发明名称 FOLATE CONJUGATES OF ALBUMIN-BINDING ENTITIES
摘要 The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.
申请公布号 US2014234216(A1) 申请公布日期 2014.08.21
申请号 US201214238954 申请日期 2012.08.10
申请人 Schibli Roger;Moser Rudolf;Muller Cristina Magdalena;Struthers Harriet;Groehn Viola;Ametamey Simon Mensah;Fischer Cindy Ramona 发明人 Schibli Roger;Moser Rudolf;Muller Cristina Magdalena;Struthers Harriet;Groehn Viola;Ametamey Simon Mensah;Fischer Cindy Ramona
分类号 A61K51/04;G01N33/569 主分类号 A61K51/04
代理机构 代理人
主权项 1. Compounds of formula I,wherein Z is a pteroate or derivative thereof, L1,L4 are independently of each other a covalent bond or a straight-chain or branched C(1-8)alkyl, which is unsubstituted or substituted by at least one CN, Hal, OR′, NHR′, CO2R′ or NO2, wherein R′ represents H or C(1-8)alkyl, L2 is a covalent bond or a linking group, such as straight-chain or branched C(1-8)alkyl, which is unsubstituted or substituted by at least one OR′, NHR′, or CO2R′, and wherein one or more of the non-adjacent CH2 groups may independently be replaced by a group selected from —O—, —CO—, —CO—O—, —O—CO—, —NR′—, —NR′—CO—, —CO—NR′, wherein R′ represents H or C(1-8)alkyl, L3 is a covalent bond or a linking group, such as straight-chain or branched C(1-8)alkyl, which is unsubstituted or substituted by at least one CN, Hal, OR′, NHR′, CO2R′ or NO2, and wherein one or more of the non-adjacent CH2 groups may independently be replaced by a group selected from —O—, —CO—, —CO—O—, —O—CO—, —NR′—, —NR′—CO—, —CO—NR′—, —NR′—CO—O—, —O—CO—NR′—, —NR′—CO—NR′—, —CH═CH—, —C≡C—, —O—CO—O—, —S—R′—, —SO3R′—, and a five-membered azaheterocycle, wherein R′ represents H or C(1-8)alkyl, Y1,Y3 are independently of each other O, N or S, A1, A2, A3 are independently of each other H, a capping group, or an albumin binder, M is a radionuclide-based therapeutic or diagnostic moiety, m1, m2 are independently of each other 0, 1, 2 or 3,with the proviso that at least one, preferably one, of A1, A2 and A3 is an albumin binder.
地址 Baden CH