| 主权项 |
1. A compound according to the formula, an epimer thereof, or a pharmaceutically acceptable salt thereof, wherein each RA is independently hydrogen, —OR1, —N(H)(R1), or —R4, wherein each R1 is independently hydrogen, a protecting group, —R3, —R4, or —R5a, wherein
R5a is each RB is independently hydrogen, —OR2, —N(H)(R2), or —R4, wherein each R2 is independently hydrogen, a protecting group, —R3, —R4, or —R5b, wherein
R5b is R3 is —C(O)OR30, —C(O)N(H)(R30), —S(O)OR30, —S(O)2OR30, —S(O)N(H)(R30), —S(O)2N(H)(R30), or —P(O)(OR30)2, wherein
R30 is hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or heterocyclyl, wherein R30 is optionally substituted with one to four groups which are each independently C1-C6 alkyl, cyano, nitro,
halogen, —OR31, —N(R31)2, —SR31, —C(O)R31, —C(O)OR31, —C(O)N(R31)2, —OC(O)OR31, —OC(O)N (R31)2, —N(R31)C(O)OR31, —N(R31)C(O)N(R31)2, —S(O)R31, —S(O)2R31, —S(O)N(R31)2,or —S(O)2N(R31)2, wherein each R31 is independently hydrogen or C1-C6 alkyl; each R4 is independently -L-(R40)q, wherein
each q is independently one or greater;each L is independently —C1-C20 alkyl-, —C2-C20 alkenyl-, —C2-C20 alkynyl-, -aryl-, -heteroaryl-, -heterocyclyl-, —C3-C8 cycloalkyl-, an oligoalkylene glycol, an oligopeptide, a dendrimer, or -(L1-Y)n-L2-X—,wherein Y is —O—, —S—, or —N(RY)—, wherein RY is hydrogen or C1-C6 alkyl; n is an integer selected from 1 to 250; L1 is —C2-C6 alkyl-; L2 is —C1-C20 alkyl-, —C2-C20 alkenyl-, —C2-C20 alkynyl-, -aryl-, -heteroaryl-, -heterocyclyl-, —C3-C8 cycloalkyl-; and X is a bond, —O—, —N(RX), —S—, —C(O)—, —S(O)—, —S(O)2—, —OC(O)—, —N(RX)C(O)—,
—N(RX)S(O)—, —N(RX)S(O)2—, —C(O)O—, —C(O)N(RX)—, —S(O)N(RX)—, —S(O)2N(RX)—, —OC(O)O—, —OC(O)N(RX)—, —N(RX)C(O)O—, —N(RX)C(O)N(RX)—, or —N(RX)S(O)2N(RX)—, wherein each RX is independently hydrogen or C1-C6 alkyl, provided that when L is a bond, then q is 1; andeach R40 is independently an imaging agent, a member of a specific binding pair, a chemotherapeutic agent, or —R41, wherein
R41 is —OH, —NH(R42), —SH, —C(O)H, —C(O)OR42, —C(O)NH(R42), —OC(O)OR42, —OC(O)N(R42)2, —N(R42)C(O)OR42, —N(R42)C(O)N(R42)2, —S(O)N(R42)2, or —S(O)2N(R42)2, wherein each R42 is independently hydrogen, C1-C6 alkyl, or benzyl; and provided that
(i) no more than one R1 is R5a and no more than one R2 is R5b;(ii) when one R1 group is R5a, then R2 is not R5b; and when one R2 group is R5b, then R1 is not R5a;(iii) no more than one R3 group is present;(iv) at least one R4 is present;(v) no more than one RA, and no more than one RB comprises R4;(vi) no more than two RA groups and no more than two RB groups are hydrogen;(vii) R40 is not (a) R41 when L is a bond; and (b) bleomycin; and(viii) the compound of formula (I) or (I′) is not bleomycin. |
