Back to results
US 8,168,786 B2Granted
Radiolabeled compounds and uses thereof
AssigneeThe Trustees of Columbia University in the City of New York
InventorsJoseph John Mann, J. S. Dileep Kumar
Life of this patent
Estimating the term…
Abstract
The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
Claims37
A compound having the formula:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- r and s are each independently an integer ranging from 0 to 6;
- R1 is —H, -aryl, —C1-C6 alkyl, —C3-C7 cycloalkyl, —C3-C7 cycloalkenyl, or -3- to 7-membered heterocycle;
- R2 is —H, -aryl, —C1-C6 alkyl, —C3-C7 cycloalkyl, —C3-C7 cycloalkenyl, -3- to 7-membered heterocycle, -halo, —CF3, —C2-C6 alkenyl, —C2-C6 alkynyl, —N(R4)2, —CN, —OR4 or —SR4;
- R3 is -aryl or -5- to 7-membered aromatic heterocycle, each of which is substituted with one R6 group and optionally substituted with one or more of the following groups:
- —C1-C6 alkyl, —C3-C7 cycloalkyl, —C3-C7 cycloalkenyl or -3- to 7-membered heterocycle, -halo, —CF3, —C2-C6 alkenyl, —C2-C6 alkynyl, —(C1-C6 alkylene)-aryl, —N(R4)2, —CN, —OR4, —SR4, —S(O)—R4, —SO2—R4, —SO2NH—R4, —SO3H, —NH—SO2—R4, —C(O)R5 or —NHC(O)R5;
- each occurrence of R4 is independently —H, —C1-C6 alkyl, —C2-C6 alkenyl, —C2-C6 alkynyl, -aryl, —(C1-C6 alkylene)-aryl, —C3-C7 cycloalkyl, —C3-C7 cycloalkenyl or -3- to 7-membered heterocycle;
- R5 is —R4, —N(R4)2 or —OR4;
- R6 is -M-Q, —O-M-Q, —S-M-Q, —NH-M-Q, —F, —18F, —18F-labeled CF3, —CF2H, —18F-labeled CF2H, or —11C-labeled CN;
- M is —11C-labeled C1-C6 alkylene-, —11C-labeled C2-C6 alkenylene-, —11C-labeled C2-C6 alkynylene-, —18F-labeled C1-C6 alkylene-, —18F-labeled C2-C6 alkenylene-, or —18F-labeled C2-C6 alkynylene-;
- Q is —H or -aryl.
9 more elements
Dependencies are inferred from the claim text.