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US 12,599,583 B2Granted
Small molecule GRB2 stabilizers for Ras map kinase inhibition
AssigneesBoard of Regents, The University of Texas System, Board of Trustees of the University of Arkansas
InventorsZamal Ahmed, John A. Tainer, Darin E. Jones
Life of this patent
Estimating the term…
Abstract
The present disclosure compounds of the formula (I-A) or (I), wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods for the use of said compounds and/or pharmaceutical compositions, such as in the treatment of cancer. The present disclosure also provides methods for the use of compounds of the formula (III), wherein the variables are defined herein.
Claims16
A compound of the formula:
- wherein:
- n is 2, 3, 4, or 5;
- Xa is O or S;
- Ra is hydrogen;
- Rb and Rc are each independently hydrogen, alkyl(C≤12), or substituted alkyl(C≤12);
- and
- Rd is in each instance independently halo, hydroxy, cyano, nitro, alkyl(C≤12), substituted alkyl(C≤12), alkoxy(C≤12), or substituted alkoxy(C≤12);
- or
- a compound of the formula:
- wherein:
- R1 is hydrogen;
- or
- alkyl(C≤12), aralkyl(C≤12), heteroaralkyl(C≤12), or a substituted version of any of these groups;
- and
- R2 is aralkyl(C≤12), heteroaryl(C≤12), heteroaralkyl(C≤12), or a substituted version of any of these groups;
- or
- a group of the formula:
- wherein:
- R3 is hydrogen, hydroxy, halo, amino, nitro, cyano, carboxy, or mercapto;
- or
- alkyl(C≤12), alkoxy(C≤12), alkylamino(C≤12), dialkylamino(C≤12), acyl(C≤12), acyloxy(C≤12), amido(C≤12), or a substituted version of any of these groups;
- or
- —C(O)NR3aR3b, wherein:
- R3a and R3b are each independently hydrogen, alkyl(C≤12), or substituted alkyl(C≤12);
- R3′ is hydrogen, hydroxy, halo, amino, nitro, cyano, carboxy, or mercapto;
- or
- alkyl(C≤12), alkylamino(C≤12), dialkylamino(C≤12), acyl(C≤12), acyloxy(C≤12), amido(C≤12), or a substituted version of any of these groups;
- or
- —C(O)NR3cR3d, wherein:
- R3c and R3b are each independently hydrogen, alkyl(C≤12), or substituted alkyl(C≤12);
- or
- R3 and R3′ are taken together and are alkenediyl(C≤12) or substituted alkenediyl(C≤12);
- or a pharmaceutically acceptable salt and/or tautomer of either of these formulae,
- wherein the compound is not
31 more elements
A compound of the formula:
- or a pharmaceutically acceptable salt and/or tautomer thereof.
Dependencies are inferred from the claim text.