid selected from the group consisting of 2-amino-2 adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9 carboxylic acid R2 is selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3C8)cycloalkylmethyl, halogen, nitro and trifluoromethyl ALK is (C2-C5)alkylidene R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and (C1-C4)alkyl under the proviso that one of R3, R4 and R5 is of the following formula (3) wherein ALK is (C2-C5)alkylidene R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl and R7 is a bond or a pharmacologically acceptable salt, solvate or hydrate thereof.
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