Back to results
US 2023/0416199 A1Published application
Inhibitors of amino acid transport
AssigneesIcahn School of Medicine at Mount Sinai, The Research Foundation for The State University of New York
InventorsChristof GREWER, Avner SCHLESSINGER, Elias NDARU, Yueyue SHI, Laura Jane ZIELEWICZ
Life of this patent
Estimating the term…
Abstract
Disclosed herein are compounds and compositions of formula I that are inhibitors of amino acid transport, specifically alanine serine cysteine transporter 2 (ASCT2): These compounds are useful as therapeutic agents for treating various cancers. Methods for inhibiting an ASCT2 transporter are also disclosed. Certain compounds are selective for an ASCT transporter.
Claims25
A compound of formula I:
- wherein:
- A is selected from:
- R1a is selected from —H and —(C1-C6)alkyl;
- R1b is selected from —H, —OH, —CON(H)2, and —NHC(═O)(H);
- R1c is —(CH2)pOH—;
- L1 is selected from —(CHR2)nOR3—, —R3O(CHR2)n—, —(CH2)mN(R4)R3—, and —R3(R4)N(CH2)m—;
- m is selected independently in each instance from 0 and 1;
- n is selected from 0, 1, and 2;
- p is selected from 0, 1, 2, and 3;
- R2 is selected independently in each instance from —H, —(CH2)mOH, and —CH3;
- R3 is selected from —C(═O)— and —CH2—;
- R4 is selected independently in each instance from —H and —(C1-C6)alkyl;
- L2 is selected from a direct bond, —C(═O)—, —CH(OH)—, —NH(C═O)—, —(C═O)NH—, and —(CH2)mO—(CH2)m—, or is absent when is absent;
- an aryl or heteroaryl moiety, optionally substituted with one or more substituents R5;
- is an aryl or heteroaryl ring, optionally substituted with one or more substituents R5, or is absent when is a bicyclic or polycyclic moiety;
- and
- R5 is selected independently in each instance from hydrogen, (C1-C6)alkyl, halogen, halo(C1-C6)alkyl, nitro, —OH, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, (C1-C6)alkylthio, halo(C1-C6)alkylthio, and amino;
- with the proviso that both of R1c and L1 are not connected to A by an oxygen or a nitrogen atom;
- and
- with the proviso that the following compounds are excluded:
17 more elements
(canceled)
(canceled)
11-12. (canceled)
(canceled)
(canceled)
Dependencies are inferred from the claim text.