Back to results
US 8,926,944 B2Granted
Radiolabeled prostate specific membrane antigen inhibitors
AssigneeMolecular Insight Pharmaceuticals, Inc.
InventorsJohn W. Babich, Craig Zimmerman, John L. Joyal, Genliang Lu
Life of this patent
Estimating the term…
Abstract
Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: The invention also provides pharmaceutical compositions of a complex of a radionuclide and a Formula I compound or a Formula II compound and methods of using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.
Claims7
A compound represented by formula II
- wherein:
- X and Y are each independently (CHR1)m or C(O);
- W is H, ═O—(CHR1)m—(CH2)p—, or —(CH2)p—U;
- represents a single or a double bond;
- L is —C(O)—(C1-C10)alkylene, —[C(O)—(CH(Z)d)—NH];
- NR2R3, —C(O)—(CHR1)—(CH2)p—U—, —(C5-C14)aryl-(C1-C10)alkylene, R7-benzyl, —(C5-C14)heteroaryl-(C1-C10)alkylene, —C(O)—[(CH2)p—V]n—(CH2)q—C(O)—U, [C(O)—CH(Z)d—NH]t—C(O)—(CHR1)m—(CH2)p—[U]r, —C(S)—NH-benzylene, —C(O)—NH-benzylene, —[C(O)—(CH(Z)d)—NH]s-benzylene-, or —(C1-C10)alkylene-NR4R5;
- T is selected from the group consisting of:
- H, —(C1-C10)alkylene, RC(O)—(C1-C10)alkylene, NR2R3—(C1-C10)alkylene, —(C5-C14)heteroaryl-(C1-C10)alkylene, —(C5-C14)aryl-(C1-C10)alkylene and R6—(C5-C14)heteroarylene-(C1-C10)alkylene;
- U is selected from the group consisting of:
- —OR, —COR, —(C5-C14)arylene and —NR4R);
- V is selected from the group consisting of:
- —NH—, —NR2— and —NR2R3;
- Z is —(CH2)p—COOH, —(CH2)p—(C5-C14)aryl, or —(CH2)p—NR2R3;
- R, Ra and Rb are each independently —H, —OH, —(C1-C10)alkyl, —O(C1-C10)alkyl, —NHR2, or —NR2R3;
- R1 and R′″ are each independently —H, —NH2, or —(CH2)p—U;
- R2, R3, R4, R5 and R6 are each independently H, bond, (C1-C10)alkylene, F, Cl, Br, I, C(O), C(S), —C(S)—NH-benzyl-, —C(O)—NH-benzyl-, —C(O)—(C1-C10)alkylene, —(CH2)v—NR4, —(CH2)p—NH—C(O)—(CH2)p—, —(CH2—CH2)t—NH—C(O)—(CH2)p—, —(CH2)p—COR, —(CH2)p—C(O)NH—C[(CH2)p—COR]3, —C[(CH2)p—COR]3, or —(CH2)p—(C5-C14)heteroaryl;
- R7 is —O(CH2)p—(C5-C14)heteroaryl-(CH2)p—U;
- D is
- and
- d, j, k, m, n, p, q, r, s, t and v are each independently 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- with the proviso that where W is —(CH2)5— or —CH(NH2)—(CH2)4—, then L is not —C(O)CH2—.
18 more elements
Dependencies are inferred from the claim text.