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2. 发明申请

WO2018167295A1 LIGANDS FOR INTEGRIN αvβ8, SYNTHESIS AND USES THEREOF 审中-公开
公开(公告)号：WO2018167295A1
公开(公告)日：2018-09-20
申请号：PCT/EP2018/056733
申请日：2018-03-16
申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN
发明人： KESSLER, Horst , KAPP, Tobias , REICHART, Florian , MALTSEV, Oleg
IPC分类号： C07K7/56 , G01N33/68 , C07K7/64 , A61K38/12 , A61K47/30
摘要： Disclosed are compounds represented by the following general formula (I): Cyclo-(Arg-Gly-Asp-X 1 -X 2 -X 3 -X 4 -X 5 ) (I) wherein the variables groups X 1 to X 5 have the following meanings X 1 : Leu, Ile, Nle, Val, Tyr, Phe; X 2 : D-amino acid such as D-Pro, N-Me-D-Phe; X 3 : Pro, N-Me-amino acid such as N-Me-Lys, N-Me-Lys(Ac); Pro-Rx3, N-Me-Lys-Rx4; X 4 : Gly, Ala, Ser, Thr; X 5 : Leu, Ala, Tyr, His, Ile, Nle, Val, Phe wherein Pro-Rx3 represents a proline residue that carries at the C-3, C-4 or C-5 carbon atom and preferably the C-4 carbon atom a functional group selected from –NH2, -OH, -NH-Ac, -NH-hexyne, and wherein Lys-R x4 represents a lysine residue, wherein the ω-amino nitrogen atom carries a group of the formula –L4-R4, wherein L4 is selected from the group consisting of covalent bond, -C(O)-, and -C(O)-O-,..., and wherein R4 is selected from the group consisting of –(CH2)n-C≡CH with n = 0, 1, 2, 3, 4, 5, 6, 7 or 8, or wherein the sub-sequence -X 2 -X 3 - represents a β-turn mimetic diffeωωring from the meanings above, or pharmaceutically acceptable salts, esters, solvates, polymorphs or modified forms thereof represented by the following general formula (II): (X 0 ) n1 L(X 8 ) n2 wherein X0 represents the compound of the general formula (I) as specified above (excluding one hydrogen atom to allow bonding to the linker), L represents a linker, X 8 represents the effector moiety and wherein n1 and n2 are each independently selected from the range of 1 to 5, preferably such that each of n1 and n2 represents 1, wherein n1+n2 represents the number of valencies of the linker and is preferably in the range of from 2 to 6, more preferably 2-5, with the proviso that each of n1 and n2 is at least 1, as well as uses therefore in therapy and imaging.

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