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US 2022/0089587 A1Published application
Eif4e inhibitors and uses thereof
AssigneePIC Therapeutics, Inc.
InventorAshis SAHA
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds inhibiting elF4E activity, and compositions and methods of using thereof. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful for treating a variety of diseases, disorders or conditions, associated with elF4E. Such diseases, disorders, or conditions include cellular proliferative disorders (e.g., cancer) such as those described herein.
Claims26
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- L1 is a bond, O, or S;
- R1 is an optionally substituted ring selected from phenyl, an 8-10 membered bicyclic aromatic carbocyclic ring, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or an 8-10 membered bicyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- L2 is a C1-8 bivalent straight or branched hydrocarbon chain, wherein 1, 2, or 3 methylene units of the hydrocarbon chain are optionally and independently replaced with —N(R)— or -Cy-;
- each R is independently selected from hydrogen or optionally substituted —C1-6 aliphatic;
- each -Cy- is independently an optionally substituted bivalent ring selected from a 3-6 membered monocyclic, saturated or partially unsaturated, carbocyclic ring, or a 3-6 membered monocyclic, saturated or partially unsaturated, heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- R2 is —COOR;
- and
- R3 is R, halogen, or an optionally substituted ring selected from phenyl, an 8-10 membered bicyclic aromatic carbocyclic ring, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or an 8-10 membered bicyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.
6 more elements
4-5. (canceled)
(canceled)
(canceled)
16-18. (canceled)
20-21. (canceled)
(canceled)
Dependencies are inferred from the claim text.