Small molecule inhibitors of a protein complex
AssigneesThe Regents of the University of California, University of New Mexico
InventorsAlexandre GINGRAS, Mark GINSBERG,, Carlo BALLATORE, Larry SKLAR, Karol Rogelle Karagdag FRANCISCO
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Abstract
Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.
Claims25
A method of treating a disease in a subject by reducing thrombosis, atherosclerosis, or inflammation comprising administering to a subject in need an effective amount of a Siritol compound or salt thereof that binds to KRIT1 FERM domain to inhibit binding with HEG1.
A method of improving laminar blood-flow in a subject comprising administering to a subject in need an effective amount of a Sirtinol compound or salt thereof that binds to KRIT1 FERM domain to inhibit binding with HEG1.
A compound or Formula (A) or Formula (B), a salt thereof, or a salt hydrate thereof;
- wherein R1 is selected from the group consisting of hydroxyl and hydrogen;
- wherein R2 is selected from the group consisting of oxygen and nitrogen, wherein the nitrogen is substituted with (a) Ra or (b) Ra and Rb, wherein i is (i) a single bond, a double bond, or a triple bond when R2 is nitrogen, or (ii) a double bond when R2 is oxygen;
- wherein R3 is selected from the group consisting of hydrogen and a C1-C20 hydrocarbyl;
- wherein R4 is selected from the group consisting of hydrogen, hydroxyl, nitrogen, and oxygen, wherein the oxygen is substituted with Rc, and the nitrogen is substituted with (i) Rd or (ii) Rd and Re;
- wherein R5 is selected from the group consisting of (i) hydrogen, (ii) hydroxyl, (iii) a C1-C20 hydrocarbyl, (iv) a halogen, (v) nitrogen, and (vi) oxygen, wherein the oxygen substituted with Rf, and the nitrogen is substituted with (a) Rg or (b) Rg and Rh;
- and
- wherein R6 is selected from the group consisting of hydrogen and a C1-C20 hydrocarbyl;
- wherein Rc, and Rf are independently selected from a C1-C20 hydrocarbyl, and
- wherein Ra, Rb, Rd, Re, Rg and Rh are independently selected from hydrogen and a C1-C20 hydrocarbyl.
Dependencies are inferred from the claim text.