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US 2026/0217693 A1Published application
Srpk1 inhibitors and methods of use
OwnerLianhai LI, Cyrille F. KUHNinventors
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Abstract
Provided herein are compounds having a structure of Formula (I) and pharmaceutically acceptable salts thereof which can act as modulators of serine/arginine-rich splicing factor protein kinase-1 (SRPK1). Further disclosed herein are methods for treating cancer and vascular diseases and disorders.
Claims27
A compound having a structure of Formula (I):
- wherein
- ring A is a 5-10-membered heterocycle having 1, 2, or 3 ring heteroatoms independently selected from N, O, and S;
- Cy is a 4-10-membered heterocycle having 1, 2, or 3 ring heteroatoms independently selected from N, O, and S and optionally substituted with 1 to 4 RA;
- each RA is independently halo, OH, oxo, C1-6alkyl, C1-6haloalkyl, C1-6hydroxyalkyl, C0-6alkylene-N(RN)2, C0-6alkylene-C(O)N(RN)2, C0-6alkylene-OC(O)C1-6alkyl, C0-6alkylene-C(O) C1-6alkyl, C0-6alkylene-CO2RN, or C0-6alkylene-4-8-membered heterocycle having 1, 2, 3 or 3 ring heteroatoms independently selected from N, O, and S;
- R1 is H, halo, C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6haloalkoxy, or C3-6cycloalkyl;
- R2 is halo, C1-6alkoxy, C1-6haloalkoxy, C1-6alkyl, C2-6alkene, C2-6alkyne, C1-6haloalkyl, CO2H, or Het;
- Het is a 5-8-membered heterocycle having 1, 2, or 3 ring heteroatoms independently selected from N, O, and S, and is optionally substituted with 1 or 2 RB;
- each RB is independently halo, OH, oxo (═O), C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6haloalkoxy, C0-6alkylene-N(RN)2, or C0-6alkylene-4-8-membered heterocycle having 1, 2, 3 or 3 ring heteroatoms independently selected from N, O, and S;
- R3 is H, halo, or C1-6alkyl;
- and
- each RN is independently H or C1-3alkyl, or a pharmaceutically acceptable salt thereof.
8 more elements
-5. (canceled)
-8. (canceled)
-13. (canceled)
-17. (canceled)
(canceled)
-24. (canceled)
A compound as listed in Table A, or a pharmaceutically acceptable salt thereof.
(canceled)
Dependencies are inferred from the claim text.