11-02-2016 дата публикации
Номер: US20160038615A1
Принадлежит:
This invention relates to compounds comprising a saccharide conjugated to an imaging agent or a reporter group, compositions comprising them and methods of using them. Specifically BLM-disaccharide and BLM-monosaccharide conjugates containing different linker groups and an imaging agent or a reporter group are provided for the targeting and imaging of tumors. 3. (canceled)4. The compound according to claim 1 , wherein the first linker is X-(L-Y)-L-Z claim 1 ,{'sub': '2', 'wherein X is CHor O;'}{'sup': '1', 'sub': 2', '6, 'Lis C-Calkyl;'}{'sup': y', 'y, 'sub': 1', '6, 'Y is O, S, or NR, wherein Ris hydrogen or C-Calkyl;'}m is an integer selected from 1 to 10;{'sup': '2', 'sub': 1', '20', '2', '20', '2', '20', '3', '5, 'Lis C-Calkyl, C-Calkenyl, C-Calkynyl, aryl, heteroaryl, heterocyclyl, C-Ccycloalkyl; and'}{'sup': x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x, 'sub': 2', '2', '2', '2, 'Z is absent, O, NR, S, C(O), S(O), S(O), OC(O), N(R)C(O), N(R)S(O), N(R)S(O), C(O)O, C(O)N(R), S(O)N(R), S(O)N(R), OC(O)O, OC(O)N(R), N(R)C(O)O, N(R)C(O)N(R), or N(R)S(O)N(R), wherein'}{'sup': 'x', 'sub': 1', '6, 'each Ris independently hydrogen or C-Calkyl.'}5. (canceled)6. The compound of claim 4 , wherein the first linker is O—(CHCH—O)—CHCH—Z claim 4 , wherein Z is O claim 4 , N(H) claim 4 , or S and m is an integer selected from 1 to 20 or the first linker is O—(CHCH—O)—CHCH—Z claim 4 , wherein Z is C(O) or S(O)and m is an integer selected from 1 to 20.7. (canceled)8. The compound according to claim 1 , wherein the second linker is (B-L)-D-E-L-F claim 1 ,{'sup': x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x', 'x, 'sub': 2', '2', '2', '2, 'wherein B is bond, O, NR, S, C(O), S(O), S(O), OC(O), N(R)C(O), N(R)S(O), N(R)S(O), C(O)O, C(O)N(R), S(O)N(R), S(O)N(R), OC(O)O, OC(O)N(R), N(R)C(O)O, N(R)C(O)N(R), or N(R)S(O)N(R);'}{'sup': '3', 'sub': 2', '6, 'Lis C-Calkyl;'}p is 2 or 3;D is CH when p is 2 and D is C when p is 3;{'sup': x', 'x', 'x', 'x', 'x', 'x', '2 ...
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