Chemical conjugates of Evans Blue derivatives and their use as radiotherapy and imaging agents for targeting prostate cancer
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsXiaoyuan Chen, Orit Jacobson Weiss
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Abstract
A compound of Formula I or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions of R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a group capable of binding to prostate-specific membrane antigen (PSMA).
Claims20
A compound of Formula I or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt,
- wherein:
- R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are independently selected from hydrogen, halogen, hydroxyl, cyano, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl, and C1-C6haloalkoxy;
- R12 is hydrogen, C1-C6alkyl, or C1-C6haloalkyl;
- L1 is —(CH2)m— wherein m is an integer from 0 to 12, wherein each CH2 is individually replaced with —O—, —NH(CO)—, or —(CO)—NH—, provided that no two adjacent CH2 groups are replaced;
- L2 is —(CH2)n— wherein n is an integer from 0 to 12, wherein each CH2 is individually replaced with —O—, —NH(CO)—, or —(CO)—NH—, provided that no two adjacent CH2 groups are replaced;
- L3 is —(CH2)p— wherein p is an integer from 0 to 12, wherein each CH2 is individually replaced with —O—, —NH(CO)—, or —(CO)—NH—, provided that no two adjacent CH2 groups are replaced;
- and
- L4 is a C1-C60 linking group, optionally including —O—, —S—, —S(O)—, —S(O)2—, —N(R)—, —C(═O)—, —C(═O)O—, —OC(═O)—, —N(R)C(═O)—, —C(═O)N(R)—, —OC(═O)O—, —N(R)C(═O)O—, or —OC(═O)N(R)—, wherein each R is H or C1-C6 alkyl;
- R13 is a chelating group;
- and
- R14 is a group capable of binding to prostate-specific membrane antigen (PSMA).
Dependencies are inferred from the claim text.