US 2026/0191999 A1Published application

Compounds and their use

AssigneeKing's College London

InventorsTimothy H. Witney, Muhammet Tanç

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Abstract

The present invention pertains generally to the field of diagnostic and therapeutic compounds. More specifically the present invention pertains to certain radiolabelled compounds, their precursors, and the respective uses. The radiolabelled compounds, inter alia, bind ALDH and emit radiation for detection by molecular imaging or for treatment of a disease mediated by ALDH.

Claims31

Dependent claims

A radiolabelled compound according to formula (I):

or a pharmaceutically acceptable salt, hydrate, or solvate thereof;
wherein:
—R4
—R4A and —R4B taken together with the carbon atom to which they are attached form a C3-5 cycloalkyl;
or —R4A and —R4B are each independently C1-3 alkyl;
—R4C is —H, —F, or —RX4C;
—R4D is phenyl, optionally substituted with:
a) one group —RX4D;
and/or
b) one or more —F;
-L1- is independently selected from —S(O)2— and —C(O)—;
—RL is independently selected from C1-6 alkyl and cyclopropyl;
—R6 is independently selected from —H, —F, —I, —RX6, and —NO2;
—R7 is independently selected from —H, —F, —I, —RX7, and —NO2;
—R8 is independently selected from —H, —F, —I, —RX8, and —NO2;
—RX4C is a radioisotope selected from 18F, 123I, 124I, 125I, 131I, and 211At;
—RX4D is a radioisotope selected from 18F, 123I, 124I, 125I, 131I, and 211At;
—RX6 is a radioisotope selected from 18F, 123I, 124I, 125I, 131I, and 211At;
—RX7 is a radioisotope selected from 18F, 123I, 124I, 125I, 131I, and 211At;
and
—RX8 is a radioisotope selected from 18F, 123I, 124I, 125I, 131I, and 211At;
wherein, the compound comprises only one group selected from —RX4C, —RX4D, —RX6, —RX7, and —RX8;
and at least one of —R6, —R7, and —R8 is —H.

20 more elements

A compound according to formula (Ia):

or a salt, hydrate, or solvate thereof;
wherein:
—R14 is
—R14A and —R14B taken together with the carbon atom to which they are attached form a C3-5 cycloalkyl;
or —R14A and —R14B are each independently C1-3 alkyl;
—R14C is —H, —F, or —RX14C;
—R14D is phenyl, optionally substituted with:
a) one group —RX14D;
and/or
b) one or more —F;
-L11- is independently selected from —S(O)2— and —C(O)—;
—R1L is independently selected from C1-6 alkyl and cyclopropyl;
—R16 is independently selected from —H, —F, —I, —RX16, and —NO2;
—R17 is independently selected from —H, —F, —I, —RX17, and —NO2;
—R18 is independently selected from —H, —F, —I, —RX18, and —NO2;
each of —RX14C, —RX14D, —RX16, —RX17, and —RX18 is, independently, a leaving group;
the compound comprises only one group selected from —RX14C, —RX14D, —RX16, —RX17, and —RX18;
and at least one of —R16, —R17, and —R18 is —H.

15 more elements

Dependencies are inferred from the claim text.

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Abstract