ЛУБ Йохан (NL),ТЕН ХУВЕ Волтер (NL),РОССИН Раффаэлла (NL),ВАН ДЕН БОС Сандра Мартина (NL),РОБИЙАР Марк Стефан (NL)
申请号：
RU2013121799/15
公开号：
RU2013121799A
申请日:
2011.10.11
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. Set directed medical imaging and / or therapeutic agent, comprising at least one probe for pretargetinga and at least one effector probe wherein probe comprises pretargetinga primary targeting moiety and a first bio-orthogonal reactive group, and wherein the effector comprises a probe The effector moiety such as a label or pharmaceutically active compound, and a second bio-orthogonal reactive group, wherein one of the first and second bio-orthogonal reactive groups yavl etsya dienophile, and the other of the first and second bio-orthogonal reactive groups is a diene, a dienophile wherein dienophile to 8-membered ring, which corresponds to the formula (1) :( 1) wherein R position is equatorial and axial position Ryavlyaetsya, wherein each of X, Y, R and independently represents H, or no more than six cases, a substituent selected from the group consisting of alkyl, aryl, O-aryl, O-alkyl, S-aryl, S-alkyl, S (O) -aryl, S (O) -alkyl, S (O) -aryl, S (O) -alkyl, Si-aryl, Si-alkyl, Si-O-alkyl, OCO-alkyl, OCO-aryl, SCO-alkyl, SC O-aryl, OCS-alkyl, OCS-aryl, SCS-alkyl, SCS-aryl, F, Cl, Br, I, N, SOH, SOH, SOH, POH, OH, SH, NO, NO, CN, OCN, SCN, NCO, NCS, CF, NRR ", wherein each R and R" is independently H or alkyl, aryl, C (= O) O-alkyl, C (= O) O-aryl, C (= S) O-alkyl, C (= S) O-aryl, C (= O) S-alkyl, C (= O) S-aryl, C (= S) S-alkyl, C (= S) S-aryl, , C (= O) NRR ", wherein each R and R" independently is H, aryl or alkyl, NRCO-alkyl, wherein R is H, alkyl or aryl, NRCO-aryl, wherein R is H, alkyl or aryl, NRC (= O) O-alkyl, wherein R is H, alkyl or aryl, NRC (= O) O-aryl, wherein R is H , alkyl or aryl, OCONR-Alki
